Spiro Diazine Patents (Class 544/231)
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Publication number: 20080176843Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: August 15, 2007Publication date: July 24, 2008Inventors: Lewis R. Makings, Dennis J. Hurley, Gabriel Raffai
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Patent number: 7378411Abstract: The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 2, 2002Date of Patent: May 27, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
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Patent number: 7371753Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.Type: GrantFiled: August 25, 2005Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Harald Engelhardt, Andreas Schoop, Martin Steegmaier, Matthias Hoffmann, Matthias Grauert
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Patent number: 7361758Abstract: The present invention relates to a new crystal of triazaspiro[5.5]undecane derivatives. The crystal of a non-solvate of (3R)-1-butyl-2,5-dioxo-3-[(1R)-1-hydroxy-1-cyclohexylmethyl]-9-[4-(4-carboxyphenyloxy)phenylmethyl]-1,4,9-triazaspiro[5.5]undecane hydrochloride have safety as drug substance, and have possibility to supply at large scale. And the crystal have an antagonistic activity against the interaction between chemokine and chemokine receptor, therefore, it is useful for manufacture of an agent for treating and/or preventing diseases such as various inflammatory diseases, asthma, atopic dermatitis, nettle rash, allergy disease, nephritis, nephropathy, hepatitis, arthritis, chronic rheumatoid arthritis, autoimmune disease, transplanted organ rejection reactions, acquired immunodeficiency syndrome and the like.Type: GrantFiled: September 17, 2003Date of Patent: April 22, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yoshikazu Takaoka, Masaki Okamoto, Yuuichi Genba
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Patent number: 7338954Abstract: A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 is selected from alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —SO2N(R4)R4a, —CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle; R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. New compounds for use in treating disorders of gastrointestinal motility are also provided.Type: GrantFiled: September 14, 2004Date of Patent: March 4, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Hannguang J. Chao, Joseph A. Tino, William R. Ewing
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Patent number: 7332491Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Christian Eickmeier, Gisela Schnapp, Norbert Redemann, Flavio Solca, Jens Juergen Quant
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Publication number: 20070281917Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Patent number: 7294631Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: June 12, 2006Date of Patent: November 13, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7294632Abstract: The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: September 7, 2005Date of Patent: November 13, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Pascal George, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20070213341Abstract: The present invention relates to spiroindolinone derivatives of the formula and enantiomers and pharmaceutically acceptable salts and esters thereof which have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: March 1, 2007Publication date: September 13, 2007Inventors: Li Chen, Qingjie Ding, Jin-Jun Liu, Song Yang, Zhuming Zhang
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Patent number: 7268128Abstract: Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, these compounds are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.Type: GrantFiled: June 14, 2004Date of Patent: September 11, 2007Assignee: Ausbio Pharma Co., Ltd.Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Patent number: 7262193Abstract: Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 is H or alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.Type: GrantFiled: May 24, 2005Date of Patent: August 28, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiromu Habashita, Shin-ichi Hamano, Shiro Shibayama, Yoshikazu Takaoka
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Patent number: 7241889Abstract: Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these 6-formyl-tetrahydropteridines and their use as medicaments.Type: GrantFiled: July 12, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Hoffmann, Matthias Grauert, Martin Steegmaier, Flavio Solca
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Patent number: 7238807Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.Type: GrantFiled: November 22, 2005Date of Patent: July 3, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Adil Duran, Guenter Linz
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Patent number: 7235538Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.Type: GrantFiled: July 17, 2003Date of Patent: June 26, 2007Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Lise Brown Christiansen, Jane Marie Lundbeck, Christian K. Sams, Marit Kristiansen
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Patent number: 7214676Abstract: The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.Type: GrantFiled: May 24, 2004Date of Patent: May 8, 2007Assignee: Warner-Lambert Company LLCInventors: Patrick Bernardelli, Pierre Ducrot, Edwige Lorthiois, Febrice Vergne
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Patent number: 7176313Abstract: An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity against Mycobacterium tuberculosis and atypical acid-fast bacteria and exhibits good pharmacokinetics and safetyType: GrantFiled: February 7, 2001Date of Patent: February 13, 2007Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Kenji Namba, Mayumi Tanaka, Rie Miyauchi
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Patent number: 7129245Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: July 29, 2003Date of Patent: October 31, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Pi{hacek over (n)}elro-Nú{hacek over (n)}ez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 7122662Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 16, 2004Date of Patent: October 17, 2006Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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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: 7067501Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.Type: GrantFiled: May 20, 2004Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
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Patent number: 7053090Abstract: Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 is H or alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.Type: GrantFiled: March 18, 2002Date of Patent: May 30, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiromu Habashita, Shin-ichi Hamano, Shiro Shibayama, Yoshikazu Takaoka
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Patent number: 6967201Abstract: The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5?, R6, R6?, R7, R7?, R8, and R8? are as described in the specification.Type: GrantFiled: July 21, 2000Date of Patent: November 22, 2005Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Brian Eugene Cunningham, Matthew Joseph Fisher, William Harlan Gritton, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Matthew Robert Reinhard, Dennis Charles Thompson, Leonard Larry Winneroski, Yanping Xu
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Patent number: 6943171Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:Type: GrantFiled: November 7, 2002Date of Patent: September 13, 2005Assignee: Schering CorporationInventors: Theodros Asberom, John W. Clader, Yueqing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
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Patent number: 6919349Abstract: Disclosed are novel spiro derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.Type: GrantFiled: September 25, 2001Date of Patent: July 19, 2005Assignee: Toray Industries, Inc.Inventors: Toshiya Takahashi, Takeshi Ishigaki, Miyuki Funahashi, Koji Taniguchi, Masayuki Kaneko, Mie Kainoh, Hiroyuki Meguro
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Patent number: 6916807Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: July 12, 2005Assignee: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Patent number: 6911452Abstract: The present invention relates to 1-oxa-3,8-diaza-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: December 23, 2002Date of Patent: June 28, 2005Assignee: Acadia Pharmaceuticals Inc.Inventor: Nathalie Schlienger
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Patent number: 6900201Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: May 31, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Kevin Freeman-Cook
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Patent number: 6894048Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neuropsychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.Type: GrantFiled: September 18, 2003Date of Patent: May 17, 2005Assignee: Transgenomic, Inc.Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
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Patent number: 6861422Abstract: The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: GrantFiled: February 26, 2003Date of Patent: March 1, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Matthias Hoffmann, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky
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Patent number: 6841671Abstract: The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: October 23, 2001Date of Patent: January 11, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Martin J. Wythes, Brian S. Bronk
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Publication number: 20040267013Abstract: Specific photochromic 3H-naphtho[2,1-b]-pyran compounds useful with various types of synthetic resin materials to form photochromic articles, especially ophthalmic lenses, and photochromic articles formed with such compounds. The compounds of the invention have especially long-wave absorption maxima in the open form thereof and enable violet to blue tints to be obtained when used in photochromic articles.Type: ApplicationFiled: July 2, 2004Publication date: December 30, 2004Applicant: Rodenstock GmbHInventors: Claudia Mann, Manfred Melzig, Udo Weigand
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Publication number: 20040259890Abstract: Compounds of the formula (I): 1Type: ApplicationFiled: April 12, 2004Publication date: December 23, 2004Inventors: Takehiro Fukami, Katsumasa Nonoshita, Takeshi Sagara, Hiroyuki Kishino
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Publication number: 20040214843Abstract: The invention provides compounds which are PDE7inhibitors, having the following formula (I), (II) and (III) 1Type: ApplicationFiled: May 24, 2004Publication date: October 28, 2004Applicant: Pfizer IncInventors: Patrick Bernardelli, Pierre Ducrot, Edwige Lorthiois, Febrice Vergne
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Publication number: 20040106631Abstract: The invention relates to compounds of formula (I) 1Type: ApplicationFiled: September 17, 2003Publication date: June 3, 2004Inventors: Patrick Bernardelli, Fabrice Vergne, ChrysteIle Mendes, Pierre G. Ducrot
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Publication number: 20040106619Abstract: A pharmaceutical composition for prevention and/or treatment for HIV infection or AIDS induced by the infection which comprises, as an active ingredient, a triazaspiro[5.5]undecane derivative, a quaternary ammonium salt thereof, an N-oxide thereof, or a non-toxic salt thereof, and if necessary, it may be combined with at least one member of other agents for prevention and/or treatment for HIV infection (wherein all symbols are as defined in the specification.).Type: ApplicationFiled: September 22, 2003Publication date: June 3, 2004Inventors: Hiroaki Mitsuya, Kenji Maeda, Shiro Shibayama, Yoshikazu Takaoka
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Patent number: 6740636Abstract: This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective amount of a non-peptide CCR1 receptor antagonist and a sub-nephrotoxic amount of cyclosporin A.Type: GrantFiled: July 25, 2001Date of Patent: May 25, 2004Assignee: Schering AktiengesellschaftInventor: Richard Horuk
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Publication number: 20040097511Abstract: Triazaspiro[5.5]undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient.Type: ApplicationFiled: May 8, 2003Publication date: May 20, 2004Inventors: Hiromu Habashita, Shin-ichi Hamano, Shiro Shibayama, Yoshikazu Takaoka
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Publication number: 20040082783Abstract: The present invention provides molecular building blocks of rigid bis(amino acids). The molecular building blocks can be linked together through the formation of rigid diketopiperazine rings, to provide oligomers having the desired three dimensional structure. Oligomers formed from the basic building blocks are also disclosed.Type: ApplicationFiled: July 2, 2003Publication date: April 29, 2004Inventor: Christian E. Schafmeister
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Publication number: 20040082584Abstract: Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 is H or alkyl).Type: ApplicationFiled: September 22, 2003Publication date: April 29, 2004Inventors: Hiromu Habashita, Shin-ichi Hamano, Shiro Shibayama, Yoshikazu Takaoka
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Patent number: 6703390Abstract: Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NMDA subtype of the ionotropic EAA receptor. The compounds further are useful as testing agents to identify and characterize other compounds for the treatment of these disorders. The compounds are useful therapeutically as sedatives or for the treatment of neurosychopharmacological disorders such as stroke, ischemia and epilepsy. The compositions may be provided in combination with a suitable carrier for oral or parenteral administration. The compounds may be administered orally or parenterally for the treatment of a variety of disorders associated with non-NMDA EEA receptor function.Type: GrantFiled: April 12, 2001Date of Patent: March 9, 2004Assignee: Transgenomic, Inc.Inventors: Xue-Feng Pei, Baoqing Li, Maria-Luisa Maccecchini
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Publication number: 20040024001Abstract: Compound having the formula (I), 1Type: ApplicationFiled: April 25, 2003Publication date: February 5, 2004Inventors: William J. Pitts, Soong-Hoon Kim, Joseph Barbosa, Wayne Vaccaro
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Publication number: 20040010141Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: April 25, 2003Publication date: January 15, 2004Applicant: Pfizer Inc.Inventors: Mark C. Noe, Kevin Freeman-Cook
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Patent number: 6677451Abstract: A new process is described for the preparation of a compound of the formula I wherein R1, R2, R3 and R4, independently of each other, are C1-C8alkyl or C1-C5hydroxyalkyl, or R1 and R2 together with the carbon atom they are attached to are C5-C12cycloalkyl, or R3 and R4 together with the carbon atom they are attached to are C5-C12cycloalkyl; R5, R6, R7, R8 and R9, independently of each other, are H, C1-C8alkyl, C2-C8alkenyl, C5-C12aryl, C1-C4haloalkyl, an electron withdrawing group, or C6-C12aryl which is substituted by a residue selected from C1-C4alkyl, C1-C4alkoxy, halogen; and R7 and R8 together may also form a chemical bond; and R is an organic linking group containing 2-500 carbon atoms and forming, together with the carbon atoms it is directly connected to and the nitrogen atom, a substituted, 5-, 6 or 7-membered cyclic ring structure; characterized in that a compound of the formula II is oxidized.Type: GrantFiled: November 20, 2001Date of Patent: January 13, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Alessandro Zedda, Gianluca Ferri, Massimiliano Sala
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Patent number: 6677336Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: January 13, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
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Publication number: 20030229104Abstract: Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I 1Type: ApplicationFiled: April 11, 2003Publication date: December 11, 2003Applicant: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul, Utz-Peter Jagusch
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Publication number: 20030225056Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: April 25, 2003Publication date: December 4, 2003Applicant: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Patent number: 6649622Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: January 26, 2001Date of Patent: November 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard Sulsky, Jeffrey A. Robl
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Publication number: 20030212062Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2003Publication date: November 13, 2003Applicant: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Publication number: 20030176697Abstract: The invention provides methods to synthesize zwitterionic pentacyclic crambescidin core intermediates having the carboxylate side chain in the natural axial orientation, and a range of crambescidin alkaloid analogs.Type: ApplicationFiled: September 24, 2002Publication date: September 18, 2003Applicant: The Regents of the University of CaliforniaInventors: Larry E. Overman, Frank Stappenbeck, Andrew I McDonald, Zachary D. Aron