- INHIBITORS OF MALT1 AND USES THEREOF
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Provided herein are compounds that inhibit MALTl, a protein whose activity is responsible for constitutive NF-κΒ signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating MALTl -related diseases and disorders (e.g., cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.
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Paragraph 00391
(2018/09/28)
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- Novel compounds
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The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
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Paragraph 0063
(2017/09/27)
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- NOVEL COMPOUNDS
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The preseent invention relates to novel retinoid-related orphan receptor gamma(RORγ)modulators and their use in the treatment ofdiseases mediated by RORγ.
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Page/Page column 22
(2015/12/17)
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- NOVEL COMPOUNDS
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The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
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Page/Page column 14
(2015/12/18)
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- NOVEL COMPOUNDS
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Disclosed are novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
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Page/Page column 76; 77
(2015/12/17)
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- NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
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Paragraph 00313
(2014/03/22)
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- Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on kilogram scale
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Reported herein is a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate, an intermediate in the synthesis of novel anti-infective agents. The key to this process is the trifluoromethylation of an aryl iodide using an inexpensive methyl chlorodifluoroacetate (MCDFA)/KF/CuI system, with an emphasis on the development work which led to this effective process.
- Mulder, Jason A.,Frutos, Rogelio P.,Patel, Nitinchandra D.,Qu, Bo,Sun, Xiufeng,Tampone, Thomas G.,Gao, Joe,Sarvestani, Max,Eriksson, Magnus C.,Haddad, Nizar,Shen, Sherry,Song, Jinhua J.,Senanayake, Chris H.
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supporting information
p. 940 - 945
(2013/07/26)
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- Novel Biaryl Benzolmidazole Derivatives and Pharmaceutical Composition Comprising The Same
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Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventi
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Page/Page column 15; 7
(2009/09/05)
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- Organic compounds
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.
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Page/Page column 22
(2009/05/29)
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- NOVEL BIARYL BENZOIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The biaryl benzoimidazole derivative of the present invention has an excellent inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further has an excellent analgesic effect, thereby
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Page/Page column 15; 26
(2008/06/13)
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- NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula (I): in which the substitutents are as defined in claim 1 and and salts, solvates, hydrates and N- oxides thereof.
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Page/Page column 51
(2008/12/08)
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- NOVEL BI-ARYL AMINES
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The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
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Page/Page column 29
(2008/06/13)
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- AMINOTHIAZOLE DERIVATIVES AS AGONISTS OF THE THROMBOPOIETIN RECEPTOR
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A compound of the formula (I) wherein R1, R2, R3, X, and d are defined as above. The presently disclosed compounds are TPO agonists useful as promoters of thrombopoiesis and megakaryocytopoiesis.
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Page/Page column 51
(2010/11/25)
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- AMINOTHIAZOLE DERIVATIVES AS AGONISTS OF THE THROMBOPOIETIN RECEPTOR
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A compound of the formula (I) wherein R1, R2, R3, X, Y, and d are defined as above. The presently disclosed compounds are TPO agonists useful as promoters of thrombopoiesis and megakaryocytopoiesis.
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Page/Page column 44-45
(2010/11/26)
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- Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H- benzimidazoles
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The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful stimuli. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Herein, we describe the synthesis and the structure-activity relationships of a series of 2-(4-pyridin-2- ylpiperazin-1-yl)-1H-benzo-[d]imidazoles as novel TRPV1 antagonists. Compound 46ad was among the most potent analogues in this series. This compound was orally bioavailable in rats and was efficacious in blocking capsaicin-induced flinch in rats in a dose-dependent manner. Compound 46ad also reversed thermal hyperalgesia in a model of inflammatory pain, which was induced by complete Freund's adjuvant (CFA).
- Ognyanov, Vassil I.,Balan, Chenera,Bannon, Anthony W.,Bo, Yunxin,Dominguez, Celia,Fotsch, Christopher,Gore, Vijay K.,Klionsky, Lana,Ma, Vu V.,Qian, Yi-Xin,Tamir, Rami,Wang, Xianghong,Xi, Ning,Xu, Shimin,Zhu, Dawn,Gavva, Narender R.,Treanor, James J. S.,Norman, Mark H.
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p. 3719 - 3742
(2007/10/03)
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- NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE OR PHENYL COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
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The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
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Page/Page column 107-108
(2008/06/13)
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- (3,4-DISUBSTITUTED)PROPANOIC CARBOXYLATES AS S1P (EDG) RECEPTOR AGONISTS
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The present invention encompasses compounds of Formula A: A as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
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Page/Page column 53-54
(2008/06/13)
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- BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS
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Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.
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- Substituted phenyl farnesyltransferase inhibitors
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Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
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