Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.05)
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Publication number: 20090264404Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: August 31, 2006Publication date: October 22, 2009Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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SELECTED CGRP-ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
Publication number: 20090253680Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: June 16, 2009Publication date: October 8, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Henri DOODS, Kirsten ARNDT, Gerhard SCHAENZLE -
Publication number: 20090221548Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: May 15, 2009Publication date: September 3, 2009Inventor: Guohua Zhao
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Publication number: 20090209510Abstract: A pharmaceutical composition useful for a prevention and/or treatment of hyperlipidemia, which comprises combining an effective amount of squalene synthase inhibitor and HMG-CoA reductase inhibitor is provided.Type: ApplicationFiled: May 31, 2006Publication date: August 20, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomoyuki Nishimoto, Ryuichi Tozawa, Takeo Wada, Eiichiro Ishikawa, Toshiya Nishi, Hiroko Yamakawa
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Patent number: 7569561Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, as well as the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: February 16, 2007Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Anke Baum, Guido Boehmelt, Harald Engelhardt, Jens Juergen Quant, Flavio Solca, Martin Steegmaier, Stephan Karl Zahn
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Publication number: 20090163465Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: February 5, 2009Publication date: June 25, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heinz STADTMUELLER, Harald ENGELHARDT, Martin STEEGMAIER, Anke BAUM, Ulrich GUERTLER, Andreas SCHOOP, Jens Juergen QUANT, Flavio SOLCA, Rudolf HAUPTMANN, Ulrich REISER, Stephan Karl ZAHN, Lars HERFURTH
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Publication number: 20090137551Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 are as described herein; compositions thereof; and uses thereof.Type: ApplicationFiled: January 22, 2009Publication date: May 28, 2009Inventors: Robert L. Dow, Michael J. Munchhof
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Publication number: 20090118255Abstract: The present invention provides a novel drug which is useful as a preventive and/or therapeutic agent for various diseases involved in elevation of CRP level, in particular, inflammatory disease and cancer comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.Type: ApplicationFiled: August 8, 2005Publication date: May 7, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yoshimi Imura, Ryuichi Tozawa, Tomoyuki Nishimoto
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Publication number: 20090105214Abstract: Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: May 23, 2006Publication date: April 23, 2009Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20090088416Abstract: The present application describes deuterium-enriched lapaquistat, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: April 2, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090082333Abstract: A preventive/remedy for xanthoma which contains a compound having an inhibitory effect on squalene synthase, its prodrug or its salt.Type: ApplicationFiled: April 21, 2006Publication date: March 26, 2009Applicants: NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY, TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masashi Shiomi, Takashi Ito, Ryuichi Tozawa, Yuichiro Amano
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Publication number: 20090069290Abstract: Methods for treating a demyelinating condition in a subject in need of treatment are provided. In some aspects the methods encompass administering to the subject an amount of a Ca2+-channel blocker effective to treat the demyelinating condition. In other aspects, the methods encompass administering to the subject an amount of a glutamate inhibitor effective to treat the demyelinating condition. In additional aspects, the methods encompass administering to the subject a Ca2+-channel blocker in combination with a glutamate inhibitor, in amounts effective to treat the demyelinating condition. In still other aspects, the methods encompass administering to the subject a Ca2+-channel blocker in combination with a hypertensive agent, in amounts effective to treat the demyelinating condition. Also provided are pharmaceutical compositions having a Ca2+-channel blocker, a glutamate inhibitor, and a pharmaceutically-acceptable carrier.Type: ApplicationFiled: October 30, 2008Publication date: March 12, 2009Inventors: Peter Werner, David Pitt, Elimor Brand-Schieber
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Patent number: 7488754Abstract: The present invention provides a method for treating, inhibiting the progression of, or eradicating polycystic kidney disease of in a patient in need thereof which comprises providing to said patient an effective amount of a TACE inhibitor compound alone or in combination with an effective amount of an EGF receptor kinase inhibitor.Type: GrantFiled: April 5, 2002Date of Patent: February 10, 2009Assignee: WyethInventors: Philip Frost, Jeremy I. Levin
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Publication number: 20090036425Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 are as described herein; compositions thereof; and uses thereof.Type: ApplicationFiled: July 17, 2008Publication date: February 5, 2009Inventors: Robert L. Dow, Michael J. Munchhof
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Publication number: 20080292584Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone ais metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.Type: ApplicationFiled: May 28, 2008Publication date: November 27, 2008Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.Inventors: Richard H. Roberts, Jie Du, Matthew W. Davis
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Patent number: 7435728Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: June 20, 2005Date of Patent: October 14, 2008Assignee: Pfizer IncInventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20080248035Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.Type: ApplicationFiled: November 8, 2006Publication date: October 9, 2008Applicant: RANBAXY LABORATORIESInventors: Jitendra A. Sattigeri, Vinay S. Bansal
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Publication number: 20080200449Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.Type: ApplicationFiled: May 14, 2007Publication date: August 21, 2008Inventors: Horst Olschewski, Robert Roscigno, Lewis J. Rubin, Thomas Schmehl, Werner Seeger, Carl Sterritt, Robert Voswinckel
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Publication number: 20080176830Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: April 13, 2006Publication date: July 24, 2008Inventors: Nicholas D. Adams, Michael Gerard Darcy, Dashyant Dhanak, Kevin J. Duffy, Duke M. Fitch, Steven David Knight, Kenneth Allen Newlander, Antony N. Shaw
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Publication number: 20080153801Abstract: This invention provides new benzoxazepine compounds represented by the formula: [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally substituted heterocyclic group having a deprotonatable hydrogen atom, R1 stands for a lower alkyl group and W stands for a halogen atom] having activities of lowering chlesterol-level and lowering trigluceride-level, and being useful for prophylaxis and therapy of hyperlipidemia.Type: ApplicationFiled: November 19, 2007Publication date: June 26, 2008Inventors: Hidefumi Yukimasa, Yasuo Sugiyama, Ryuichi Tozawa
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080139530Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 28, 2007Publication date: June 12, 2008Applicant: WyethInventors: Puwen Zhang, Jay Edward Wrober, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Publication number: 20080132483Abstract: The present invention provides an agent for preventing or treating organ functional disorders, an agent for preventing or treating organ dysfunction and an agent for preventing or treating obesity and deuteropathy thereof, each of which comprises a compound having an effect of increasing ubiquinone or a salt thereof or a prodrug thereof; as well as a ubiquinone increasing agent comprising a compound having a squalene synthase inhibitory effect or a salt thereof or a prodrug thereof.Type: ApplicationFiled: January 17, 2008Publication date: June 5, 2008Inventors: Yasuo Sugiyama, Tomoyuki Nishimoto, Yoshihiro Kiyota
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Publication number: 20080113964Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 28, 2007Publication date: May 15, 2008Applicant: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Patent number: 7323455Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 22, 2005Date of Patent: January 29, 2008Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Patent number: 7196108Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: GrantFiled: March 6, 2003Date of Patent: March 27, 2007Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Patent number: 7151097Abstract: Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.Type: GrantFiled: October 22, 2004Date of Patent: December 19, 2006Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Robert L. Dow, David A. Griffith
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Patent number: 7060698Abstract: The invention relates to benzoxazepinone derivatives of formula wherein R1, R2, R3, R4, and n are as defined in the specification and to a pharmaceutically suitable acid addition salt thereof. These compounds are good ?-secretase inhibitors for the treatment of Alzheimer's disease.Type: GrantFiled: May 3, 2004Date of Patent: June 13, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Robert Alan Goodnow, Jr., Jens-Uwe Peters
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Patent number: 7053081Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: December 24, 2003Date of Patent: May 30, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Richard E. Olson, Michael G. Yang
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Patent number: 7030107Abstract: A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): wherein the rings A and B are each a benzene ring which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring having a hydrogen atom substituted with a nitrogen atom; R1 and R2 are each independently a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylsulfonyl group, a C1 to C6 alkylcarbonyl group, or a C1 to C6 alkoxycarbonyl group, or R1 and R2 are bound to one another to form the ring D; m is 1 or 2; n is 2 or 3; and q is an integer from 1 to 4.Type: GrantFiled: December 6, 2002Date of Patent: April 18, 2006Assignee: Kyorin Pharmaceutical.Co., Ltd.Inventors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
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Patent number: 7026309Abstract: A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring) that are each independently selected from the group consisting of a halogen atom, a substituted or unsubstituted C1 to C6 alkyl group, and a substituted or unsubstituted C1 to C6 alkoxyl group; R is a C1 to C6 alkylsulfonyl group, a C1 to C6 alkylcarbonyl group, a C1 to C6 alkoxycarbonyl group, or a formyl group; m is 1 or 2; n is 2 or 3; and q is 1 or 2.Type: GrantFiled: March 24, 2003Date of Patent: April 11, 2006Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
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Patent number: 6995153Abstract: A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein the rings A and B are each a benzene ring having 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring); the ring C is a nitrogen-containing ring; m is 1 or 2; and n is 2 or 3.Type: GrantFiled: January 15, 2003Date of Patent: February 7, 2006Assignee: Kyorin Pharmaceutical. Co., Ltd.Inventors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru Izawa
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Patent number: 6977252Abstract: The present invention relates to use of compounds represented by the following general formula [1] or salts or prodrugs thereof: [where R1 represents hydrogen atom or lower alkoxy group; R2 represents hydrogen atom, lower alkoxy group, optionally substituted phenyl group, (where R3 represents acyl group); X represents —CO— or —CH2—; and n-represents 1 or 2], as drugs for overcoming a resistance to anticancer drugs or drugs for enhancing an effect of anticancer drugs. The compounds represented by the general formula [1] have not only a function of overcoming the resistance to various anticancer drugs but also a function of enhancing the effect of various anticancer drugs to anticancer-drug sensitive cells. Thus, these compounds have excellent effects on resistant cells and also on sensitive cells, and in particular effective in the treatment of a cancer having an acquired resistance to an anticancer drug.Type: GrantFiled: May 19, 2000Date of Patent: December 20, 2005Assignee: Noboru KanekoInventors: Noboru Kaneko, Kazuhito Nishio, Takashi Nakamura
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Patent number: 6946459Abstract: Two new crystalline forms of 1S-[1alpha(2S*, 3R*), 9alpha]6, 10-dioxo-N-(2-ethoxy-5-oxo-tetrahydro-3-furany1)-9 [[(1-isoquinolyl) carbony1]amino]octahydro-6H-pyridazino [1,2-a][1,2]diazepin-1-carboxamide (anhydrous or hydrated), their preparation process and the pharmaceutical compositions containing them.Type: GrantFiled: November 18, 2002Date of Patent: September 20, 2005Assignee: Aventis Pharma S. A.Inventors: Jean-Yves Godard, Valerie Rognon
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Patent number: 6924277Abstract: Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: September 27, 2001Date of Patent: August 2, 2005Assignee: AstraZeneca ABInventor: Peter Bernstein
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Patent number: 6897305Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities thereof.Type: GrantFiled: December 8, 1999Date of Patent: May 24, 2005Assignee: Theravance, Inc.Inventors: Yu-Hua Ji, Maya Natarajan, John H. Griffin, Thomas E. Jenkins
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Patent number: 6890918Abstract: A pharmaceutical composition comprising an inhibitor of angiotensin converting enzyme and neutral endopeptidase, such as sampatrilat, and at least one bioavailability enhancer such as an organic acid, e.g., ascorbic acid. Such a composition has improved systemic bioavailability.Type: GrantFiled: April 30, 2002Date of Patent: May 10, 2005Assignee: Shire Laboratories, Inc.Inventors: Beth Burnside, Rong-Kun Chang, Amir Shojaei
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Publication number: 20040235819Abstract: The invention relates to benzoxazepinone derivatives of formula 1Type: ApplicationFiled: May 3, 2004Publication date: November 25, 2004Inventors: Guido Galley, Robert Alan Goodnow, Jens-Uwe Peters
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Patent number: 6797504Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1. The invention provides recombinant serine protease domains and methods of using peptides comprising a recombinant serine protease domain to screen for compounds that inhibit serine protease activity of matriptase or MTSP1.Type: GrantFiled: September 8, 2000Date of Patent: September 28, 2004Assignee: Dendreon San Diego LLCInventors: Edwin L. Madison, Joseph Edward Semple, Gary Samuel Coombs, John Eugene Reiner, Edgar O. Ong, Gian Luca Araldi
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Patent number: 6759404Abstract: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: April 3, 2001Date of Patent: July 6, 2004Inventors: Richard E. Olson, Michael G. Yang
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Publication number: 20040072819Abstract: This invention provides new benzoxazepine compounds represented by the formula: 1Type: ApplicationFiled: June 24, 2003Publication date: April 15, 2004Applicant: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Yasuo Sugiyama, Ryuichi Tozawa
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Patent number: 6713470Abstract: There is described a method of treatment of a patient requiring analgesia which comprises the separate, simultaneous or sequential administration of a therapeutically effective amount of an opioid analgesic, devazepide and a surfactant. There is also described a monophasic pharmaceutical composition comprising an amount of devazepide effective in the enhancement of opioid analgesia and a pharmaceutically acceptable surfactant.Type: GrantFiled: January 22, 2003Date of Patent: March 30, 2004Assignee: ML Laboratories PLCInventor: Karen Jackson
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Publication number: 20040058900Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: January 6, 2003Publication date: March 25, 2004Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. Mcdaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20040005358Abstract: A modified-release vasopeptidase inhibitor formulation is provided which is capable of releasing vasopeptidase inhibitor, preferably omapatrilat or gemopatrilat, in a manner to provide therapeutically effective NEP inhibitory activity and therapeutically effective ACE inhibitory activity, in a balanced manner, for a predetermined duration to lower blood pressure and/or treat heart failure. In a preferred formulation, the NEP inhibitory activity and ACE inhibitory activity have balanced release characteristics.Type: ApplicationFiled: April 21, 2003Publication date: January 8, 2004Inventors: Peter H. Slugg, Nemichand B. Jain, Rajesh Krishna, Robert L. Jerzewski, Ronald L. Smith, Jatin M. Patel, Bimal K. Malhotra
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Publication number: 20030236245Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: 1Type: ApplicationFiled: August 29, 2002Publication date: December 25, 2003Applicant: Molecumetics, Ltd.Inventors: Vincent Huber, Jan Urban, Hiroshi Nakanishi, Masakatsu Eguchi, Jessymol Mathew, Min Sang Lee
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Publication number: 20030225056Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: April 25, 2003Publication date: December 4, 2003Applicant: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Publication number: 20030191109Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, the &bgr;-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The &bgr;-sheet mimetics have utility as inhibitors of one or more of proteases, kinases, CAAX, peptides binding to SH2 domains and MHC-I and/or MHC-II presentation of peptides to T cell receptors in warm-blooded animals.Type: ApplicationFiled: October 25, 2001Publication date: October 9, 2003Inventor: Michael Kahn
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Patent number: 6613761Abstract: This invention provides new benzoxazepine compounds represented by the formula: [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally substituted heterocyclic group having a deprotonatable hydrogen atom, R1 stands for a lower alkyl group and W stands for a halogen atom] having activities of lowering cholesterol-level and lowering trigluceride-level, and being useful for prophylaxis and therapy of hyperlipidemia.Type: GrantFiled: June 6, 2000Date of Patent: September 2, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Yasuo Sugiyama, Ryuichi Tozawa
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Publication number: 20030162768Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: December 12, 2002Publication date: August 28, 2003Inventors: James E. Audia, Bruce A. Dressman, Qing Shi