- 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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- 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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- 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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- Imidazopyrazine Derivatives as Modulators of TNF Activity
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A series of imidazo[1,2-α]pyrazine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorder; and oncological disorders.
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Paragraph 0476
(2015/07/15)
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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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- IMIDAZOPYRAZINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of imidazo[1,2-α]pyrazine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 93
(2014/02/15)
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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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- 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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- Tetrahydropyridinyl and Dihydropyrrolyl Compounds and the Use Thereof
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The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
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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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- 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 186-187
(2010/11/28)
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- Convenient preparation of aryl-substituted nortropanes by Suzuki-Miyaura methodology
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The synthesis of a new bicyclic vinyl boronate (5) was accomplished from N-Boc-nortropinone (6) in two steps. The Suzuki-Miyaura coupling of 5 to a variety of aryl bromides and triflates afforded 3-aryl-8-azabicyclo[3.2.1]oct-2- enes in good yields by adj
- Ghosh, Shyamali,Kinney, William A.,Gauthier, Diane A.,Lawson, Edward C.,Hudlicky, Tomas,Maryanoff, Bruce E.
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p. 555 - 560
(2007/10/03)
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