The Additional Hetero Ring Is A 1,3 Diazine (including Hydrogenated) Patents (Class 514/217.06)
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Publication number: 20110195956Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: August 31, 2009Publication date: August 11, 2011Inventors: Matthew Burger, Jiong Lan
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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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Publication number: 20110160185Abstract: Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: March 31, 2008Publication date: June 30, 2011Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marc Vendrell Escobar
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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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Patent number: 7968544Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: GrantFiled: June 26, 2008Date of Patent: June 28, 2011Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
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Publication number: 20110151018Abstract: The present invention is directed towards methods of inhibiting thermo- and chemo-sensing in insects and pests by inhibiting TRPA1 ion gated channel or family members. The present invention is also directed towards methods of insect control by modulating the TRPA1 ion gated channel or family members. The methods are applicable to a wide variety of insects and pests including agricultural and horticultural pests.Type: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Applicant: BRANDEIS UNIVERSITYInventors: Paul Garrity, KyeongJin Kang
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Publication number: 20110144095Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: February 23, 2011Publication date: June 16, 2011Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20110130364Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: ApplicationFiled: November 22, 2010Publication date: June 2, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Atsuro NAKAZATO, Taketoshi Okubo, Dai Nozawa, Mikako Yamaguchi, Tomoko Tamita, Ludo E.J. Kennis, Marcel F.L. De Bruyn, Jean-Pierre A.M. Bongartz, Frans M.A. Van Den Keybus, Yves E.M. Van Roosbroeck, Marcel G.M. Luyckx, Robert J.M. Hendrickx
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Patent number: 7935693Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: GrantFiled: December 29, 2007Date of Patent: May 3, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Jing Zhang, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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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: 20110098279Abstract: Use of compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in the description for protecting engineered materials.Type: ApplicationFiled: December 31, 2010Publication date: April 28, 2011Applicant: LANXESS DEUTSCHLAND GMBHInventors: Rainer Bruns, Martin Kugler, Thomas Jaetsch, Hans-Ludwig Elbe, Dietmar Kuhnt, Olaf Gebauer, Heiko Rieck
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Patent number: 7932259Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: GrantFiled: April 21, 2008Date of Patent: April 26, 2011Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Dai Nozawa, Mikako Yamaguchi, Tomoko Tamita, Ludo E. J. Kennis, Marcel F. L. De Bruyn, Jean-Pierre A. M. Bongartz, Frans M. A. Van Den Keybus, Yves E. M. Van Roosbroeck, Marcel G. M. Luyckx, Robert J. M. Hendrickx
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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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: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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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: 7902182Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: November 10, 2006Date of Patent: March 8, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson, Yasutsugu Ueda, John D. Matiskella, Michael A. Walker
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Patent number: 7897593Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: May 29, 2007Date of Patent: March 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Publication number: 20110014271Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.Type: ApplicationFiled: January 13, 2010Publication date: January 20, 2011Applicant: UCB PHARMA S.A.Inventors: Andrew David CARR, Judi Charlotte NEUSS, Michael Glen ORCHARD, David William PORTER
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Patent number: 7872000Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: January 18, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingu Ding, Jiaxin Yu, Joane Litvak
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Publication number: 20100305096Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
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Publication number: 20100298298Abstract: The invention relates to quinazolinedione derivatives, processes for the preparation thereof and their therapeutic applications.Type: ApplicationFiled: April 5, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTISInventors: Annie CLAUSS, Christophe GLAESS, Gilbert MARCINIAK, Nicolas MUZET, Jean-Francois NAVE, André SEYER, Bertrand VIVET
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Publication number: 20100298297Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: ApplicationFiled: March 20, 2007Publication date: November 25, 2010Applicant: BAYER HEALTHCARE AGInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaeten Ladouceur, Qian Zhao, Zheng Liu, Kristen Allegue, Chetan Darne, Jason Newcom
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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: 20100286111Abstract: The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.Type: ApplicationFiled: November 2, 2009Publication date: November 11, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Zhi-Liang Chu, James N. Leonard, Hussien A. Al-Shamma, Robert M. Jones
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Publication number: 20100256118Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: ApplicationFiled: June 3, 2010Publication date: October 7, 2010Applicant: Dainippon Sumitomo Pharma Co.,Ltd.Inventors: Yoshiaki ISOBE, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100239525Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
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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: 20100227853Abstract: Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders.Type: ApplicationFiled: April 17, 2009Publication date: September 9, 2010Applicant: Trustees of Boston CollegeInventors: Charles S. Hoffman, Frank Douglas Ivey, Arlene Wyman Petri
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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: 20100197656Abstract: Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: April 2, 2010Publication date: August 5, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christoph HOENKE, Birgit JUNG, Domnic MARTYRES, Peter NICKOLAUS, Pascale POUZET
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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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Publication number: 20100144705Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: December 5, 2008Publication date: June 10, 2010Applicant: Principia Biopharma Inc.Inventor: Richard MILLER
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100113420Abstract: Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: March 31, 2008Publication date: May 6, 2010Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marc Vendrell Escobar
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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: 20100093702Abstract: This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.Type: ApplicationFiled: June 5, 2009Publication date: April 15, 2010Inventors: J. Kent Barbay, Devraj Chakravarty, Brian Christopher Shook, Aihua Wang
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Publication number: 20100056494Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.Type: ApplicationFiled: January 10, 2008Publication date: March 4, 2010Applicants: IRM LLC, THE SCRIPPS RESEARCH INSTITUTEInventors: Elizabeth Winzeler, Nathanael S. Gray, Dong Han, Dai Cheng
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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: 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: 20100016289Abstract: The present invention provides compounds of general formula I: (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: January 21, 2010Inventors: Kevin Sprott, Prakash Raman, Shomir Ghosh, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20090325933Abstract: The present application relates to new pyrimidinone derivatives. These products have a good affinity for certain sub-types of cannabinoid receptors, especially the CB2 receptors. They are particularly attractive for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a drug.Type: ApplicationFiled: July 13, 2007Publication date: December 31, 2009Applicant: Ipsen Pharma S.A.S.Inventors: Lydie Poitout, Carole Sackur, Eric Ferrandis
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Publication number: 20090318424Abstract: Novel substituted 1,5,7-trisubstituted-3,4-dihydro-pyrimido[4,5-d]pyrimidin-2-(1H)-one compounds and compositions, and their use in therapy as CSBP/RK/p38 kinase inhibitors.Type: ApplicationFiled: June 15, 2007Publication date: December 24, 2009Inventors: Mauro Corsi, Isidore Faiferman, Emilio Merlo-Pich, Emiliangelo Ratti, Paul Bryan Wren
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Publication number: 20090291938Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: November 19, 2008Publication date: November 26, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. Kaldor, Andre A. Kiryanov, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Publication number: 20090264412Abstract: Combination therapy comprising the administration of an 11?-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy.Type: ApplicationFiled: June 25, 2009Publication date: October 22, 2009Applicant: High Point Pharmaceuticals, LLCInventors: Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen
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Patent number: 7605154Abstract: The present invention is directed to novel thiazolopyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.Type: GrantFiled: August 2, 2006Date of Patent: October 20, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Eva Binnun, Peter J. Connolly, Sigmond G. Johnson, Ronghui Lin, Steven A. Middleton, Sandra J. Moreno-Mazza, Niranjan B. Pandey, Steven K. Wetter
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Publication number: 20090238828Abstract: Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.Type: ApplicationFiled: May 7, 2009Publication date: September 24, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerd MUNZERT, Martin STEEGMAIER, Anke BAUM