- Compound and application thereof
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The invention provides a novel compound. The novel compound has certain inhibitory activity for indoleamine 2,3-dioxygenase (IDO) which is oxido-reductase, and accordingly the novel compound can be used for treating diseases related to the indoleamine 2,3-dioxygenase and can be applied to cancer and immunity related diseases.
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- HPK1 inhibitor and application thereof
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The invention belongs to the technical field of medicines, and specifically relates to an HPK1 inhibitor compound as shown in a formula (I) which is described in the specification or a pharmaceutically-acceptable salt and a stereoisomer of the HPK1 inhibi
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Paragraph 0515-0518
(2019/05/16)
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- OXALAMIDES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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The present invention relates to novel compounds which act as modulators of indoleamine 2,3-dioxygenase (IDOl) and to the use of said compounds in the prophylaxis and/or treatment of diseases or conditions mediated by indoleamine 2,3-dioxygenase. The inve
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Page/Page column 71; 72
(2019/07/19)
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- TETRAHYDROPYRIDO[4,3-D]PYRIMIDINE INHIBITORS OF ATR KINASE
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The present invention relates to tetrahydropyrido[4,3-d]pyrimidine based compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
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Paragraph 0372; 0373
(2018/12/13)
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- Tyrosine Kinase Inhibitor And Uses Thereof
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Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
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- SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition of thrombin and/or kallikrein.
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Paragraph 0343
(2017/05/27)
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- IDO INHIBITORS
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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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Paragraph 2867
(2016/10/27)
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- PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
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Page/Page column 458
(2014/09/29)
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- CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 146; 147
(2014/10/03)
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- A β-tryptase inhibitor with a tropanylamide scaffold to improve in vitro stability and to lower hERG channel binding affinity
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Tropanylamide was investigated as a possible scaffold for b-tryptase inhibitors with a basic benzylamine P1 group and a substituted thiophene P4 group. Comparing to piperidinylamide, the tropanylamide scaffold is much more rigid, which presents less oppor
- Liang, Guyan,Choi-Sledeski, Yong Mi,Shum, Patrick,Chen, Xin,Poli, Gregory B.,Kumar, Vasant,Minnich, Anne,Wang, Qingping,Tsay, Joseph,Sides, Keith,Kang, Jiesheng,Zhang, Ying
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supporting information; experimental part
p. 1606 - 1610
(2012/04/10)
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- FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN
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This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example c
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Page/Page column 41
(2012/03/26)
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- FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN
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This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example c
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Page/Page column 49
(2012/03/26)
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- TROPANE UREA DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS MODULATORS OF THE ACTIVITY OF 11BETAHSD1
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The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11β-hydroxysteroid dehydrogenose type 1 (11βHSD1).
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Page/Page column 7
(2011/12/13)
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- Process for preparing an intermediate to opioid receptor antagonists
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The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1 ]oct-2-en-3-yl)benzamide intermediate in which the amino-prot
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- 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists
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The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 12
(2009/04/24)
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- UREA DERIVATIVES OF TROPANE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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The present invention is related to a compound of formula (I) wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R4, p, r and are as defined herein, its preparation, pharmaceutical composition and use as a modulator of the activity of the 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1).
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Page/Page column 7-8
(2009/07/17)
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- UROTENSIN II RECEPTOR ANTAGONISTS
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The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
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Page/Page column 186
(2010/11/28)
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- HETEROCYCLIC INHIBITORS OF PROTEIN ARGININE METHYL TRANSFERASES
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A compound of formula I, or a stereoisomer, a tautomer, a pharmaceutically acceptable salt or solvate thereof, methods of using such compounds in the treatment of hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases; and to pharmaceutical compositions containing such compounds
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Page/Page column 59
(2010/11/24)
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- Benzimidazolidinone derivatives as muscarinic agents
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Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
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Page/Page column 13
(2010/02/06)
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- Substituted bridged phenyl piperidines: Orally active growth hormone secretagogues
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A new series of growth hormone secretagogues have been discovered. The best compound, 26j, shows excellent ability to release growth hormone both in vitro and in vivo. The synthesis and biological activity of these compounds are discussed.
- Lu, Zhijian,Tata, James R.,Cheng, Kang,Wei, Liente,Chan, Wanda W.-S.,Butler, Bridget,Schleim, Klaus D.,Jacks, Thomas M.,Hickey, Gerard,Patchett, Arthur A.
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p. 1817 - 1820
(2007/10/03)
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