Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/278.4)
-
Patent number: 7470790Abstract: Compounds inhibiting neuronal nitric oxide synthase (nNOS) for potential treatment in neurodegenerative diseases, such as stroke, Alzheimer's disease, Parkinson's disease, Huntington's disease, such compounds of a formula.Type: GrantFiled: September 8, 2004Date of Patent: December 30, 2008Assignee: Northwestern UniversityInventors: Richard B. Silverman, Haitao Ji
-
Patent number: 7452999Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular ?-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.Type: GrantFiled: February 20, 2004Date of Patent: November 18, 2008Assignee: Novartis AGInventors: Mahavir Prashad, Hong-Yong Kim, Bin Hu, Joel Slade, Prasad Koteswara Kapa, Michael John Girgis
-
Publication number: 20080275043Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.Type: ApplicationFiled: October 26, 2005Publication date: November 6, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, John Gordon Allen, Zhaogen Chen, Thomas Edward Mabry, Jefferson Ray McCowan, Nancy June Snyder, Leonard Larry Winneroski
-
Publication number: 20080275086Abstract: The invention relates to compounds of formula (I) wherein Z, R1-7, X and n have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.Type: ApplicationFiled: February 20, 2006Publication date: November 6, 2008Inventors: Paul John Edwards, Silvia Cerezo-Galvez, Meritxell Lopez-Canet, Victor Giulio Matassa, Claudia Rosenbaum, Christian Rummey, Sonja Nordhoff
-
Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
-
Publication number: 20080262042Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity, which is represented by the formula (I) wherein R1 is an optionally substituted cyclic group, R2 is a substituent, R3 is an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R4 and R5 are each a hydrogen atom, an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R6 and R6? are each a hydrogen atom or an alkyl group, and n is an integer of 0-3, or a salt thereof.Type: ApplicationFiled: February 26, 2008Publication date: October 23, 2008Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Haruyuki Nishida, Yasuyoshi Arikawa, Keizo Hirase, Koji Ono
-
Patent number: 7439371Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 11, 2006Date of Patent: October 21, 2008Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Richard C. Yee
-
Publication number: 20080214815Abstract: A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.Type: ApplicationFiled: August 27, 2007Publication date: September 4, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Tomohiro Matsushima, Atsushi Kamada, Kazunori Wakasugi, Shuji Shirotori, Shinya Abe, Kazumasa Nara, Takahisa Sakaguchi
-
Publication number: 20080214621Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G1 is methylene or ethylene; L is —(C1-C4)alkylene-, —S—, —CH(OH)—, or —O—; R0 is Formula II or Formula III and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: September 4, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Cassandra A. Gauthier, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, Alexei Pavlovych Krasutsky, John Gordon Allen
-
Publication number: 20080194643Abstract: Disclosed are crystalline forms A, B and C of 1,2-Pyrrolidinedicarboxamide, N1-(4-chlorophenyl)-N2-[2-fluoro-4-(2-oxo-1(2H)-pyridinyl)phenyl]-4-methoxy-, (2R,4R)-(9Cl). These crystalline forms are characterized by their powder X-ray diffraction, solid-state NMR, as well as methods for the preparation and pharmaceutical compositions of the same which are useful for the treatment of acute, subacute, or chronic thrombotic disorders including treatment of venous thrombosis, arterial thrombosis, pulmonary embolism, myocardial infarction, cerebral infarction, restenosis, atherosclerosis, angina, primary and secondary deep vein thrombosis, thromboembolism associated with cardiovascular disease, including, but not limited to, acute coronary syndrome, atrial fibrillation, cardiac valve replacement and deep vein thrombosis. The crystalline forms of the present invention are also useful for the treatment of cancer, sepsis and diabetes.Type: ApplicationFiled: March 13, 2006Publication date: August 14, 2008Inventors: Brian Samas, Derek Vrieze
-
Publication number: 20080188520Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.Type: ApplicationFiled: December 12, 2007Publication date: August 7, 2008Applicant: SANOFI-AVENTISInventors: Joachim BRENDEL, Heinrich Christian ENGLERT, Stefan PEUKERT, Klaus WIRTH, Michael WAGNER, Jean-Marie RUXER, Fabienne PILORGE
-
Patent number: 7407972Abstract: 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: December 20, 2004Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Jeremy John Edmunds
-
Publication number: 20080176826Abstract: The present invention relates to new pyridine compounds which are useful for combating animal pests, in particular insects, arachnids and nematodes. The invention also relates to a method for combating insects, nematodes and arachnids. The pyridine compounds have the formula I as defined below. Likewise, compounds of the formula II are suitable for combating pests. In formulae I and II n is 1 or 2, and R1, R2, R3, R4 and R5 are as defined in the claims and in the specification.Type: ApplicationFiled: May 24, 2006Publication date: July 24, 2008Inventors: Michael Puhl, Michael Rack, Thomas Schmidt, Michael Hofmann, Ernst Baumann, Markus Kordes, Wolfgang Von Deyn, David G. Kuhn, Deborah L. Culbertson, Douglas D. Anspaugh, Henry Van Tuyl Cotter, Hassan Oloumi-Sadeghi, Tony Bucci, Henricus Maria Martinus Bastiaans
-
Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
-
Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
-
Patent number: 7361663Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: October 16, 2003Date of Patent: April 22, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
-
Patent number: 7345063Abstract: The invention provides compounds of general formula (I), wherein R1, X, Y, n, R2, Z1, Z2, A1, A2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: March 19, 2002Date of Patent: March 18, 2008Assignee: AstraZeneca ABInventors: Tomas Eriksson, Karolina Lawitz
-
Publication number: 20080027080Abstract: This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.Type: ApplicationFiled: July 25, 2007Publication date: January 31, 2008Inventors: Percy H. Carter, Robert J. Cherney, John Hynes, Soo S. Ko, Anurag S. Srivastava, Zili Xiao, Michael G. Yang
-
Patent number: 7312218Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 15, 2006Date of Patent: December 25, 2007Assignee: Bristol Myers Squibb Co.Inventors: Wei Han, Zilun Hu, Timur Gungor
-
Patent number: 7288541Abstract: The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors.Type: GrantFiled: October 2, 2002Date of Patent: October 30, 2007Assignee: SmithKline Beecham CorporationInventors: David Norman Deaton, John George Catalano
-
Patent number: 7241745Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: GrantFiled: August 5, 2002Date of Patent: July 10, 2007Assignee: Astellas Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
-
Patent number: 7223765Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.Type: GrantFiled: March 15, 2006Date of Patent: May 29, 2007Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
-
Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
-
Patent number: 7183260Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: August 25, 2004Date of Patent: February 27, 2007Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S Karanewsky, Robert J Ternansky, Steven D Linton, Thang Dinh
-
Patent number: 7179835Abstract: The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.Type: GrantFiled: November 13, 2002Date of Patent: February 20, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Matthew Campbell, Chuen Chan, Henry Anderson Kelly, Nigel Paul King, Savvas Kleanthous, Andrew McMurtrie Mason, Stefan Senger, Paul William Smith, Nigel Stephen Watson, Robert John Young
-
Patent number: 7176222Abstract: The present invention provides intermediates, synthetic methods and novel urea compositions of matter.Type: GrantFiled: January 11, 2005Date of Patent: February 13, 2007Assignee: Cytokinetics, Inc.Inventors: Bradley Paul Morgan, George Petros Yiannikouros, Michael P. Cruskie, Jr., Christopher Roy Goss
-
Patent number: 7160902Abstract: Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal disorders, pain, and pruritus are also disclosed.Type: GrantFiled: November 14, 2003Date of Patent: January 9, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Guo-Hua Chu, Minghua Gu
-
Patent number: 7151111Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: December 19, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
-
Patent number: 7148242Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Jeffrey Jacobs, Rakesh K. Jain, Dinesh V. Patel, Zhengyu Yuan
-
Patent number: 7148069Abstract: The present invention provides a method for the analysis of a compound with amino group (e.g., an amino acid or peptide) contained in a sample and convenient manner with a high sensitivity. The compound with amino group in a sample containing the compound with amino group is labeled with a specific carbamate compound such as p-trimethylammonium anilyl-N-hydroxysuccinimidyl carbamate iodide to enhance the selectivity and sensitivity. The present invention is preferably used in conjunction with mass spectrometry such as MS/MS method to facilitate quantitative analysis. The present invention further provides labeling reagents for mass spectrometry.Type: GrantFiled: August 16, 2004Date of Patent: December 12, 2006Assignee: Ajinomoto Co., Inc.Inventors: Hiroshi Miyano, Akihisa Yahashi, Kazutaka Shimbo, Masakazu Nakazawa, Kazuo Hirayama
-
Patent number: 7132543Abstract: The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenylene derivative as at least one oxidation base, and to a process for dyeing keratin fibers and a multi-compartment kit using the claimed dye composition. Such a composition makes it possible to obtain a chromatic, powerful, unselective and fast coloration of keratin fibers.Type: GrantFiled: March 29, 2004Date of Patent: November 7, 2006Assignee: L'Oreal S.A.Inventors: Laure Ramos, Stéphane Sabelle
-
Patent number: 7132434Abstract: Compounds of the formula (I), useful as metal-loproteinase inhibitors, especially as inhibitors of MMP12Type: GrantFiled: November 6, 2002Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Kristina Stenvall, Pavol Zlatoidsky
-
Patent number: 7122562Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: January 5, 2006Date of Patent: October 17, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
-
Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
-
Patent number: 7101897Abstract: This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.Type: GrantFiled: December 18, 2000Date of Patent: September 5, 2006Assignee: AstraZeneca ABInventors: James Michael Wardleworth, Francis Thomas Boyle, Zbigniew Matusiak
-
Patent number: 7094791Abstract: Chemical agents of the general formula (I) and (II), such as derivatives of 3-hydroxy-pyrrole containing hydroxamic acid, and including salts thereof, that modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: GrantFiled: July 31, 2003Date of Patent: August 22, 2006Assignee: Avalon Pharmaceuticals, Inc.Inventors: Wieslaw M. Cholody, Valentina Petukhova, Sean O'Brien, Norman Ohler, Stanislaw Pikul
-
Patent number: 7053056Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: January 16, 2001Date of Patent: May 30, 2006Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky, Steven D. Linton, Thang Dinh
-
Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
-
Patent number: 7030141Abstract: 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: October 23, 2002Date of Patent: April 18, 2006Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
-
Patent number: 7030114Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 30, 1998Date of Patent: April 18, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Reinhardt Bernhard Baudy
-
Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
-
Patent number: 6989446Abstract: Process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.Type: GrantFiled: June 12, 2002Date of Patent: January 24, 2006Assignee: Ciba Specialty Chemicals Corp.Inventors: Michael Tinkl, Samuel Evans, Peter Nesvadba
-
Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
-
Patent number: 6946468Abstract: The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing upto 5 heteroatoms where the heteroatoms are independently selected from O, N & S; or a —S—S— dimer thereof when R2?H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation their use as therapeutic agents and pharmaceutical compositions containing them.Type: GrantFiled: August 13, 1997Date of Patent: September 20, 2005Assignee: Zeneca LimitedInventors: Francis Thomas Boyle, James Michael Wardleworth
-
Patent number: 6936633Abstract: The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.Type: GrantFiled: December 31, 2003Date of Patent: August 30, 2005Assignee: UCB S.A.Inventors: Dong Zou, Olivier Dasse, Janelle Evans, Paul Higgins, Jeremy Kintigh, Rama Kondru, Eric Schwartz, Laurent Knerr, Hai-Xiao Zhai
-
Patent number: 6927225Abstract: The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X3 and X4 are CR?; wherein R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORz in which Rz is H or C1-C3 alkyl; and c) A represents (i) C2-C14 alkenyl, or C2-C14 alkynyl, all of which may be branched or unbranched, unsubstituted or substituted with halogen, hydroxy, nitro, aroyl, aryloxy, C1-C8 acyloxy, C1-C6 alkylthio, arylthio, aryl, heteroaryl, heteroarylthio, heteroaryloxy, C1-C6 acyl, C1-C6 haloalkyl, C1-C6 alkoxy or C1-C6 haloalkoxy, and (ii) C3-C14 cycloalkyl, containing 0 heteroatoms and 0-2 unsaturations, substituted with aryloxy, heteroaryloxy, C1-C6 alkylthio, aType: GrantFiled: December 2, 2002Date of Patent: August 9, 2005Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
-
Patent number: 6913748Abstract: Disclosed is a method of making conjugates of cell binding agents and small molecule drugs comprising reacting a cell binding agent with a bifunctional cross-linking moiety to thereby provide the cell binding agent with a reactive disulfide group and then reacting the modified cell binding agent with a small molecule drug comprising a free thiol group. Bifunctional cross-linking moieties are also disclosed.Type: GrantFiled: August 5, 2003Date of Patent: July 5, 2005Assignee: Immunogen, Inc.Inventor: Wayne Charles Widdison
-
Patent number: 6897226Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.Type: GrantFiled: July 9, 2003Date of Patent: May 24, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
-
Patent number: 6867221Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.Type: GrantFiled: July 10, 2002Date of Patent: March 15, 2005Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Shunji Takemura, Takeshi Doi, Yoshinori Kyotani, Masao Ohkuchi
-
Patent number: 6855730Abstract: The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: March 10, 2003Date of Patent: February 15, 2005Assignee: Sugen, Inc.Inventors: Pen Cho Tang, Li Sun, Todd Anthony Miller, Congxin Liang, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla