Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 546/120)
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Publication number: 20130211090Abstract: The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) which serves as a synthesis intermediate for production of medicaments, especially for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Jens Ackerstaff
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Publication number: 20130203803Abstract: Disclosed are CCR1 inhibitor compounds of the formula (I): which are useful in the treatment of autoimmune and other diseases. Also disclosed a pharmaceutical compositions containing the same, and methods of making and using same.Type: ApplicationFiled: April 26, 2011Publication date: August 8, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: John D. Huber
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Publication number: 20130196993Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: September 28, 2011Publication date: August 1, 2013Inventors: Michael Berger, Christopher Kern, Marko Eck
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Publication number: 20130178497Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: September 1, 2011Publication date: July 11, 2013Inventors: Tatsuki Koike, Minoru Nakamura, Yoshihide Tomata, Takafumi Takai, Yasutaka Hoashi, Yuichi Kajita, Tetsuya Tsukamoto, Makoto Kamata
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Patent number: 8481562Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: September 22, 2009Date of Patent: July 9, 2013Assignee: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Publication number: 20130172549Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: January 29, 2013Publication date: July 4, 2013Applicant: H. Lundbeck A/SInventor: H. Lundbeck A/S
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Publication number: 20130172341Abstract: Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I).Type: ApplicationFiled: September 12, 2011Publication date: July 4, 2013Inventors: Gerald W. Shipps, JR., Yongqi Deng, Alan B. Cooper, Xiaolei Gao, Binyuan Sun, James Wang, Liang Zhu
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Publication number: 20130150340Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 25, 2012Publication date: June 13, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130150578Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 1, 2011Publication date: June 13, 2013Applicant: CADILA PHARMACEUTICALS LIMITEDInventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
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Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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Publication number: 20130096155Abstract: The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.Type: ApplicationFiled: September 6, 2012Publication date: April 18, 2013Applicant: JAPAN TOBACCO INC.Inventors: Ikuo Mitani, Yosuke Ogoshi, Takuya Matsui, Masahiro Yokota, Masakazu Terashita, Dai Motoda, Kazuhito Ueyama, Hiroyuki Abe, Takahiro Hotta, Takashi Ito
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Publication number: 20130085128Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130065894Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 12, 2011Publication date: March 14, 2013Applicant: SANOFIInventors: Matthias LOEHN, Maria MENDEZ-PEREZ, Stefania PFEIFFER-MAREK, Aimo KANNT, Guillaume BEGIS, Olivier DUCLOS, Federic JEANNOT
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Publication number: 20130059849Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: March 7, 2013Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Publication number: 20130040914Abstract: Compounds of Formula I are described: (I), wherein RP and RQ are defined herein. The compounds transcriptase, the prophylaxis and treatment of infection by HIV, and the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: April 4, 2011Publication date: February 14, 2013Inventors: Samson M. Jolly, Neville Anthony, Robert Gomez, David C. Dubost, Rick G. Woodward
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Patent number: 8357698Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.Type: GrantFiled: July 20, 2010Date of Patent: January 22, 2013Assignee: SanofiInventors: Gerhard Zoller, Stefan Petry, Gunter Muller, Hubert Heuer, Norbert Tennagels
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Publication number: 20130005743Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Applicant: H. Lundbeck A/SInventors: Jørgen Eskildsen, Christian Wenzel Tornøe
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Publication number: 20120322821Abstract: The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.Type: ApplicationFiled: February 28, 2011Publication date: December 20, 2012Applicant: RAQUALIA PHARMA INC.Inventors: Kaoru Shimada, Masaki Sudo, Masaomi Tajimi, Nobuyuki Takahashi, Kazuhiko Nonomura
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Publication number: 20120322790Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Rajashekhar BETAGERI, Brian Nicholas COOK, Darren DiSALVO, Christian HARCKEN, Daniel KUZMICH, Pingrong LIU, John LORD, Can MAO, Hossein RAZAVI
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Patent number: 8329907Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: March 9, 2010Date of Patent: December 11, 2012Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
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Patent number: 8299252Abstract: It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents —(O)n—R; R represents a C1-C6 alkyl group or the like; n represents 0 or 1; X represents O or the like; R2, R3 and R4 are independently selected from a hydrogen atom or C1-C3 alkyl; or R2 and R3 may join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.Type: GrantFiled: August 4, 2006Date of Patent: October 30, 2012Assignees: Chugai Seiyaku Kabushiki Kaisha, The University of TokyoInventors: Sawako Ozawa, Nobuhiro Oikawa, Eisaku Mizuguchi, Hirosato Ebiike, Fumio Watanabe, Kenji Morikami, Nobuo Shimma, Nobuya Ishii, Toshiyuki Tsukaguchi
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Publication number: 20120270858Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Publication number: 20120270870Abstract: Diclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1, X and G are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).Type: ApplicationFiled: October 19, 2010Publication date: October 25, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Daniel Kuzmich, Can Mao, Hossein Razavi
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Patent number: 8283465Abstract: The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.Type: GrantFiled: July 16, 2010Date of Patent: October 9, 2012Assignee: Japan Tobacco Inc.Inventors: Ikuo Mitani, Yosuke Ogoshi, Takuya Matsui, Masahiro Yokota, Masakazu Terashita, Dai Motoda, Kazuhito Ueyama, Hiroyuki Abe, Takahiro Hotta, Takashi Ito
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Publication number: 20120252809Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
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Patent number: 8163918Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.Type: GrantFiled: October 14, 2011Date of Patent: April 24, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, John Lord, Can Mao
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Publication number: 20120087978Abstract: The present invention relates to a Factor Xa inhibitor dosage form comprising apixaban in a solubility-improved form wherein the dosage form provides controlled release of apixaban and methods for preventing or treating venous thromboembolisms, deep vein thrombosis and acute coronary syndrome with said dosage form.Type: ApplicationFiled: June 15, 2010Publication date: April 12, 2012Applicants: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.Inventor: Richard G. Nause
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Publication number: 20120064181Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: March 15, 2010Publication date: March 15, 2012Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
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Publication number: 20120065227Abstract: The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: ApplicationFiled: November 23, 2011Publication date: March 15, 2012Applicant: Gilead Sciences, Inc.Inventors: Dmitry Koltun, Jeff Zablocki
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Publication number: 20120059030Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: September 1, 2011Publication date: March 8, 2012Inventors: Tatsuki KOIKE, Minoru Nakamura, Yoshihide Tomata, Takafumi Takai, Yasutaka Hoashi, Yuichi Kajita, Tetsuya Tsukamoto, Makoto Kamata
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Publication number: 20120035370Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Brian Nicholas COOK, Darren DiSALVO, Daniel Robert FANDRICK, Christian HARCKEN, Daniel KUZMICH, Thomas Wai-Ho LEE, Pingrong LIU, John LORD, Can MAO, Jochen NEU, Brian Christopher RAUDENBUSH, Hossein RAZAVI, Jonathan Timothy REEVES, Jinhua J. SONG, Alan David SWINAMER, Zhulin TAN
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Publication number: 20120028975Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.Type: ApplicationFiled: April 5, 2010Publication date: February 2, 2012Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
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Publication number: 20120015976Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: March 9, 2010Publication date: January 19, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANK TER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Wolfgang Staehle
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Publication number: 20110301148Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; orType: ApplicationFiled: June 29, 2011Publication date: December 8, 2011Applicant: SANOFIInventors: Jean-Michel ALTENBURGER, Valérie FOSSEY, Stéphane ILLIANO, Géraldine MANETTE
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Publication number: 20110294790Abstract: Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.Type: ApplicationFiled: November 19, 2009Publication date: December 1, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
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Patent number: 8063065Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: GrantFiled: December 16, 2010Date of Patent: November 22, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Darren Di Salvo, Christian Harcken, Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, John Lord, Can Mao, Jochen Neu, Brian Christopher Raudenbush, Hossein Razavi, Alan David Swinamer
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Publication number: 20110275609Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110212971Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: May 5, 2011Publication date: September 1, 2011Inventors: Tao Wang, Yasutsugu Ueda, Lawrence G. Hamann, Zhongxing Zhang, Zhiwei Yin, Alicia Regueiro-Ren, David J. Carini, Jacob Swidorski, Zheng Liu, Nicolas A. Meanwell, John F. Kadow, Barry L. Johnson
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Publication number: 20110190292Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Inventors: T. G. Murali Dhar, Stephen T. Wrobleski
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Publication number: 20110190257Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: July 1, 2009Publication date: August 4, 2011Applicant: Genetech, Inc.Inventors: Robert Andrew Heald, Philip Jackson, Joseph P. Lyssikatos, Stephen Price, Pascal Pierre Alexandre Savy
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Publication number: 20110183919Abstract: The present invention is directed to novel compounds of formula I and pharmaceutically acceptable salts, enantiomers thereof having inhibiting properties of dipeptidyl peptidase IV enzyme (DP-IV inhibitors). The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds along with its composition in the prevention or treatment of diseases associated with DP-IV enzyme.Type: ApplicationFiled: September 11, 2009Publication date: July 28, 2011Applicant: CADILA PHARMACEUTICALS LTD.Inventors: Bakulesh Mafatlal Khamar, Singh Chandan, Rajiv Indravadan Modi
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Publication number: 20110173726Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.Type: ApplicationFiled: September 23, 2009Publication date: July 14, 2011Applicant: BASF SEInventors: Steffen Groß, Karsten Körber, Wolfgang Von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Publication number: 20110172266Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: September 22, 2009Publication date: July 14, 2011Applicant: GENKYOTEX SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 7968719Abstract: The present invention relates to indazole derivatives of the general formulae I or II having the meanings indicated in the description, to the pharmaceutically useful salts thereof and the use thereof as drugs.Type: GrantFiled: April 28, 2009Date of Patent: June 28, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Gerhard Zoller, Stefan Petry, Gunter Muller, Hubert Heuer, Karl-Heinz Baringhaus
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Publication number: 20110144121Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: June 16, 2010Publication date: June 16, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110077248Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: May 28, 2009Publication date: March 31, 2011Inventors: Chi B. Vu, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20110077267Abstract: The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.Type: ApplicationFiled: July 16, 2010Publication date: March 31, 2011Applicant: JAPAN TOBACCO INC.Inventors: Ikuo Mitani, Yosuke Ogoshi, Takuya Matsui, Masahiro Yokota, Masakazu Terashita, Dai Motoda, Kazuhito Ueyama, Hiroyuki Abe, Takahiro Hotta, Takashi Ito
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Patent number: 7915286Abstract: The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).Type: GrantFiled: September 11, 2006Date of Patent: March 29, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Vinayak Vasantrao Khairnar, Mandadapu Raghuramaiah, Abhijit Ray, Sunanda Ghose Dastidar
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Patent number: 7910602Abstract: The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) useful as inhibitors of beta-adrenergic receptor kinase 1 (?ARK-1), compositions containing such compounds and their use for the treatment and prevention of chronic heart failure, hypertension, myocardial ischemia and hepatitis C virus (HCV) infections, and for the prevention of opiate addiction.Type: GrantFiled: December 20, 2007Date of Patent: March 22, 2011Assignee: Sanofi-AventisInventors: Henning Steinhagen, Jochen Huber, Kurt Ritter, Bernard Pirard, Kirsten Bjergarde, Marcel Patek, Martin Smrcina, Linli Wei