Additional Hetero Ring Containing Patents (Class 544/60)
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Publication number: 20110306606Abstract: The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyridine derivative compound of the present invention increases osteoblast activity and effectively inhibits the differentiation of osteoclasts, and thus can be usefully used for the prevention and treatment of osteoporosis.Type: ApplicationFiled: December 4, 2009Publication date: December 15, 2011Inventors: Jei Man Ryu, Jin Soo Lee, Whui Jung Park, Yun Ha Hwang, Ki Yoon Kim
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Patent number: 8067409Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: November 20, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
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Publication number: 20110288065Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom,; and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)R3 (R3 is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.Type: ApplicationFiled: February 5, 2010Publication date: November 24, 2011Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
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Publication number: 20110251188Abstract: The present invention relates to acenaphtho heterocyclic compounds, cyclodextrin inclusion compounds and complexes thereof, and their uses in manufacturing the inhibitors of BH3 analogue, Bcl-2 family proteins. The acenaphtho heterocyclic compounds are obtained by introducing oxo-, thio-, carbonyl, ester or acyl in the 3-, 4- and 6-position of 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile, or further substituting 9-cyano with carboxyl, ester or amide. The compounds can simulate BH3-only protein, competitively binding and antagonizing Bcl-2, Bel-XL and Mcl-1 proteins in vitro or intracellular, to induce cell apoptosis. The cyclodextrin inclusion compounds and complexes can improve the effects. Therefore, they all can be used in the manufactures of anticancer compounds.Type: ApplicationFiled: October 25, 2009Publication date: October 13, 2011Applicant: DALIAN UNIVERSITY OF TECHNOLOGYInventors: Zhichao Zhang, Guiye Wu, Ting Song, Feibo Xie
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Publication number: 20110224187Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: October 14, 2009Publication date: September 15, 2011Inventors: Anandan Palani, Michael Y. Berlin, Aslanian G. Robert, Vaccaro M. Henry, Chan Tin-Yau, Xiao Dong, Degrado Sylvia, Rao U. Ashwin, Chen Xiao, Lee Yoon Joo, Sofolarides J. Michael, Shao Ning, Huang R. Ying, Liu Zhidan, Wang Li Yuan, Pu Haiyan
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Publication number: 20110224198Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Scott D. Kuduk, Douglas C. Beshore, ChristinaNg Di Marco, Thomas J. Greshock
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Patent number: 8012959Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.Type: GrantFiled: September 22, 2008Date of Patent: September 6, 2011Assignee: Astellas Pharma Inc.Inventors: Shinya Nagashima, Hiroshi Nagata, Masashiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
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Publication number: 20110207926Abstract: A compound represented by formula (1), a tautomer thereof, or a salt of the compound or tautomer, which is useful as a bactericide/disinfectant. In the formula, R1 represents a hydrogen atom, an optionally substituted alkyl group or the like, R2 represents a hydrogen atom or an optionally substituted alkyl group, or alternatively R1 and R2 may combine together with an adjacent nitrogen atom to form an optionally substituted nitrogen-containing heterocyclic group; R4 represents a hydrogen atom or an optionally substituted alkyl group; R3 represents an optionally substituted alkyl group; and R5 and R6 each represents a hydrogen atom or a methyl group, excluding a compound wherein both R2 and R4 represent a hydrogen atom and a compound wherein both R1 and R4 represent a hydrogen atom are excluded.Type: ApplicationFiled: August 24, 2009Publication date: August 25, 2011Applicant: HAMARI CHEMICALS, LTD.Inventors: Shirou Maeda, Akihisa Maeda
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Patent number: 7998951Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: March 3, 2008Date of Patent: August 16, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, John F. Kadow
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Patent number: 7994338Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.Type: GrantFiled: August 16, 2007Date of Patent: August 9, 2011Assignees: The J. David Gladstone Institutes, University Of Maryland, BaltimoreInventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Patent number: 7989446Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: GrantFiled: September 22, 2010Date of Patent: August 2, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Patent number: 7968591Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
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Patent number: 7964592Abstract: Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: March 12, 2004Date of Patent: June 21, 2011Assignee: Novartis AGInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Patent number: 7960560Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, canceType: GrantFiled: December 1, 2009Date of Patent: June 14, 2011Assignee: N.V. OrganonInventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
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Publication number: 20110136796Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: April 24, 2009Publication date: June 9, 2011Applicants: NEWLINK GENETICS, LANKEANAU INSTITUTE FOR MEDICAL RESEARCHInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski
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Patent number: 7947830Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 23, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Sven Franciscus Anna Van Brandt, Kristof Van Emelen, Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Janine Arts
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Publication number: 20110118230Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 10, 2009Publication date: May 19, 2011Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum Macleod, Karen Williams
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Patent number: 7943605Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: GrantFiled: October 25, 2006Date of Patent: May 17, 2011Assignee: UCB Pharma S.A.Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
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Publication number: 20110105456Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: December 22, 2010Publication date: May 5, 2011Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Matin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Publication number: 20110105485Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: July 21, 2010Publication date: May 5, 2011Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Publication number: 20110098285Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: August 3, 2010Publication date: April 28, 2011Applicant: ABBOTT LABORATORIESInventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
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Patent number: 7910581Abstract: The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.Type: GrantFiled: March 3, 2006Date of Patent: March 22, 2011Inventors: Mariangela Biava, Fabrizio Manetti, Delia Deidda, Raffaello Pompei, Maurizio Botta, Giulio Cesare Porretta
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Patent number: 7910582Abstract: Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: GrantFiled: January 28, 2010Date of Patent: March 22, 2011Assignee: Janssen Pharmaceutica NVInventors: Brett D. Allison, Cheryl A. Grice
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Patent number: 7897597Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: August 27, 2004Date of Patent: March 1, 2011Assignee: 3M Innovative Properties CompanyInventors: Kyle J. Lindstrom, Hugues M. H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Tushar A. Kshirsagar, Philip D. Heppner, Shri Niwas, George W. Griesgraber, Matthew R. Radmer
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Patent number: 7879882Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.Type: GrantFiled: October 6, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
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Publication number: 20110021511Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: ApplicationFiled: December 21, 2007Publication date: January 27, 2011Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
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Patent number: 7863446Abstract: Novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof are described. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell-damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.Type: GrantFiled: February 8, 2008Date of Patent: January 4, 2011Assignee: Orchid Research Laboratories LimitedInventors: Akella Satya Surya Visweswara Srinivas, Ravikumar Tadiparthi, Ganapavarapu Veera Raghava Sharma, Sappanimuthu Thirunavukkarasu, Durairaj Peter Bhakiaraj, Virendra Kachhadia, Kilambi Narsimhan, Sathya Narayana Thara, Sriram Rajagopal, Gaddam Om Reddy, Sukunath Narayanan, Venkatesan Parameswaran, Venkatesan Janarthanam, Maruthikumar Narayanam, Sathyanarayana Gadde, Uma Ramachandran
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Patent number: 7851469Abstract: The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.Type: GrantFiled: June 16, 2008Date of Patent: December 14, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
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Patent number: 7842808Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: January 5, 2007Date of Patent: November 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
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Publication number: 20100298558Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.Type: ApplicationFiled: December 5, 2008Publication date: November 25, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
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Patent number: 7834002Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: GrantFiled: April 28, 2005Date of Patent: November 16, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Patent number: 7834003Abstract: The invention relates to 5-Aminopyrazole derivatives of formula (I) or salts thereof, a process for their preparation, to compositions thereof and to their use for the control of pests, including arthropods and helminths.Type: GrantFiled: June 7, 2007Date of Patent: November 16, 2010Assignee: Merial LimitedInventors: Stefan Schnatterer, Michael Maier, Friederike Petry, Werner Knauf, Karl Seeger
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Patent number: 7834007Abstract: The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: August 23, 2006Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Han, Prasad V. Chaturvedula
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Publication number: 20100273764Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: April 27, 2010Publication date: October 28, 2010Applicant: Amgen Inc.Inventors: Kristin Andrews, Yunxin Y. Bo, Shon Booker, Victor J. Cee, Noel D'Angelo, Bradley J. Herberich, Fang-Tsao Hong, Claire L.M. Jackson, Brian A. Lanman, Hongyu Liao, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Anthony B. Reed, Adrian L. Smith, Seifu Tadesse, Nuria A. Tamayo, Bin Wu, Ryan Wurz, Kevin Yang
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Patent number: 7820654Abstract: The present invention is directed to a compounds, methods and compositions for making the compounds and methods of treating a variety of diseases and disease states including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan, comprising the administration of new heterocyclic compounds, particularly substituted pyrimidines.Type: GrantFiled: September 23, 2005Date of Patent: October 26, 2010Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Manojit Pal, Srinivas Kalleda, Srinivas Padakanti, Nalivela Kumara Swamy, Koteswar Rao Yeleswarapu, Christopher W. Alexander, Ish Khanna, Javed Iqbal, Sivaram Pillarisetti, Deepak Barange
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100267706Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1 or 2 or encompassed by formulas I, Ia, II, III, and IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Inventors: Michael Geoffrey Neil Russell, Stephen David Penrose, Kevin James Doyle
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Publication number: 20100267709Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: December 9, 2008Publication date: October 21, 2010Inventors: Jonathan R. Young, Jongwon Lim, Michelle R. Machacek, Brandon Mitsuo Taoka, Ryan D. Otte
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Patent number: 7816349Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 23, 2007Date of Patent: October 19, 2010Assignee: Eli Lilly and CompanyInventors: John Gordon Allen, Alexei Pavlovych Krasutsky, Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Publication number: 20100249402Abstract: The present invention relates to novel benzamidine derivatives, a process for the preparation thereof and a pharmaceutical composition for preventing or treating osteoporosis comprising the same. The benzamidine derivatives of the present invention effectively inhibit osteoclast differentiation at an extremely low concentration, and thus can be advantageously used for the prevention and treatment of osteoporosis.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Applicant: DONG WHA PHARMACEUTICAL CO. LTD.Inventors: Jei Man Ryu, Jin Soo Lee, Young Goo Jin, Jae Hoon Park, Bo Kyung Kim, Dae Yeon Won, Yun-Ha Hwang, Ki Yoon Kim, Sae Kwang Ku
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Patent number: 7795271Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: May 4, 2009Date of Patent: September 14, 2010Assignee: Pharmacia CorporationInventor: Richard C. Durley
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Publication number: 20100227855Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: ApplicationFiled: March 16, 2010Publication date: September 9, 2010Applicant: ENDORECHERCHE, INC.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, René Maltais
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Patent number: 7786110Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: November 8, 2007Date of Patent: August 31, 2010Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20100215618Abstract: The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and L are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of hepatitis C virus.Type: ApplicationFiled: February 23, 2010Publication date: August 26, 2010Applicant: Arrow Therapeutics LimitedInventors: Malcolm Clive Carter, Neil Mathews
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Patent number: 7781426Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
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Publication number: 20100197672Abstract: The present invention relates to a compound having the general formula (3): synthesis, intermediates and uses thereof.Type: ApplicationFiled: September 25, 2008Publication date: August 5, 2010Applicants: UNIVERSITA DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITA DEGLI STUDI DI SIENAInventors: Mariangela Biava, Giulio Cesare Porretta, Raffaello Pompei, Maurizio Botta, Fabrizio Manetti, Alessandro De Logu
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Publication number: 20100173891Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Inventors: Brian Herbert, Wenge Xie, Truc Minh Nguyen, Allen T. Hopper, Ashok Tehim