Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Type:
Grant
Filed:
October 21, 2008
Date of Patent:
March 15, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
Abstract: Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
July 9, 2007
Date of Patent:
March 8, 2011
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Albert C. Pierce, Michael Arnost, Robert J. Davies, Cornelia J. Forster, Vincent Galullo, Ronald Grey, Jr., Mark Ledeboer, Shi-Kai Tian, Jinwang Xu, Hayley Binch, Brian Ledford, David Messersmith, Suganthi Nanthakumar, Andrew Jayaraj, Greg Henkel, Francesco G. Salituro, Jian Wang
Abstract: A ?-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X?N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The ?-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.
Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
December 10, 2008
Date of Patent:
March 8, 2011
Assignee:
AstraZeneca AB
Inventors:
Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
Type:
Grant
Filed:
June 25, 2007
Date of Patent:
March 8, 2011
Assignee:
SmithKline Beecham (Cork) Limited
Inventors:
Christopher S. Brook, Wei Chen, Philip C. Dell'Orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
Abstract: The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
March 1, 2011
Assignee:
Sanofi-Aventis
Inventors:
Stefan Petry, Gerhard Zoller, Norbert Tennagels, Günter Müller
Abstract: The present invention provides a novel substance having an excellent color purity of blue, a light-emitting element and a light-emitting device using the novel substance. A stilbene derivative has a structure shown by the general formula (1). In the general formula (1), R1 is hydrogen, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 25 carbon atoms. R2 is an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 25 carbon atoms. Each of R3 to R5 is hydrogen or an alkyl group having 1 to 4 carbon atoms. Ar1 is an aryl group having 6 to 25 carbon atoms.
Type:
Grant
Filed:
January 9, 2009
Date of Patent:
March 1, 2011
Assignee:
Semiconductor Energy laboratory Co., Ltd.
Abstract: The present invention provides a means which can inhibit release of I2 in production or storage of 1,3-diiodohydantoin compound, and thereby solve decrease in purity of the compound and various problems caused by I2. The present invention provides a production method for 1,3-diiodohydantoin compound comprising a step to prepare a wet body containing a 1,3-diiodohydantoin compound, and (1) a step to dry the wet body by contacting the wet body with heated gas or (2) a step to lyophilize the wet body, a storage method for 1,3-diiodohydantoin compound comprising a step to store a 1,3-diiodohydantoin compound under a temperature condition of 15° C. or lower, and a 1,3-diiodohydantoin compound wherein content of released I2 is 1% by mass or less.
Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 independently represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 and X2 represent hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom), provided that R1 and R2 do not simultaneously represent hydrogen atom; R3 and R6 represent an alkyl group; R4 and R7 represent hydrogen atom, an alkyl group, carboxy group, an alkoxycarbonyl group, or sulfo group; and R5 and R8 represents an alkyl group, an aryl group, an alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group], or a salt thereof, which is usable for efficient screening for a chemical substance having applicability as a catalyst of the reaction of Michael addition.
Abstract: The present invention relates to novel processes for preparing DPP-IV inhibitors having the structure of formula I, and pharmaceutically acceptable salt thereof, which are useful for treatment of Type 2 diabetes.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
February 22, 2011
Assignee:
Glenmark Pharmaceuticals, S.A.
Inventors:
Abraham Thomas, V. S. Prasada Rao Lingam, Ashok Bhausaheb Kadam, Suresh M. Kadam, Shantaram Kashinath Phatangare, Deepak Vitthal Ukride
Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
Type:
Grant
Filed:
April 1, 2008
Date of Patent:
February 22, 2011
Assignee:
Virobay, Inc.
Inventors:
John O. Link, Craig J. Mossman, Jie Liu, Soon Hyung Woo
Abstract: Cyanine-type fluorescent dyes modified with an alkynyl linker arm of formula (I), suitable for the conjugation of biomolecules, such as for example nucleosides, nucleotides, oligonucleotides, nucleic acids, proteins, peptides, vitamins and hormones. A method and intermediates for the synthesis of the alkynyl cyanines of the invention are also described, as well as alkynyl cyanine-biomolecule conjugates and methods for preparing thereof. The alkynyl cyanines can be advantageously used as markers for biomolecules or as quenchers.
Abstract: The present invention relates to 4,5-bis(4-methoxyphenyl)imidazole compound inducing differentiation of myoblasts or muscle fibers into neuron cells, a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation. More specifically, it relates to 2-{2-[5-(3-chlorophenyl)]furanyl}-4,5-bis(4-methoxyphenyl)imidazole that induces differentiation of myoblasts or muscle fibers into neuron cells, all pharmaceutically acceptable isomers, salts, and a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation.
Type:
Grant
Filed:
March 30, 2010
Date of Patent:
February 15, 2011
Assignee:
Industry-Academic Cooperation Foundation, Yonsei University
Inventors:
In-Jae Shin, Myung-Ryul Lee, Darren Williams
Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.
Type:
Grant
Filed:
March 2, 2004
Date of Patent:
February 15, 2011
Assignee:
Bayer CropScience AG
Inventors:
Reiner Fischer, Klaus Kunz, Stefan Lehr, Michael Ruther, Udo Schneider, Markus Dollinger, Mark Wilhelm Drewes, Dieter Feucht, Jörg Konze, Ulrike Wachendorff-Neumann, Guido Bojack, Thomas Auler, Martin Jeffrey Hills, Thomas Bretschneider, Olga Malsam, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Alfred Angermann, Heinz Kehne, Christopher Hugh Rosinger
Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
July 23, 2009
Date of Patent:
February 15, 2011
Assignee:
Theravance, Inc.
Inventors:
Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
Abstract: The invention provides a compound of general formula (I) wherein the compounds are of the class ureido-thiazole glucokinase activators, useful for the treatment of various diseases, for example, type 2 diabetes.
Type:
Grant
Filed:
July 14, 2006
Date of Patent:
February 8, 2011
Assignee:
Novo Nordisk A/S
Inventors:
Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
Abstract: The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4?-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan.
Abstract: The present invention relates to the use of bora-tetraazapentalenes with the general formula A as redox-dopant and/or emitter in electronic, optoelectronic or electroluminescent structural elements.