At 1-position Patents (Class 546/226)
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Publication number: 20090005355Abstract: The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino group, R2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or —N(R3)—, R3 is hydrogen atom or an optionally substituted alkyl group, R4a and R4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or may be bonded to each other at the both ends to form an alkylene group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.Type: ApplicationFiled: July 1, 2005Publication date: January 1, 2009Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Tsutomu Miyake, Takeshi Yamanaka, Hidetoshi Asai, Yoshihiro Terakawa
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Publication number: 20080306054Abstract: The invention provides a compound for use as an inhibitor of Hsp90, the compound having 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; C1-5 hydrocarbyl and C1-5 hydrocarbyloxy; wherein the C1-5 hydrocarbyl and C1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C1-2 alkoxy, amino, mono- and di-C1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C1-5 hydrocarbyl-amino, wherein the acyclic C1-5 hydrocarbyl group and the mono and di-C1-5 hydrocarbylamino moieties in each instance are optionally substitType: ApplicationFiled: April 13, 2006Publication date: December 11, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead
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Publication number: 20080293753Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.Type: ApplicationFiled: October 6, 2006Publication date: November 27, 2008Inventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20080293701Abstract: 1-Acylamino-2-hydroxy-3-amino-?-arylalkanes of formula I. and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.Type: ApplicationFiled: February 1, 2006Publication date: November 27, 2008Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng, Salvacion Cacatian, Colin Tice, Robert D. Simpson, Wei Zhao
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Patent number: 7452878Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: May 18, 2005Date of Patent: November 18, 2008Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
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Publication number: 20080262226Abstract: A method is provided for making compounds comprising a beta-adrenergic inhibiting moiety and a linking moiety, the method comprising: a) reacting a compound of formula (A): (R1—(CH—O—CH2)) with at least one of NH3, NH4, NH4ClNH3 and R12?NH2 thereby forming a compound of formula (B): (R1—CH(OH)—CH2—NHR12?); and b) reacting a compound of formula (B) with a compound of formula (C): (R3?O), thereby forming a compound of formula (D): (R1—COH—CH2—N(R3)(R12?)), wherein R1 comprises the beta-adrenergic inhibiting moiety or comprises the beta-adrenergic inhibiting moiety when bonded to —COH—CH2—N(R12?)— of formula (D); R3 comprises the linking moiety and is bonded to the =0 of formula (C) via a carbon atom; and R12? is selected from hydrogen and a protecting group.Type: ApplicationFiled: November 7, 2007Publication date: October 23, 2008Applicant: ARTESIAN THERAPEUTICS, INC.Inventor: Gang Chen
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Patent number: 7435851Abstract: The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.Type: GrantFiled: September 29, 2006Date of Patent: October 14, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: Mark A. Scialdone
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Publication number: 20080234281Abstract: The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: March 18, 2005Publication date: September 25, 2008Inventors: Robert M. Garbaccio, Christy M. Olson, Edward S. Tasber, Maricel Torrent
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Patent number: 7425641Abstract: The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.Type: GrantFiled: September 10, 2004Date of Patent: September 16, 2008Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Henning Priepke, Armin Heckel, Herbert Nar, Wolfgang Wienen, Jean Marie Stassen
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Publication number: 20080200512Abstract: The invention provides a compound of formula: and methods for making and using the same, where R1 and R2 are independently hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 is hydrogen, halogen, C1-6 alkyl or C1-6 alkoxy; R4 is hydrogen or halogen; and R5 is a mono- or di-amino acid moiety, a succinic acid moiety, a urea moiety, or a derivative thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, and methods for making and using the same.Type: ApplicationFiled: February 14, 2008Publication date: August 21, 2008Inventors: Jeffrey Mark Blaney, Normand Hebert, Stephanie Ann Hopkins, Elizabeth A. Jefferson, Masaki Tomimoto
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Publication number: 20080200466Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.Type: ApplicationFiled: May 22, 2006Publication date: August 21, 2008Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine Leblanc, David Andrew Sandham
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Publication number: 20080200511Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).Type: ApplicationFiled: June 16, 2004Publication date: August 21, 2008Applicant: ASTON UNIVERSITYInventors: Martin Griffin, Ian George Coutts, Robert Edward Saint
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Publication number: 20080194537Abstract: The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.Type: ApplicationFiled: May 23, 2006Publication date: August 14, 2008Inventors: Ole Thastrup, Jens Chr. Norrild
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Publication number: 20080194633Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 1, 2007Publication date: August 14, 2008Inventors: Xiangping Qian, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
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Publication number: 20080194536Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: April 14, 2006Publication date: August 14, 2008Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
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Patent number: 7410971Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.Type: GrantFiled: December 24, 2004Date of Patent: August 12, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Publication number: 20080188654Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory, diseases, immunological diseases and cancer.Type: ApplicationFiled: December 20, 2007Publication date: August 7, 2008Applicant: Theracos, Inc.Inventors: Partha Neogi, Debedranath Dey, Joseph C. Fuller, Liang Chen, Ta-Kai Li
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Publication number: 20080188659Abstract: This invention relates to methods for preparing halogenated amines.Type: ApplicationFiled: February 7, 2008Publication date: August 7, 2008Applicant: WyethInventors: Eddine Saiah, Huan-Qiu Li, Adrian Huang
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Publication number: 20080161325Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 13, 2007Publication date: July 3, 2008Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
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Patent number: 7390905Abstract: The present invention relates to a piperidine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted hydoxyl group, a substituted thiol group, a substituted sulfonyl group, etc., or a group represented by the formula: R11 represents a substituted carbonyl group or a substituted sulfonyl group, R12 represents hydrogen atom or an optionally substituted alkyl group, R2 represents hydrogen atom, etc., Z represent oxygen atom or a group represented by —N(R3)—, R3 represents an optionally substituted alkyl group, etc., R4a represents an optionally substituted alkyl group, R4b represents an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, having an excellent tachykinin receptor antagonistic action.Type: GrantFiled: November 26, 2004Date of Patent: June 24, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masami Takahashi, Tsutomu Miyake, Takeshi Yamanaka, Hidetoshi Asai, Rikako Kono
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Publication number: 20080146572Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: February 26, 2008Publication date: June 19, 2008Applicant: ABBOTT LABORATORIESInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Publication number: 20080132480Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: August 22, 2005Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 7381721Abstract: 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: March 17, 2003Date of Patent: June 3, 2008Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Patent number: 7378440Abstract: The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.Type: GrantFiled: July 27, 2004Date of Patent: May 27, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Dieter Kadereit, Elisabeth Defossa, Karl Schoenafinger, Thomas Kalbunde, Andreas Herling
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Publication number: 20080119459Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: ApplicationFiled: February 16, 2006Publication date: May 22, 2008Inventors: Bruno Roux, Isabelle Berard
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Patent number: 7361666Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: April 11, 2002Date of Patent: April 22, 2008Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7358251Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 29, 2005Date of Patent: April 15, 2008Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7351742Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: January 19, 2005Date of Patent: April 1, 2008Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Kim James, Charlotte Alice Louise Lane, Ian Brian Moses, Nicholas Murray Thomson
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Patent number: 7351721Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: May 6, 2003Date of Patent: April 1, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Publication number: 20080058374Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-[2-({3-[2-(4-hydroxybenzylamino)ethylcarbamoyl]benzoyl}methylamino)ethyl]piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase (Form I or II), a salt such as a hemiedisylate salt or a heminapadisylate salt, or a solvate of a salt such as a heminapadisylate methanolate or a heminapadisylate ethanolate. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: ApplicationFiled: March 8, 2007Publication date: March 6, 2008Inventors: YongQi Mu, Sean M. Dalziel, Yu-Hua Ji, Leticia Maria Preza
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Patent number: 7323563Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: August 22, 2005Date of Patent: January 29, 2008Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Michael George Hunter, Paul Raymond Beckett, John Martin Clements, Mark Whittaker, Zoe Marie Spavold
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Patent number: 7309714Abstract: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 26, 2003Date of Patent: December 18, 2007Assignee: Merck & Co., Inc.Inventors: Joseph L. Duffy, Robert J. Mathvink, Ann E. Weber, Jinyou Xu
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Publication number: 20070249674Abstract: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.Type: ApplicationFiled: April 24, 2007Publication date: October 25, 2007Inventors: Jennifer Bolton, Robert S. Chao, Miroslav Rapta, Lisa Williams, Richard D. Wilson
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Patent number: 7285568Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: May 24, 2005Date of Patent: October 23, 2007Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
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Publication number: 20070238710Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Applicant: ARDEA BIOSCIENCESInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
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Patent number: 7262208Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: April 30, 2003Date of Patent: August 28, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7253171Abstract: Novel antagonists of ?4?1 integrin and/or ?4?7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.Type: GrantFiled: January 15, 2002Date of Patent: August 7, 2007Assignee: Laboratorios Almirall, S.A.Inventors: Juan Miguel Jimenez Mayorga, Jordi Bach Tana, Jesus Maria Ontoria Ontoria, Eloisa Navarro Romero
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Patent number: 7247748Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.Type: GrantFiled: March 26, 2003Date of Patent: July 24, 2007Assignee: SmithKline CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph P. Marino, Michael J. Neeb, Ning Wang
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Patent number: 7247730Abstract: The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.Type: GrantFiled: March 4, 2004Date of Patent: July 24, 2007Assignee: ISP Investments Inc.Inventors: Arie Gutman, Igor Zaltsman, Anton Shalimov, Maxim Sotrihin, Gennady Nisnevich, Lev Yudovich, Irina Fedotev
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Patent number: 7244766Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: January 19, 2005Date of Patent: July 17, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
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Patent number: 7241810Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 21, 2005Date of Patent: July 10, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7241757Abstract: There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 2, 2004Date of Patent: July 10, 2007Assignee: AstraZeneca ABInventors: Tord Inghardt, Olle Karlsson, Marcel Linschoten, Jan-Erik Nyström
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Patent number: 7238709Abstract: This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.Type: GrantFiled: December 7, 2000Date of Patent: July 3, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, David Oare
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Patent number: 7132539Abstract: The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.Type: GrantFiled: October 20, 2003Date of Patent: November 7, 2006Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Xinrong Tian, Wieslaw Adam Mazur, Anny-Odile Colson
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7053057Abstract: This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.Type: GrantFiled: May 23, 2001Date of Patent: May 30, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, David Bebbington, Guy Brenchley, Ronald Knegtel, Michael Mortimore
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Patent number: 7030115Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 21, 2003Date of Patent: April 18, 2006Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7015235Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 21, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Patent number: 7012084Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 14, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner