The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen (e.g., 2 Benzamidomethyl - Pyrrolidines, Etc.) Patents (Class 548/567)
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Publication number: 20100016374Abstract: Compounds of formula (I) and salts and solvates are provided: wherein R2 is selected from phenyl substituted with n R1 groups, and pyridyl substituted with n R1 groups; n=0, 1 or 2; each R1 is independently selected from the group consisting of halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and cyano; R3 is selected from hydrogen and C1-2 alkyl; R4 is selected from the group consisting of ethyl, n-propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C1-4alkyl, and haloC1-4alkyl; R12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R13 is selected from hydrogen, chloro and trifluoromethyl; R14 is selected from hydrogen, trifluoromethyl and chloro; R15 is selected from hydrogen, chloro and trifluoromethyl; R16 is selectedType: ApplicationFiled: April 3, 2007Publication date: January 21, 2010Inventors: Steven Coulton, Martin Gilpin, Roderick Alan Porter
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Patent number: 7649011Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.Type: GrantFiled: December 22, 2003Date of Patent: January 19, 2010Assignee: Chemocentryx, Inc.Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, J. J. Wright
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Patent number: 7638639Abstract: 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: December 29, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7632858Abstract: The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula I wherein R1, R2, R3, X, Y, Z and G are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.Type: GrantFiled: November 13, 2003Date of Patent: December 15, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence G. Hamann, David J. Augeri, Mark C. Manfredi
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Publication number: 20090286833Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.Type: ApplicationFiled: June 20, 2008Publication date: November 19, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Beatrix MERLA, Bernd SUNDERMANN, Werner ENGLBERGER, Hagen-Heinrich HENNIES, Achim KLESS, Petra BLOMS-FUNKE, Babette-Yvonne KOEGEL, Heinze GRAUBAUM
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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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Patent number: 7601868Abstract: The present invention provides a compound represented by the formula or salts thereof, wherein, Ar1, Ar, R, R1, R2, Ra1, Ra2, Ra3, Ra4 and Y have meanings described in the specification, having a melanin-concentrating hormone antagonistic, action and useful as an agent for the prophylaxis or treatment of obesity and the like.Type: GrantFiled: February 12, 2004Date of Patent: October 13, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Yuji Ishihara, Makoto Kamata, Shiro Takekawa
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Patent number: 7544716Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.Type: GrantFiled: November 28, 2003Date of Patent: June 9, 2009Assignee: Xention LimitedInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20090118330Abstract: The present invention relates to novel diurea derivatives that block intracellular signal transduction and thereby inhibit the production of pro-inflammatory cytokines, especially interleukin-2 (IL-2) and/or induce apoptosis in activated T-cells. It further discloses such a compound for use as a medicament, the use of said compound for the manufacturing of a medicament for the treatment of immune disorders which benefit from inhibition of production of IL-2 and other pro-inflammatory cytokines and/or induction of apoptosis in activated T-cells, a pharmaceutical composition comprising said compound and a method of treatment comprising administration of a pharmaceutically effective amount of said compound.Type: ApplicationFiled: January 19, 2005Publication date: May 7, 2009Inventors: Aina Lisbeth Abramo, Lars Olof Goran Pettersson, Kerstin Ingalill Andersson, Asa Anette Sundstedt
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Patent number: 7517880Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 1, 2002Date of Patent: April 14, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20090043099Abstract: The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds.Type: ApplicationFiled: October 31, 2007Publication date: February 12, 2009Applicant: The Burnham InstituteInventors: John C. Reed, Richard A. Houghten, Adel Nefzi, John M. Ostresh, Clemencia Pinilla, Kate Welsh
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090017489Abstract: The present invention relates to a composition for modulating the activation of Nurr1, the composition comprising an agonist or an antagonist of a dopamine D2 receptor, methods for modulating the activation of Nurr1 by the dopamine D2 receptor, a method and composition for treating Nurr1-related diseases using the dopamine D2 receptor, and methods for screening a modulator of a dopamine D2 receptor of a test compound. Accordingly, the activation of Nurr1 can be modulated by treating the dopaminergic neurons with the agonist or the antagonist of the dopamine D2 receptor, thereby enhancing or inhibiting generation of the dopaminergic neurons.Type: ApplicationFiled: June 22, 2006Publication date: January 15, 2009Applicant: Korea University Industry And Academy Cooperation FoundationInventors: Ja hyun Baik, Sung yul Kim
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Publication number: 20090018116Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: May 20, 2005Publication date: January 15, 2009Applicant: ASTRAZENECA ABInventors: Shujuan Jin, Ziping Liu, Claire Milburn, Miroslaw Tomaszewski, Christopher Walpole, Zhong-Yong Wei, Hua Yang
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080275028Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.Type: ApplicationFiled: July 19, 2005Publication date: November 6, 2008Inventors: Giovanni Gaviraghi, Chiara Ghiron, Hendrik Bothmann, Renza Roncarati, Georg Christian Terstappenn
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Patent number: 7446125Abstract: This invention relates to nitroproline derivative compounds and procedures for their preparation and the preparation of pharmaceutical compositions containing the compounds. The invention also relates to the administration of compounds of the invention as agents for the treatment of mammalian diseases whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable cellular and molecular activities or responses induced by integrin-dependent molecular interactions.Type: GrantFiled: April 14, 2006Date of Patent: November 4, 2008Assignees: Universidad del Pais Vasco, Dominion Pharmakine S.L.Inventors: Fernando Pedro Cossio, Eneko Aldaba Arévalo, Yosu Ion Vara Salazr, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, María Valcárcel Cuesta, Fernando Vidal Vanaclocha
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Publication number: 20080234247Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Applicant: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Publication number: 20080210907Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X) ??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: ApplicationFiled: January 30, 2006Publication date: September 4, 2008Applicant: NAATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
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Publication number: 20080207736Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: February 21, 2008Publication date: August 28, 2008Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
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Patent number: 7417062Abstract: Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.Type: GrantFiled: August 11, 2005Date of Patent: August 26, 2008Assignee: ChemoCentryx, Inc.Inventors: Anita Melikian, John J. Kim Wright
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Publication number: 20080194549Abstract: The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine 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 activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesisType: ApplicationFiled: March 21, 2006Publication date: August 14, 2008Inventors: Claus Ehrhardt, Osamu Irie, Edwige Liliane Jeanne Lorthiois, Juergen Klaus Maibaum, Nils Ostermann, Holger Sellner
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Patent number: 7407974Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: April 18, 2005Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Publication number: 20080176925Abstract: The present invention is directed to the tosylate salt of trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.Type: ApplicationFiled: January 18, 2008Publication date: July 24, 2008Inventors: Todd W. Butler, Travis T. Wager
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Patent number: 7368462Abstract: The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provide a means for reducing body mass and controlling obesity.Type: GrantFiled: July 13, 2005Date of Patent: May 6, 2008Assignee: The Procter & Gamble CompanyInventor: Xiufeng Eric Hu
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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: 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: 7323492Abstract: A compound of formula (I): wherein: A represents an aromatic 5 membered heterocycle, optionally containing, in addition to the nitrogen atom indicated in formula (I), one to three additional nitrogen atoms.Type: GrantFiled: January 5, 2004Date of Patent: January 29, 2008Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Fiandor, Roger Frechette
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Patent number: 7312191Abstract: Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and/or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).Type: GrantFiled: July 29, 2004Date of Patent: December 25, 2007Assignee: Arizona Biomedical Research CommissionInventors: Seth D. Rose, Karl J. Okolotowicz, Rosemarie F. Hartman, Jason Houtchens
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Patent number: 7253185Abstract: 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: April 29, 2005Date of Patent: August 7, 2007Assignees: The Regents of the University of Michigan, Genzyme CorporationInventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Patent number: 7232817Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 27, 2005Date of Patent: June 19, 2007Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 7220777Abstract: The invention provides compounds of formula (I) a salt, or solvate thereof.Type: GrantFiled: October 15, 2002Date of Patent: May 22, 2007Assignee: SmithKline Beecham P.L.C.Inventors: Sula Anne Armstrong, Dieter Wolfgang Hamprecht, Martin Jones, David Richard Witty, Kamal A Al-Barazanji, Mohammad Tadayyon
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Patent number: 7202404Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1–C2 alkoxy; C1–C2 haloalkoxy; cyano; or C1–C2 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R3 is hydrogen; halogen; C1–C4 alkoxy; C1–C4 haloalkoxy; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1–C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)?C(R7)R6; R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: November 25, 2002Date of Patent: April 10, 2007Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
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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: 7166601Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 26, 2006Date of Patent: January 23, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7144881Abstract: The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said arylcyclopropylcarboxylic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Alexandre L'Heureux, Li-Qiang Sun
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Patent number: 7138414Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.Type: GrantFiled: July 11, 2003Date of Patent: November 21, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7112586Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: February 25, 2005Date of Patent: September 26, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7109217Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 6, 2003Date of Patent: September 19, 2006Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
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Patent number: 7098202Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: January 20, 2004Date of Patent: August 29, 2006Assignee: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 7049317Abstract: The invention provides compounds of Formula (I): wherein R1–R4 have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: September 12, 2002Date of Patent: May 23, 2006Assignee: Syntex (U.S.A.) LLCInventor: Daisy Joe Du Bois
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Patent number: 7026485Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 5, 2004Date of Patent: April 11, 2006Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
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Patent number: 6995283Abstract: The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.Type: GrantFiled: February 28, 2002Date of Patent: February 7, 2006Assignee: SmithKline Beecham CorporationInventor: Joseph Howing Chan
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Patent number: 6989402Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).Type: GrantFiled: December 23, 1999Date of Patent: January 24, 2006Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
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Patent number: 6984651Abstract: 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: August 7, 2003Date of Patent: January 10, 2006Assignee: Bristol-Myers Squibb Pharma, CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
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Patent number: 6967199Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: November 8, 2002Date of Patent: November 22, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 6951874Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: February 23, 2001Date of Patent: October 4, 2005Assignee: AstraZeneca ABInventors: Peter Hansen, Lars Pettersson
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Patent number: 6949567Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.Type: GrantFiled: February 26, 2002Date of Patent: September 27, 2005Assignee: 4SC AGInventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
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Patent number: 6949546Abstract: 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: July 10, 2003Date of Patent: September 27, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt