Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/323)
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Patent number: 7790751Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Wyeth LLCInventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Kevin Liu, Geraldine Ruth McFarlane, Cristina Grosanu, Jennifer Rebecca Lo, Albert Jean Robichaud
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Patent number: 7790752Abstract: This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the azaspiro-head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.Type: GrantFiled: September 21, 2006Date of Patent: September 7, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20100221247Abstract: The present application describes compositions that are useful for the treatment, prevention and/or amelioration of cancer.Type: ApplicationFiled: September 29, 2009Publication date: September 2, 2010Inventors: Robert BENDER, Charles H. GRAHAM, Christine D. COPPLE
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Publication number: 20100222363Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: September 2, 2010Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Publication number: 20100222322Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: September 2, 2010Applicant: MERCK & CO., INC.Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
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Publication number: 20100222324Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).Type: ApplicationFiled: February 3, 2010Publication date: September 2, 2010Applicant: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Publication number: 20100222388Abstract: The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT1B/1D receptor agonist, a tryptamine derivative, an ergoline derivative, a non-steroidal anti-inflammatory drug, or an analgesic, or any combination thereof.Type: ApplicationFiled: February 26, 2010Publication date: September 2, 2010Applicant: Helsinn Therapeutics (U.S.), Inc.Inventor: William J. Polvino
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Patent number: 7786142Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I), as IL-6 inhibitors, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, their metabolites and prodrugs thereof. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).Type: GrantFiled: October 12, 2006Date of Patent: August 31, 2010Assignee: Orchid Research Laboratories, Ltd.Inventors: Siripragada Mahender Rao, Akella Satya Surya Visweswara Srinvas, Shikha Rani, Gaddam Om Reddy, Sriram Rajagopal, Uma Ramachandran, Duddu Savaraiah Sharada, Rajagopalan Nirmala, Velaiah Sivasudar, Lakshmanan Manikandan, Ramachandran Balaji
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Publication number: 20100216833Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Patent number: 7781436Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: GrantFiled: July 25, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7776884Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.Type: GrantFiled: February 10, 2006Date of Patent: August 17, 2010Assignee: Bristol-Myers Squibb CompanyInventor: Robert J. Cherney
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Publication number: 20100204276Abstract: Compounds of formula (I): wherein: R1 represents an alkyl, cycloalkyl or cycloalkylalkyl group, R2 and R3, together with the nitrogen atom carrying them, form a heterocycle having from 5 to 8 ring members, and n represents from 2 to 6. Medicinal products containing the same which are useful in treating disorders of the to melatoninergic system.Type: ApplicationFiled: October 17, 2007Publication date: August 12, 2010Applicant: LES LABORATOIRES SERVIERInventors: Pascal Marchand, Vincent Babonneau, Sylvie Piessard, Muriel Duflos, Jean Albert Boutin, Valerie Audinot, Philippe Delagrange, Daniel-Henri Caignard
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Patent number: 7772253Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: May 26, 2006Date of Patent: August 10, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
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Publication number: 20100196369Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Inventor: Jerome B. Zeldis
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Publication number: 20100197657Abstract: The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents.Type: ApplicationFiled: September 22, 2008Publication date: August 5, 2010Inventors: Ronald K. Chang, Christina Ng Di Marco, Scott D. Kuduk
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Publication number: 20100197723Abstract: Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.Type: ApplicationFiled: December 3, 2009Publication date: August 5, 2010Inventors: Shomir GHOSH, Gali Golan, Boaz Inbal, Vincent Jacques, Mercedes Lobera
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Publication number: 20100197673Abstract: The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.Type: ApplicationFiled: August 18, 2008Publication date: August 5, 2010Applicant: LG Life Sciences LtdInventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Chul Woong Chung, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Patent number: 7767692Abstract: 4-substituted 1-amidomethylcarbonyl-piperidine compounds having motilin-agonistic properties and their acid addition salts, pharmaceutical compositions containing these compounds, processes and intermediate products for the preparation of these compounds, and methods of treatment utilizing these compounds.Type: GrantFiled: November 10, 2003Date of Patent: August 3, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Jochen Antel, Ulf Preuschoff, Reinhard Brueckner, Holger Sann, Michael Wurl, Peter Eickelmann
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Publication number: 20100190768Abstract: The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof: wherein R1 is aralkyl, etc.; R2 is H, etc.; —W4?W5—W6?W7— is a group of the formula: —CR4?CR5—CR6?CR7— (in which R4, R5, R6 and R7 are independently a group of the formula: -E-A (E is a single bond, etc., A is H or nitro, etc.)), etc.; R8 is a group of the formula: —OR11 (R11 is H, etc.), etc.; R9 is trifluoromethyl, etc.; R10 is a group of the formula: —[C(R13)(R14)]n—R15 (R13 and R14 are independently H, etc., n is an integer of 0 to 10, R15 is a group of the formula: N(R18)R19 (R18 and R19 form a nitrogen-containing heteromonocycle together with a nitrogen atom to which they are bonded), etc.).Type: ApplicationFiled: September 29, 2006Publication date: July 29, 2010Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Toshihiko Sone, Rieko Sawaki, Tomoko Nakajima
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Publication number: 20100189683Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Ascenta Therapeutics, Inc.Inventors: Jon T. Holmlund, Mel Sorensen, Lance Leopold, Dajun Yang
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Publication number: 20100190767Abstract: Compounds of formula 1 and hetero derivatives thereof and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Inventors: Ralf ANDERSKEWITZ, Horst Dollinger, Rolf Goeggel, Birgit Jung, Joerg Kley, Juergen Mack, Peter Nickolaus, Rainer Walter
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Patent number: 7759365Abstract: Disclosed are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, R7, A, B, D-E, Y, i, j, n and m are defined as below. The compounds of formula 1 are useful as agonists or antagonists of CCR-3. The present invention is also directed to pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 26, 2006Date of Patent: July 20, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Domnic Martyres, Pascale Pouzet, Christoph Hoenke, Peter Seither, Silke Hobbie, Thierry Bouyssou
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Publication number: 20100179146Abstract: 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: ApplicationFiled: June 26, 2009Publication date: July 15, 2010Inventors: 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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Publication number: 20100178331Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.Type: ApplicationFiled: December 25, 2007Publication date: July 15, 2010Inventors: Ryoichi Nagata, Shunji Haruta
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Publication number: 20100179122Abstract: Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Craig W. Lindsley, William H. Leister, Scott E. Wolkenberg
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Publication number: 20100179145Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: July 15, 2010Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Patent number: 7754737Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: GrantFiled: October 7, 2005Date of Patent: July 13, 2010Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Patent number: 7754725Abstract: Compounds having the formula (I): and in particular, those of subgenus VIIa are disclosed as inhibits or modulators of the activity of the heat shock protein Hsp90. As such they are useful for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma.Type: GrantFiled: March 1, 2007Date of Patent: July 13, 2010Assignee: Astex Therapeutics Ltd.Inventors: Gianni Chessari, Maria Grazia Carr, Miles Stuart Congreve, Robert Downham, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
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Patent number: 7754736Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4 and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: October 7, 2008Date of Patent: July 13, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Jean-Marc Plancher, Olivier Roche, Rosa Maria Rodriguez-Sarmiento
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Publication number: 20100172959Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.Type: ApplicationFiled: December 31, 2009Publication date: July 8, 2010Applicant: ACINO AGInventors: Heike HAUSNER, Sebastian BRAUN, Heiko SPILGIES
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Publication number: 20100173925Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R1, R2, R3, R4 and R5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.Type: ApplicationFiled: June 24, 2009Publication date: July 8, 2010Inventors: Chikara Uchida, Hiroki Sone, Kiyosho Kawamura
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Publication number: 20100173935Abstract: Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G1, G2, G3, G4, R1, R2, X, Y, Z and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: June 8, 2007Publication date: July 8, 2010Applicant: AstraZeneca ABInventors: Yun-Xing Cheng, Shujuan Jin, Mehrnaz Pourashraf, Miroslaw Tomaszewski
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Patent number: 7750039Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: GrantFiled: February 13, 2009Date of Patent: July 6, 2010Assignee: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
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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: 20100168168Abstract: The present invention provides aminoaryl sulphonamide derivatives of formula (I), useful in the treatment of a CNS disorder related to or affected by the 5-HT6 receptor. Pharmacological profiles of these components include high affinity binding with 5-HT6 receptors along with good selectivity towards the receptor. The present invention also includes stereoisomers, the salts, methods of preparation and medicine containing the aminoaryl sulphonamide derivatives.Type: ApplicationFiled: October 26, 2005Publication date: July 1, 2010Applicant: Suven Life Sciences, Ltd.Inventors: Venkata Satya Nirogi Ramakrishna, Vikas Shreekrishna Shirsath, Rama Sastri Kambhampati, Santosh Vishwakarma, Nagaraj Vishwottam Kandikere, Srinivasulu Kota, Venkateswarlu Jasti
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Patent number: 7745479Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 27, 2006Date of Patent: June 29, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Valerie Runtz-Schmitt, Sven Taylor
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Publication number: 20100159034Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100160318Abstract: 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.Type: ApplicationFiled: December 3, 2007Publication date: June 24, 2010Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D CO., LTD.Inventors: Feng Tang, Han Shen, Qiu Jin, Lei Ding, Jie Yang, Xiaojin Yin, Shiyue Lu
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Publication number: 20100160305Abstract: 3,4,5-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 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds are of the formula I, wherein the substitutents are as defined in the specification.Type: ApplicationFiled: March 7, 2006Publication date: June 24, 2010Applicant: NOVARTIS AGInventors: Keiichi Masuya, Fumiaki Yokokawa, Osamu Irie, Atsuko Nihonyanagi, Takeru Ehara, Kazuhide Konishi, Takanori Kanazawa, Masaki Suzuki
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Publication number: 20100160378Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject, as well as compositions and methods for providing migraine pain relief. The compositions include at least one alkyl glycoside and at least one therapeutic agent, such as a 5-HT receptor agonist, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Applicant: Aegis Therapeutics LLCInventor: Edward T. Maggio
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Patent number: 7741343Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.Type: GrantFiled: October 30, 2007Date of Patent: June 22, 2010Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
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Patent number: 7741342Abstract: Thalidomide derivative (I) and their bases or salts are new: where R represents CHR1NR2R3, CHR1NR4C(O)CHR5NR2R3, W or CHR5NR4C(O)W, where R1, R4 and R5 represent independently each other H, C1-4 alkyl, R2 is a C1-4 alkyl, R3 is a C1-4 alkyl, or R2 and R3 together represents 1,3-propylene, 1,4-butylene, 1,5-pentylene, 1,6-hexylene, W represents 4-, 5-, 6-, 7-, or 8-mumbered, saturated or unsaturated heterocycle. The invention also relates to processes of production thereof and the use of thereof as an active pharmaceutical ingredient.Type: GrantFiled: March 4, 2004Date of Patent: June 22, 2010Inventor: Hesheng Zhang
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Patent number: 7741326Abstract: Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.Type: GrantFiled: November 8, 2007Date of Patent: June 22, 2010Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
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Publication number: 20100152166Abstract: Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.Type: ApplicationFiled: July 11, 2008Publication date: June 17, 2010Applicant: ELI LILLY AND COMPANYInventors: Michael James Genin, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Alan M. Warshawsky
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Publication number: 20100144790Abstract: ?-secretase (BACE) is a biomarker for MCI and Alzheimer's disease. BACE1 protein level and the enzymatic activity level increase in the brain, and in the CSF in AD and MCI patients. Increased BACE1 levels in CSF are related to neuronal death and synaptic damages, which contribute to AD-related cognitive deficits. BACE1 inhibitors may be used as therapeutic compounds for clinical use for the disease treatment and prevention. Use of Thalidomide, an effective BACE1 inhibitor, reduces the BACE1 enzymetic activity and protein levels, and the A? production that marks the neurodegenerative progression associated with AD.Type: ApplicationFiled: December 4, 2009Publication date: June 10, 2010Inventors: Yong Shen, Marwan N. SABBAGH
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Publication number: 20100137363Abstract: The present invention relates generally to substituted indoles and methods of using them.Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Applicant: Wyeth LLCInventors: Baihua HU, James W. Jetter
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Patent number: 7728008Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: June 1, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Patent number: 7723361Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.Type: GrantFiled: March 31, 2005Date of Patent: May 25, 2010Assignee: Celgene CorporationInventor: Robert D'Amato
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Patent number: 7723357Abstract: Described herein are methods and compositions for the treatment of spinal disorders mediated by nucleus pulposus. The compositions can include thalidomide or a thalidomide derivative.Type: GrantFiled: April 14, 2008Date of Patent: May 25, 2010Assignee: Sciaticon ABInventors: Kjell Olmarker, Bjorn Rydevik