1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte
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Publication number: 20110257178Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: October 7, 2010Publication date: October 20, 2011Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20110245223Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.Type: ApplicationFiled: December 1, 2010Publication date: October 6, 2011Applicant: Japan Tobacco Inc.Inventors: Hiroshi Yamamoto, Yasuhiro Ohe, Hiroyuki Goto, Kazuhito Harada, Shinji Yata, Takashi Ito, Jun Nishiu, Makoto Kakutani, Shunsuke Fujii, Kota Asahina
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Publication number: 20110230521Abstract: Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus 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 pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: May 1, 2009Publication date: September 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Christian Harcken, Thomas Wai-Ho Lee, Pingrong Liu, John Lord, CAN Mao, Wang Mao, Brain Christopher Raudenbush, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer
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Publication number: 20110218201Abstract: The compounds of Formula (I), are novel effective inhibitors of the type 4 phosphodiesterase.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Applicant: NYCOMED GMBHInventors: Imre Schlemminger, Beate Schmidt, Dieter Flockerzi, Hermann Tenor, Christof Zitt, Armin Hatzelmann, Degenhard Marx, Clemens Braun, Raimund Külzer, Anke Heuser, Hans-Peter Kley, Geert Jan Sterk
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Patent number: 8013163Abstract: The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.Type: GrantFiled: January 20, 2006Date of Patent: September 6, 2011Assignee: Astex Therapeutics LimitedInventors: Paul Graham Wyatt, David Charles Rees, Mladen Vinkovic, Gary Trewartha
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Patent number: 7989485Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.Type: GrantFiled: March 5, 2007Date of Patent: August 2, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Patent number: 7989475Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: GrantFiled: March 19, 2009Date of Patent: August 2, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110172274Abstract: This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, methods for preparing these compounds, novel intermediates useful for the synthesis of said compounds, methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as active ingredient, as well as the use of these pharmaceutical compositions for the treatment of obesity and obesity-related cardiovascular disorders, drug addiction, cognition deficits, liver fibrosis and inflammatory disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: ApplicationFiled: June 15, 2009Publication date: July 14, 2011Inventors: Josephus H.M. Lange, Bernard J. Vliet, Van
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Publication number: 20110172415Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 14, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Patent number: 7977358Abstract: The invention is concerned with novel pyrazol derivatives of formula (I), wherein R1, R2, R3, R4, X and Y are as defined herein, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor and/or CCR-5 receptor and can be used as medicaments.Type: GrantFiled: July 16, 2008Date of Patent: July 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20110166139Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: ApplicationFiled: June 15, 2009Publication date: July 7, 2011Applicant: ASTRAZENECA ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
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Publication number: 20110160188Abstract: Embodiments of the present disclosure include methods for identifying a compound or compounds useful as therapeutic agents in the treatment of paramyxovirus infections, compounds for the treatment of measles, and high throughput screening methods for identifying compounds capable of inhibiting the proliferation of a paramyxovirus.Type: ApplicationFiled: February 11, 2008Publication date: June 30, 2011Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
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Publication number: 20110152520Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.Type: ApplicationFiled: January 28, 2011Publication date: June 23, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Yoshikazu TAKAOKA, Shiro SHIBAYAMA, Rena NISHIZAWA
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Publication number: 20110144080Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: December 23, 2004Publication date: June 16, 2011Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITALInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Publication number: 20110144345Abstract: The benzoyl derivative of the present invention is represented by formula (I) (in the formula, E represents an alkoxy group, an alkoxycarbonyl group or the like, R1 represents a halogen atom, an organic group or the like, p represents an integer of 0 to 3, R2 and R3 each independently represents an alkyl group or the like, Q represents a group selected from the groups represented by the following formulas Q1 to Q8: (in the formula, * represents binding site, G represents oxygen atom or the like), R4 to R5, R8 to R13 represents hydrogen atom, an alkyl group or the like), R6 represents cyano group or the like, X represents —C(R12)(R13)— or —N(R12)—, Y represents oxo group, an alkyl group or the like, m represents an integer of 0 to 4)) or salt thereof.Type: ApplicationFiled: August 3, 2009Publication date: June 16, 2011Applicant: NIPPON SODA CO., LTD.Inventors: Tetsuo Tamai, Kazuaki Tsukuda, Shigeo Yamada, Yasuhiro Miyashita, Shingo Hirai
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Publication number: 20110137040Abstract: The invention relates to a novel chemical route to 3,4-diaryl-4,5-dihydro-(1H)-pyrazole-1-carbox-amidine derivatives, known as potent cannabinoid-CB1 receptor antagonists, and to novel intermediates of these compounds. The synthetic route produced considerably higher yields than those reported, without the use of corrosive reagents. The process concerns the preparation of a compound of formula (I): wherein the symbols have the meanings given in the description.Type: ApplicationFiled: July 30, 2009Publication date: June 9, 2011Inventors: Josephus H.M. Lange, Hans J. Sanders, Jeroen Van Rheenen
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Patent number: 7943653Abstract: This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: August 11, 2008Date of Patent: May 17, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Mingde Xia, Meng Pan, Michael P. Wachter
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Publication number: 20110112088Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110105505Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 28, 2009Publication date: May 5, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNGInventors: Frank Stieber, Timo Heinrich, Dirk Wienke
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Publication number: 20110105562Abstract: The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: Michael H. Parker, Dennis J. Hlasta, Yifang Huang, Allen B. Reitz, Edward C. Lawson, Carsten Schubert, Eric Strobel, Brett A. Tounge, Kimberly White, Michael P. Winters, Shyamali Ghosh
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Publication number: 20110105456Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: December 22, 2010Publication date: May 5, 2011Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Matin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Patent number: 7932401Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: July 14, 2005Date of Patent: April 26, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7923004Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: GrantFiled: October 15, 2007Date of Patent: April 12, 2011Assignee: XTL Biopharmaceuticals Ltd.Inventors: Guolin Li, Reza Fathi, Zhen Yang, Yun Liao, Qiang Zhu, Angela Lam, Anthony Sandrasagra, Kenneth Nawoschik, Hyun-Joon Cho, Jie Cao, Wu Ruoqiu, C. Richard Wobbe, Yixin Liu
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Patent number: 7919496Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: April 5, 2011Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vishnumurthy Kodumuru, Shifeng Liu, Shaoyi Sun, Nagasree Chakka
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Publication number: 20110071289Abstract: Disclosed is a compound represented by the formula (1) below or a pharmaceutically acceptable salt thereof, which is useful as an agent for prevention and/or treatment of diabetes and the like. (In the formula, RA and RB independently represent an optionally substituted alkyl group or the like; RC represents an optionally substituted alkyl group or the like; RD represents a hydrogen atom or the like; RE represents a hydrogen atom or the like; and RF represents a group selected from those represented by the formulae (G1) below: wherein one hydrogen atom serves as a bonding hand, or the like.Type: ApplicationFiled: August 6, 2008Publication date: March 24, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Yoshihiro Horiuchi, Noriko Nunami, Hiroto Tatamidani, Eiko Ohata
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Publication number: 20110065707Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Publication number: 20110059938Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
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Patent number: 7902181Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 10, 2008Date of Patent: March 8, 2011Assignee: AstraZeneca ABInventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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(5R)-1,5-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-3-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY
Publication number: 20110053983Abstract: Embodiments of the invention relate to (5R)-1,5-diaryl-4,5-dihydro-1H-pyrazole-3-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said dihydropyrazole derivatives, to methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders involving cannabinoid receptors. The compounds of embodiments of the invention are compounds of formula (I) wherein the symbols have the meanings given in the specification.Type: ApplicationFiled: April 22, 2009Publication date: March 3, 2011Inventors: Josephus H.M. Lange, Arnold P. Den Hartog, Bernard J. Van Vliet -
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: 20110039829Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: June 17, 2010Publication date: February 17, 2011Applicant: SANOFI-AVENTISInventors: Marc NAZARÉ, Gernot ZECH, Jochen GOERLITZER, Melitta JUST, Tilo WEISS, Gerhard HESSLER, Werngard CZECHTIZKY, Sven RUF
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Publication number: 20110034511Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)? or N?; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively.Type: ApplicationFiled: September 28, 2010Publication date: February 10, 2011Applicant: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Michael Philip Cohen, Sandra Ann Filla, Kevin John Hudziak, Daniel Timothy Kohlman, Dana Rae Benesh, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Brian Michael Mathes
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Patent number: 7884102Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: April 28, 2008Date of Patent: February 8, 2011Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20110028517Abstract: The present invention relates to 4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide, and pharmaceutically acceptable salts and solvates thereof. It further concerns pharmaceutical compositions comprising this compound as active ingredient as well as processes and intermediates for preparing this compound and compositions. The referred compound is a cannabinoid CB1 neutral antagonist useful in the prophylaxis and treatment of food intake disorders.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Susana Yenes Minguez
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Publication number: 20110020460Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: June 4, 2010Publication date: January 27, 2011Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20110015178Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: March 13, 2009Publication date: January 20, 2011Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003799Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: September 8, 2010Publication date: January 6, 2011Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20100324091Abstract: A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis.Type: ApplicationFiled: June 23, 2008Publication date: December 23, 2010Applicant: Kowa Company, Ltd.Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
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Publication number: 20100323965Abstract: The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.Type: ApplicationFiled: August 10, 2010Publication date: December 23, 2010Applicant: STATegics, Inc.Inventors: Jeffrey R. SPENCER, Juha Punnonen
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Publication number: 20100305085Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.Type: ApplicationFiled: October 12, 2007Publication date: December 2, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
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Patent number: 7834046Abstract: This invention relates to thiophene compounds of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to treat cannabinoid-receptor mediated disorders.Type: GrantFiled: October 2, 2007Date of Patent: November 16, 2010Assignee: National Health Research InstitutesInventors: Kak-shan Shia, Chia-Liang Tai, Jyh-hsiung Liao, Ming-shiu Hung, Yu-Sheng Chao
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Publication number: 20100280066Abstract: This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity, and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: ApplicationFiled: July 9, 2010Publication date: November 4, 2010Inventors: Jay S. Tung, Lee H. Latimer, Jing Wu, Albert Garofalo, Michael A. Pleiss, Darren Dressen, Ashley Guinn, Scott A. Jenkins, Jennifer Sealy, John Tucker, David W.G. Wone
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Publication number: 20100267687Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: ApplicationFiled: November 13, 2008Publication date: October 21, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Patent number: 7816361Abstract: Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 independently represent H, or C1-C6 alkyl; R3 represents H; F; CI; Br, —NO2; —CN; C1-C6 alkyl optionally substituted by F or CI; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O)NR6R7, —NR7C(?O)R6, —NR7C(?O)OR6, —NHC(?O)NR7R6 or —NHC(?S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —CF3; —OH; —SH; —Type: GrantFiled: November 2, 2004Date of Patent: October 19, 2010Assignee: Medigene LimitedInventor: Ian Richard Matthews
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Publication number: 20100256186Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 31, 2010Publication date: October 7, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20100249091Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally subsType: ApplicationFiled: September 17, 2009Publication date: September 30, 2010Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Patent number: 7803799Abstract: This invention relates to selenophene compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat cannabinoid-receptor mediated disorders.Type: GrantFiled: July 3, 2007Date of Patent: September 28, 2010Assignee: National Health Research InstitutesInventors: Kak-Shan Shia, Jing-Po Tsao, Chia-Liang Tai, Wan-Ping Hsieh, Ming-Shiu Hung, Jen-Shin Song, Yu-Sheng Chao