- PYRAZOLO[3,4-b]PYRIDINE AND PYRROLO[2,3-b]PYRIDINE INHIBITORS OF BRUTON'S TYROSINE KINASE
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Disclosed are pyrazolo[3,4-b]pyridine and pyrrolo[2,3-b]pyridine inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combin
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- SUBSTITUTED BICYCLIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted bicyclic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
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- Preparation, physical properties and n-type FET characteristics of substituted diindenopyrazinediones and bis(dicyanomethylene) derivatives
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A series of halogen and alkyl substituted diindenopyrazinediones and bis(dicyanomethylene) derivatives have been synthesized as new n-type organic semiconductors based on nitrogen-containing heterocycles. Halogen groups were introduced to improve the electron injection. Their crystal structures and solid physical properties are discussed. Alkyl groups were introduced to increase the solubility in organic solvents. Furthermore, hexanoyl groups were introduced by oxidation of alkyl groups to increase the solubility and electron affinity. Dicyanomethylene groups were also introduced to further enhance the electron-accepting properties. Drop-cast as well as vapour deposited thin films showed n-type FET properties.
- Nishida, Jun-Ichi,Deno, Hironori,Ichimura, Satoru,Nakagawa, Tomohiro,Yamashita, Yoshiro
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p. 4483 - 4490
(2012/07/28)
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- SEROTONIN RECEPTOR MODULATORS
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The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.
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Page/Page column 125
(2010/07/10)
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- INHIBITORS OF BURTON'S TYROSINE KINASE
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This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2′, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
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Page/Page column 73
(2010/02/16)
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- Inhibitors of Bruton's Tyrosine Kinase
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This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
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Page/Page column 99-101
(2010/09/07)
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- NOVEL PYRIDINONES AND PYRIDAZINONES
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This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one deriva-tives according to generic Formulae I-III : wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat in-flammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
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Page/Page column 77-78
(2009/10/09)
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- Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
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Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
- Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
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p. 392 - 395
(2008/09/17)
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- Development of a large scale asymmetric synthesis of vanilloid receptor (TRPV1) antagonist ABT-102
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A highly efficient asymmetric synthesis of TRPV1 antagonist ABT-102 was developed and successfully demonstrated on a multi-kilogram scale. This process incorporates a new asymmetric synthesis of (R)-tert-butylaminoindan, which is based on a chiral auxiliary induced diastereoselective reduction of its iminoindan precursor.
- Lukin, Kirill,Hsu, Margaret C.,Chambournier, Gilles,Kotecki, Brian,Venkatramani,Leanna
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p. 578 - 584
(2012/12/31)
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- Prodrugs of compounds that inhibit TRPV1 receptor
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Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladd
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Page/Page column 28
(2010/11/27)
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- Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
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- Aromatic compounds, processes for their preparation and their use in perfumery
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The compounds of formula a. STR1 wherein symbol X represents a --CHO group or a group of formula STR2 in which symbols R', taken separately, represent each a C1 to C4, linear or branched, saturated or unsaturated alkyl radical, or taken together represent a substituted or unsubstituted C2 to C4 alkylene radical; symbol R2 represents a hydrogen atom or a methyl radical; and R1 and R3 are different and represent each a hydrogen atom or a methyl radical; or of formula b. STR3 wherein the tert-butyl radical is located in position 5 or 6 of the aromatic ring and, either Y represents hydrogen and X and R2 have the meaning indicated above, or X and R2 represent each a hydrogen atom and Y represents a --CH2 CHO group or a group of formula STR4 in which R' is defined as in a.; or of formula c. STR5 wherein X and R2 have the meaning indicated in formula (Ia) and R represents a hydrogen atom or a methyl radical, the groups R being identical or different, are useful as perfuming ingredients for the preparation of perfuming compositions and perfumed articles to which they impart floral odor notes.
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- SCHWEFELVERBINDUNGEN DES ERDOELS XXII. ALKYL-10,11-DIHYDRODIINDENOTHIOPHENE
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The one-pot syntheses of alkyl-10,11-dihydrodiindenothiophenes (3) by bromination and sulfurization of alkylindan-1-ones without substituents at C-2 (1) has been studied with 14 1 with C1-C4-rests at the benzene and or the cyclopentane ring. 9 dialkyl-3 and 3 tetraalkyl-3 are prepared in yields of 7-66percent; an octamethyl-3 is detected by tlc and ms. 2 dialkyl-3 are prepared too by an independent syntheses from dimethyl 2,5-bis(methylphenyl)thiophene-3,4-dicarboxylates (13).The mechanism of the one-pot syntheses, which gives diindeno-1,4-dithiines too,is discussed.The oxidation of 4 3 has been studied.Key words: Alkylindan-1-ones, alkyl-10,11-dihydrodiindenothiophenes, alkyldiindeno-1,4-dithiines, one-pot syntheses of anellated thiophenes, oxidation of anellated thiophenes.
- Boberg, Friedrich,Deters, Karin,Schulz, Juergen,Torges, Karl-Franz
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- Occupational medicine in Belgium
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In 1965 occupational medicine was extended to all Belgian industries. In view of the economical structure of the country, most of them became affiliated to occupational medical services. The supervision of workers' health and of the problems of industrial hygiene are the two main objectives of such a service.
- Brouwers
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p. 189 - 194
(2007/10/05)
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