Abstract: The invention relates to substituted anthranylalkyl and -cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
January 20, 2009
Assignee:
Novartis AG
Inventors:
Dieter Seidelmann, Martin Krueger, Eckhard Ottow, Andreas Huth, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey
Abstract: The present invention relates to an acid salt of amlodipine gentisate and a method of its preparation. More particularly, the present invention relates to a crystalline acid salt of amlodipine gentisate of the following formula 1 prepared by reacting amlodipine and gentisic acid, which is useful for the treatment of cardiovascular diseases and has the advantages of low toxicity, excellent stability, improved pharmaceutical efficacies and long-lasting concentration in blood.
Type:
Grant
Filed:
December 15, 2004
Date of Patent:
October 28, 2008
Assignee:
SK Chemicals Co., Ltd.
Inventors:
Jae-Sun Kim, Jin Young Choi, Je Ho Ryu, Nam Kyu Lee, Jeong-soo Jang, Woo Jae Jang, Key An Um, Do Seung Kum
Abstract: The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt thereof, a process for t he preparation of a compound of Formula (1a) and pharmaceutical compositions of a compound of Formula (1a).
Type:
Grant
Filed:
March 14, 2006
Date of Patent:
July 22, 2008
Assignee:
AstrZenca AB
Inventors:
Francis Thomas Boyle, Keith Hopkinson Gibson, Kevin Michael Foote
Abstract: The present invention provides, in a method for transporting charge using the molecular orientation in a liquid-crystalline state, a novel benzene derivative having a long, linear conjugated structure expected to have satisfactory charge-transport properties without photoexcitation, a process for producing the benzene derivative, and a liquid-crystal material including the benzene derivative.
Abstract: The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein.
Type:
Grant
Filed:
July 5, 2005
Date of Patent:
June 10, 2008
Assignee:
Roche Colorado Corporation
Inventors:
Peter J. Harrington, David A. Johnston, L. Mark Hodges
Abstract: Saturated and unsaturated heteroarylcycloalkylmethyl-amine compounds corresponding to formula I, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of saturated and unsaturated heteroarylcycloalkylmethyl-amines for the preparation of pharmaceutical formulations. pharmaceutical formulations and related methods of treatment or prophylaxis of certain condition, especially depression and/or pain, are also disclosed.
Type:
Grant
Filed:
June 20, 2005
Date of Patent:
June 10, 2008
Assignee:
Gruenenthal GmbH
Inventors:
Petra Bloms-Funke, Claudia Puetz, Ivars Graudums, Achim Kless, Carsten Griebel, Hagen-Heinrich Hennies, Dagmar Kaulartz, Sabine Reinardy, Derek Saunders, Klaus Schiene, Bernd Sundermann, Werner Englberger, Oswald Zimmer
Abstract: The present invention provides an amide-type carboxamide derivative of the formula [1]: wherein X is a group of the formula: —N? or the formula: —CH?; R1 is a halogen atom, a lower alkyl group, and the like; R2 is a group of the formula: and the like; Y1 and Y2 are the same or different and each is a group selected from a halogen atom, a lower alkyl group, a lower alkoxy group, and the like; Ring A is phenyl group, and the like, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of FXa.
Abstract: The present invention relates to a novel compound of formula (IV) which is an intermediate that can be used for the preparation of pioglitazone. It also relates to a method of obtaining the novel compound (IV) starting from the natural product L-tyrosine, in which the amino group is protected in the form of aromatic imino group, and a method of obtaining pioglitazone from the said intermediate.
Abstract: Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
Abstract: The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.
Abstract: 2-Chloro-5-trichloromethylpyridine is obtained by chlorinating ?-picoline in the vapor phase using a Mordenite zeolite or a supported palladium catalyst.
Type:
Grant
Filed:
April 26, 2005
Date of Patent:
March 18, 2008
Assignee:
Dow AgroSciences LLC
Inventors:
Kent Douglas Campbell, Dana Alan Livingston, Hawk Suewah Wan, Kenneth Michael Larson, Brian John Schoeman, Steven Roy Lakso
Abstract: A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof.
Abstract: A process is disclosed for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
Type:
Grant
Filed:
June 18, 2003
Date of Patent:
March 4, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Richard Bell, Paul John Beswick, Romain Luc Marie Gosmini, Richard Martin Grimes, Christopher Charles Frederick Hamlett, Nigel Paul King, Vipulkumar Kantibhai Patel
Abstract: The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Type:
Grant
Filed:
December 15, 2004
Date of Patent:
February 26, 2008
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Johannes Aebi, Denise Blum, Alexander Chucholowski, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand, Rene Trussardi, Elisabeth von der Mark, Sabine Wallbaum, Thomas Weller
Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.
Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
June 27, 2006
Date of Patent:
February 26, 2008
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong, Ronald A. Aungst, Jr.
Abstract: N-(Sulfonyloxybiarylmethyl) aminocyclopropanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Type:
Grant
Filed:
August 3, 2004
Date of Patent:
February 19, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert Gomez, Samson M. Jolly, John Jin Lim, Dai-shi Su
Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and pharmaceutically acceptable salts of the compounds of formula (I) and N-oxides thereof, Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmnaceutical compositions comprising compoundS of formula (I), their phatmaceUtical use and methods for their preparation.
Type:
Grant
Filed:
September 1, 2004
Date of Patent:
February 12, 2008
Assignee:
Aventis Pharma Limited
Inventors:
Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
Abstract: Benzimidazoles of general formula I and the use of benzimidazole derivatives for the production of pharmaceutical agents for treatment and prophylaxis of diseases that are associated with a microglia activation are described.
Type:
Grant
Filed:
December 8, 2005
Date of Patent:
February 12, 2008
Assignee:
Schering Aktiengesellschaft
Inventors:
Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning