Additional Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/217.03)
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Publication number: 20110201589Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.Type: ApplicationFiled: August 10, 2009Publication date: August 18, 2011Applicant: EVOTEC AGInventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xialou Wang
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Publication number: 20110200553Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: April 7, 2011Publication date: August 18, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammed Arshad Siddiqui, Wuyi Wang, Constanin G. Yannopoulos
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Publication number: 20110172208Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Patent number: 7973030Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: GrantFiled: February 25, 2005Date of Patent: July 5, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
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Publication number: 20110152234Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
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Publication number: 20110129542Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 12, 2008Publication date: June 2, 2011Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil
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Patent number: 7915249Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. 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: January 25, 2006Date of Patent: March 29, 2011Assignee: Janssen Pharmaceutical NVInventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20110015182Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.Type: ApplicationFiled: July 16, 2010Publication date: January 20, 2011Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
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Publication number: 20100292218Abstract: The present invention provides compounds of formulae Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va and the therapeutic use thereof. The present invention also includes methods of treating NF2-deficient or NF1-deficient cells or neurodegenerative diseases with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. Furthermore, the present invention is directed to methods of inhibiting the growth of NF2-deficient or NF1-deficient tumors. The methods comprise contacting NF2-deficient or NF1-deficient tumor cells with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. The present invention is also directed to the combinational use of radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va with at least one additional active agent, such as one or more HSP90 inhibitors.Type: ApplicationFiled: December 4, 2009Publication date: November 18, 2010Inventors: Ruihong CHEN, Allan E. Rubenstein, Jin-Chen Yu, Nicolas Winssinger, Sofia Barluenga
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Publication number: 20100267696Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: December 11, 2008Publication date: October 21, 2010Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20100184745Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2 NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 mType: ApplicationFiled: January 25, 2010Publication date: July 22, 2010Applicant: UNIVERSITY OF KENTUCKYInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20100179130Abstract: The present invention relates to the use of piperine and derivatives thereof for the preparation of a pharmaceutical composition for treating and/or preventing a neuronal condition where there is a need of neuroprotection and/or neuroregeneration. The invention furthermore relates to the use of piperine and derivatives thereof for the in vitro differentiation of neural stem cells and the use of such pre-treated cells for stem cell therapy von neurological conditions.Type: ApplicationFiled: July 3, 2008Publication date: July 15, 2010Applicant: SYNGIS Bioscience GmbH & Co. KGInventors: Armin Schneider, Anja Moraru, Carola Krüger, Rico Laage, Claudia Pitzer
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Publication number: 20100130468Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 20, 2008Publication date: May 27, 2010Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Patent number: 7700584Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.Type: GrantFiled: May 26, 2005Date of Patent: April 20, 2010Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
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Publication number: 20100035861Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both ACHE and A? aggregation. The most potent compound inhibited both ACHE and BCHE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.Type: ApplicationFiled: July 24, 2007Publication date: February 11, 2010Inventors: Zhuibai Qiu, Qiong Xie, Hongzhuan Chen, Hao Wang, Zheng Xia, Meiyan Lu
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Patent number: 7615549Abstract: The present invention relates to new substituted pyrrolidinones of general formula wherein A, X, B and R1 to R9 are as defined above, or a tautomer or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: December 16, 2005Date of Patent: November 10, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Henning Priepke, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar, Peter Kuehn, Georg Dahmann
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Patent number: 7598237Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2007Date of Patent: October 6, 2009Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Patent number: 7576088Abstract: The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.Type: GrantFiled: February 22, 2005Date of Patent: August 18, 2009Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Konrad Bleicher, Wolfgang Guba, Wolfgang Haap, Dagmar Kube, Thomas Luebbers, Jean-Marc Plancher, Olivier Roche, Mark Rogers-Evans, Gisbert Schneider, Jochen Zuegge
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Patent number: 7569604Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: GrantFiled: June 22, 2005Date of Patent: August 4, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
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Patent number: 7563784Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: April 25, 2006Date of Patent: July 21, 2009Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20090176761Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor.Type: ApplicationFiled: July 12, 2006Publication date: July 9, 2009Applicant: LABORATORIES SERONO SAInventors: Stephen S. Palmer, Selvaraj Nataraja
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Publication number: 20090176762Abstract: This invention relates to the use of a JNK inhibitor for treating and/or preventing skin diseases selected from psoriasis and dermatitis.Type: ApplicationFiled: June 1, 2007Publication date: July 9, 2009Applicant: LABORATOIRES SERONO SAInventors: Chiara Ferrandi, Jean-Pierre Gotteland, Christoph H. Ladel, Paola Zaratin
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Publication number: 20090054396Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: ApplicationFiled: September 8, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Mei Su, Dingwei Yu, Stephanie Springer
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Publication number: 20090036428Abstract: An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety. The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric/duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.Type: ApplicationFiled: February 22, 2007Publication date: February 5, 2009Applicant: Astellas Pharma Inc.Inventors: Masakatsu Kawakami, Yoshihiro Keto, Ken Ikeda, Mari Fukuda, Junji Sato
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Patent number: 7476663Abstract: The present invention relates to new substituted thiophene-2-carboxylic acid amides of general formula wherein A, and R1 to R8c are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: May 10, 2005Date of Patent: January 13, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Roland Pfau, Henning Priepke, Kai Gerlach, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar, Sandra Handschuh
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Publication number: 20080306047Abstract: The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R1 denotes amino, alkylamino, dialkylamino, amidino, alkylamidino, N-hydroxyamidino, or N-alkoxyamidino, Y denotes sulfonyl or carbonyl and R2 and R4 independently represent various organic residues, in the treatment or prevention of cardiac arrhythmia and/or in treatment or prevention of diseases in association with ischemic heart conditions.Type: ApplicationFiled: November 16, 2006Publication date: December 11, 2008Inventors: Manica Cerne, Uros Urleb, Metka V. Budihna, Gorazd Drevensek, Luka Peternel
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Publication number: 20080260837Abstract: The present invention concerns methods of making physically stable aqueous suspensions of sparingly soluble to insoluble in water, active pharmaceuticals. More particularly, the invention provides an aqueous pharmaceutical suspension composition comprising an active pharmaceutical component which is sparingly soluble to insoluble in water; a water soluble, low viscosity grade cellulose polymer with a viscosity range of 3 mPa·s to 50 mPa·s as a surfactant; a suspending agent; and water.Type: ApplicationFiled: April 20, 2007Publication date: October 23, 2008Inventors: Ranga R. Namburi, Bala Murali K. Vattikuti, Ratna Prabha Mulamalla, Burgise F. Palkhiwala
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Patent number: 7405209Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 14, 2005Date of Patent: July 29, 2008Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Robert Wells Marquis, Jr., Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080146545Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: August 10, 2007Publication date: June 19, 2008Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20080113945Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: August 20, 2007Publication date: May 15, 2008Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Patent number: 7329654Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.Type: GrantFiled: December 2, 2002Date of Patent: February 12, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
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Patent number: 7279468Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the ?v?3 integrin receptor, their use, and pharmaceutical preparations comprising these compounds.Type: GrantFiled: June 15, 2001Date of Patent: October 9, 2007Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Andreas Kling, Udo Lange, Werner Seitz, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger, Arnulf Lauterbach
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Patent number: 7253205Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a variety of substituents, ring A is a phenyl or pyridyl ring; d is zero, 1 or 2; and pharmaceutically acceptable salts and N-oxides thereof.Type: GrantFiled: June 10, 2002Date of Patent: August 7, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7223750Abstract: Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl, (C1–C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1–C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. Therapeutic application.Type: GrantFiled: January 3, 2003Date of Patent: May 29, 2007Assignee: Sanofi-AventisInventors: Frédéric Galli, Odile LeClerc, Alistair Lochead, Alain Nedelec
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Patent number: 7202237Abstract: The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.Type: GrantFiled: May 19, 2004Date of Patent: April 10, 2007Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet Østergaard Nielsen
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Patent number: 7148221Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: December 12, 2006Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 6974808Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.Type: GrantFiled: November 27, 2001Date of Patent: December 13, 2005Assignee: Bristol-Myers Squibb CompanyInventor: James R. McCarthy
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Patent number: 6953789Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.Type: GrantFiled: January 13, 2004Date of Patent: October 11, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Patent number: 6927209Abstract: The present invention relates to novel compounds of formula (I): in which: R1, R2 and R3, which are identical or different, are each independently: a (C1-C6)alkyl group, a pyridinyl group or a group —CH2—NR4R5, in which R4 and R5 are each independently a hydrogen atom or a (C1-C4)alkyl group, or alternatively R4 and R5 form, with the nitrogen atom to which they are bonded, a pyrrolidinyl, piperidinyl, hexahydroazepinyl, morpholinyl or piperazinyl group, with the proviso that at least one of the substituents R1, R2 and R3 is other than a (C1-C6)alkyl group, and their salts, solvates and hydrates, especially those which are pharmaceutically acceptable. These compounds are useful particularly for the treatment of disorders of the venous circulation.Type: GrantFiled: May 6, 2002Date of Patent: August 9, 2005Assignee: Laboratoires Fournier S.A.Inventors: Véronique Barberousse, Soth Samreth
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Patent number: 6908914Abstract: The invention relates to benzene derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of psychotic disorders.Type: GrantFiled: June 27, 2000Date of Patent: June 21, 2005Assignee: Sanofi-SynthelaboInventors: Robert Boigegrain, Martine Bourrie, Pierre Lair, Raymond Paul, Martine Poncelet, Jean Claude Vernieres
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6881733Abstract: The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification.Type: GrantFiled: July 21, 2000Date of Patent: April 19, 2005Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Brian Eugene Cunningham, Matthew Joseph Fisher, William Harlan Gritton, Cynthia Darshini Jesudason, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Matthew Robert Reinhard, Roger Ryan Rothhaar, Freddie Craig Stevens, Leonard Larry Winneroski, Yanping Xu, Yao-Chang Xu
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Patent number: 6858623Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: May 29, 2003Date of Patent: February 22, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene R. Hickey, Weimin Liu, Usha R. Patel, Denice M. Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Patent number: 6852713Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.Type: GrantFiled: April 16, 2003Date of Patent: February 8, 2005Assignee: Adolor CorporationInventors: Roland E. Dolle, Paul Anson Tuthill
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Publication number: 20040220179Abstract: The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.Type: ApplicationFiled: April 21, 2004Publication date: November 4, 2004Inventors: Tianbao Lu, Karen L. Milkiewicz, Pierre Raboisson, Maxwell David Cummings, Raul R. Calvo, Daniel J. Parks, Louis V. Lafrance, Juan Jose Marugan Sanchez, Joan Gushue, Kristi Leonard
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Publication number: 20040209865Abstract: The present invention relates to alkyne compounds of general formula I 1Type: ApplicationFiled: October 30, 2003Publication date: October 21, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Klaus Rudolf, Philipp Lustenberger, Kirsten Arndt, Ralf R.H. Lotz, Martin Lenter
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Patent number: 6803370Abstract: Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 20, 2001Date of Patent: October 12, 2004Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu