The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Patent number: 8119673Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.Type: GrantFiled: June 23, 2009Date of Patent: February 21, 2012Assignee: AstraZeneca ABInventors: Jonas Brånalt, David Gustafsson, Ingemar Nilsson, Magnus Polla
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Publication number: 20120029201Abstract: The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid.Type: ApplicationFiled: October 6, 2011Publication date: February 2, 2012Inventor: Silvo Zupancic
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Patent number: 8106216Abstract: The present invention relates to an improved process for the preparation of 2-n-butyl-3-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]-1,3-diazaspiro[4.4]non-1-en-4-one (Irbesartan).Type: GrantFiled: April 23, 2007Date of Patent: January 31, 2012Assignee: Aurobindo Pharma Ltd.Inventors: Venkata vara prasada rao Korrapati, Venkata subramanyeswara rao Inti, Rani Ananta, Ramesh Dandala, Sivakumaran Meenakshisunderam
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Publication number: 20120022119Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 16, 2009Publication date: January 26, 2012Applicant: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
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Publication number: 20120022268Abstract: The invention relates to new forms of salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventor: Erwin Ernst Marti
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Publication number: 20120015944Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: September 22, 2011Publication date: January 19, 2012Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20120015990Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.Type: ApplicationFiled: June 17, 2011Publication date: January 19, 2012Applicant: THE WASHINGTON UNIVERSITYInventors: James Hsieh, Emily Cheng
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Publication number: 20120010250Abstract: The present invention relates to novel anthranilamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q, Y and n are each as defined in the description—, to the use thereof as insecticides and acaricides for control of animal pests, and to several processes for preparation thereof.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicant: BAYER CROPSCIENCE AGInventors: Rüdiger FISCHER, Ernst Rudolf GESING, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Arnd VOERSTE, Ulrich GORGENS
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Publication number: 20110319438Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Patent number: 8084451Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: GrantFiled: January 10, 2006Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Rao Vemuri, Teresa Olszewska
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Patent number: 8084467Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: June 24, 2005Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally, Venkata Kiran Vemuri
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Patent number: 8084398Abstract: Benzoylpyrazoles represented by the following formula (I), and use thereof as herbicides. R1 represents alkyl; R2 represents alkyl or cycloalkyl; R3 represents hydrogen, alkyl, alkenyl, alkynyl, aralkyl, alkylsulfonyl, optionally substituted phenylsulfonyl, acyl or acylalkyl; X represents halogen or alkyl; Y represents halogen; n represents 2 or 3, and T represents the above group T1 or T2, wherein R4 represents hydrogen, alkyl, alkoxy or alkylthio.Type: GrantFiled: October 2, 2007Date of Patent: December 27, 2011Assignee: Bayer Cropscience AGInventors: Shinichi Narabu, Yasushi Yoneta, Akihiko Yanagi, Shinichi Shirakura, Seiji Ukawa, Teruyuki Ichihara, Shin Nakamura, Martin Hills, Heinz Kehne, Jan Dittgen, Dieter Feucht, Christopher Rosinger
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Publication number: 20110313003Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20110312953Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: December 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Rùdiger FISCHER, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Ernst Rudolf GESING, Arnd VOERSTE, Ulrich GÖGENS
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Patent number: 8076492Abstract: A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, b) deesterifying the compound of formula (V) with a base; and c) reacting the product of step (b) with 4-halomethyl-5-methyl-2-oxo-1,3-dioxolene of formula (IV), wherein X is halogen selected from F or Cl or Br or I, to obtain trityl olmesartan medoxomil of formula. The trityl olmesartan medoxomil may be deprotected to produce olmesartan medoxomil.Type: GrantFiled: October 9, 2007Date of Patent: December 13, 2011Assignee: Cipla LimitedInventors: Srinivas Laxminarayan Pathi, Ravikumar Puppala, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
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Publication number: 20110301196Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.Type: ApplicationFiled: January 28, 2011Publication date: December 8, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Publication number: 20110300104Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Patent number: 8071628Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: GrantFiled: September 8, 2010Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Patent number: 8063082Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: August 1, 2007Date of Patent: November 22, 2011Assignee: Cytokinetics, Inc.Inventors: Xiangping Qian, Jeffrey T. Finer, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
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Publication number: 20110281795Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: January 15, 2010Publication date: November 17, 2011Inventors: Songnian Lin, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
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Publication number: 20110281811Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.Type: ApplicationFiled: November 12, 2009Publication date: November 17, 2011Inventor: Sabine Rupprecht
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Patent number: 8058449Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: November 7, 2007Date of Patent: November 15, 2011Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20110275828Abstract: The present invention relates to a process for the preparation of 2-butyl-3-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]-1,3-diazaspiro[4,4]non-1-en-4-one by reaction of the corresponding nitrile with sodium azide and piperazine or its acid salt.Type: ApplicationFiled: June 21, 2010Publication date: November 10, 2011Applicant: DIVI'S LABORATORIES LTD.Inventors: Murali Krishna Prasad DIVI, Mysore Aswatha Narayana RAO, Surendra Kalyan NUTHI, Yugandar Phaniram BANDARU
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Patent number: 8053455Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;??2) Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—R3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: April 25, 2011Date of Patent: November 8, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent Whitehead
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Patent number: 8053453Abstract: A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): wherein A is a C?2-14#191 aryl group, B is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, D is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, and E is a C?2-14#191 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the activator or a solvate thereof, as an active ingredient.Type: GrantFiled: October 9, 2003Date of Patent: November 8, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Norihisa Ishiwata, Takanori Nakamura
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Publication number: 20110263666Abstract: The present invention relates to a process for the preparation and purification of olmesartan medoxomil hydrohalide salts and optionally converting them to olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.Type: ApplicationFiled: August 7, 2008Publication date: October 27, 2011Applicant: LEK PHARMACEUTICALS D.D.Inventors: Samo Pirc, Lovro Selic
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Publication number: 20110257191Abstract: The present invention constitutes new hydrazine-substituted anthranilic acid derivatives of the general formula (I), in which R1, R2, R3, R4, R5, R6, Qx, A, Qy and n have the definitions indicated in the description, application thereof as insecticides and acaricides for controlling animal pests, alone and in combination with further agents for activity boosting, and a number of processes for their preparation.Type: ApplicationFiled: February 8, 2011Publication date: October 20, 2011Applicant: Bayer CropScience AGInventors: Rüdiger Fischer, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christoph Grondal, Achim Hense, Arnd Voerste
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Publication number: 20110257164Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.Type: ApplicationFiled: January 7, 2010Publication date: October 20, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
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Patent number: 8039495Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: October 15, 2010Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110251248Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: December 9, 2009Publication date: October 13, 2011Inventors: Songnian Lin, Xibin Liao, Roman Kats-Kagan, John E. Stelmach, Emma R. Parmee
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Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Publication number: 20110224188Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: ApplicationFiled: November 20, 2008Publication date: September 15, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
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Publication number: 20110224271Abstract: The present invention relates to a process for the preparation and purification of trityl olmesartan medoxomil and olmesartan medoxomil.Type: ApplicationFiled: August 7, 2008Publication date: September 15, 2011Applicant: LEK PHARMACEUTICALS D.D.Inventor: Renata Toplak Casar
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Publication number: 20110224228Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: August 10, 2009Publication date: September 15, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: Mark L Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Ahmed Mamai
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Patent number: 8017607Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: GrantFiled: October 6, 2010Date of Patent: September 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Patent number: 8008290Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: GrantFiled: August 9, 2010Date of Patent: August 30, 2011Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
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Patent number: 8003680Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: September 8, 2009Date of Patent: August 23, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20110201621Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Applicant: MERCK SHARP & DOHME CORP.Inventors: Amjad ALI, Michael Man-Chu LO, Christopher FRANKLIN, Brent R. WHITEHEAD
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Publication number: 20110196111Abstract: Disclosed herein is a surface functionalized poly(dimethylsiloxane) (PDMS) and methods for making the same. The surface functionalized PDMS disclosed herein is applicable in the general field of microfluidics, bioMEMS (bio-microelectromechanical systems), soft lithography, and other related biotechnology fields.Type: ApplicationFiled: August 29, 2008Publication date: August 11, 2011Inventors: Hongwei Ma, Long Fu
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Patent number: 7994339Abstract: Disclosed is a phthalamide derivative represented by the general formula (I) or a salt thereof, which shows an excellent controlling effect for use as an agricultural or horticultural insecticide alone or in combination with other agricultural or horticultural insecticide, acaricide, nematicide, fungicide, herbicide, plant growth regulator, biopesticide or the like.Type: GrantFiled: December 14, 2006Date of Patent: August 9, 2011Assignee: Nihon Nohyaku Co., Ltd.Inventors: Hiroto Harayama, Masanori Tohnishi, Shinsuke Fujioka, Akiyuki Suwa
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Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. 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: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110178007Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: September 30, 2009Publication date: July 21, 2011Inventors: Andrew Stamford, Michael W Miller, Duane Eugene Demong, William J Greenlee, Joseph A Kozlowski, Brian J Lavey, Michael K.C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
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Publication number: 20110166138Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.Type: ApplicationFiled: March 17, 2009Publication date: July 7, 2011Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
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Patent number: 7964737Abstract: Disclosed herein a process for producing 2-(n-butyl)-3-[[2?-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one of formula (I) in pure form by using selective solvent system and cost efficient raw materials and reagents.Type: GrantFiled: July 27, 2006Date of Patent: June 21, 2011Assignee: Jubilant Organosys LimitedInventors: Charugundla Kishore, Vinod Vishwanath Bandi, Rajappa Murali, Mysore A. Sathish, Sulur G. Manjunatha
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Publication number: 20110144110Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 7960369Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.Type: GrantFiled: November 6, 2003Date of Patent: June 14, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
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Publication number: 20110136881Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 9, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20110130432Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.Type: ApplicationFiled: June 22, 2009Publication date: June 2, 2011Applicant: ASTRAZENECA ABInventors: Jonas Branalt, David Gustafsson, Ingemar Nilsson, Magnus Polla