Abstract: The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
Abstract: The present invention relates to a synthesis study of novel cyclic compounds having a quinolylalkylthio group represented by the formula (1), and pharmacological actions of the compounds. In the formula, the ring X represents: which may have halogen and/or alkyl; R1 and R2 independently represent hydrogen, alkyl, cycloalkyl, aryl or a (non) aromatic heterocycle; R3 represents qinolyl; A represents sulfur, sulfinyl or sulfonyl; and B represents alkylene.
Abstract: A compound of formula (I) is provided, wherein B, A, R1, R2, R3, R4, R5 and R6 are as defined herein and X? represents a pharmaceutically acceptable anion of a mono or polyvalent acid. Processes for the preparation of such compounds and pharmaceutical compositions containing them are also provided.
Type:
Grant
Filed:
August 31, 2006
Date of Patent:
February 22, 2011
Assignee:
Almirall, S.A.
Inventors:
Maria Prat Quinones, Maria Dolors Fernandez Forner, Maria Antonia Buil Albero
Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
Type:
Grant
Filed:
November 21, 2007
Date of Patent:
February 22, 2011
Assignee:
Plexxikon, Inc.
Inventors:
Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Hongyao Zhu, Marika Nespi, Chao Zhang
Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
Type:
Grant
Filed:
May 17, 2006
Date of Patent:
February 22, 2011
Assignee:
Merck Patent GmbH
Inventors:
Kai Schiemann, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Nina Heiss, Frank Zenke
Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Grant
Filed:
July 1, 2008
Date of Patent:
February 15, 2011
Assignee:
Neurosearch A/S
Inventors:
Dan Peters, Birgitte L. Eriksen, Elsebet Østergaard Nielsen, Jørgen Scheel-Krüger, Gunnar M. Olsen
Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.
Type:
Grant
Filed:
April 24, 2008
Date of Patent:
February 8, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ?4 integrin in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. wherein R1 is a methyl group and R2 is a methoxy group.
Abstract: The present invention relates to a compound which is N-(4-{4-[(6-butyl-8-quinolinyl)oxy]-1-piperidinyl}butyl)ethanesulfonamide and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various diseases, such as allergic rhinitis.
Type:
Grant
Filed:
August 13, 2008
Date of Patent:
February 8, 2011
Assignee:
Glaxo Group Limited
Inventors:
Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Panayiotis Alexandrou Procopiou, Sadie Vile
Abstract: A compound of formula (I) is provided, wherein B, A, R1, R2, R3, R4, R5 and R6 are as defined herein and X? represents a pharmaceutically acceptable anion of a mono or polyvalent acid. Processes for the preparation of such compounds and pharmaceutical compositions containing them are also provided. group or a —CH2OH group; and X? represents a pharmaceutically acceptable anion of a mono or polyvalent acid.
Type:
Grant
Filed:
August 31, 2006
Date of Patent:
February 1, 2011
Assignee:
Almirall, S.A.
Inventors:
Maria Prat Quinones, Maria Dolors Fernandez Forner, Maria Antonia Buil Albero
Abstract: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
Type:
Grant
Filed:
June 8, 2009
Date of Patent:
February 1, 2011
Assignee:
3M Innovative Properties Company
Inventors:
David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
Abstract: Disclosed are compounds that have excellent insecticidal activity and are usable as agricultural and horticultural insecticides. Compounds represented by formula (I) or agriculturally and horticulturally acceptable acid addition salts thereof have excellent insecticidal activity and are usable as agricultural and horticultural insecticides.
Abstract: The present invention relates to a medicine, particularly a medicine comprising a novel cyclohepta[b]pyridine-3-carbonylguanidine derivative having an inhibitory effect on an Na+/H+ exchanger (NHE). There is provided a cyclohepta[b]pyridine-3-carbonylguanidine derivative represented by Formula (1): wherein R1 is a group selected from a sulfo group, a sulfoxy group, —OCONH—(CH2CH2O)n—SO3H and the following formulas: R2 represents a halogen atom, a lower alkyl group or a lower alkoxy group; and n represents an integer from 1 to 10, or a pharmaceutically acceptable salt thereof.
Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
September 22, 2008
Date of Patent:
January 25, 2011
Assignee:
Theravance, Inc.
Inventors:
Adam A. Goldblum, Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Lan Jiang, Daniel D. Long, Daniel Marquess, S. Derek Turner
Abstract: The present invention relates to 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Abstract: The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.
Type:
Grant
Filed:
December 2, 2005
Date of Patent:
January 25, 2011
Assignee:
Abbott Laboratories
Inventors:
Sean C. Turner, Tammie K. Jinkerson, Arthur R. Gomtsyan, Chih-Hung Lee
Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
Type:
Grant
Filed:
December 20, 2007
Date of Patent:
January 18, 2011
Assignee:
Plexxikon, Inc.
Inventors:
Prabha N. Ibrahim, Ryan Bremer, Chao Zhang, Jiazhong Zhang, Klaus-Peter Hirth, Guoxian Wu, Hongyao Zhu
Abstract: The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.
Type:
Grant
Filed:
September 29, 2006
Date of Patent:
January 11, 2011
Assignee:
N.V. Organon
Inventors:
Susan Elizabeth Napier, Matilda Jane Bingham, Margaret Jean Huggett, Mark Huggett, Yasuko Kiyoi, Olaf Nimz