At 2-position Patents (Class 544/315)
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Patent number: 8222266Abstract: The present invention relates to certain azabicyclo compounds of formula (I)?: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.Type: GrantFiled: March 30, 2007Date of Patent: July 17, 2012Assignee: Glaxo Group LimitedInventors: Barbara Bertani, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Silvia Terreni
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Patent number: 8222412Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: GrantFiled: September 23, 2010Date of Patent: July 17, 2012Assignee: AstraZeneca UK LimitedInventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Patent number: 8217155Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —OH or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms.Type: GrantFiled: July 31, 2008Date of Patent: July 10, 2012Assignees: Gilead Colorado, Inc., Abbott GmbH & Co. KGInventors: Lawrence S. Melvin, Jr., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
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Patent number: 8178700Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.Type: GrantFiled: May 4, 2009Date of Patent: May 15, 2012Assignee: International Business Machines CorporationInventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Publication number: 20120021909Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Patent number: 8101615Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 15, 2005Date of Patent: January 24, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Patent number: 8048883Abstract: This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as ?2 Form, which is stable at room temperature and even at higher temperatures up to 120° C. and accelerated stress conditions and, freely soluble in water. This invention also discloses a pharmaceutical composition containing the novel stable ?2 form of Imatinib mesylate and other usually employed excipients, useful in the treatment of Chronic Myelogenous Leukemia (CML). This new ?2 Form of imatinib mesylate is prepared by slurrying Imatinib base in isopropanol at room temperature followed by addition of methane sulfonic acid and maintaining 50-60 ° C. followed by filtration. This invention also discloses another process for the preparation of the novel, stable ?2 crystalline form of Imatinib Mesylate by the conversion of Imatinib mesylate ?-polymorphic modification by suspending it in water and organic solvents, distilling off water azeotropically, cooling and filtering to obtain the ?2 crystal form.Type: GrantFiled: November 16, 2004Date of Patent: November 1, 2011Assignee: Natco Pharma LimitedInventors: Kompella Amala, Thungathurthi Srinivasa Rao, Bhujanga rao Adibhatla Kali Satya, Sreenivas Rachakonda, Nannapaneni Venkaiah Chowdary, Khadgapathi Podili
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Patent number: 8008488Abstract: The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C?CH, C?CH—CH2 or CH—CH?CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents.Type: GrantFiled: March 12, 2004Date of Patent: August 30, 2011Assignee: Abbott GmbH & Co. KGInventors: Hervé Geneste, Andreas Kling, Wilfried Braje, Andreas Haupt, Liliane Unger
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Patent number: 7998959Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.Type: GrantFiled: January 11, 2007Date of Patent: August 16, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, David M. Burns, Lihua Chen, Jincong Zhuo, Chunhong He
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Publication number: 20110178297Abstract: A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R1—C (O)—X, to a vinyl ether of formula (II): CH2?CH—OR2, to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.Type: ApplicationFiled: September 25, 2009Publication date: July 21, 2011Applicant: SOLVAY SAInventor: Max Braun
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Publication number: 20110124619Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: November 17, 2010Publication date: May 26, 2011Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Patent number: 7939523Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.Type: GrantFiled: January 5, 2009Date of Patent: May 10, 2011Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yen-Shian Wu, Sheng-Ju Hsu, Yueh Andrew Yueh, Yu-Sheng Chao
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Patent number: 7923556Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, and solvates thereof, are useful as kinase inhibitors, wherein: two of X1, X2, and X3 are N, and the remaining one of X1, X2, and X3 is —CR1; R1 is hydrogen or —CN; and N, G, Z, R2, R3, R4, R5, and R6 are described in the specification. Also disclosed are pharmaceutical compositions containing compounds of formula (I), and methods of treating conditions associated with the activity of p38 kinase and/or conditions associated with the activity of LIM kinase.Type: GrantFiled: September 30, 2009Date of Patent: April 12, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Shuqun Lin, Katerina Leftheris, Liqi He, Steven P. Seitz, Tai-An Lin, Wayne Vaccaro
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Publication number: 20110077153Abstract: The present invention relates to heteroarylylmethyl sulfonamides of formula I wherein B, E, Ra, n, R, A, Y and Cy are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.Type: ApplicationFiled: May 18, 2009Publication date: March 31, 2011Applicant: BASF SEInventors: Jan Klaas Lohmann, Alice Glaettli, Wassilios Grammenos, Bernd Mueller, Marianna Vrettou, Jens Renner, Sarah Ulmschneider, Jochen Dietz
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Patent number: 7915271Abstract: 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. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: GrantFiled: December 29, 2006Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Patent number: 7893073Abstract: The invention relates to novel 3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in compositions, and in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 15, 2005Date of Patent: February 22, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Patent number: 7872012Abstract: Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia.Type: GrantFiled: December 23, 2005Date of Patent: January 18, 2011Assignee: Zhejiang Hisun Pharma Co., Ltd.Inventor: Hui Yao
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Publication number: 20110009398Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.Type: ApplicationFiled: July 18, 2008Publication date: January 13, 2011Inventors: Toshiyuki Sakai, Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Patent number: 7863445Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: August 17, 2009Date of Patent: January 4, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20100331326Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Mark G. BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100280242Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.Type: ApplicationFiled: May 4, 2009Publication date: November 4, 2010Applicant: International Business Machines CorporationInventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Patent number: 7816528Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: GrantFiled: November 1, 2007Date of Patent: October 19, 2010Assignee: AstraZeneca UK LimitedInventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Publication number: 20100228028Abstract: A process for the manufacture of a compound of formula (V), useful for making rosuvastatin, by a stereoselective aldol reaction is described. Novel intermediates and processes to make them are also described.Type: ApplicationFiled: July 3, 2006Publication date: September 9, 2010Inventors: Michael Butters, David Kenneth Cox, Jeffrey Norman Crabb, Steven Robert Lenger, Paul Michael Murrray, Evan William Snape
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Publication number: 20100204206Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 3, 2009Publication date: August 12, 2010Applicant: SANOFI-AVENTISInventors: Thomas BOHME, Uwe GERLACH, Dirk GRETZKE, Heinz-Werner KLEEMANN, Stefania PFEIFFER-MAREK, Henning VOLLERT, Jean-Michel ALTENBURGER, Sergio MALLART
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Publication number: 20100184758Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: July 15, 2008Publication date: July 22, 2010Inventors: Peter H. Dobbelaar, Wu Du, Liangqin Guo, William K. Hagmann, Shuwen He, Tianying Jian, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Shrenik K. Shah, Quang T. Truong, Zhixiong Ye, James Deliureficio, Raman Bakshi
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Patent number: 7745623Abstract: The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I): wherein R1 represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent chain hydrocarbon group, a represents 0, 1, or 2, X1 represents an optionally substituted lower alkylene or an optionally substituted lower alkenylene, Y1 represents —C(O)—, —S(O)— or —S(O)2—, A represents a piperazine ring which may be further substituted or a piperidine ring which may be further substituted, X2 represents a bond or an optionally substituted lower alkylene, Y2 represents —C(O)—, —S(O)—, —S(O)2— or —C(?NR7)—, X3 represents an optionally substituted C1-4 alkylene or an optionally substituted C2-4 alkenylene, Z3 represents —N(R4)—, —O— or a bond, Z1 represents —C(R2)(R2?)—, —N(R2)—, etc., and Z2 represents —C(R3)(R3?)—, —N(R3)—, etc., or a salt thereof.Type: GrantFiled: May 20, 2005Date of Patent: June 29, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kubo, Yasuhiro Imaeda
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Publication number: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Publication number: 20100130458Abstract: Provided are polymorphs of fluticasone furoate and processes for preparation thereof.Type: ApplicationFiled: August 6, 2009Publication date: May 27, 2010Inventors: Peter Lindsay Macdonald, Pierluigi Rossetto, Adrienne Kovacsne-Mezei, Roman Gabriel, Alexandr Jegorov, Jiri Faustmann
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Patent number: 7723380Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 19, 2007Date of Patent: May 25, 2010Assignee: Gilead Sciences, Inc.Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Patent number: 7709468Abstract: The present invention is directed to novel imidazopyrazine and imidazopyrimidine compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: September 1, 2006Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Kristine E. Frank, Patrick Betschmann, Gavin C. Hirst, Eric C. Brieinlinger, Michael J. Morytko, Richard W. Dixon
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Patent number: 7709637Abstract: 5-Phenylpyrimidines of the formula I, in which the substituents have the following meanings: R1 is a five- to ten-membered saturated, partially unsaturated or aromatic mono- or bicyclic heterocycle comprising one to four hetero atoms selected from the group consisting of O, N or S, which heterocycle can be substituted as defined in the description, R2 is hydrogen, halogen, cyano, alkyl, haloalkyl or alkoxy; R3, R4 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, R3 and R4 together with the nitrogen atom to which they are bonded may also form a five- or six-membered ring which can be interrupted by a hetero atom and have attached to it one or more substituents; R5, R6 are hydrogen, halogen, alkyl, haloalkyl or alkoxy; R7, R8 are hydrogen, halogen, alkyl or haloalkyl; R9 is hydrogen, halogen, alkyl, alkoxy, cycloalkoxy, haloalkoxy or alkoxycarbonyl, Processes and intermediates for the preparation of these compounds, and tType: GrantFiled: October 12, 2006Date of Patent: May 4, 2010Assignee: BASF SEInventors: Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Hubert Sauter, Markus Gewehr, Bernd Müller, Jordi Tormo i Blasco, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7709500Abstract: The invention provides compounds of formula (I): wherein: X is CH2, O, S(O)2 or NR10; Y is a bond, CH2, NR35, CH2NH, CH2NHC(O), CH(OH), CH(NHCOR33), CH(NHSO2R34), CH2O or CH2S; Z is C(O), or when Y is a bond Z can also be S(O)2; R1 is optionally substituted aryl, optionally substituted heterocyclyl or C4-6 cycloalkyl fused to a benzene ring; and R2, R3, R4, R5, R6, R7 and R8, R9, R10, R32, R33, R34 and R35 are as defined herein; are modulators of chemokine (especially CCR3) activity (for use in, for example, treating asthma). The invention also provides a process for making 4-(3,4-dichlorophenoxy)piperidine, which is useful as an intermediate for making certain compounds of the invention.Type: GrantFiled: February 17, 2003Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Mark Purdie, Brian Springthorpe
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Patent number: 7709494Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n, V, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.Type: GrantFiled: November 10, 2008Date of Patent: May 4, 2010Assignee: Sanofi-AventisInventors: Elisabeth Defossa, Jochen Goerlitzer, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Stefan Bartoschek
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Publication number: 20100105659Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: March 19, 2008Publication date: April 29, 2010Applicant: ARRAY BIOPPHARMA INC.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
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Patent number: 7705008Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: GrantFiled: August 14, 2008Date of Patent: April 27, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7700771Abstract: The present invention is to provide a novel heterocyclic compound of the formula [I]: wherein R1 is a halogen, nitro, an alkyl, etc.; R2 is hydrogen, an alkyl, etc.; Ring A is 2-oxo-4-imidazolin-3,4-diyl, etc.; Ring B is a cycloalkyl, monocyclic saturated heterocyclic group; X is CH, N; Y is a single bond, CO, SO2; Z is O, NH, etc.; and Ring C is an aryl, a heterocyclic group, or a pharmaceutically acceptable salt thereof, which is useful as a p38 MAP kinase inhibitor.Type: GrantFiled: April 28, 2005Date of Patent: April 20, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Kubo, Tetsu Nakane, Tatsuo Nakajima, Takanori Murakami, Hidetaka Miyoshi, Akihito Ogasawara
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Publication number: 20100093746Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.Type: ApplicationFiled: December 15, 2009Publication date: April 15, 2010Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY
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Publication number: 20100087434Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.Type: ApplicationFiled: November 13, 2009Publication date: April 8, 2010Inventors: Andrew P. Degnan, Kevin W. Gillman, Derek J. Denhart, Jonathan L. Ditta, Ramkumar Rajamani, Ying Han, George O. Tora
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Patent number: 7687510Abstract: The invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases.Type: GrantFiled: August 28, 2003Date of Patent: March 30, 2010Assignee: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7678796Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: GrantFiled: April 25, 2007Date of Patent: March 16, 2010Assignee: AstraZeneca ABInventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
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Publication number: 20100063282Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: ApplicationFiled: April 7, 2008Publication date: March 11, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Hossein Razavi, Daniel Kuzmich
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Publication number: 20100029589Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: September 14, 2009Publication date: February 4, 2010Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Patent number: 7652018Abstract: Compounds of the following structure are described: wherein R1-R6, R10, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: GrantFiled: August 13, 2007Date of Patent: January 26, 2010Assignee: Wyeth LLCInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Jr., Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Patent number: RE42462Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 7, 1995Date of Patent: June 14, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: RE42477Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: June 21, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack