Hydrogen Or Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., 2 Pyrrolidine Acrylamide, Etc.) Patents (Class 548/568)
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Patent number: 7615566Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: January 30, 2008Date of Patent: November 10, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Publication number: 20090270417Abstract: Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described.Type: ApplicationFiled: June 11, 2007Publication date: October 29, 2009Applicant: NOVARTIS AGInventors: Juergen Klaus Maibaum, Edwige Liliane Jeanne Lorthiois, Peter Buehimayer
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Publication number: 20090263407Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.Type: ApplicationFiled: April 16, 2009Publication date: October 22, 2009Applicant: ABBOTT LABORATORIESInventors: Prasad A. Dande, Todd M. Hansen, Robert D. Hubbard, Carol K. Wada, Lu Tian, Xiaobin Zhao
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Publication number: 20090253701Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
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Patent number: 7592373Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.Type: GrantFiled: December 23, 2004Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Philipp Lustenberger, Stephan Georg Mueller, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Dirk Stenkamp, Leo Thomas
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Publication number: 20090118291Abstract: This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: ApplicationFiled: August 22, 2005Publication date: May 7, 2009Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Publication number: 20080248093Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: July 24, 2007Publication date: October 9, 2008Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
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Publication number: 20080161577Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: ApplicationFiled: January 30, 2008Publication date: July 3, 2008Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7351718Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: November 21, 2006Date of Patent: April 1, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7351717Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: November 21, 2006Date of Patent: April 1, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7351719Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: GrantFiled: October 31, 2003Date of Patent: April 1, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Philipp Lustenberger, Klaus Rudolf, Thorsten Lehmann-Lintz, Kirsten Arndt, Ralf Lotz, Martin Lenter, Heike-Andrea Wieland
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Patent number: 7335681Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: September 15, 2006Date of Patent: February 26, 2008Assignee: The Regents of the University of MichiganInventor: James A. Shayman
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Patent number: 7265228Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.Type: GrantFiled: August 12, 2004Date of Patent: September 4, 2007Assignee: Genzyme CorporationInventors: Bradford H. Hirth, Craig Siegel
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Patent number: 7250415Abstract: The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, ?-aminoacids, ?-aminoacids and derivatives thereof of Formula I: P-M-M1I or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: June 1, 2004Date of Patent: July 31, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Donald J. Pinto
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Patent number: 7250414Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: July 31, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Yan Chen, Craig Husfeld
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Patent number: 7214804Abstract: The present invention relates to novel heterocyclic compounds, according to Formula I, that stimulate endogenous production and/or release of growth hormone, wherein R1, R2, R3, R4 and X are defined herein.Type: GrantFiled: January 12, 2005Date of Patent: May 8, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Weixu Zhai, Samuel Gerritz, Charles John Andres, Jr., Joseph A. Tino
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Patent number: 7208515Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: October 5, 2006Date of Patent: April 24, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Sarah Dunham, Li Li
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Patent number: 7202269Abstract: Certain ?-, ?-, and ?-amino acid derivatives are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain.Type: GrantFiled: October 28, 2004Date of Patent: April 10, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Tristin K. Barclay, Alejandro Santillán, Jr., Liu Y. Tang, Hariharan Venkatesan, Ronald L. Wolin
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Patent number: 7199158Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 18, 2005Date of Patent: April 3, 2007Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 7183292Abstract: This invention is directed to compounds of formula I: wherein R1–R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: June 10, 2004Date of Patent: February 27, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7148251Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: January 10, 2002Date of Patent: December 12, 2006Assignee: The Regents of the University of MichiganInventor: James A. Shayman
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Patent number: 7125825Abstract: Viscoelastic surfactants are described for use in aqueous systems to generate thickened fluids. The surfactants are alkyl amidoamine salts of inorganic acids and/or organic acids. The fluids may also contain inorganic salts, organic salts or mixtures thereof. Additionally, the fluids may contain a co-surfactant. These fluids are particularly useful in oilfield applications such as hydraulic fracturing, gravel packing, drilling, completion, etc. Viscoelastic fluids of the invention are also useful in industrial and consumer product fluid applications as rheology control agents.Type: GrantFiled: April 25, 2003Date of Patent: October 24, 2006Assignee: Tomah Products, Inc.Inventor: David Kelly Moss
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Patent number: 7119214Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: April 12, 2005Date of Patent: October 10, 2006Assignee: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Patent number: 7071224Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7 and R8are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: July 4, 2006Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Sarah Dunham, Li Li
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Patent number: 7045628Abstract: The present invention relates to a one-pot process for preparing a compound of formula I: I; by reacting a compound of formula II with a compound of formula III: in the presence of a suitable solvent, a suitable base, a palladium catalyst and a suitable ligand.Type: GrantFiled: November 15, 2001Date of Patent: May 16, 2006Assignee: Eli Lilly and CompanyInventors: Scott Allan May, Thomas Michael Wilson, Tony Yantao Zhang
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Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6949662Abstract: The present invention relates to an antimicrobial compound having high safety as well as potent antimicrobial activity on a broad range of microorganisms represented by the following formula:Type: GrantFiled: March 28, 2002Date of Patent: September 27, 2005Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Youichi Kimura, Hisashi Takahashi, Yohhei Ishida
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Patent number: 6949553Abstract: The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts: wherein A represents an optionally substituted CH3CnH(2n-2m)— (wherein n denotes an integer of 4 to 22, and m represents an unsaturation number which is an integer of 0 to 7), l represents an integer of 0 to 10, s represents 0 or 1, provided that when s is 0, p+q=4 or 5, but when s is 1, p+q=3 or 4, and in each case, either p or q is an integer of 1 or more, R represents an alkyl group having 1 to 10 carbon atoms which may be straight-chain or branched-chain, and RA represents hydrogen or an alkyl group having 1 to 10 carbon atoms which may be straight-chain or branched-chain, and their use in suppression of platelet aggregation, in suppression of inflammation, and in prevention and treatment of circulatory diseases.Type: GrantFiled: June 18, 2002Date of Patent: September 27, 2005Assignee: Maruha CorporationInventors: Tadakazu Tamai, Kazuyoshi Yoshikai, Masazumi Nishikawa, Kunio Ogasawara, Itsuki Murota
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Patent number: 6916802Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: May 5, 2004Date of Patent: July 12, 2005Assignees: Genzyme Corporation, The Regents of the University of MichiganInventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Patent number: 6890949Abstract: Novel amino ceramide-like compounds (1) are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: July 7, 2000Date of Patent: May 10, 2005Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6693137Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Buddy Eugene Cantrell, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Edward C. R. Smith, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6683074Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: September 26, 2001Date of Patent: January 27, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Publication number: 20030191316Abstract: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); 1Type: ApplicationFiled: January 10, 2003Publication date: October 9, 2003Inventors: Yoshio Ogino, Hideki Kurihara, Kenji Matsuda, Tomoshige Numazawa, Norikazu Otake, Kazuhito Noguchi
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Patent number: 6583296Abstract: A pyrrolesulfonamide compound having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl.Type: GrantFiled: August 28, 2001Date of Patent: June 24, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6569889Abstract: Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: May 31, 2001Date of Patent: May 27, 2003Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6555570Abstract: Compounds of peptide mimetic nature having the general formula I wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.Type: GrantFiled: March 23, 2000Date of Patent: April 29, 2003Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Peschke, Jesper Lau, Behrend Friedrich Lundt, Michael Ankersen, Brett Watson, Kjeld Madsen
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Patent number: 6521592Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: October 23, 2001Date of Patent: February 18, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Daniel S. Gardner
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Patent number: 6521707Abstract: The invention relates to novel isocyanates containing tertiary amino groups, a process for preparing them, and also their use for the synthesis and modification of polymers. The invention provides isocyanates of the formula (I) where R1 and R2 are, independently of one another, alkyl having from 1 to 6 carbon atoms, where R1 and R2 may be joined to form a ring, Z is alkylene having from 2 to 6 carbon atoms, n is an integer from 0 to 20, Y is alkylene having from 2 to 6 carbon atoms. The alkyl radicals R1 and R2 may be linear or branched or joined to form an aliphatic ring. The alkylene radical Z preferably contains from 2 to 4 carbon atoms.Type: GrantFiled: November 1, 2001Date of Patent: February 18, 2003Assignee: Bayer AktiengesellschaftInventors: Wolfgang Podszun, Joachim Krüger, Kamelia Karlou-Eyrisch
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Patent number: 6515024Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 11, 2001Date of Patent: February 4, 2003Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6512120Abstract: This invention is directed to methods of synthesizing densely functionalized pyrrolidine compounds through the use of intramolecular Diels Alder reactions.Type: GrantFiled: March 12, 2002Date of Patent: January 28, 2003Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Pranab Mishra, Sengen Sun, William V. Murray
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Patent number: 6492547Abstract: The present application relates to carboxylic acid amides of general formula wherein A, B and R1 to R3 are defined as in claim 1, processes for preparing them, pharmaceutical compositions containing these compounds and the use thereof and their preparation.Type: GrantFiled: December 19, 2001Date of Patent: December 10, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Henning Priepke, Norbert Hauel, Klaus Damm, Andreas Schnapp
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Patent number: 6486178Abstract: The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R1 represents hydrogen atom, nitro group, cyano group, C1-6 alkylcarbonylamino, R2 and R3 each independently represent C1-6 alkyl group, R4 represents hydroxyl group or C1-6 alkylcarbonyloxy group or represents a bond or oxygen atom together with R5, R5 represents hydrogen atom or represents a bond or oxygen atom together with R4, R6 represents hydrogen atom, hydroxyl group or NR7R8, n means 0 or an integer of 1 to 4, X represents C═O, CH2, SO2 or NR16, Y represents NR17 when X is C═O, CH2 or SO2 and represents C═O when X is NR16, Z is absent when Y represents NR17 or represents NR18 when Y is C═O, W represents aromatic groups or lactam rings, or pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2000Date of Patent: November 26, 2002Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Masayuki Sato, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Yamashita
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Publication number: 20020173508Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: December 3, 2001Publication date: November 21, 2002Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6476027Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 6, 1999Date of Patent: November 5, 2002Assignee: Monsanto CompanyInventors: Clara I. Villamil, John N. Freskos, Brent V. Mischke, Patrick B. Mullins, Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Thomas E. Barta, Daniel P. Becker
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Patent number: 6455531Abstract: Compounds having therapeutic utility are of the formula wherein NB2 is heterocycloalkyl and R1 and R2 are each various substituents or a cyclic group.Type: GrantFiled: March 28, 2001Date of Patent: September 24, 2002Assignee: Darwin Discovery, Ltd.Inventors: David Alan Owen, Andrew Douglas Baxter, Robert John Watson, Duncan Robert Hannah, John Gary Montana
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Patent number: 6452012Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl) propionamide derivatives, and to processes for preparing the same.Type: GrantFiled: November 13, 2001Date of Patent: September 17, 2002Assignee: Sanofi-SynthelaboInventors: Bertrand Castro, Hélène Mattras, Aldo Previero
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Patent number: 6423689Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: December 16, 1998Date of Patent: July 23, 2002Assignees: Warner-Lambert Company, Neurex CorporationInventors: Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge