Carbocyclic Ring Containing Patents (Class 546/194)
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Publication number: 20100093775Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: July 24, 2009Publication date: April 15, 2010Applicant: VIROCHEM PHARMA INC.Inventors: Real DENIS, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constatin G. Yannopoulos, Laval Chan Chun Kong
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Publication number: 20100093753Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20100093689Abstract: The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: ApplicationFiled: November 17, 2009Publication date: April 15, 2010Inventors: James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y.S. Lam
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Publication number: 20100087465Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.Type: ApplicationFiled: August 14, 2009Publication date: April 8, 2010Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
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Publication number: 20100081690Abstract: The present invention provides new compounds of formula I, wherein P, A, W, B, Q, R1 and R2 are defined as in formula I; invention compounds are positive allosteric modulators of metabotropic receptors—subtype 5 (“mGluR5”) which are useful for the treatment or prevention of central nervous system disorders such as for example: cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders in which the mGluR5 subtype of glutamate metabotropic receptor is involved.Type: ApplicationFiled: November 7, 2007Publication date: April 1, 2010Applicant: ADDEX PHARMA SAInventors: Emmanuel Le Poul, Giovanni Palombi, Jean-Philippe Rocher
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Publication number: 20100081691Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.Type: ApplicationFiled: December 8, 2009Publication date: April 1, 2010Applicant: LEXICON PHARMACEUTICALS, INC.Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
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Publication number: 20100075971Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: ApplicationFiled: December 1, 2009Publication date: March 25, 2010Inventors: Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
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Publication number: 20100075944Abstract: A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: ApplicationFiled: September 14, 2009Publication date: March 25, 2010Inventors: Tomohiro MATSUSHIMA, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
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Publication number: 20100076021Abstract: The present invention provides a compound of formula (I): said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: ApplicationFiled: November 13, 2007Publication date: March 25, 2010Inventors: Hidetomo Imase, Masashi Kishida
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Publication number: 20100075960Abstract: The present invention provides bezimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: March 25, 2010Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Patent number: 7683065Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 4, 2006Date of Patent: March 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Dewey Fanning, Paul Krenitsky, Pramod Joshi
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Publication number: 20100069363Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: November 17, 2007Publication date: March 18, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Joerg Keldenich
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Publication number: 20100069350Abstract: The present invention relates to certain new pyridin analogues of Formula (I), to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: July 2, 2007Publication date: March 18, 2010Applicant: ASTRAZENECA ABInventors: Thomas Antonsson, Peter Bach, David Brown, Ruth Bylund, Fabrizio Giordanetto, Lotta Jakobsson, Johan Johansson
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Publication number: 20100063091Abstract: The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: November 14, 2007Publication date: March 11, 2010Inventors: Daniel Dube, Michel Gallant, Erich L. Grimm, Helene Juteau, Sebastien Laliberte, Tom Yao-Hsiang Wu
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Publication number: 20100063092Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy.Type: ApplicationFiled: March 7, 2008Publication date: March 11, 2010Applicant: Ortho-Mcneil-Janssen Pharmaceuticals, Inc.Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lütjens
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Publication number: 20100063067Abstract: The present application describes modulators of MIP-1? of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R1, R2 and R8, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.Type: ApplicationFiled: October 3, 2007Publication date: March 11, 2010Inventors: Percy H. Carter, Lyndon A.M. Cornelius
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Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 7674803Abstract: The present invention relates to thiazolylpiperidine derivatives of the general formula (I): in which: A represents a radical chosen from the radicals a1 and a2 below: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3 below: and R1, R2, R2?, R3, R4, R5, Y and Z are as defined in the description. Application of the compounds of the formula (I) to the treatment of hypertriglyceridaemia, hypercholesterolaemia and dyslipidaemia.Type: GrantFiled: June 2, 2004Date of Patent: March 9, 2010Assignee: Merck Patent GmbHInventors: Philippe Guèdat, Francois Collonges, Hervé Dumas, Jean-Yves Ortholand, Jacques Decerprit, Jaxques Barbanton, Robert J. Foster, Peter Kane, Bernd Went
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Publication number: 20100056541Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: October 26, 2009Publication date: March 4, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Patent number: 7671055Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: October 20, 2005Date of Patent: March 2, 2010Assignee: FMC CorporationInventors: Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
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Patent number: 7671201Abstract: Certain novel phenyl substituted cyclic derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where B is a cyclic bridging group containing at least one N or N oxide link and a, A, b, B, c, d, D, L, M, R1 through R9, inclusively, and R13, R14 and R15 are fully described herein. In addition, novel intermediates useful in preparing compounds of Formula I, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: April 27, 2004Date of Patent: March 2, 2010Assignee: FMC CorporationInventors: George Theodoridis, Edward J. Barron, John W. Lyga, Y. Larry Zhang, Ping Ding, Frank J. Zawacki, Daniel H. Cohen, Matthew P. Whiteside
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Publication number: 20100048585Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicaType: ApplicationFiled: June 26, 2006Publication date: February 25, 2010Inventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guilliemont, David Francis Alain Lancois, Magali Madeleine Simone Motte, Ismet Dorange, Leo Jacobus Jozef Backx, Lieven Meerpoel
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Publication number: 20100048626Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Inventors: Bin SHAO, R. Richard Goehring, Samuel F. Victory, Qun Sun
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100041702Abstract: The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: March 25, 2008Publication date: February 18, 2010Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20100041667Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: September 19, 2007Publication date: February 18, 2010Inventor: Shaun R. Stauffer
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Publication number: 20100035880Abstract: This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)Type: ApplicationFiled: October 13, 2009Publication date: February 11, 2010Inventors: TAKESHI HANAZAWA, MISATO HIRANO, TADASHI INOUE, SATOSHI NAGAYAMA, KAZUNARI NAKAO, YUJI SHISHIDO, HIROTAKA TANAKA
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Publication number: 20100029651Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: May 25, 2007Publication date: February 4, 2010Inventors: Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan heitmeier
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Publication number: 20100029718Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: September 19, 2007Publication date: February 4, 2010Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov
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Publication number: 20100029687Abstract: [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: ApplicationFiled: November 14, 2007Publication date: February 4, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Publication number: 20100029650Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: December 5, 2007Publication date: February 4, 2010Inventors: Jing Fang, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy
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Patent number: 7655675Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: October 1, 2004Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Alan John Nadin, Andrew Pate Owens, Martin Richard Teall
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Publication number: 20100022589Abstract: Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are described.Type: ApplicationFiled: July 26, 2007Publication date: January 28, 2010Inventors: William McCoull, Martin Packer, James Stewart Scott, Paul Robert Owen Whittamore
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Patent number: 7652015Abstract: The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 25, 2006Date of Patent: January 26, 2010Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Jesus Andres Blas de Blas, Alfonso De Dios, Kevin John Hudziak, Tiechao Li, Beatriz López De Uralde-Garmendia, Mary Margaret Mader, Michael Ray Myers, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
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Publication number: 20100016343Abstract: The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate ?7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: ApplicationFiled: July 16, 2009Publication date: January 21, 2010Applicants: WYETH, SIENA BIOTECH S.P.A.Inventors: Chiara Ghiron, Michela Valacchi, Ugo Zanelli, Simon N. Haydar
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Publication number: 20100016598Abstract: The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate ?7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: ApplicationFiled: July 16, 2009Publication date: January 21, 2010Applicants: WYETH, SIENA BIOTECH S.P.A.Inventors: Michela Valacchi, Simon N. Haydar
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Publication number: 20100016360Abstract: The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate ?7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: ApplicationFiled: July 16, 2009Publication date: January 21, 2010Applicants: WYETH, SIENA BIOTECH S.P.A.Inventors: Simon N. Haydar, Chiara Ghiron, Michela Valacchi, Ugo Zanelli
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Publication number: 20100016358Abstract: The present invention is directed to a ?-globin inducer, to a prophylactic and/or therapeutic agent for sickle cell disease, and to a prophylactic and/or therapeutic agent for ?-thalassemia, each containing, as an active ingredient, 4-[N-(4-methoxyphenyl)-N-[[5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]methyl]amino]-1-[[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl]piperidine, a salt thereof, or a solvate of either of these.Type: ApplicationFiled: October 12, 2007Publication date: January 21, 2010Applicant: KOWA CO., LTD.Inventors: Masaki Yamabi, Takeshi Doi
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Publication number: 20100016337Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: ApplicationFiled: June 17, 2009Publication date: January 21, 2010Applicant: SANOFI-AVENTISInventors: Hartmut STROBEL, Paulus WOHLFART, Heinz-Werner KLEEMANN, Gerhard ZOLLER, David William WILL
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Publication number: 20100016361Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification.Type: ApplicationFiled: February 18, 2008Publication date: January 21, 2010Inventors: Rene Hersperger, Philipp Janser, Wolfgang Miltz
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Publication number: 20100009971Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20100009972Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20100010219Abstract: Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. A method of producing a compound represented by the following formula [8]: or a salt thereof, or a solvate thereof, from a compound represented by the following formula [2]: or a reactive derivative thereof, or a salt thereof, or a solvate thereof.Type: ApplicationFiled: June 5, 2009Publication date: January 14, 2010Applicant: JAPAN TOBACCO INC.Inventors: Kazuhito Harada, Takashi Ito
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Patent number: 7645775Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 21, 2005Date of Patent: January 12, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Cornelia Forster, Michael Arnost, Jian Wang
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Publication number: 20100004284Abstract: The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R1 and R2 are defined in the description. Invention compounds are useful for treating central or peripheral nervous system disorders and other disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia.Type: ApplicationFiled: May 17, 2006Publication date: January 7, 2010Applicant: ADDEX PHARMA SAInventors: Marco Farina, Stefania Gagliardi, Emmanuel Le Poul, Giovanni Palombi, Jean-Philippe Rocher
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Publication number: 20100004438Abstract: An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group -Z-R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: ApplicationFiled: December 4, 2006Publication date: January 7, 2010Inventors: Hironori Matsuyama, Kenji Ohnishi, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Kumi Higuchi, Keisuke Miyajima, Satoshi Yamada, Masaaki Motoyama, Yutaka Kojima, Koichi Yasumura, Takeshi Kodama, Shun Otsuji, Keizo Kan, Takumi Sumida
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Publication number: 20090325923Abstract: The present invention relates to the use of an inhibitor of the formation of nicotinamide adenyl dinucleotide for the preparation of a medicament used in the treatment of inflammatory diseases such as rheumatoid arthritis and endotoxemia.Type: ApplicationFiled: September 3, 2007Publication date: December 31, 2009Applicant: TOPOTARGET SWITZERLAND SAInventors: Oberdan Leo, Thibaut De Smedt, Frederic Van Gool, Mara Galli
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Publication number: 20090325980Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: ApplicationFiled: October 22, 2007Publication date: December 31, 2009Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Patent number: 7638531Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(?O)—, —C(?NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combinatioType: GrantFiled: December 19, 2006Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: Mwangi W. Mutahi, Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Manuel de Lera Ruiz, Kevin D. McCormick, Daniel M. Solomon, Henry A. Vaccaro, Junying Zheng, Purakkattle Biju, Younong Yu, Wei Zhou, Xiaohong Zhu
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Publication number: 20090318467Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: ApplicationFiled: June 15, 2009Publication date: December 24, 2009Inventors: Jean-Michel Adam, Johannes Aebi, Alferd Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche