cas 77992-44-0, 5-BROMO-2-HYDRAZINOPYRIDINE

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Dual Reactivity of 1,2,3,4-Tetrazole: Manganese-Catalyzed Click Reaction and Denitrogenative Annulation
A general catalytic method using a Mn-porphyrin-based catalytic system is reported that enables two different reactions (click reaction and denitrogenative annulation) and affords two different classes of nitrogen heterocycles, 1,5-disubstituted 1,2,3-triazoles (with a pyridyl motif) and 1,2,4-triazolo-pyridines. Mechanistic investigations suggest that although the click reaction likely proceeds through an ionic mechanism, which is different from the traditional click reaction, the denitrogenative annulation reaction likely proceeds via an electrophilic metallonitrene intermediate rather than a metalloradical intermediate. Collectively, this method is highly efficient and offers several advantages over other methods. For example, this method excludes a multi-step synthesis of the N-heterocyclic molecules described and produces only environmentally benign N2 gas a by-product.
Chattopadhyay, Buddhadeb,Das, Sandip Kumar,Khatua, Hillol,Roy, Satyajit
supporting information
p. 304 - 312
(2020/10/29)

Compound and application thereof
The invention provides a compound and application thereof. The compound has a structure as shown in a formula I, and is used as a material of an electron transport layer in an organic electroluminescent device. The organic electroluminescent device comprises a first electrode, a second electrode and an organic layer between the first electrode and the second electrode, wherein the organic layer contains any one or a combination of at least two of the compounds. The compound has relatively high electron injection and migration performance. When the compound is used as an electron transport layer material in an organic electroluminescent device, the luminous efficiency of the device can be improved, and the starting voltage of the device can be reduced.
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Paragraph 0126-0130

(2021/11/10)

CD206 MODULATORS THEIR USE AND METHODS FOR PREPARATION
Compounds of Formula I, Formula II, and Formula III and the pharmaceutically acceptable salts thereof are disclosed. The variables X, a, b, c, d, R1-4, R10-15 and R17-22 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving M2 phenotype of macrophages. Pharmaceutical compositions containing compounds of Formula I or Formula II or Formula III and methods of treatment comprising administering compounds of Formula I and Formula II and Formula III are also disclosed.
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Paragraph 0263

(2021/06/26)

TrkB POSITIVE ALLOSTERIC MODULATORS
The present invention relates to the field of pharmaceutical composition comprising "LIT-TB" derivatives of formula I. More particularly it relates to "LIT-TB" derivatives for use in the treatment of neurodegenerative diseases, and more particularly in th
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Page/Page column 62-63

(2021/02/12)

TRIAZOLOPYRIDIN-3-ONES OR THEIR SALTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
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Paragraph 018-0184

(2020/07/07)

Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
1,2,4-Triazolo[3,4-a]pyridines and related heterocycles and substituted triazines were commonly discovered scaffolds in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as a catalyst, the mild reaction condition tolerates a broad substrate range and substitutes. The prepared 3-unsubstituted 1,2,4-triazolo[3,4-a]pyridine and derivatives allow further introduction of a variety of functional group1 at 3-position.
Liu, Lingfeng,Qiao, Chunhua,Shen, Bei,Xu, Yiwen
supporting information

(2020/04/01)

Iron(II)-Based Metalloradical Activation: Switch from Traditional Click Chemistry to Denitrogenative Annulation
A unique concept for the intermolecular denitrogenative annulation of 1,2,3,4-tetrazoles and alkynes was discovered by using a catalytic amount of Fe(TPP)Cl and Zn dust. The reaction precludes the traditional, more favored click reaction between an organic azide and alkynes, and instead proceeds by an unprecedented metalloradical activation. The method is anticipated to advance access to the construction of important basic nitrogen heterocycles, which will in turn enable discoveries of new drug candidates.
Roy, Satyajit,Khatua, Hillol,Das, Sandip Kumar,Chattopadhyay, Buddhadeb
supporting information
p. 11439 - 11443
(2019/07/17)

ION CHANNEL MODULATORS
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
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Paragraph 00419

(2019/12/25)

TRIAZOLONES DERIVATIVES FOR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, codrug, cocrystal, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Page/Page column 32

(2017/04/18)

SUBSTITUTED FUSED HETEROCYCLES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Page/Page column 57

(2015/11/17)

Preparation of 2,3-Disubstituted 5-Bromo-1 H -pyrrolo[2,3- b ]pyridine Framework by Fischer Cyclization
A simple synthesis of some hard-to-reach heterocycles containing 2,3-disubstituted 5-bromo-1H-pyrrolo[2,3-b]pyridine framework by FisNher indole cyclization in polyphosphoric acid has been developed. A particularly valuable feature of this synthetic route is the possibility to build a 5-bromo-7-azaindole scaffold with alkyl or aryl substituents at positions 2 and 3 from available starting materials.
Alekseyev, Roman S.,Amirova, Sabina R.,Terenin, Vladimir I.
p. 3169 - 3178
(2015/10/19)

AMIDOPYRIDINE DERIVATIVE, AND USE THEREOF
The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.
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Paragraph 0362; 0363

(2016/10/08)

Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same
Hydroxamate substituted azaindoline cyanine dyes, conjugates thereof and methods of using the same are provided. The subject cyanine dyes include an azaindoline ring having a hydroxamate substituent. The dyes may further include a reactive group moieties (RGM) and/or a water soluble group. Also provided are conjugates of the subject dyes. Also provided are tandem conjugates including a fluorescent protein capable of energy transfer to the dye. Methods of detecting an analyte in a sample by contacting the sample with a detection reagent are provided. The detection agent may be a dye-conjugate that specifically binds the analyte, or may be a reactive dye which conjugates to the analyte. Also provided are compositions, e.g., kits, etc., incorporating such dyes which facilitate use in such methods.
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Paragraph 0423; 0424

(2015/04/28)

MODIFIED CARBOCYANINE DYES AND THEIR CONJUGATES
Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
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Paragraph 0176

(2015/09/22)

HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 0448

(2014/05/20)

6 - SUBSTITUTED 3 - (QUINOLIN- 6 - YLTHIO) - [1,2,4] TRIAZOLO [4, 3 -A] PYRADINES AS TYROSINE KINASE
The invention relates to compounds of formula (I) and salts thereof: Formula (I) wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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Page/Page column 82

(2013/03/28)

TRIAZOLOPYRIDINE COMPOUNDS
The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound o f formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I)
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Paragraph 0732

(2013/09/26)

TRIAZOLOPYRIDINONE PDE10 INHIBITORS
The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Page/Page column 37

(2013/06/05)

3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
Disclosed are 3-aryl-6-aryl-[1,2,4]triazolo[4,3-a]pyridines thereof, represented by the Formula (I) wherein Ar1, Ar2, R1-R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation.
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Page/Page column 19

(2012/06/01)

3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
Disclosed are 3-aryl-6-aryl-[1,2,4]triazolo[4,3-a]pyridines thereof, represented by the Formula (I) wherein Ar1, Ar2, R1-R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation.
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Page/Page column 19

(2012/06/01)

TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
The present invention is directed to pyridotriazole and benztriazole compounds of formula (I) (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis,
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Page/Page column 28-29

(2012/10/07)

Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-Like Proteins
The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
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Page/Page column 77

(2011/11/30)

SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES
The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.
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Page/Page column 17

(2010/12/29)

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition
The structure based drug design, synthesis and structure-activity relationship of a series of C6 sulfur linked triazolopyridine based p38 inhibitors are described. The metabolic deficiencies of this series were overcome through changes in the C6 linker fr
Jerome, Kevin D.,Rucker, Paul V.,Xing, Li,Shieh, Huey S.,Baldus, John E.,Selness, Shaun R.,Letavic, Michael A.,Braganza, John F.,McClure, Kim F.
scheme or table
p. 469 - 473
(2010/04/05)

TRIAZOLOPYRIDINE COMPOUNDS
A compound of formula (Ia): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, or a compound of formula (Ib): or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof, and the use of a compound of formula (Ia) or (Ib) in the treatment of a TNF -mediated disease, disorder, or condition, or a p38 -mediated disease,. disorder, or condition, in particular the allergic and non-allergic airway diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
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Page/Page column 48

(2008/06/13)

4-(PYRIDIN-3-YL)-2-(PYRIDIN-2-YL)-1,2-DIHYDRO-3H-PYRAZOL-3-ONE DERIVATIVES AS SPECIFIC HIF-PROLYL-4-HYDROXYLASE INHIBITORS FOR TREATING CARDIOVASCULAR AND HAEMATOLOGICAL DISEASES
The object of the invention is to provide new compounds which can be used for the treatment of diseases, in particular cardiovascular and haematological diseases. The present invention describes compounds which act as specific HIF-prolyl-4-hydroxylase inhibitors and which, because of this specific in vivo action mechanism, induce HIF target genes, such as erythropoietin, and the thus produced biological processes, such as erythropoiesis, after parenteral or oral administration. The present invention relates to compounds having the general formula (I), in which A stands for CH or N, R1 stands for a substituent selected from the group formed by (C1-C6)-alkyl, trifluoromethyl, halogen, cyano, nitro, hydroxy, (C1-C6)-alkoxy, amino, (C1-C6)-alkoxycarbonyl, hydroxycarbonyl and C(=O)-NH-R4; R2 stands for a substituent selected from the group formed by halogen, cyano, nitro, (C1-C6)-alkyl, trifluoromethyl, hydroxy, (C1-C6)-alkoxy, trifluoromethoxy, amino, hydroxycarbonyl and C(=O)-NH-R8; m equals 0, 1 or 2; n equals 0, 1, 2 or 3, it being possible for these meanings to be the same or different when R1 or R2 occurs multiple times; and R3 stands for hydrogen, (C1-C6)-alkyl or (C3-C7)-cycloalkyl. The invention also relates to the salts, solvates, and salt solvates of these compounds.
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Page/Page column 40

(2008/06/13)

Triazolopyridinylsulfanyl derivatives as p38 MAP kinase inhibitors
A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
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Page/Page column 31

(2008/06/13)

AMIDOPYRAZOLE DERIVATIVE
A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I): wherein Ar1 and Ar2 independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
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Page/Page column 25

(2010/11/23)

NOVEL TRIAZOLOPYRIDINE COMPOUNDS
This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula (I): wherein R
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Page/Page column 33

(2008/06/13)

Theoretical and experimental design of atypical kinase inhibitors: Application to p38 MAP kinase
Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described. A set of calculated descriptors relevant to the anticipated binding interaction for the fragments 1-methyl-
McClure, Kim F.,Abramov, Yuriy A.,Laird, Ellen R.,Barberia, John T.,Cai, Weiling,Carty, Thomas J.,Cortina, Santo R.,Danley, Dennis E.,Dipesa, Alan J.,Donahue, Kathleen M.,Dombroski, Mark A.,Elliott, Nancy C.,Gabel, Christopher A.,Han, Seungil,Hynes, Thomas R.,LeMotte, Peter K.,Mansour, Mahmoud N.,Marr, Eric S.,Letavic, Michael A.,Pandit, Jayvardhan,Ripin, David B.,Sweeney, Francis J.,Tan, Douglas,Tao, Yong
p. 5728 - 5737
(2007/10/03)

DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS
The present invention relates to novel triazolo-pyridines of the formula (I) wherein R1 is fluoro; s is an integer from two to three; R2 is (C3-C6)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (Cl-C4)alkyl, hydroxy, (Cl-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; or R2 is (Cl-C6)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 39,46,50,55,60

(2008/06/13)

NOVEL PROCESSES AND INTERMEDIATES FOR PREPARING TRIAZOLO-PYRIDINES
The present invention relates and intermediates to a novel process for preparing triazolo-pyridines of the formula I wherein R1 is selected from the group consisting of hydrogen, (C,-C6)alkyl or other suitable substituents; R3 is selected from the group consisting óf hydrogen, (Cl-C6)alkyl or other suitable substituents; s is an integer from 0-5; R4is hydrogen or a suitable substituent and to intermediates for their preparation. The compounds prepared by the methods of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 45

(2010/02/06)

Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines
The present invention relates to novel alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates and methods for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 17; 21

(2010/02/06)

Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 16

(2010/02/06)

Alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
The present invention relates to novel alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page/Page column 16-17; 20-21

(2010/02/06)

Novel crystalline forms of 3-isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-A]pyridine
The present invention relates to novel crystalline forms of 3-isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine to pharmaceutical compositions containing such crystal forms and to methods of treatment. 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is a potent inhibitor of MAP kinases, preferably p38 kinase (MAPK14/CSBP/RK kinase). 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 7

(2010/02/07)

Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines
The present invention relates to novel cycloalkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 17; 21

(2010/02/08)

TRIAZOLO-PYRIDINES AS ANTI-INFLAMMATORY COMPOUNDS
The present invention relates to novel triazolo-pyridines of the formula (I) wherein X is >CH2, >NH, sulfur, >S=O, >S02 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (Cl-C6)alkyl and other suitable 10 substituents; s is an integer from 0-4; R3 is R4, R5-(NR6)-, R5-S-, R5-(S=O)-, R5-(S02)-, R5-S02-NR6-, R5-(NR6)-S02-, R5-O-,R5-(C=O)-, R5-(NR6)-(C=O)-, R5-(C=O)-NR6-, R5-O-(C=O)-, R5-(C=O)-O-, R5-CR7=CR8- or R5-C=-C-; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 15 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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Page 50; 55; 82-83

(2010/02/08)

Method for optical measurement of multi-stranded nucleic acid using cyanine dyes
A method for optical measurement of a multi-stranded nucleic acid which comprises the step of bringing a compound into contact with a multi-stranded nucleic acid wherein said compound is capable of interacting with the multi-stranded nucleic acid, wherein the compound has the following properties:(a) the compound can exist in a substantially colorless and non-fluorescent state under at least one condition in an aqueous solution in the absence of the multi-stranded nucleic acid, and(b) when the multi-stranded nucleic acid is allowed to exist in the condition defined in the above (a), the compound changes to a substantially colored state based on an interaction with the multi-stranded nucleic acid and substantially expresses fluorescent property based on said interaction.
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(2008/06/13)

Novel triazolo-pyridines anti-inflammatory compounds
The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms
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(2008/06/13)

Modified carbocyanine dyes and their conjugates
Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
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(2008/06/13)