The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/601)
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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: 7968537Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C6 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: GrantFiled: April 17, 2009Date of Patent: June 28, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Akio Manabe
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Publication number: 20110098280Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 4, 2011Publication date: April 28, 2011Applicants: Novartis AG, IRM LLCInventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura, Ruo Steensma, Greg Chopiuk, Jiqing Jiang, Yongqin Wan, Qiang Ding, Qiong Zhang, Nathanael Schiander Gray, Donald Karanewsky
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Publication number: 20110065681Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: February 27, 2009Publication date: March 17, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Patent number: 7902184Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein formula I is: wherein X, Y, Z, R1 and R2 are as defined in the description and claims. The compounds of the present invention act as antagonists and/or inverse agonists at the histamine 3 receptor and are useful for the treatment and/or prevention of diseases such as obesity, metabolic syndrome (syndrome X), and other eating disorders.Type: GrantFiled: May 21, 2007Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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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: 20110009620Abstract: 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: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Publication number: 20100292205Abstract: The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders.Type: ApplicationFiled: August 13, 2007Publication date: November 18, 2010Applicant: PFIZER INC.Inventors: Bruce A. Lefker, Michael A. Brodney, Subas M. Sakya, Bruce A. Hay, Matthew D. Wessel, Edward L. Conn
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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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Publication number: 20100234354Abstract: Compounds of the formula (I), in which R1, R2, R, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: April 29, 2008Publication date: September 16, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
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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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Publication number: 20100204208Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 21, 2010Publication date: August 12, 2010Inventors: Rajinder Singh, Hui Li, Haoran Zhao, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu, Carlos Valdez, Jing Zhang, Emily Stauffer, Matthew Duncton, Salvador Alvarez
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Publication number: 20100184746Abstract: An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.Type: ApplicationFiled: May 30, 2008Publication date: July 22, 2010Inventors: Eijirou Umemura, Kou Kumura, Satomi Masaki, Kazutaka Ueda, Yoshinari Wakiyama, Yasuo Sato, Mikio Yamamoto, Keiichi Ajito, Takashi Watanabe, Chizuko Kaji
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Publication number: 20100152167Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: ApplicationFiled: February 24, 2010Publication date: June 17, 2010Applicants: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Georg DAHMANN, Frank HIMMELSBACH, Bernd KRIST, Martin LENTER, Alexander PAUTSCH, Gisela SCHNAPP, Martin STEEGMAIER, Helmut WITTNEBEN, Anthony S. PROKOPOWICZ, Walter SPEVAK, Andreas SCHOOP, Steffen STEURER
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Publication number: 20100144706Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, X and n are defined as in claim 1, which are suitable for the treatment of ailments characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: December 20, 2007Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl Zahn, Guido Boehmelt, Ulrich Guertler, Andreas Mantoulidis, Andreas Schoop, Flavio Solca, Ulrike Tontsch-Grunt, Matthias Treu
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Patent number: 7704996Abstract: The present invention relates to the use of a 2-cyanopyrimidine compound of the formula wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.Type: GrantFiled: August 16, 2005Date of Patent: April 27, 2010Assignee: Novartis AGInventors: Terance William Hart, Allan Hallett, Fumiaki Yokokawa, Hajime Hirao, Takeru Ehara, Atsuko Iwasaki, Junichi Sakaki, Keiichi Masuya, Masashi Kishida, Osamu Irie
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Publication number: 20100048539Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR? and PDGFR? kinases. Formula (I).Type: ApplicationFiled: November 2, 2007Publication date: February 25, 2010Applicants: IRM LLC, NOVARTIS AGInventors: Donatella Chianelli, Xiaolin Li, Xiaodong Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Laszlo Revesz, Lawrence B. Perez, Clinton Brooks, Wojciech Wrona, Paul William Manley, Werner Breitenstein
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Publication number: 20100036117Abstract: The present invention relates to a pyrimidine compound of the formula (II?): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X3 represents C5 polymethylene, in which a single CH2—CH2 may be replaced with a single CH?CH, substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls.Type: ApplicationFiled: October 15, 2009Publication date: February 11, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hajime MIZUNO, Akio Manabe
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Publication number: 20100022516Abstract: 4,5-disubstituted-2-arypyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: January 26, 2009Publication date: January 28, 2010Inventors: George D. MAYNARD, Manuka GHOSH, Jun YUAN, Kevin S. CURRIE, Scott MITCHELL, Qin GUO, He ZHAO
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Publication number: 20090318407Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: April 16, 2009Publication date: December 24, 2009Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Qing Xu, Mukund Mehrota, Jack W. Rose, Wolin Huang, Chandrasekar Venkataramani, Anjali Pandey
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Publication number: 20090275750Abstract: Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.Type: ApplicationFiled: September 15, 2006Publication date: November 5, 2009Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Paul R. Brodluahrer, Bruce Elder, Paul Isbester, Richard S. Fornicola, Philip B. Kisanga, Bingidimi I. Mobele, Grant J. Palmer, Maxwell M. Reeve, Jonathon S. Salsbury, Luckner Ulysse, Sripathy Venkatraman
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Publication number: 20090264649Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.Type: ApplicationFiled: May 29, 2009Publication date: October 22, 2009Applicants: IRM LLC, Novartis AGInventors: Valentina Molteni, Xiaolin Li, Donatella Chianelli, Jon Loren, Juliet Nabakka, Xiaodong Liu, Shifeng Pan, Yi Liu, Donald S. Karanewsky, Pascal Furet, Vito Guagnano, Shuli You
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Publication number: 20090233908Abstract: A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.Type: ApplicationFiled: February 24, 2006Publication date: September 17, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiroshi Ochiai, Akira Ohhata, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20090221555Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: October 23, 2007Publication date: September 3, 2009Applicants: Cephalon, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Gulzar Ahmed, Adolph Bohnstedt, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Koc-Kan Ho, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jonathan Parrish, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Jason C. Wagner, Linda Weinberg, Gregory J. Wells, Ming You, Craig A. Zificsak
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Publication number: 20090209519Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C7 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: ApplicationFiled: April 17, 2009Publication date: August 20, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hajime MIZUNO, Akio Manabe
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Publication number: 20090209518Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C6 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: ApplicationFiled: April 17, 2009Publication date: August 20, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hajime MIZUNO, Akio MANABE
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Publication number: 20090203674Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C4 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: ApplicationFiled: April 17, 2009Publication date: August 13, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hajime MIZUNO, Akio Manabe
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Publication number: 20090203903Abstract: 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: ApplicationFiled: October 6, 2005Publication date: August 13, 2009Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph 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: 20090203673Abstract: The present invention encompasses compounds of general Formula (I) wherein X and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: July 5, 2007Publication date: August 13, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Patent number: 7563784Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: April 25, 2006Date of Patent: July 21, 2009Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20090176763Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 19, 2008Publication date: July 9, 2009Inventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Patent number: 7544675Abstract: The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: March 29, 2003Date of Patent: June 9, 2009Assignee: UCB, S.A.Inventors: Laurent Provins, Berend Jan Van Keulen, John Surtees, Patrice Talaga, Bernard Christophe
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Patent number: 7501407Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: November 18, 2004Date of Patent: March 10, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
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Publication number: 20090054392Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.Type: ApplicationFiled: August 19, 2008Publication date: February 26, 2009Applicant: WyethInventors: Jeffrey Claude Pelletier, Luciana de Araujo Felix, Daniel Michael Green, Diane Barbara Hauze, Joseph Theodore Lundquist, IV, Charles William Mann, John Francis Mehlmann, John Francis Rogers, JR., Matthew Douglas Vera, Albert John Molinari
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Patent number: 7405209Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 14, 2005Date of Patent: July 29, 2008Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Robert Wells Marquis, Jr., Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Publication number: 20080176831Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N— or —S—; R1 may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: ApplicationFiled: May 17, 2005Publication date: July 24, 2008Applicant: BASF AktiengesellschaftInventors: Anja Schwogler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Muller, Thomas Grote, Wassilios Grammenos, Udo Hunger, Carsten Blettner, Peter Schafer, Oliver Wagner, Reinhard Stierl, Ulrich Schofl, Siegfried Strathmann, Maria Scherer
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Publication number: 20080177064Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: ApplicationFiled: October 30, 2007Publication date: July 24, 2008Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 7390815Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2?, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2? are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.Type: GrantFiled: October 23, 2003Date of Patent: June 24, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, David Bebbington, Ronald Knegtel, Marion Wannamaker, Pan Li, Cornelia Forster, Albert Pierce
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Patent number: 7351700Abstract: The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.Type: GrantFiled: February 23, 2005Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Pari Malherbe, Raffaello Masciadri, Eric Prinssen, Will Spooren, Andrew William Thomas
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Publication number: 20070281921Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein formula I is: wherein X, Y, Z, R1 and R2 are as defined in the description and claims. The compounds of the present invention act as antagonists and/or inverse agonists at the histamine 3 receptor and are useful for the treatment and/or prevention of diseases such as obesity, metabolic syndrome (syndrome X), and other eating disorders.Type: ApplicationFiled: May 21, 2007Publication date: December 6, 2007Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Patent number: 7223750Abstract: Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl, (C1–C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1–C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. Therapeutic application.Type: GrantFiled: January 3, 2003Date of Patent: May 29, 2007Assignee: Sanofi-AventisInventors: Frédéric Galli, Odile LeClerc, Alistair Lochead, Alain Nedelec
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Patent number: 7186827Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:Type: GrantFiled: October 27, 2004Date of Patent: March 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Carl Alan Busacca, Nizar Haddad, Suresh R. Kapadia, Lana Smith Keenan, Jon Charles Lorenz, Chris Hugh Senanayake, Xudong Wei
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Patent number: 7166597Abstract: Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, R2, and R4 are various substituent groups, are protein kinase inhibitorsType: GrantFiled: August 22, 2001Date of Patent: January 23, 2007Assignee: Glaxo Group LimitedInventors: Michael John Alberti, Ian Robert Baldwin, Mui Cheung, Stuart Cockerill, Stephen Flack, Philip Anthony Harris, David Kendall Jung, Gregory Peckham, Michael Robert Peel, Jennifer Gabriel Badiang, Kirk Stevens, James Marvin Veal
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Patent number: 7115597Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: October 2, 2003Date of Patent: October 3, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, George D. Hartman, Jacob M. Hoffman, Jr., John T. Sisko, Peter J. Manley, Anthony M. Smith, Thomas J. Tucker, William C. Lumma, Jr., Leonard Rodman
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 6921821Abstract: This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.Type: GrantFiled: June 11, 2003Date of Patent: July 26, 2005Assignee: Abbott LaboratoriesInventors: Christopher Blackburn, Su-Jen Lai, Jennifer L. Che, Martin P. Maguire, Michael A. Patane, Matthew J. LaMarche, Courtney A. Cullis, James Brown, Anil Vasudevan, Jennifer C. Freeman, Mathew M. Mulhern, John K. Lynch, Ju Gao, Dariusz Wodka, Andrew J. Souers, Rajesh Iyengar, Mary Katherin Verzal, Philip R. Kym
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Patent number: 6916804Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20040220172Abstract: Novel uracil substituted phenyl sulfanoyl carboxamides I 1Type: ApplicationFiled: October 15, 2003Publication date: November 4, 2004Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi