Pyridine Ring Or Partially Hydrogenated Pyridine Ring Patents (Class 546/193)
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Publication number: 20090099200Abstract: Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: June 8, 2006Publication date: April 16, 2009Inventors: Chun Sing Li, Yeeman K. Ramtohul, Zheng Huang, Nicolas Lachance
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Publication number: 20090099199Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Inventors: Joachim Nozulak, David Orain, Simona Cotesta
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Patent number: 7504420Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: GrantFiled: August 9, 2006Date of Patent: March 17, 2009Assignees: CoMentis, Inc., The Board of Trustees of the University of Illinois, Oklahoma Medical Research Foundation, Purdue Research FoundationInventors: Arun K. Ghosh, Nagaswamy Kumaragurubaran, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, Jordan J. N. Tang, Geoffrey M. Bilcer
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Patent number: 7501418Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1.Type: GrantFiled: August 13, 2003Date of Patent: March 10, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Manuel Bartolomé -Nebreda, Francisco Javier Fernández-Gadea, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Megens
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Patent number: 7501518Abstract: Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.Type: GrantFiled: October 28, 2004Date of Patent: March 10, 2009Assignee: Genzyme CorporationInventors: Gang Chen, Jason Crawford, Renato Skerlj
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Publication number: 20090062261Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: February 21, 2007Publication date: March 5, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Publication number: 20090062342Abstract: The invention relates to novel amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.Type: ApplicationFiled: March 7, 2007Publication date: March 5, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Olivier Bezencon, Daniel Bur, Olivier Corminboeuf, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thomas Weller
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Publication number: 20090054487Abstract: The invention refers to the use of O-(3-piperidino-2-hydroxypropyl)nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof for the preparation of a pharmaceutical composition increasing the mitochondrial genesis.Type: ApplicationFiled: June 13, 2005Publication date: February 26, 2009Inventors: Attila Kolonics, Kalman Tory, Peter Literati Nagy, Zoltan Szilvassy, Lajos Laszlo
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Patent number: 7495014Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: January 29, 2004Date of Patent: February 24, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven M. Ronkin, Dean Stamos, Emanuele Perola, Tiensheng Wang, Arnaud LeTiran, Joseph Drumm
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Publication number: 20090048228Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: December 9, 2005Publication date: February 19, 2009Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
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Patent number: 7491713Abstract: Compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, D, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, pharmaceutical compositions comprising these compounds, use of these compounds and compositions to prevent or treat diseases involving CGRP.Type: GrantFiled: January 25, 2005Date of Patent: February 17, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W Shaw, Craig A. Stump, Theresa M. Williams
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Publication number: 20090042938Abstract: The use of a compound of formula (I), Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring (II) is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are ?C— or —N— provided that both are not N; R1, R2 R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: June 22, 2005Publication date: February 12, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Peter Maienfisch, Louis-Pierre Molleyres, Jerome Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
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Publication number: 20090042852Abstract: The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: January 4, 2006Publication date: February 12, 2009Applicant: ASTRAZENECA ABInventors: Peter Bach, Jonas Bostrom, Kay Brickmann, Leifeng Cheng, Fabrizio Giordanetto, Robert D. Groneberg, Darren Martin Harvey, Michael F. O'Sullivan, Fredrik Zetterberg, Krister Osterlund
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Publication number: 20090036447Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: June 16, 2005Publication date: February 5, 2009Applicant: CYTOKINETICS, INC.Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
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Patent number: 7482341Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: September 29, 2005Date of Patent: January 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Publication number: 20090018166Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: January 11, 2008Publication date: January 15, 2009Applicant: ASTRAZENECA ABInventors: Kosrat Amin, Thomas Antonsson, Christoffer Bengtsson, David Brown, Ruth Bylund, Daniel Hovdal, Fabrizio Giordanetto, Johan Johansson
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Publication number: 20090012063Abstract: The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: ApplicationFiled: June 25, 2008Publication date: January 8, 2009Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20080319018Abstract: The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.Type: ApplicationFiled: June 25, 2008Publication date: December 25, 2008Inventors: Fumiaki Yokokawa, Takeru Ehara, Shimpei Kawakami, Osamu Irie, Masaki Suzuki, Yuku Hitomi, Atsushi Toyao
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Publication number: 20080312255Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: June 11, 2008Publication date: December 18, 2008Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Pamela Hill, Fei Zhou
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Publication number: 20080312208Abstract: The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-thrombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: July 4, 2006Publication date: December 18, 2008Applicant: ASTRAZENECA ABInventors: Soren Andersen, Peter Bach, Kay Brickmann, Fabrizio Giordanetto, Fredrik Zetterberg, Krister Osterlund
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Publication number: 20080306046Abstract: [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: February 16, 2006Publication date: December 11, 2008Applicant: FMC CORPORATIONInventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20080306068Abstract: The present invention provides kinase inhibitors of Formula I:Type: ApplicationFiled: June 15, 2005Publication date: December 11, 2008Applicant: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Patent number: 7462612Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 25, 2005Date of Patent: December 9, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, Gabriel Martinez-Botella, Qing Tang
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Publication number: 20080300232Abstract: Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 21, 2005Publication date: December 4, 2008Applicant: ASTRAZENECA ABInventors: Kay Brickmann, Bryan J. Egner, Fabrizio Giordanetto, Tord Inghardt, Anna Linusson Jonsson, Fritiof Ponten
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Publication number: 20080293768Abstract: The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the process for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thrombosis or cardiac insufficiency.Type: ApplicationFiled: March 24, 2006Publication date: November 27, 2008Inventors: Veronique Barberousse, Michel Bondoux, Didier Thomas, Vincent Peyrou
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Publication number: 20080293767Abstract: This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.Type: ApplicationFiled: January 18, 2005Publication date: November 27, 2008Inventors: Tomoki Kato, Kiyoshi Kawamura, Chikara Uchida
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Patent number: 7452906Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 18, 2008Assignee: SmithKline Beecham P.L.C.Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
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Patent number: 7449583Abstract: A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-3-methyl-pyridine, a new intermediate to obtain loratadine. 2-(4,4-dimethyl-4, 5-dihydrooxazol-2-yl)-3-methyl-pyridine is condensed with 3-chloro-benzyl-chloride and the resultant product is treated with Grignard reagent of 4-chloro-N-methyl-piperidine. [3-(2-(3-chloro-phenyl)-ethyl]-pyridin-2-yl]-1-(methyl-piperidin-4-yl)-methanone is obtained for subsequent hydrolysis. Starting from this last compound it is possible to obtain loratadine with known methods.Type: GrantFiled: October 29, 2002Date of Patent: November 11, 2008Assignee: ZaCh System S.p.A.Inventors: Vincenzo Cannata, Livius Cotarca, Ivan Michieletto, Stefano Poli
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Publication number: 20080269059Abstract: Compounds of the formula (I), or salts thereof, in which R1 to R4 are as defined in formula (I) of claim 1 are suitable as useful-plant-protecting agents for reducing or preventing harmful effects of agrochemicals on the useful plants and their method of preparation are described.Type: ApplicationFiled: April 29, 2008Publication date: October 30, 2008Inventors: Frank Ziemer, Lothar Willms, Christopher Rosinger, Thomas Auler, Erwin Hacker, Udo Bickers
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Patent number: 7442795Abstract: A compound of formula (I), or a pharmaceutically acceptable derivative, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: May 1, 2006Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Justin Stephen Bryans, Patrick Stephen Johnson, Thomas Ryckmans, Alan Stobie
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Publication number: 20080261961Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Patent number: 7432378Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: September 29, 2004Date of Patent: October 7, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Patent number: 7427632Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.Type: GrantFiled: December 22, 2003Date of Patent: September 23, 2008Assignee: Eli Lilly and CompanyInventors: Scott Martin Sheehan, Brian Morgan Watson, John Walter Liebeschuetz
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Patent number: 7427631Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: March 13, 2002Date of Patent: September 23, 2008Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Patent number: 7423050Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.Type: GrantFiled: March 27, 2003Date of Patent: September 9, 2008Assignee: Eli Lilly and CompanyInventors: Michael Philip Cohen, Daniel Timothy Kohlman, Sidney Xi Liang, Vincent Mancuso, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Frantz Victor
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20080194584Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts, hydrates, solvates, geometrical isomers, tautomers, optical isomers, or prodrug forms thereof, wherein X, Y, Z, R1, R2, R3 and R4 are as defined herein are capable of binding to the active site of protein kinase enzymes. In particular, they are inhibitors of a serine/threonine kinase more particularly Rho kinase (ROK, ROCK).Type: ApplicationFiled: November 11, 2005Publication date: August 14, 2008Inventors: Veronique Birault, Jose Antonio Bravo, Roger Crossley
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Patent number: 7408066Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(?O)—, —C(?S)—, —(CH2)q—, —C(?NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.Type: GrantFiled: June 19, 2006Date of Patent: August 5, 2008Assignee: Schering CorproationInventors: Robert G. Aslanian, Michael Y. Berlin, Ying Huang, Kevin D. McCormick, Mwangi W. Mutahi, Neng-Yang Shih, Pauline C. Ting, Wing C. Tom, Junying Zheng
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Publication number: 20080176827Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: January 11, 2008Publication date: July 24, 2008Applicant: ASTRAZENECA ABInventors: Thomas Antonsson, Peter Bach, Kay Brickmann, Ruth Bylund, Fabrizio Giordanetto, Johan Johansson, Fredrik Zetterberg
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Publication number: 20080171739Abstract: The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.Type: ApplicationFiled: December 18, 2007Publication date: July 17, 2008Applicant: SANOFI-AVENTISInventors: Harmut STROBEL, Paulus WOHLFART, Gerhard ZOLLER, David William WILL
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Publication number: 20080171732Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: AstraZeneca ABInventors: Thomas Antonsson, Ruth Bylund, Johan Johansson, Peter Bach, David Brown, Fabrizio Giordanetto
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Publication number: 20080161354Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).Type: ApplicationFiled: March 1, 2007Publication date: July 3, 2008Applicant: LACER, S.A.Inventors: Jose Repolles Moliner, Francisco Pubill Coy, Marisabel Mourelle Mancini, Juan Carlos del Castillo Nieto, Lydia Cabeza Llorente, Juan Martinez Bonin, Ana Modolell Saladrigas
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Patent number: 7388020Abstract: The invention provides compounds of general formula (I) wherein A, X, m, R1, N, R2, Z1, Z2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: March 18, 2002Date of Patent: June 17, 2008Assignee: AstraZeneca ABInventors: Tomas Eriksson, Svetlana Ivanova, Hans Lönn
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Publication number: 20080132536Abstract: The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x) or (z): and wherein R3 is optionally substituted C3-8cycloalkyl, optionally substituted C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R4 is H, C1-3alkyl, C1-2fluoroalkyl, cyclopropyl, —CH2OR4a, —CH(Me)OR4a, or —CH2CH2OR4a; and R5 is inter alia H, C1-8alkyl, C1-3fluoroalkyl, C3-8cycloalkyl, certain substituted alkyl groups, —(CH2)n13-Het, or optionally substituted phenyl or —CH2-Ph; or R4 and R5 taken together are —(CH2)p1— or —(CH2)p3—X5—(CH2)p4—; provided that at least one of R4 and R5 is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.Type: ApplicationFiled: January 30, 2008Publication date: June 5, 2008Inventors: David George Allen, Diane Mary Coe, Caroline Mary Cook, Michael Dennis Dowle, Christopher David Edlin, Julie Nicole Hamblin, Martin Redpath Johnson, Paul Spencer Jones, Mika Kristian Lindvall, Charlotte Jane Mitchell, Alison Judith Redgrave, John Edward Robinson, Naimisha Trivedi
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Publication number: 20080125429Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.Type: ApplicationFiled: November 1, 2005Publication date: May 29, 2008Applicant: BANYU PHARMACEUTICAL CO., LTD.Inventors: Noriaki Hashimoto, Keiji Takahashi, Chisato Nakama, Yoshio Ogino, Fumiko Sakai, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20080125409Abstract: The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.Type: ApplicationFiled: October 19, 2005Publication date: May 29, 2008Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Naoaki Kanaya, Kunihiko Fujii
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Publication number: 20080119518Abstract: The present invention provides a compound represented by the formula (1) or a pharmacologically acceptable salt thereof, or a hydrate thereof (provided that a compound in which all of R4a, R4b, and R4c are hydrogen atoms is excluded.): [wherein R1 represents a hydrogen atom, R2 represents a hydrogen atom, R3 represents the formula: wherein R4a, R4b, and R4c are the same as or different from each other and each represents a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, etc.Type: ApplicationFiled: February 2, 2006Publication date: May 22, 2008Inventors: Yuichi Suzuki, Koichi Ito, Atsushi Sasaki, Koshi Ueno, Daisuke Shinmyo, Miyuki Sakai, Hiroki Ishihara, Atsuhiko Kubota
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Patent number: 7371748Abstract: This invention relates to compounds of formula I wherein R1 and R2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.Type: GrantFiled: May 17, 2004Date of Patent: May 13, 2008Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7361655Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: GrantFiled: July 12, 2004Date of Patent: April 22, 2008Assignee: CytRx CorporationInventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
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Patent number: 7361657Abstract: This invention concerns the use of compounds of formula (I) wherein ?a1=a2?a3=a4—is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries