- BICYCLOHEPTANE PYRROLIDINE OREXIN RECEPTOR AGONISTS
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The present invention is directed to bicyclo[4.1.0]heptane pyrrolidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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- Arylamine compound, pharmaceutical composition containing arylamine compound as well as preparation method and application of arylamine compound
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The present invention relates to an arylamine compound of a formula (I), a pharmaceutical composition comprising the same, a preparation method of the arylamine compound and application of the pharmaceutical composition in the prevention or treatment of diseases or conditions associated with RET activity.
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- Development of a Stereoselective and Scalable Synthesis for the Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor, BMT-297376; N-((R)-1-((cis)-4-(3-(Difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl)propyl)-6-methoxynicotinamide
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The current work describes a stereoselective and scalable route to N-((R)-1-((cis)-4-(3-(difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl)propyl)-6-methoxynicotinamide (1) from readily available 1,4-dioxaspiro[4.5]decan-8-one. The developed process encompasses an efficient 1,4-trans-selective synthesis of (trans)-4-(3-(difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl methanesulfonate as the key intermediate and the use of Ellman sulfinamine methodology to install an alkyl amine in a stereoselective manner. Various synthetic routes were screened to accomplish a stereoselective and scalable protocol to access the title compound (1). This advancement enabled a competent route to the title compound in an enantioselective, safe, cost-effective, and scalable manner.
- Arunachalam, Pirama Nayagam,Balog, Aaron,Borzilleri, Robert M.,Cherney, Emily C.,Gupta, Anuradha,Hong, Zhenqiu,Kempson, James,Krishnamoorthy, Suresh,Kuppusamy, Prakasam,Manoharan, Haridhas,Mathur, Arvind,Nimje, Roshan Y.,Ramasamy, Duraisamy,Rampulla, Richard R.,Shanmugam, Yoganand,Zhang, Liping
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p. 1680 - 1689
(2021/07/28)
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- INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND USE OF SAME IN MEDICINE
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The present invention relates to a compound represented by formula I, a pharmaceutical composition containing the compound of formula I, a method for inhibiting indoleamine 2,3-dioxygenase, and its use in medicine.
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- SPIRO COMPOUND AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR
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Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
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Paragraph 0158; 0159; 0160
(2020/12/29)
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- Compound and purpose thereof
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The invention provides a novel compound with certain inhibition activity on oxidoreductase indoleamine 2,3-dioxygenase (IDO), or a purpose of the compound for treating related diseases including cancer and immunization-related diseases.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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The present invention provides compounds of formula (I), formula (II) or formula (III), wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treat
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- CYCLIC COMPOUNDS AS IMMUNOMODULATING AGENTS
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The present disclosure describes novel IDO inhibitors and methods for preparing them. The pharmaceutical compositions comprising such IDO inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described
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- Five-membered heteroaromatic ring derivative, preparation method thereof, pharmaceutical composition and application thereof
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The invention discloses a five-membered heteroaromatic ring derivative, a preparation method thereof, a pharmaceutical composition and application thereof. The five-membered heteroaromatic ring derivative (I), isomers, prodrugs, stable isotope derivatives or pharmaceutically acceptable salts thereof have the following structure. The five-membered heteroaromatic ring derivative has a good IDO inhibitory effect, and can effectively treat, relieve and/or prevent various related diseases such as tumors, virus infection or autoimmune diseases, and the like caused by immunosuppression.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3 -dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
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- Polycyclic compound and its pharmaceutical composition and application
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The invention discloses a polycyclic compound and its preparation method, pharmaceutical composition and application. The polycyclic compound (I) and its isomer, prodrug, stable isotope derivative ora pharmaceutically acceptable salt have the structure shown in the description. The polycyclic compound has good IDO1 inhibitory effects and can be used for effectively treating, alleviating and/or preventing various related diseases such as tumors and infectious diseases caused by immunosuppression.
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- Compounds used as JAK inhibitor, and use of compounds
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The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
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- IMMUNOREGULATORY AGENTS
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Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
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- CARBOXAMIDE DERIVATIVES
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The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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- ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
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Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
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- Design and synthesis of novel small molecule CCR2 antagonists: Evaluation of 4-aminopiperidine derivatives
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A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure-affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide.
- Vilums,Zweemer,Dekkers,Askar,De Vries,Saunders,Stamos,Brussee,Heitman,Ijzerman
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p. 5377 - 5380
(2015/01/09)
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- Kinase inhibitors and methods of their use
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New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
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Page/Page column 20
(2010/04/23)
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- Imidazopyridine Kinase Inhibitors
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The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 102
(2009/01/20)
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- 2-AMINOCARBONYL-PYRIDINE DERIVATIVES
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The present invention relates to 2-aminocarbonyl-pyridine derivatives and their use as P2Yi2 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
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Page/Page column 102
(2008/06/13)
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- Substituted benzo[e] [1,4] oxazino [3,2-g] isoindole compounds
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A compound selected from those of formula (I): wherein: W1, with the carbon atoms to which it is bonded, represents phenyl or pyridyl, Z represents a group selected from hydrogen, halogen, linear or branched (C1-C6)alkyl,
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Page/Page column 7
(2010/02/15)
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