Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/323)
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Publication number: 20110150873Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.Type: ApplicationFiled: December 10, 2008Publication date: June 23, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventor: David John Grainger
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Publication number: 20110151018Abstract: The present invention is directed towards methods of inhibiting thermo- and chemo-sensing in insects and pests by inhibiting TRPA1 ion gated channel or family members. The present invention is also directed towards methods of insect control by modulating the TRPA1 ion gated channel or family members. The methods are applicable to a wide variety of insects and pests including agricultural and horticultural pests.Type: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Applicant: BRANDEIS UNIVERSITYInventors: Paul Garrity, KyeongJin Kang
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Patent number: 7964593Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.Type: GrantFiled: November 20, 2009Date of Patent: June 21, 2011Assignee: UCB Pharma, S.A.Inventors: Jean-Philippe Starck, Benoit Kenda
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Publication number: 20110144158Abstract: This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: February 17, 2011Publication date: June 16, 2011Inventors: George W. MULLER, Roger Shen-Chu Chen, Hon-Wah Man, Alexander L. Ruchelman
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Publication number: 20110144108Abstract: Novel 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: ApplicationFiled: January 17, 2011Publication date: June 16, 2011Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Publication number: 20110136807Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: June 29, 2007Publication date: June 9, 2011Applicant: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, JR.
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Patent number: 7956070Abstract: Compounds of formula (I): are modulators of chemokine (for example CCR3) activity (for use in, for example, treating asthma).Type: GrantFiled: January 31, 2005Date of Patent: June 7, 2011Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Peter Cage, Mark Furber, Elizabeth Kinchin, Christopher Luckhurst, Aaron Rigby
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Patent number: 7956082Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: July 20, 2006Date of Patent: June 7, 2011Assignee: Shionogi & Co., LtdInventors: Akira Kugimiya, Michitaka Shichijo, Yoshiharu Hiramatsu, Natsuki Ishizuka
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Publication number: 20110124674Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
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Publication number: 20110124656Abstract: The present invention relates to methods for the treatment or prevention of symptoms associated with post-traumatic stress disorder, and related pharmaceutical compositions. Of particular interest are pharmaceutical compositions comprising a very low dose of cyclobenzaprine, alone, or in combination with an alpha-1-adrenergic receptor antagonist, a beta-adrenergic antagonist, an anticonvulsant, a selective serotonin reuptake inhibitor or a serotonin-norepinephrine reuptake inhibitor.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Applicant: TONIX PHARMACEUTICALS, INC.Inventors: Lederman Seth, Harris Herbert
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Publication number: 20110118189Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 24, 2009Publication date: May 19, 2011Inventors: Stephen J. Farr, John Turanin, Roger Hawley, Jeffrey A. Schuster
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Publication number: 20110105503Abstract: 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: ApplicationFiled: June 20, 2008Publication date: May 5, 2011Applicants: NHWA PHARMA. CORPORATION, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
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Patent number: 7932394Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.Type: GrantFiled: November 1, 2005Date of Patent: April 26, 2011Assignee: MSD K.K.Inventors: Noriaki Hashimoto, Keiji Takahashi, Chisato Nakama, Yoshio Ogino, Fumiko Sakai, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20110091459Abstract: The present invention relates to new imidazole modulators of M3 muscarinic acetylcholine receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 11, 2009Publication date: April 21, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
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Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Publication number: 20110086836Abstract: The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.Type: ApplicationFiled: April 5, 2007Publication date: April 14, 2011Applicant: Santhera Pharmaceuticals (Schweiz) AGInventors: Michael Soeberdt, Holger Deppe, Philipp Weyermann, Stephan Bulat, Andreas Von Sprecher, Achim Feurer, Cyrille Lescop, Marco Hennebohle, Sonja Nordhoff
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Publication number: 20110086839Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: June 18, 2009Publication date: April 14, 2011Inventors: Jose Luis Castro Pineiro, Xichen Lin, Quan Liu, Kevin Meng, Feng Ren, David R. Vesey, Baowei Zhao
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Publication number: 20110086860Abstract: A compound represented by Formula (I) is provided: wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar2 represents a phenyl group which may be substituted with 1 to 3 substituents; X1 represents (1) —C?C— or (2) a double bond etc., which may be substituted; R1 and R2 represent, for example, a C1-6 alkyl group which may be substituted, or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.Type: ApplicationFiled: December 21, 2010Publication date: April 14, 2011Inventors: Teiji KIMURA, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Kogyoku Shin, Takehiko Miyagawa, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Hiroaki Hagiwara
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Publication number: 20110082117Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 27, 2010Publication date: April 7, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20110077269Abstract: Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: September 10, 2010Publication date: March 31, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Corey Anderson
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Publication number: 20110077272Abstract: A pharmaceutical composition includes triptans, such as sumatriptan, and may be used in therapy. The composition may be administered via the inhaled route.Type: ApplicationFiled: February 2, 2009Publication date: March 31, 2011Applicant: Vectura LimitedInventor: Mark Jonathan Main
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Patent number: 7915283Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: January 17, 2008Date of Patent: March 29, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Kap-Sun Yeung, Zhongxing Zhang, Zhiwei Yin, Zhilei Qui, Daniel H. Deon, Clint A. James, Edward H. Ruediger, Carol Bachand
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Publication number: 20110071132Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.Type: ApplicationFiled: July 30, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
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Publication number: 20110064698Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Publication number: 20110065750Abstract: The present invention provides for new crystalline and amorphous forms of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione, and methods of making the same.Type: ApplicationFiled: September 17, 2010Publication date: March 17, 2011Applicant: ScinoPharm Taiwan Ltd.Inventors: Chen-Tung CHEN, Inze Lin
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Publication number: 20110065685Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: ApplicationFiled: June 14, 2010Publication date: March 17, 2011Applicant: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
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Publication number: 20110059971Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: IPSEN S.A.S.Inventors: Christophe THURIEAU, Jérôme Gonzalez, Christophe Moinet
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Publication number: 20110059965Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: ApplicationFiled: July 6, 2010Publication date: March 10, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
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Publication number: 20110059953Abstract: Compounds of formula (I): wherein X is selected from CRX and N; RN1 is selected from H and C1-4 alkyl, which may be substituted by SH or halo; RG1 is selected from H and SH; RC2 is selected from H and optionally substituted C1-7 alkyl; RC3 is selected from H and optionally substituted C1-7 alkyl; Rx is selected from H, OH and NH2; RC4 is selected from: (i) an optionally substituted C3-12 N-containing heterocyclyl; (ii) C(?O)NRN5RN6, where RN5 and RN6 are independently selected from H, optionally substituted C1-7 alkyl, optionally substituted C3-20 heterocyclyl and optionally substituted C5-20 aryl or RN5 and RN6 and the nitrogen atom to which they are attached form an optionally substituted N-containing C5-7 heterocyclyl group; (iii) C(?O)ORO1, where RO1 is selected from H, optionally substituted C1-7 alkyl, optionally substituted C3-20 heterocyclyl and optionally substituted C5-20 aryl; (iv) C(?O)NHNHSO2RS1, where RS1 is selected from H, optionally substituted C1-7 alkyl, optionally substituted C3-20 heterocType: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Inventors: Frank Boeckler, Andreas Joerger, Alan Fersht
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Publication number: 20110059966Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.Type: ApplicationFiled: November 10, 2010Publication date: March 10, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emilie Porter Huck
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Publication number: 20110059955Abstract: The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.Type: ApplicationFiled: August 18, 2010Publication date: March 10, 2011Applicant: SANOFI-AVENTISInventors: Loic FOULON, Laurent GOULLIEUX, Brigitte POUZET, Claudine SERRADEIL-LE GAL, Gerard VALETTE
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Publication number: 20110053925Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: March 3, 2011Inventors: Young Shin CHO, Lei JIANG, Michael SHULTZ, Christine Hiu-Tung CHEN, Gang LIU, Jianke LI
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Patent number: 7897602Abstract: Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decreasing the activity of a protein kinase and for treating a protein kinase-related disease, such as cancer, with these compounds.Type: GrantFiled: June 26, 2009Date of Patent: March 1, 2011Assignee: Development Center for BiotechnologyInventors: Jiann-Jyh Huang, Chao-Cheng Chiang, Chiawei Liu, Chun-Liang Lai, Shu Fu Lin, Yu-Hsiang Lin, Ru-Wen Wang, Sheng-Chuan Yang, Jia-Ming Chang, Shih-Hsien Chuang, Paonien Chen
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Patent number: 7897601Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.Type: GrantFiled: January 16, 2007Date of Patent: March 1, 2011Assignees: Intervet, Inc., Intervet International B.V.Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Keith A. Eagen, Jack D. Scott, Yuguang Wang, Yan Xia, William J. Greenlee
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Publication number: 20110045064Abstract: Pharmaceutical compositions and single unit dosage forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer or an inflammatory disease.Type: ApplicationFiled: May 19, 2010Publication date: February 24, 2011Inventors: Anthony TUTINO, Michael T. Kelly
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Publication number: 20110039800Abstract: The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.Type: ApplicationFiled: July 2, 2010Publication date: February 17, 2011Inventors: Jean-Marc AIACHE, Dominique Costantini, Christine Chaumont
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Publication number: 20110038856Abstract: Methods of treating cancer and autoimmune and inflammatory diseases are provided.Type: ApplicationFiled: November 2, 2007Publication date: February 17, 2011Applicant: Seattle Genetics, Inc.Inventors: Jonathan G. Drachman, May Kung Sutherland, Eric Sievers, Grant Risdon, Ezogelin Gruyters, Alan Wahl, Tim Lewis
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Publication number: 20110039830Abstract: The present invention relates to cyclic indole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 28, 2010Publication date: February 17, 2011Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Bodo SCHEIPER, Hans MATTER, Hans Ulrich STILZ, Gary MCCORT
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Publication number: 20110038832Abstract: Provided herein are methods of treating macular degeneration, which comprises administering to a patient in need thereof a therapeutically effective amount of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: August 16, 2010Publication date: February 17, 2011Inventor: Jerome B. ZELDIS
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Patent number: 7888510Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: GrantFiled: July 29, 2004Date of Patent: February 15, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Publication number: 20110034417Abstract: Novel 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: ApplicationFiled: October 5, 2010Publication date: February 10, 2011Applicant: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Publication number: 20110034440Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: April 10, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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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: 20110028474Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.Type: ApplicationFiled: August 10, 2010Publication date: February 3, 2011Applicant: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORKInventors: David G. Hangauer, JR., Moustafa E. El-Araby, Karen L. Milkiewicz
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Publication number: 20110021567Abstract: Processes for the preparation of substantially pure lenalidomide. The application also relates to an enriched, substantially pure, and pure amorphous form of lenalidomide and solid dispersions containing amorphous lenalidomide.Type: ApplicationFiled: March 11, 2009Publication date: January 27, 2011Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Rajasekhar Kadaboina, Veerender Murki, Amarendhar Manda, Venkata Rao Badisa, Naresh Vemula, Rama Seshagiri Rao Pulla, Venu Nalivela
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Publication number: 20110014205Abstract: The present invention provides methods and compositions for treating chronic pelvic pain syndrome. In particular, the present invention provides methods and compositions for treating chronic pelvic pain syndrome with an agent that targets MCP-1, MIP-1?, or the CCR-2 receptor.Type: ApplicationFiled: September 14, 2010Publication date: January 20, 2011Inventors: Anthony J. Schaeffer, David Klumpp, Praveen Thumbikat
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Publication number: 20110015228Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: September 27, 2010Publication date: January 20, 2011Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20110009384Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: February 5, 2008Publication date: January 13, 2011Inventors: Taisuke Tawaraishi, Hiroshi Imoto, Nobuo Cho