At Least Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 548/360.5)
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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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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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Patent number: 8053459Abstract: The present invention synthesizes a series of selenolo[3,2-c]pyrazole and selenolo[2,3-c]pyrazole derivatives, and discovers their anticancer activity.Type: GrantFiled: July 15, 2010Date of Patent: November 8, 2011Assignee: China Medical UniversityInventors: Sheng-Chu Kuo, Li-Jiau Huang, Li-Chen Chou, Jai-Sing Yang, Mei-Hua Hsu, Shi-Hong Zhuang, Mei-Chi Fang, Hui-Yi Lin
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Publication number: 20110243940Abstract: The present invention relates to Bicyclic Pyranone Derivatives, their compositions and uses for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complication, obesity, an obesity-related disorder or non-alcoholic fatty liver disease. Formula (I). Y is —C— when an optional and additional bond is present and Y is —CH— when an optional and additional bond is not present; Z is —O—, —NH— or —N(alkyl)- when the optional and additional bond between Y and Z Is absent, and Z Is —N— when the optional and additional bond between Y and Z is present; R1 is H1 halo or —CN; R2 is alkyl, alkenyl or -(alkyleneVcydoalkyl; t is 0 or 1; R3 is O when the optional and additional bond between Y and R3 is present, and R3 is alkyl.haloalkyl.—C(0)0R5.Type: ApplicationFiled: December 15, 2009Publication date: October 6, 2011Applicant: Schering CorporationInventors: Dong Xiao, Anandan Palani, Xianhai Huang, Xiaohong Zhu, Robert G. Aslanian
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Publication number: 20110195934Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.Type: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Pratik Devasthale, Wliiam N. Washburn, Wei Wang, Andres Hernandez, Saleem Ahmad, Guohua Zhao
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Publication number: 20110183939Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.Type: ApplicationFiled: September 24, 2009Publication date: July 28, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Tohru Horiguchi, Kentaro Asahi, Hiroyuki Tobinaga
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Publication number: 20110166343Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: ApplicationFiled: March 14, 2011Publication date: July 7, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Publication number: 20110118278Abstract: There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.Type: ApplicationFiled: May 14, 2009Publication date: May 19, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Paolo Polucci
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Patent number: 7943654Abstract: There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR5 is at the ortho position to the CONH linker; R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C?O, or —C(?O)NH—; R5 is hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: July 10, 2006Date of Patent: May 17, 2011Assignee: Nerviano Medical Sciences S.R.L.Inventors: Daniele Fancelli, Jurgen Moll, Maurizio Pulici, Francesca Quartieri, Tizizno Bandiera
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Patent number: 7932250Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: GrantFiled: July 1, 2005Date of Patent: April 26, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Patent number: 7928231Abstract: Thienopyrazoles of formula I, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).Type: GrantFiled: March 26, 2009Date of Patent: April 19, 2011Assignee: Aventis Pharmaceuticals Inc.Inventors: John Gerard Jurcak, Matthieu Barrague, Timothy Alan Gillespy, Michael Louis Edwards, Kwon Yon Musick, Philip Marvin Weintraub, Yan Du, Ramalinga M. Dharanipragada, Ashfaq Ahmad Parkar
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Publication number: 20110086898Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism.Type: ApplicationFiled: October 7, 2010Publication date: April 14, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Kogyoku SHIN, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda, Kodo Shikata, Akira Inomata
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Patent number: 7906649Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: May 19, 2006Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
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Patent number: 7902376Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: January 22, 2009Date of Patent: March 8, 2011Assignees: Merck Sharp & Dohme Corp., Banyu Pharmaceutical Co., Ltd.Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110040088Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 25, 2010Publication date: February 17, 2011Inventors: Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Ovorak, Annette K. Kwok, Jimmiy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
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Patent number: 7884123Abstract: Compounds of formula (I), wherein R1 and R3 have the meanings given in the description, said compounds being in all isomeric forms; and salts thereof; processes for the preparation of the compounds and intermediates; compositions containing them, and the use thereof as medicaments, particularly as anti-cancer agents.Type: GrantFiled: May 23, 2007Date of Patent: February 8, 2011Assignee: Aventis Pharma S.A.Inventors: Jean-Christophe Carry, Gilles Doerflinger, Antony Bigot, Dominique Barbalat-Damour, François Clerc, Arielle Genevois-Borella, Baptiste Ronan, Hervé Minoux, Claude Barberis, Yves Janin
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Patent number: 7884117Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: GrantFiled: December 12, 2006Date of Patent: February 8, 2011Assignee: Pfizer Inc.Inventors: Junhun Zhang, Anle Yang, Susan Elizabeth Kephart, Liming Dong, Chuangxing Guo, Yufeng Hong, Mary Catherine Johnson, Indrawan James McAlpine, Jayashree Tikhe, Haitao Li
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Patent number: 7772261Abstract: The disclosure relates to a compound of formula (I): in which: R1, R2, R3 and R4 are as described in the specification, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these compounds and to certain intermediate products.Type: GrantFiled: January 21, 2009Date of Patent: August 10, 2010Assignee: sanofi-aventisInventors: Gilles Doerflinger, Jean-Christophe Carry
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Publication number: 20100184759Abstract: The present invention relates to compounds having the structural formula below and pharmacological activity towards the sigma (?) receptor, and more particularly to pyrano-pyrazole-amines, to processes of preparing such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: April 16, 2008Publication date: July 22, 2010Inventors: Bernhard Wünsch, Dirk Schepmann, Torsten Schläger, Daniel Zamanillo-Castanedo
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Patent number: 7750034Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 19, 2007Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7741350Abstract: 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: GrantFiled: October 20, 2009Date of Patent: June 22, 2010Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Patent number: 7737156Abstract: The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory.Type: GrantFiled: August 11, 2003Date of Patent: June 15, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Frank-Gerhard Böβ, Christina Erb, Martin Hendrix, Marja van Kampen, Frank Wunder
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Publication number: 20100137276Abstract: Compounds of formula (I), and salts and solvates thereof are provided: Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.Type: ApplicationFiled: November 1, 2007Publication date: June 3, 2010Inventors: Daniel Marcus Bradley, Wai Ngor Chan, Kevin Michael Thewlis, Simon Eward
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Publication number: 20100120863Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: November 12, 2009Publication date: May 13, 2010Inventors: Tesfaye Biftu, Ping Chen, Jason M. Cox, Ann E. Weber
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Publication number: 20100069341Abstract: This invention is directed to a tetrahydro-pyranopyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: ApplicationFiled: November 19, 2009Publication date: March 18, 2010Inventors: Fina Liotta, Huajun Lu, Michael P. Wachter, Mingde Xia
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Publication number: 20100056514Abstract: Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).Type: ApplicationFiled: March 26, 2009Publication date: March 4, 2010Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: John Gerard JURCAK, Matthieu BARRAGUE, Timothy Alan GILLESPY, Michael Louis EDWARDS, Kwon Yon MUSICK, Philip Marvin WEINTRAUB, Yan DU, Ramalinga M. DHARANIPRAGADA, Ashfaq Ahmad PARKAR
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Patent number: 7655683Abstract: The present invention is directed to novel imidazolopyrazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: February 1, 2007Date of Patent: February 2, 2010Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Zhihua Sui
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Publication number: 20100010008Abstract: Substituted pyrrolo-pyrazole 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 associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: October 9, 2007Publication date: January 14, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
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Publication number: 20090318440Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: December 12, 2006Publication date: December 24, 2009Inventors: Junhu Zhang, Anle Yang, Susan Elizabeth Kephart, Liming Dong, Chuangxing Guo, Yufeng Hong, Mary Catherine Johnson, Indrawan James Mc Alpine, Jayashree Tikhe, Haitao Li
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Publication number: 20090270467Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 19, 2007Publication date: October 29, 2009Applicant: MERCK & CO., INC.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7595320Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.Type: GrantFiled: August 29, 2007Date of Patent: September 29, 2009Assignee: Aventis Pharma S.A.Inventors: Claude Barberis, Jean-Christophe Carry, Gilles Doerflinger, Dominique Barbalat-Damour, Francois Clerc, Herve Minoux
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Publication number: 20090239924Abstract: Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C?O, or —C(?O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A 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 associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.Type: ApplicationFiled: May 25, 2007Publication date: September 24, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Daniele Fancelli, Maurizio Pulici, Jurgen Moll, Tiziano Bandiera
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Patent number: 7576087Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: June 19, 2007Date of Patent: August 18, 2009Assignee: WyethInventors: Ronald Charles Bernotas, Yinfa Yan
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Publication number: 20090187028Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: January 22, 2009Publication date: July 23, 2009Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Publication number: 20090149457Abstract: There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-NHZR5 is at the ortho position to the CONH linker; R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C?O, or —C(?O)NH—; R5 is hydrogen or an organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 10, 2006Publication date: June 11, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Daniele Fancelli, Jurgen Moll, Maurizio Pulici, Francesca Quartieri, Tiziano Bandiera
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Patent number: 7541378Abstract: Bicyclo-pyrazole compound of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, processes for their preparation, combinatorial libraries comprising a plurality of them and pharmaceutical compositions thereof, are herewith disclosed: the compounds of the invention are useful, in therapy, as protein kinase inhibitors, for instance in the treatment of cancer.Type: GrantFiled: July 11, 2003Date of Patent: June 2, 2009Assignee: Pfizer Italia S.r.l.Inventors: Roberto Tonani, Simona Bindi, Daniele Fancelli, Valeria Pittala′, Mario Varasi
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Publication number: 20090136513Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.Type: ApplicationFiled: March 2, 2007Publication date: May 28, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.LInventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
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Publication number: 20090131413Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: ApplicationFiled: July 1, 2005Publication date: May 21, 2009Applicant: ASUBIO PHARMA CO., LTD.Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Patent number: 7524964Abstract: The invention relates to a CB modulator compound of Formula (I) or a pharmaceutically acceptable form thereof and a method for use in treating, ameliorating or preventing a CB receptor mediated syndrome, disorder or disease.Type: GrantFiled: December 7, 2007Date of Patent: April 28, 2009Assignee: Janssen Pharmaceutica NVInventors: Fina Liotta, Huajun Lu, Mingde Xia, Michael P. Wachter
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Publication number: 20090099235Abstract: The invention provides compounds of Formula I wherein A, Y, R1, R1a, R2, and R2a are as described in the specification. Compounds of Formula I are useful in treating and/or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of preparing compounds of Formula I, and methods of treating cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: May 21, 2008Publication date: April 16, 2009Inventors: Darren Dressen, Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Matthew N. Mattson
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Patent number: 7518000Abstract: Thienopyrazoles of formula I, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).Type: GrantFiled: March 6, 2006Date of Patent: April 14, 2009Assignee: Aventis Pharmaceuticals, Inc.Inventors: John Gerald Jurcak, Matthieu Barrague, Timothy Alan Gillespy, Michael Louis Edwards, Kwon Yon Musick, Phillip Marvin Weintraub, Yan Du, Ramalinga M. Dharanipragada, Ashfaq Ahmed Parkar
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Publication number: 20090054397Abstract: The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 designates —(CO)h—(NRa)j—(CRb?CRc)k—Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like; Cy designates a 5- or 6-membered heteroaryl; and V each independently designate the formula -L-X—Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).Type: ApplicationFiled: April 29, 2008Publication date: February 26, 2009Inventors: Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Takashi Doko, Taro Terauchi, Yoshimitsu Naoe, Takafumi Motoki
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Patent number: 7485661Abstract: Bicyclo-pyrazoles of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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 associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: January 18, 2005Date of Patent: February 3, 2009Assignee: Pfizer Italia S.r.l.Inventors: Roberto Tonani, Simona Bindi, Daniele Fancelli, Valeria Pittala′, Matteo D'Anello
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Publication number: 20080293714Abstract: Disclosed are compounds of formula (I): (F) wherein Ri, R2, X and Ar are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: Joerg Martin Bentzien, Brian Nicholas Cook, Hidenori Takahashi
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Patent number: 7407971Abstract: A new class of pyrazolo derivative compounds having the formula where R and R1 have the meanings given herein. The pyrazolo derivative compounds are useful in treating cell proliferative disorders caused by and/or associated with an altered cell cycle dependent kinase activity in mammals. The compounds may be provided in pharmaceutical compositions or in a kit.Type: GrantFiled: December 4, 2003Date of Patent: August 5, 2008Assignee: Pfizer Italia S.r.l.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Patent number: 7402680Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: GrantFiled: September 15, 2004Date of Patent: July 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Dvorak, Annette K. Kwok, Jimmy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
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Publication number: 20080146542Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.Type: ApplicationFiled: August 29, 2007Publication date: June 19, 2008Applicant: Aventis Pharma S.A.Inventors: Claude BARBERIS, Jean-Christophe CARRY, Gilles DOERFLINGER, Dominique BARBALAT-DAMOUR, Francois CLERC, Herve MINOUX
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Patent number: 7365211Abstract: This invention relates to a method for modulating ?2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical compositions containing said compounds.Type: GrantFiled: August 11, 2004Date of Patent: April 29, 2008Assignee: Roche Palo Alto LLCInventors: Xao-Fa Lin, David Garrett Loughhead, Sanja Novakovic, Counde O'Yang, Michael Soth, David George Putman
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Patent number: 7351831Abstract: An intramolecular [3+2] cycloaddition reaction of a hydrazone is carried out under a mild condition with a high stereoselectivity and yield by reacting a hydrazone derivative in the presence of an asymmetric catalyst system obtained by mixing a zirconium alkoxide represented by the following formula (I): Zr(OR)4 ??(I) (wherein R is a hydrocarbon group which may have a substituent) with a binaphthol derivative represented by the following formula (II): (wherein Y1 and Y2 are each identical or different and denote a hydrogen atom or a halogen atom, and at least one of Y1 and Y2 denotes a halogen atom).Type: GrantFiled: March 11, 2003Date of Patent: April 1, 2008Assignee: Japan Science and Technology AgencyInventors: Shu Kobayashi, Yasuhiro Yamashita, Haruro Ishitani