Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/277.7)
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Publication number: 20080227794Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: ApplicationFiled: February 15, 2006Publication date: September 18, 2008Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20080161579Abstract: A process for preparation of rabeprazole sodium comprising oxidation of wet or dry rabeprazole sulphide with sodium hypohalite in water or a mixture of water and water miscible solvent using alkali metal hydroxide and catalyst is disclosed herein. The present invention also discloses process for preparation of rabeprazole sulphide.Type: ApplicationFiled: February 21, 2006Publication date: July 3, 2008Inventors: Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Patent number: 7390907Abstract: 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: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080146594Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.Type: ApplicationFiled: November 8, 2007Publication date: June 19, 2008Applicant: Ligand Pharmaceutical, Inc.Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penuliar, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
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Publication number: 20080119465Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Laboratories Fournier S.A.Inventors: Luc LEBRETON, Christine Dumas, Christine Massardier, Michel Bondoux
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Publication number: 20080058386Abstract: A series of indoline-sulfonamide compounds is disclosed. The formula of indoline-sulfonamide compounds is shown as formula (I). In formula (I), R1 is H or halogen; R2 is Ar, Ar—C(O)—, Ar—CH2—, Ar—SO2—, Ar—O—C(O), or R?—C(O)—, and Ar is a substituted or unsubstituted C5-C20 aryl, cyclyl, heterocyclyl, or heteroaryl, R? and R? independently is C1-C10 alkyl, or C1-C10 alkoxyl; and R3 is C5-C15 aryl or C1-C10 alkyl. The indoline-sulfonamide compounds disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier.Type: ApplicationFiled: May 10, 2007Publication date: March 6, 2008Applicants: Taipei Medical University, National Health Research InstitutesInventors: Jing-Ping Liou, Jang-Yang Chang, Hsing-Pang Hsieh
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Patent number: 7338966Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: June 9, 2005Date of Patent: March 4, 2008Assignee: SmithKline Beecham CorporationInventors: Karen Elizabeth Lackey, Edgar Raymond Wood, III
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Patent number: 7253203Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: March 17, 2006Date of Patent: August 7, 2007Assignee: WyethInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 7189755Abstract: Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.Type: GrantFiled: February 10, 2004Date of Patent: March 13, 2007Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
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Patent number: 7148249Abstract: The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: September 5, 2003Date of Patent: December 12, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Joerg Kley, Frank Hilberg, Armin Heckel, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Ulrike Tontsch-Grunt, Jacobus C. A. Van Meel
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Patent number: 7109231Abstract: A novel class of tricyclic compounds of the following formula (I): (formula I); is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shockType: GrantFiled: July 29, 2002Date of Patent: September 19, 2006Assignee: Eli Lilly and CompanyInventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Jr., Daniel Jon Sall, Jason Scott Sawyer
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Patent number: 7105543Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent seleceted from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C 1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: September 1, 2005Date of Patent: September 12, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 7071217Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: GrantFiled: August 23, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio, Edgar Raymond Wood, III
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Patent number: 7071332Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: December 2, 2003Date of Patent: July 4, 2006Assignee: Sugen, Inc.Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6958338Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: February 4, 2003Date of Patent: October 25, 2005Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 6911463Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: August 6, 2002Date of Patent: June 28, 2005Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Theo Schotten, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz
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Patent number: 6846819Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: GrantFiled: October 6, 2000Date of Patent: January 25, 2005Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Jr., Dalia R. Jakas
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Publication number: 20040110770Abstract: The present invention relates to a compound of formula (I): 1Type: ApplicationFiled: August 20, 2003Publication date: June 10, 2004Applicant: AVENTIS PHARMA SAInventors: Jean-Francois Riou, Michel Maratrat, Lucile Grondard, Fabienne Thompson, Odile Petitgenet, Patrick Mailliet, Jacques Lavayre
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Publication number: 20040087625Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1Type: ApplicationFiled: August 13, 2003Publication date: May 6, 2004Applicant: Pfizer IncInventors: Peter Bertinato, Brian S. Bronk, Alan E. Blize, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
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Publication number: 20040082615Abstract: This invention is directed to indolone derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.Type: ApplicationFiled: August 7, 2003Publication date: April 29, 2004Inventors: Michael Konkel, John M. Wetzel, Jamie Talisman
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Patent number: 6727263Abstract: The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: August 16, 2002Date of Patent: April 27, 2004Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Jens Kristian Perregaard, Ivan Mikkelsen, Garrick Paul Smith
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Publication number: 20040039196Abstract: The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: ApplicationFiled: June 13, 2003Publication date: February 26, 2004Applicant: SUGEN, INC.Inventors: Chung Chen Wei, Peng Cho Tang
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Patent number: 6689792Abstract: Compounds of formula (1) are provided: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by C, CR4, [[CHR4]] and CHCH2; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or A and B may be concatenated together to form indole, benzimidazole, indolone or indoline moieties; oType: GrantFiled: October 12, 2001Date of Patent: February 10, 2004Assignee: WyethInventors: Michael G. Kelly, Young H. Kang
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Patent number: 6673790Abstract: The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.Type: GrantFiled: October 2, 2002Date of Patent: January 6, 2004Assignee: Sanofi-SynthelaboInventors: Loïc Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gérard Valette
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Publication number: 20030225109Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: 1Type: ApplicationFiled: April 22, 2003Publication date: December 4, 2003Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Jay E. Wrobel, Edward G. Melenski, Lin Zhi, Todd K. Jones, Christopher M. Tegley, James P. Edwards
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Publication number: 20030220388Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1Type: ApplicationFiled: June 6, 2003Publication date: November 27, 2003Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030195234Abstract: The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhihit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.Type: ApplicationFiled: February 27, 2003Publication date: October 16, 2003Inventors: Scott Howard Dickerson, Robert N Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael J. Luzzio
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Publication number: 20030191157Abstract: An injectable composition comprises a benzimidazole compound having an antiulcer action and a strong alkali (e.g., an alkali metal hydroxide such as sodium hydroxide) in a proportion of about 1 equivalent of the latter relative to 1 mol of the former, and is substantially free from a nonaqueous solvent. The injectable composition may comprise N-methylglucamine, and a saccharide (such as mannitol). The injectable composition may be a freeze-dried preparation. The freeze-dried preparation is dissolvable in or dilutive with a distilled water for injection or an infusion solution without a nonaqueous solvent. The injectable composition is useful as an antiulcer agent.Type: ApplicationFiled: February 14, 2003Publication date: October 9, 2003Inventors: Takayuki Doen, Masao Nagao, Naoki Asakawa, Nobuyuki Takechi
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Publication number: 20030171591Abstract: The present invention relates to a production method of an optically active form of a compound represented by formula (II) 1Type: ApplicationFiled: October 24, 2002Publication date: September 11, 2003Inventors: Hideo Hashimoto, Tadashi Urai
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Patent number: 6613781Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: December 20, 2001Date of Patent: September 2, 2003Assignee: WyethInventors: Ping Zhou, Michael Gerard Kelly, Yanfang Li
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Publication number: 20030158405Abstract: Compounds of the formula 1Type: ApplicationFiled: November 22, 2002Publication date: August 21, 2003Applicant: WyethInventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 6603006Abstract: An intermediate for the synthesis of amlodipine, a process for the preparation thereof and the corresponding use are disclosed. The intermediate is ethyl 3-amino-4-(2-(phthalimido)ethoxy)crotonate and is of formula III: The process for the preparation thereof comprises reacting the acetoacetate of formula: with ammonium acetate; and the use thereof is for the preparation of the compound of formula: the process being conducted by reacting ethyl 3-amino-4-[2-(phthalimido)ethoxy]crotonate with a benzylidene derivative.Type: GrantFiled: January 10, 2002Date of Patent: August 5, 2003Assignee: Esteve Química, S.A.Inventors: Laura Coppi, Yolanda Gasanz Guillén, Julio Campón Pardo
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Publication number: 20030125371Abstract: This invention provides compounds of the formula: 1Type: ApplicationFiled: June 18, 2002Publication date: July 3, 2003Applicant: WyethInventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li, Lee D. Jennings, David LeRoy Crandall
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Patent number: 6573293Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 15, 2001Date of Patent: June 3, 2003Assignees: Sugen, Inc., Pharmacia & Upjohn Co.Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
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Publication number: 20030073846Abstract: A compound of the formula (I) wherein X1 ? is bond or —O(CH2)m— (in which m is an integral number of 1, 2 or 3); X2 is bond, —(CH2)n—, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.Type: ApplicationFiled: August 6, 2002Publication date: April 17, 2003Inventors: Kiyoshi Taniguchi, Hiroshi Kayakiri, Minoru Sakurai, Naokaki Fujii, Kenichi Washizuka, Hitoshi Hamashima, Yasuyo Tomishima, Kaori Hamada, Nobuhiro Yamamoto, Hirofumi Ishikawa, Naoko Unami, Toshiko Miura
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Publication number: 20030069430Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by canType: ApplicationFiled: November 30, 2001Publication date: April 10, 2003Inventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Publication number: 20030018053Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: June 28, 2002Publication date: January 23, 2003Applicant: The Institute for Pharmaceutical Discovery LLC.Inventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Patent number: 6506763Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: July 30, 2001Date of Patent: January 14, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Publication number: 20020187978Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.Type: ApplicationFiled: June 29, 2001Publication date: December 12, 2002Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
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Patent number: 6476028Abstract: A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 8, 2000Date of Patent: November 5, 2002Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: William E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
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Patent number: 6476035Abstract: The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: January 25, 2000Date of Patent: November 5, 2002Inventors: Ejner Knud Moltzen, Jens Kristian Perregaard, Ivan Mikkelsen, Garrick Paul Smith
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Publication number: 20020115692Abstract: Tryptophan derivatives of formula (1) are described: 1Type: ApplicationFiled: November 20, 2001Publication date: August 22, 2002Inventors: Sarah Catherine Archibald, David Festus Charles Moffat, Martin Clive Hutchings, Anne Marie Foley
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Patent number: 6436965Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 1, 2001Date of Patent: August 20, 2002Assignee: Merck Frosst Canada & Co.Inventors: Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
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Patent number: 6353109Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 1, 1998Date of Patent: March 5, 2002Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Publication number: 20020026053Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: ApplicationFiled: July 30, 2001Publication date: February 28, 2002Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6350747Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.Type: GrantFiled: February 28, 2000Date of Patent: February 26, 2002Assignee: Glaxo Wellcome Inc.Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
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Patent number: 6302837Abstract: A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others rType: GrantFiled: October 13, 2000Date of Patent: October 16, 2001Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Christine Lila, Tony Verbeuren, Alain Rupin
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Publication number: 20010020035Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: June 1, 1998Publication date: September 6, 2001Inventors: PAMELA ALBAUGH, GANG LIU, ALAN HUTCHISON
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Patent number: 6268391Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.Type: GrantFiled: April 7, 2000Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal