Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Additional Six-membered Nitrogen Hetero Ring Patents (Class 514/253.13)
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Publication number: 20100234391Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Publication number: 20100234377Abstract: The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.Type: ApplicationFiled: April 7, 2008Publication date: September 16, 2010Applicant: Evotec AGInventors: Babette Aicher, Arndt-Rene Kelter, Thomas Stephen Coulter, Steven Taylor, Adams James Davenport, Thomas Hesterkamp, Christian Kirchhoff
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Publication number: 20100222319Abstract: The disclosure relates to compounds of formula (I): wherein A, Z, Z?, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.Type: ApplicationFiled: March 26, 2010Publication date: September 2, 2010Applicant: SANOFI-AVENTISInventors: Claude BERNHART, Monsif BOUABOULA, Pierre CASELLAS, Samir JEGHAM, Jèrome ARIGON, Romain COMBET, Sandrine HILAIRET, Pierre FRAISSE
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Publication number: 20100215661Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
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Publication number: 20100215652Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
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Publication number: 20100216784Abstract: Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing ?-amyloid production, ?-amyloid deposition, ?-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease ?-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.Type: ApplicationFiled: April 29, 2010Publication date: August 26, 2010Inventors: Michael J. Mullan, Daniel Paris, Pancham Bakshi
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Patent number: 7776862Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: August 17, 2010Assignee: Schering CorporationInventors: Brian F. McGuinness, Stuart B. Rosenblum, Joseph A. Kozlowski, Gopinadhan N. Anilkumar, Seong Heon Kim, Neng-Yang Shih, Chung-Her Jenh, Paul J. Zavodny, Douglas W. Hobbs, Guizhen Dong, Yuefei Shao, Lisa Guise Zawacki, Cangmeng Yang, Carolyn Dilanni Carroll
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Publication number: 20100190802Abstract: Disclosed are carboxamide compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: January 28, 2010Publication date: July 29, 2010Applicant: Rigel Pharmaceuticals Inc.Inventors: Ihab S. Darwish, Hui Hong, Rajinder Singh, Xiang Xu
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Publication number: 20100173888Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 17, 2009Publication date: July 8, 2010Inventors: Atli Thorarensen, John I. Trujillo, Wei Huang, Steve R. Turner, Simon Mantell, Ross Strang, Siew Kuen Yeap
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Publication number: 20100166889Abstract: The invention provides methods of treating depressive disorders, in particular major depression but other depressive orders also, with prodrug stimulants or analogs including amphetamine prodrugs, methylphenidate prodrugs, and methylphenidate analogs, Such methods of treatment may utilize the prodrug stimulant or analog as monotherapy or, more commonly, as an adjunct to antidepressant medication treatment to augment their effect. The invention includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered to an individual in need with one or more other active agents, either in separate forms or as a single pharmaceutical formulation. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: LCS GROUP, LLCInventor: Louis Sanfilippo
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Publication number: 20100168103Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N.Type: ApplicationFiled: September 14, 2007Publication date: July 1, 2010Applicant: NEUROMED PHARMACEUTICALS LTD.Inventors: Hassan Pajouhesh, Yanbing Ding, Hossein Pajouhesh, Richard Holland, Gabriel Hum
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Publication number: 20100152171Abstract: CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.Type: ApplicationFiled: February 17, 2010Publication date: June 17, 2010Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS
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Patent number: 7737142Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.Type: GrantFiled: January 20, 2006Date of Patent: June 15, 2010Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Publication number: 20100137332Abstract: The present invention relates to new piperazine modulators of NK-1 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 3, 2009Publication date: June 3, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
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Publication number: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100113405Abstract: The present invention relates to new methylindazole modulators of 5-HT3 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100105693Abstract: The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: January 5, 2010Publication date: April 29, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani
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Publication number: 20100105682Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X1 and X2 are linkers.Type: ApplicationFiled: October 12, 2007Publication date: April 29, 2010Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Ramesh Kaul
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Publication number: 20100093692Abstract: The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.Type: ApplicationFiled: February 27, 2008Publication date: April 15, 2010Applicant: Schering Corporation Sechering-Plough CorporationInventors: Robert G. Aslanian, Jean E. Lachowicz, Michael Y. Berlin, Joyce J. Hwa
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Publication number: 20100081667Abstract: The present invention provides a method for the treatment of emesis in a mammal being treated with an opiod analgesicType: ApplicationFiled: December 3, 2009Publication date: April 1, 2010Inventors: Giuseppe Alvaro, Romano Di Fabio, Paolo Maragni, Marsia Tampieri, Maria Elvira Tranquillini
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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: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20100035895Abstract: The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis.Type: ApplicationFiled: October 12, 2007Publication date: February 11, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Emmanuel Meyers
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Publication number: 20100029652Abstract: The invention provides a method of treating hepatitis C, by providing compound of Formula I (shown below) in combination with a second active agent to a patient infected with the hepatitis C virus. Also provided herein are pharmaceutical combinations comprising a compound of Formula I and a second active agent. The pharmaceutical combination may be a unit dosage form or a packaged pharmaceutical composition. Packaged pharmaceutical combinations include a compound of Formula I and a second active agent in a package with instructions for using the formulation to treat a hepatitis C infection.Type: ApplicationFiled: December 17, 2007Publication date: February 4, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Mingjun Huang, Joanne Fabrycki, Wengang Yang, Xingtie Nie, Avinash Phadke, Milind Deshpande
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Publication number: 20100029680Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: June 11, 2009Publication date: February 4, 2010Inventors: Bradley P. Morgan, David J. Morgans, JR., Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
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Publication number: 20100022539Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: September 15, 2009Publication date: January 28, 2010Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20100022556Abstract: A medicament comprising (±)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-[4-(diphenylmethyl)-1-piperazinyl]ethyl methyl ester (manidipine) or a physiologically acceptable salt and a statin or a physiologically acceptable salt.Type: ApplicationFiled: September 28, 2009Publication date: January 28, 2010Inventors: Roberto Fogari, Carmen Dell'Anna
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Publication number: 20100022555Abstract: The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.Type: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Paul John Beswick, Alister Campbell, Andrew Cridland, Robert James Gleave, Jag Paul Heer, Neville Hubert Nicholson, Lee William Page, Sadie Vile
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Patent number: 7648990Abstract: The present invention provides a method for the treatment of emesis in a mammal being treated with an opiod analgesic.Type: GrantFiled: October 1, 2007Date of Patent: January 19, 2010Assignee: GlaxoSmithKline LLCInventors: Giuseppe Alvaro, Paola Maragni, Marsia Tampieri
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Publication number: 20100003260Abstract: The present invention relates to compounds of general formula (I): wherein: R1 and R2, identical or different, represent: an atom of hydrogen or halogen, CN or NO2, with R1 and R2 not representing hydrogen simultaneously, m represents: 1 or 2 n represents: 0, 1 or 2 R3 represents: phenyl substituted or not by one or more residues chosen among halogen, hydroxyl or C1-C6 alkyl; C2-C6 alkyl substituted or not by one or more residues chosen among halogen or hydroxyl; cycloalkyl; pyridine; thiophene; pyrrole substituted or not by C1-C6 alkyl; thiazole or furan; or the therapeutically-acceptable salts or solvates thereof.Type: ApplicationFiled: June 19, 2007Publication date: January 7, 2010Inventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
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Publication number: 20090325964Abstract: The present teachings relate to piperazine metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators having Formula I: wherein the constituent variables are as defined herein. The present teachings further relate to methods for the preparation of the compounds, and to methods for using the compounds for treatment of diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety.Type: ApplicationFiled: May 22, 2009Publication date: December 31, 2009Applicant: WyethInventors: Matthew Gregory Bursavich, Adam Matthew Gilbert, Joseph Raymond Stock
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Publication number: 20090318448Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: ApplicationFiled: June 24, 2009Publication date: December 24, 2009Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Publication number: 20090312307Abstract: Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 11, 2009Publication date: December 17, 2009Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Publication number: 20090298833Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. 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 transplant rejection using said modulators are disclosed.Type: ApplicationFiled: July 20, 2009Publication date: December 3, 2009Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Publication number: 20090286801Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.Type: ApplicationFiled: June 21, 2007Publication date: November 19, 2009Inventors: Marc Capet, Denis Danvy, Nicolas Levoin, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Xavier Ligneau
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Publication number: 20090281089Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: April 8, 2009Publication date: November 12, 2009Applicant: Genentech, Inc.Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca L. LaLonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Patent number: 7615556Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b 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 said modulators are disclosed.Type: GrantFiled: January 23, 2007Date of Patent: November 10, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
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Publication number: 20090270409Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: September 4, 2008Publication date: October 29, 2009Applicant: IRM LLCInventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
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Publication number: 20090247499Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequalae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: August 17, 2007Publication date: October 1, 2009Inventors: Joan M. Fletcher, Tung M. Fong, William K. Hagmann, Petr Vachal
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Patent number: 7592347Abstract: The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: April 21, 2004Date of Patent: September 22, 2009Assignee: Glaxo Group LimitedInventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
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Publication number: 20090221583Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: June 23, 2008Publication date: September 3, 2009Applicants: FOREST LABORATORIES HOLDINGS LIMITED, AURIGENE DISCOVERY TECHNOLOGIES LIMITEDInventors: Alexander BISCHOFF, Hosahalli SUBRAMANYA, Kumar SUNDARESAN, Srinivasa Raju SAMMETA, Anil Kumar VAKA
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Publication number: 20090203676Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 30, 2006Publication date: August 13, 2009Inventors: Oscar Barba, Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Simon Andrew Swain
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Patent number: 7572786Abstract: This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: August 11, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Francois Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20090197894Abstract: 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 m, n, p, V, R1, R2, R3, R4, R5 and R6 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: April 14, 2009Publication date: August 6, 2009Applicant: XENON PHARMACEUTICALS INC.Inventors: Jian-Min Fu, Vishnumurthy Kodumuru, Shaoyi Sun, Michael D. Winther, Richard M. Fine, Daniel F. Harvey, Boris Klebansky, Mark P. Gray-Keller, Heinz W. Gschwend, Wenbao Li
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Publication number: 20090192160Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.Type: ApplicationFiled: April 2, 2009Publication date: July 30, 2009Inventors: Darren Jason MITCHELL, Jonathan Thomas Seal, Mervyn Thompson, Susan Marie Westway, Samantha Louisa Brown
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Publication number: 20090186876Abstract: The present invention relates to certain new pyridin analogues of Formula (I) [Chemical formula should be inserted here. Please see paper copy] Formula (I) to processes for preparing such compounds, to their utility in medicine in general and especially 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: June 26, 2007Publication date: July 23, 2009Applicant: ASTRAZENECA ABInventors: Kay Brickmann, Fredrik Zetterberg
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Publication number: 20090131447Abstract: This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.Type: ApplicationFiled: February 8, 2006Publication date: May 21, 2009Applicant: XENON PHARMACEUTICALS INC.Inventors: Rajender Kamboj, Michael D. Winther, Robert Fraser, Mikhail Chafeev, Sultan Chowdhury, Jian-Min Fu, Duanjie Hou, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Serguei Sviridov, Kashinath Sadalapure, Shaoyi Sun, Vishnumurthy Kodumuru, Nagasree Chakka, Zaihui Zhang, Melwyn Abreo, Mikhail A. Kondratenko, Daniel F. Harvey, Cindy J. Hudson, Wenbao Li, Chi Tu, Sengen Sun, Mark W. Holladay, Heinz W. Gschwend
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Publication number: 20090111831Abstract: Disclosed herein are novel compositions useful for the treatment of androgen dependant diseases.Type: ApplicationFiled: December 9, 2008Publication date: April 30, 2009Inventors: Larry Yun Fang, Prudence K. Bradley, Ping L. Lee
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Patent number: 7511141Abstract: One aspect of the present invention relates to piperidine-piperazine compounds. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. 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, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.Type: GrantFiled: August 29, 2005Date of Patent: March 31, 2009Assignee: Sepracor, Inc.Inventors: Paul E. Persons, Heike Radeke
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Publication number: 20090054456Abstract: The present invention relates to novel benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.Type: ApplicationFiled: July 24, 2006Publication date: February 26, 2009Inventors: Christopher Norbert Johnson, David Timothy Macpherson, Steven James Stanway, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway