Plural Double Bonds Between The Ring Members Of The Oxazole Ring Patents (Class 548/235)
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080167310Abstract: The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to Syndrome X as well as cardiovascular diseases.Type: ApplicationFiled: October 3, 2007Publication date: July 10, 2008Inventors: Lynn Stacy Gossett, Jonathan Edward Green, James Robert Henry, Winton Dennis Jones, Donald Paul Matthews, Quanrong Shen, Daryl Lynn Smith, Jennifer Ann Vance, Alan M. Warshawsky, Maria Rosario Gonzalez-Garcia
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Publication number: 20080167354Abstract: The invention relates to arylcycloalkyl-substituted alkanoic acid derivatives and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for the treatment and/or prevention of disorders of the fatty acid metabolism and glucose utilization disorders and also disorders in which insulin resistance is involved.Type: ApplicationFiled: January 14, 2008Publication date: July 10, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Christian Stapper, Stefanie Keil, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Dirk Gretzke, Hans-Ludwig Schaefer, Wolfgang Wendler
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Publication number: 20080161308Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.Type: ApplicationFiled: December 22, 2005Publication date: July 3, 2008Inventors: Catherine Vidal, Nathalie Adje, Stephane Yvon, Jean Jacques Zeiller
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Publication number: 20080153812Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: December 18, 2007Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: David Buttar, Kevin Micheal Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20080139599Abstract: Compounds of the formula (1) in which R1, R2,X, Y and Z are as defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.Type: ApplicationFiled: December 22, 2005Publication date: June 12, 2008Inventors: Michel Brunet, Nathalie Adje, Valerie Guyard-Dangremont, Francis Contard
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Patent number: 7384964Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: August 18, 2004Date of Patent: June 10, 2008Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexey Rivkin, Fumihiko Yoshimura, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong, Kaida Wu, Malcolm A. S. Moore, David Dorn
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Publication number: 20080114035Abstract: The present invention is directed to compounds of Formula III wherein the R1-R7 groups or substituents are defined herein. The present invention also comprises improved methods in the preparation of oxazoles in which the compounds of Formula III are intermediates and which results in higher yields with less impurities and contaminants. Oxazoles constitute valuable intermediates in the synthesis of pharmaceutically active substances such as, for example peroxisome proliferator activated receptor (PPAR) agonists which are pharmaceutical actives which can have a positive influence on both lipid and glucose metabolism.Type: ApplicationFiled: October 30, 2007Publication date: May 15, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wolfgang HOLLA, Rolf-Ludwig HOERLEIN, Berndt KULITZSCHER, Wolfgang LAUX, Thomas STUEDEMANN, Christoph TAPPERTZHOFEN, Robert J. H. SCHEFFER
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7365084Abstract: Provided herein are cycloalkyl-substituted amino acid derivatives, processes for their preparation and their use as pharmaceuticals.Type: GrantFiled: February 27, 2004Date of Patent: April 29, 2008Assignee: SanoFi-Aventis Deutschland GmbHInventors: Christian Stapper, Stefanie Keil, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Dirk Gretzke, Hans-Ludwig Schaefer, Wolfgang Wendler
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Patent number: 7365207Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and/or esters are pharmaceutically active substances.Type: GrantFiled: June 8, 2007Date of Patent: April 29, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Puentener, Michelangelo Scalone
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Patent number: 7358254Abstract: A method is provided for treating atherosclerosis and related diseases, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antiatherosclerotic agent, for example, an HMG CoA reductase inhibitor such as pravastatin.Type: GrantFiled: June 21, 2004Date of Patent: April 15, 2008Assignees: Bristol-Myers Squibb Company, President & Fellows of Harvard CollegeInventors: Jeffrey A. Robl, Rex A. Parker, Scott A. Biller, Haris Jamil, Bruce L. Jacobson, Krishna Kodukula, Gokhan Hotamisligil
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Patent number: 7358386Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: GrantFiled: May 5, 2006Date of Patent: April 15, 2008Assignee: Bayer Pharmaceuticals CorporationInventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
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Patent number: 7351728Abstract: Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubstituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is II, alkyl or haloalkyl, R4 is II, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.Type: GrantFiled: July 14, 2005Date of Patent: April 1, 2008Assignee: Eli Lilly and CompanyInventors: Dawn Alisa Brooks, Scott Eugene Conner, Samuel James Dominianni, Alexander Glenn Godfrey, Lynn Stacy Gossett, Christopher John Rito, Allie Edward Tripp, Alan M. Warshawsky, Leonard Larry Winneroski, Jr., Guoxin Zhu
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Patent number: 7348349Abstract: The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.Type: GrantFiled: July 18, 2005Date of Patent: March 25, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Markus Boehringer, Uwe Grether, Hans Hilpert, Georges Hirth, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Fabienne Ricklin
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Publication number: 20080070928Abstract: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.Type: ApplicationFiled: December 28, 2004Publication date: March 20, 2008Inventors: Katsumasa Nonoshita, Makoto Ishikawa, Hiroshi Nakashima, Daisuke Tsukahara, Yoshio Ogino, Fumiko Sakai, Yoshikazu Nagae, Keisuke Arakawa, Teruyuki Nishimura, Jun-Ichi Eiki
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Publication number: 20080064679Abstract: Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.Type: ApplicationFiled: June 23, 2005Publication date: March 13, 2008Inventors: Billy R. Martin, Raj K. Razdan, Anu Mahadevan
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Patent number: 7342041Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 11, 2008Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
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Patent number: 7332514Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.Type: GrantFiled: August 29, 2003Date of Patent: February 19, 2008Assignee: Japan Tobacco Inc.Inventors: Kimiya Maeda, Hironobu Nagamori, Hiroshi Nakamura, Hisashi Shinkai, Yasunori Suzuki, Daisuke Takahashi, Toshio Taniguchi
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Patent number: 7320995Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.Type: GrantFiled: July 31, 2003Date of Patent: January 22, 2008Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Jose Eugenio De Diego Gomez, Alfonso De Dios, Chafiq Hamdouchi Hamdouchi, Tiecho Li, Beatriz Lopez De Uralde Garmendia, Michal Vieth, Jeremy Schulenberg York, Robert Dean Dally, Miriam Filadelfa Del Prado Catalina, Carlos Jaramillo Aguado, Luisa Maria Martin-Cabrejas, Carlos Montero Salgado, Sheila Pleite Selgas, Concepcion Sanchez-Martinez, Timothy Alan Shepherd, James Howard Wikel
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Patent number: 7320978Abstract: This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.Type: GrantFiled: August 1, 2006Date of Patent: January 22, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Joelle Arnaud-Taillades, Christian Congy, Murielle Rinaldi-Carmona
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Patent number: 7319104Abstract: Compounds of formula (1) or a pharmaceutically acceptable salt, solvate, acid isostere, or hydrolyzable ester thereof, are disclosed. Methods of making and using the compounds are also disclosed.Type: GrantFiled: February 25, 2003Date of Patent: January 15, 2008Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Brad Richard Henke, Millard H. Lambert, III, Guangcheng Kevin Liu, Jennifer Susan Smith
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Patent number: 7319152Abstract: Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds.Type: GrantFiled: September 18, 2006Date of Patent: January 15, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Publication number: 20080006797Abstract: The present invention provides a photochromic compound that is colored when irradiated with visible light and quickly faded when set in a dark place. The photochromic compound according to the present invention is expressed by the following general formula (I): where each of A1, A2 and A3 is a five-member rings forming a 6?-electron system, the three rings being identical, partially identical or totally different from each other, and each ring may have a substituent; B1 and B2 are functional groups, each having an atomic number of five or larger, including a ring compound, and bonded to the 2-carbon of each of A2 and A3, respectively; and R1, R2 and R3 are substituents identical to or different from each other. This compound is highly colorable and durable even when it is dispersed into plastic macromolecular materials. Therefore, it is suitable as a dye material for sunglasses or similar products.Type: ApplicationFiled: March 21, 2007Publication date: January 10, 2008Applicant: NATIONAL UNIVERSITY CORPORATION NARA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
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Patent number: 7314884Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: December 13, 2004Date of Patent: January 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd Michael Loeffler, Ramakanth Sarabu, Hans Peter Wessel
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Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Patent number: 7307095Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: January 5, 2007Date of Patent: December 11, 2007Assignee: IRM LLCInventors: Hong Liu, David Tully, Phillip Alper, Robert Epple, Arnab Chatterjee, Michael Roberts
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Patent number: 7288557Abstract: The present invention relates to the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing such compounds and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: September 14, 2005Date of Patent: October 30, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Ulrike Reiff, Thomas von Hirschheydt, Edgar Voss
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Patent number: 7279485Abstract: Substituted heterocyclic derivatives are provided which have the structure wherein Z1 is (CH2)q or C?O; Z2 is (CH2)p or C?O; D is —CH? or C?O or (CH2)m where m is 0, 1, 2 or 3; n=0, 1 or 2; p=1 or 2; q=0, 1 or 2; Q is C or N; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4, X5 and X6 is N; and at least one of X2, X3, X4, X5 and X6 is C; A, B, R1, R2, R2a, R2b, R4, R3, E, Z and Y are as defined herein. In addition, a method is provided for treating diabetes, Type 2 diabetes, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids or glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, or atherosclerosis, wherein the substituted heterocyclic derivatives are administered in a therapeutically effective amount to a patient.Type: GrantFiled: July 8, 2003Date of Patent: October 9, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. W. Cheng, Sean Chen, Pratik Devasthale, Charles Z. Ding, Timothy F. Herpin, Shung Wu, Hao Zhang, Wei Wang, Xiang-Yang Ye
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Patent number: 7276526Abstract: Provided herein are novel substituted thiazoles and oxazoles of the Formula (I): as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof in the treatment of various neurological and psychological disorders, e.g., affective disorder, anxiety and depression, treatable by antagonizing CRF receptors.Type: GrantFiled: July 10, 2002Date of Patent: October 2, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Andreas Termin, Peter Grootenhuis, Dean Wilson, Valentina Molteni, Long Mao
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Patent number: 7268132Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: GrantFiled: April 28, 2005Date of Patent: September 11, 2007Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo
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Patent number: 7262303Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and/or esters are pharmaceutically active substances.Type: GrantFiled: September 2, 2004Date of Patent: August 28, 2007Assignee: Hoffman-La Roche Inc.Inventors: Kurt Puentener, Michelangelo Scalone
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Patent number: 7259178Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: June 27, 2005Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Patent number: 7259176Abstract: A novel process for the preparation of compounds of formula I and optionally converting a compound of formula I into a pharmaceutically acceptable salt is disclosed. The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances. Processes for the creation of intermediates are also disclosed.Type: GrantFiled: June 21, 2004Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wolfgang Goehring, Ursula Hoffmann, Michelangelo Scalone, Helmut Stahr, Shaoning Wang
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Patent number: 7259262Abstract: There are presented compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms thereof, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: October 15, 2004Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Ulrike Reiff, Matthias Rueth, Edgar Voss
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Patent number: 7259177Abstract: Provided herein are novel compounds of formula I below: in which the radicals are as defined, their physiologically acceptable salts, processes for their preparation, as well as methods of treating and/or preventing disorders of disorders of fatty acid metabolism and glucose utilization disorders, and also of disorders in which insulin resistance is involved, in a patient.Type: GrantFiled: February 27, 2004Date of Patent: August 21, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Christian Stapper, Stefanie Keil, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Dirk Gretzke, Hans-Ludwig Schaefer, Wolfgang Wendler
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Patent number: 7256206Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.Type: GrantFiled: February 11, 2004Date of Patent: August 14, 2007Assignee: IRM LLCInventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Wenqi Gao, Yi Fan, Sophie Lefebvre
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Patent number: 7250412Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: March 15, 2004Date of Patent: July 31, 2007Assignee: Auspex Pharmaceuticals, Inc.Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
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Patent number: 7247649Abstract: The present invention relates to novel oxazoles of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: August 3, 2004Date of Patent: July 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Ulrike Reiff, Matthias Rueth, Edgar Voss
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Patent number: 7241785Abstract: The present invention relates to a compound represented by the formula wherein R1 is an optionally substituted 5-membered heterocyclic group; X is a bond etc.; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond etc.; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n—Z1— (n is an integer of 0 to 8 and Z1 is a bond etc.) and the like; ring B is a 5-membered heterocycle optionally further having 1 to 3 substituents; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; R2 is —OH etc., or a salt thereof. A pharmaceutical composition containing this compound is useful as a prophylactic or therapeutic agent of diseases such as diabetes mellitus and the like.Type: GrantFiled: March 22, 2002Date of Patent: July 10, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Tsuyoshi Maekawa, Hiroshi Imoto, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7235574Abstract: The present invention provides the compounds of formula I-A their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: March 4, 2005Date of Patent: June 26, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Guy Georges, Matthias Rueth, Edgar Voss
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Patent number: 7229987Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.Type: GrantFiled: May 6, 2003Date of Patent: June 12, 2007Assignee: Eli Lilly and CompanyInventors: Jochen Ammenn, James Ronald Gillig, Lawrence Joseph Heinz, Philip Arthur Hipskind, Michael Dean Kinnick, Yen-Shi Lai, John Michael Morin, Jr., James Arthur Nixon, Carsten Ott, Kenneth Allen Savin, Theo Schotten, Lawrence John Slieker, Nancy June Snyder, Michael Alan Robertson
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Patent number: 7226920Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: August 6, 2004Date of Patent: June 5, 2007Assignee: Vertex Pharmaceuticals Inc.Inventors: Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang
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Patent number: 7208505Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g.Type: GrantFiled: August 6, 2002Date of Patent: April 24, 2007Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Rushad Eruch Karanjawala, Cynthia Darshini Jesudason, Theo Schotten, Britta Evers, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz
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Patent number: 7205324Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.Type: GrantFiled: June 19, 2003Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Henry H. Gu, T. G. Murali Dhar, Edwin J. Iwanowicz
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Patent number: 7205330Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: April 17, 2007Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Patent number: 7205326Abstract: Compounds of formula (I) are useful in the therapy and/or prevention of illnesses with known over-expression of receptor tyrosine kinases of the HER-family like HER-2 and EGFR (HER-1). Accordingly, these compounds are useful for the treatment of diseases such as cancer in humans or animals.Type: GrantFiled: April 28, 2004Date of Patent: April 17, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Ulrike Reiff, Matthias Rueth, Edgar Voss
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Patent number: 7196107Abstract: A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5.Type: GrantFiled: December 18, 2001Date of Patent: March 27, 2007Assignee: SmithKline Beecham CorporationInventors: Paul John Beswick, Vipulkumar Patel, Michael Lawrence Sierra
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Patent number: RE39575Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: GrantFiled: November 23, 2004Date of Patent: April 17, 2007Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught, Matthew S. Miller