Abstract: 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:
Grant
Filed:
September 3, 2010
Date of Patent:
September 4, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
Type:
Application
Filed:
October 26, 2011
Publication date:
August 23, 2012
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
Type:
Grant
Filed:
February 16, 2007
Date of Patent:
August 14, 2012
Assignee:
Luitpold Pharmaceuticals, Inc.
Inventors:
James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G. Schiro, Hongmei Huang, Michael Evans, Yongxin Han
Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
Type:
Grant
Filed:
November 22, 2006
Date of Patent:
May 29, 2012
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.
Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
Abstract: An object of the present invention is to provide a base generator which has sensitivity and is applicable to a wide range of applications, and a photosensitive resin composition which is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The base generator generates a base by exposure to electromagnetic radiation and heating. The photosensitive resin composition comprises a polymer precursor in which reaction into a final product is promoted by the base generator and a basic substance or by heating in the presence of a basic substance.
Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
Abstract: The invention relates to a process for the preparation of secondary nitroxide radicals from their corresponding secondary amines by oxidation with an organic peracid, comprising the steps a) adding to a reaction vessel a secondary amine, optionally together with an organic solvent and in one batch a base selected from the group consisting of alkali metal, alkaline earth metal or ammonium bicarbonates and alkaline earth metal or ammonium carbonates or mixtures thereof in the form of a solid together with water or as an aqueous slurry; b) dosing a peracid under stirring to the reaction mixture in an amount of 1.0 to 2.5 mol per mol of secondary amine; and c) isolating the organic phase.
Type:
Grant
Filed:
August 11, 2010
Date of Patent:
March 13, 2012
Assignee:
BASF SE
Inventors:
Peter Nesvadba, Lucienne Bugnon, Martin Von Büren
Abstract: 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:
Grant
Filed:
December 17, 2009
Date of Patent:
March 13, 2012
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
Abstract: 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:
Grant
Filed:
October 26, 2009
Date of Patent:
February 28, 2012
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
Abstract: The invention relates to novel substituted piperidines, 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 cardiovascular disorders and tumour disorders.
Type:
Application
Filed:
March 12, 2010
Publication date:
February 23, 2012
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
Type:
Application
Filed:
October 24, 2011
Publication date:
February 16, 2012
Applicant:
INCYTE CORPORATION
Inventors:
Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
Abstract: The invention relates to substituted tetrahydronaphthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one substituted tetrahydronaphthalene according to the invention or derivative thereof, and to the use of the substituted tetrahydronaphthalenes according to the invention and to derivatives thereof as MCH antagonists.
Type:
Application
Filed:
February 12, 2010
Publication date:
January 19, 2012
Applicant:
SANOFI
Inventors:
Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.
Type:
Grant
Filed:
November 15, 2007
Date of Patent:
January 3, 2012
Assignee:
Sanofi-Aventis
Inventors:
Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Application
Filed:
February 16, 2010
Publication date:
December 22, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W 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:
Grant
Filed:
November 3, 2010
Date of Patent:
November 29, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Eric L. Stangeland, Aaron Kushner, Craig Husfeld
Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
Type:
Grant
Filed:
May 4, 2010
Date of Patent:
November 22, 2011
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
Abstract: Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
Type:
Grant
Filed:
November 30, 2007
Date of Patent:
November 22, 2011
Assignee:
Merck Canada Inc.
Inventors:
Nicolas Lachance, Chun Sing Li, Jean-Philippe Leclerc, Yeeman K. Ramtohul
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
Type:
Application
Filed:
June 23, 2011
Publication date:
November 17, 2011
Applicant:
ELI LILLY AND COMPANY
Inventors:
Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
Type:
Application
Filed:
July 6, 2011
Publication date:
October 27, 2011
Applicant:
NOVARTIS AG
Inventors:
Werner BREITENSTEIN, Takeru EHARA, Claus EHRHARDT, Philipp GROSCHE, Yuko HITOMI, Yuki IWAKI, Takanori KANAZAWA, Kazuhide KONISHI, Juergen Klaus MAIBAUM, Keiichi MASUYA, Atsuko Nihonyanagi, Nils OSTERMANN, Masaki SUZUKI, Atsushi TOYAO, Fumiaki YOKOKAWA
Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as “MC compounds”), which, inter alia, are useful in treatment of cancer. 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 treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
Type:
Application
Filed:
November 24, 2009
Publication date:
September 29, 2011
Applicant:
MERLION PHARMACEUTICALS PTE LTD
Inventors:
Rustum S. Boyce, Muhammad Sofian Asi Sihombing, Hiroki Sone
Abstract: Novel compounds of the formula (I), wherein the substituents are as defined in claim 1; compositions containing them and their use as insecticides, acaricides, nematicides or molluscicides.
Type:
Application
Filed:
November 30, 2009
Publication date:
September 15, 2011
Applicant:
SYNGENTA CROP PROTECTION LLC
Inventors:
Michel Muehlebach, Thomas Pitterna, Andre Jeanguenat, Myriem El Qacemi, Roger Graham Hall, Andrew Edmunds, Camilla Corsi, Andre Stoller, Christopher Richard Godfrey, Jurgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Jerome Yves Cassayre
Abstract: The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is —NH—R1 or of Formula (V) or (VI), R1 is —(CH2)n—R2, R2 is a linear, branched or cyclic C1C6 aliphatic group, —O—(CH2)n—CH3, —NH—CO—(CH2)n—CH3, a 5- or 6-membered aliphatic or aromatic ring optionally comprising a heteroatom, a 5- or 6-membered aromatic ring substituted by one or two substituents, said substituents being selected from the group consisting of —OH, —O(alkyl C1C3) and —OCO(alkyl C1C3), or of Formula (V), R3 is H or a C1-C3 aliphatic group and R4 is a linear C1-C3 or a branched C3-C12 aliphatic group, or R3 is a C1-C3 aliphatic group and R4 is a linear C1-C12 aliphatic group, Y is O, CH—(CH2)n—CH3 or N(CO)(CH2)n—CH3, and n is an integer from O to 6.
Type:
Application
Filed:
November 6, 2009
Publication date:
September 1, 2011
Inventors:
Mario Brufani, Ilaria Medici, Rinaldo Marini Bettolo, Luisa Maria Migneco, Rolando Marzella, Rocco Figliola, Angela La Bella
Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.
Type:
Application
Filed:
August 4, 2009
Publication date:
August 11, 2011
Applicant:
SUMMIT CORPORATION PLC
Inventors:
Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed.
Abstract: The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.
Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
Type:
Application
Filed:
December 19, 2007
Publication date:
June 2, 2011
Applicants:
GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITED
Inventors:
Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.
Abstract: Disclosed are salts of methyl 2-((R)-(3-chlorophenyl)((R)-1-((S)-2-(methylamino)-3-((R)-tetrahydro-2H-pyran-3-yl)propylcarbamoyl)piperidin-3-yl)methoxy)ethylcarbamate and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.
Type:
Application
Filed:
June 24, 2009
Publication date:
May 12, 2011
Inventors:
Nicole Marie Deschamps, David H. Igo, Mark Bryan Mitchell
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
Type:
Grant
Filed:
May 15, 2007
Date of Patent:
May 10, 2011
Assignee:
IRM LLC
Inventors:
David C. Tully, Arnab K. Chatterjee, Hank Michael James Petrassi, Badry Bursulaya, Glen Spraggon
Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.
Type:
Application
Filed:
June 20, 2008
Publication date:
May 5, 2011
Applicants:
NHWA PHARMA. CORPORATION, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
Inventors:
Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
Abstract: An embodiment of the composition contains any of compounds of the formula A-LG in which A represents any of residues of general formula (A-1) below and LG represents any of groups that are cleaved to generate acids of the formula A-H when acted on by an acid. The composition further contains at least one of a compound that generates an acid when exposed to actinic rays or radiation and a compound that generates an acid when heated.
Type:
Application
Filed:
October 28, 2010
Publication date:
May 5, 2011
Applicant:
FUJIFILM Corporation
Inventors:
Tomotaka TSUCHIMURA, Takeshi Kawabata, Takayuki Ito
Abstract: Mucic acid salts of a compound represented by the following structural formula: are disclosed. In particular, single crystalline mucic acid salts of the compound represented by structural formula (I) are characterized by a variety of properties and physical measurements. Methods of producing the mucic acid salts, using the salts to antagonize one or more aspartic proteases, and methods of treating a number of aspartic protease mediated disorders using the salts are described herein.
Type:
Application
Filed:
August 5, 2010
Publication date:
April 28, 2011
Inventors:
David A. Claremon, Robert D. Simpson, Lanqi Jia
Abstract: This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.
Type:
Grant
Filed:
June 1, 2004
Date of Patent:
March 29, 2011
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Usha V. Ramesh, Gary Charles Look, Rajinder Singh, Sarkiz D. Issakani
Abstract: According to one embodiment, an actinic-ray- or radiation-sensitive resin composition includes any of the compounds (A) of general formula (I) below that when exposed to actinic rays or radiation, generates an acid and a resin (B) whose rate of dissolution into an alkali developer is increased by the action of an acid. (The characters used in general formula (I) have the meanings mentioned in the description.
Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I): and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Abstract: [Problems] To provide a modulator for signaling of TLR [Means for solving the problems] A medicament containing cathepsin inhibitor such as monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate as a active ingredient is used as a modulator for signaling of TLR, a therapeutic agent for treating diseases associated with TLR signaling, a therapeutic agent for treating diseases associated with induction of Th17 cells, a therapeutic agent for treating diseases associated with production of IL-6, IL-12, IL-17, or IL-23, or a therapeutic agent for treating systemic lupus erythematosus, lupus nephritis, crohn's disease, psoriasis, or acute disseminated encephalomyelitis.
Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 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:
Grant
Filed:
July 19, 2007
Date of Patent:
December 14, 2010
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.
Type:
Grant
Filed:
March 4, 2008
Date of Patent:
December 7, 2010
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins
Abstract: The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
Type:
Grant
Filed:
September 25, 2006
Date of Patent:
November 16, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
H. Donald Burns, Terence G. Hamill, Craig W. Lindsley
Abstract: A method of generating synthetic metabolites of CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples.
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Type:
Grant
Filed:
March 12, 2009
Date of Patent:
October 19, 2010
Assignee:
Sepracor Inc.
Inventors:
Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
Type:
Grant
Filed:
November 6, 2008
Date of Patent:
October 5, 2010
Assignee:
Galderma Research & Development
Inventors:
Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
Abstract: The present invention relates to small molecule modulators of melanin expression and methods of making the small molecules. Also disclosed are methods of increasing pigmentation in a cell which involve providing compounds of the present invention and contacting a cell with the compounds under conditions effective to induce melanin expression in the cell, thereby increasing pigmentation. The present invention also relates to compositions containing compounds of the present invention and a carrier.
Type:
Application
Filed:
March 28, 2008
Publication date:
September 16, 2010
Applicant:
UNIVERSITY OF ROCHESTER
Inventors:
Benjamin L. Miller, Brian R. McNaughton, Peter Gareiss, Glynis Scott
Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each indepen
Type:
Grant
Filed:
October 20, 2006
Date of Patent:
September 7, 2010
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn