Three Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/228.5)
-
Publication number: 20110230462Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: March 4, 2011Publication date: September 22, 2011Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
-
Publication number: 20110230464Abstract: This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110? isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.Type: ApplicationFiled: October 27, 2008Publication date: September 22, 2011Inventors: Paul Goldsmith, Timothy Colin Hancox, Nei Anthony Pegg, Janusz Josef Kulagowski, Alan John Nadin, Stephen Price
-
Publication number: 20110224199Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: May 20, 2011Publication date: September 15, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
-
Publication number: 20110218185Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.Type: ApplicationFiled: October 8, 2009Publication date: September 8, 2011Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishnan Sridhar
-
Publication number: 20110218189Abstract: The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKC? mediated disorders.Type: ApplicationFiled: April 8, 2009Publication date: September 8, 2011Applicant: N.V. ORGANONInventors: Andrew Laird Roughton, Koc-kan Ho, Michael Ohlmeyer, David Diller, Irina Neagu, Celia Kingsbury, Jui-Hsiang Chan, Johannes Petrus, Mmaria Lommerse, Neeltje Miranda Teerhuis, Jacobus Comelis Henricus Maria Wijkmans, Ralf Plate
-
Publication number: 20110218184Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: March 9, 2011Publication date: September 8, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Johnny Yasuo NAGASAWA, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
-
Publication number: 20110190281Abstract: This invention relates to novel sulfone 2I3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 13, 2009Publication date: August 4, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Hentemann, William Scott, Jill Wood, Jeffrey Johnson, Aniko Redman, Ann-Marie Bullion, Leatte Guernon
-
Publication number: 20110189130Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: ApplicationFiled: March 22, 2011Publication date: August 4, 2011Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
-
Publication number: 20110190260Abstract: [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.Type: ApplicationFiled: July 24, 2009Publication date: August 4, 2011Inventors: Christel Jeanne Marie Menet, Nolwenn Jouannigot, Javier Blanc, Luc Juliaan Corina Van Rompaey, Stephen Robert Fletcher, Alastair James Hodges, Koen Kurt Smits
-
Patent number: 7981886Abstract: The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(?O)—, —C(?NOR6)—; Z—B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z—B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.Type: GrantFiled: May 24, 2006Date of Patent: July 19, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Daniel Bur, Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20110172216Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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: January 29, 2009Publication date: July 14, 2011Applicants: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
-
Publication number: 20110172217Abstract: The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 2, 2009Publication date: July 14, 2011Applicant: Shionogi & Co., Ltd.Inventors: Masahiko Fujioka, Susumu Mitsumori, Akira Kugimiya, Daisuke Taniyama
-
Publication number: 20110166122Abstract: Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.Type: ApplicationFiled: September 21, 2009Publication date: July 7, 2011Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
-
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
-
Publication number: 20110152254Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: January 24, 2011Publication date: June 23, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
-
Publication number: 20110136780Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.Type: ApplicationFiled: June 8, 2010Publication date: June 9, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Toufike Kanouni, John David Lawson, Michael B. Wallace
-
Publication number: 20110124634Abstract: The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.Type: ApplicationFiled: May 8, 2009Publication date: May 26, 2011Inventors: Connie L. Sun, Xiaoyuan Li
-
Publication number: 20110118230Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 10, 2009Publication date: May 19, 2011Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum Macleod, Karen Williams
-
Publication number: 20110118238Abstract: This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents.Type: ApplicationFiled: August 20, 2008Publication date: May 19, 2011Applicant: ASTRAZENECA ABInventors: David Michael Andrews, Clifford David Jones, Iain Simpson, Richard Andrew Ward
-
Publication number: 20110118246Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 19, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
-
Publication number: 20110118199Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.Type: ApplicationFiled: January 11, 2007Publication date: May 19, 2011Inventor: Matthias Dormeyer
-
Publication number: 20110105427Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.Type: ApplicationFiled: November 2, 2010Publication date: May 5, 2011Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
-
Publication number: 20110097349Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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: December 23, 2010Publication date: April 28, 2011Inventors: Tracy Bayliss, Irina Chuckowree, Adrian Folkes, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzner, Tim Heffron, Simon Mathieu, Alan Olivero, Steven Staben, Daniel P. Sutherlin, Bing-Yan Zhu
-
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
-
Publication number: 20110077235Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula (I); wherein the variables are as defined herein. The invention also relates to 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: March 30, 2009Publication date: March 31, 2011Inventors: Edcon Chang, Tracy Duong, Takehiro Hirano, Matthew H. McNiell, Yoshito Terao, Angie Vassar
-
Publication number: 20110059934Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.Type: ApplicationFiled: July 9, 2010Publication date: March 10, 2011Applicant: IRM LLCInventors: Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
-
Publication number: 20110059943Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: ApplicationFiled: September 2, 2010Publication date: March 10, 2011Inventors: Ashok V. Purandare, James W. Grebinski, Amy Hart, Jennifer Inghrim, Gretchen Schroeder, Honghe Wan
-
Publication number: 20110059118Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: September 9, 2010Publication date: March 10, 2011Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
-
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
-
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
-
Publication number: 20110053912Abstract: A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.Type: ApplicationFiled: March 29, 2010Publication date: March 3, 2011Applicant: Astellas Pharma Inc.Inventors: Yuji Matsushima, Hirokazu Kubota, Hisao Hamaguchi, Yoshinori Okamoto, Takeshi Hondo, Fusako Nishigaki
-
Publication number: 20110053920Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: ApplicationFiled: November 4, 2010Publication date: March 3, 2011Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
-
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
-
Publication number: 20110046109Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: August 19, 2010Publication date: February 24, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
-
Patent number: 7893049Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: February 22, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Bodo Betzemeier, Thomas Gerstberger, Maria Impagnatiello, Steffen Steurer, Lars van der Veen, Ulrike Weyer-Czernilofsky
-
Publication number: 20110039822Abstract: The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention. In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: Astellas Pharma Inc.Inventors: Takayuki INOUE, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
-
Publication number: 20110021425Abstract: The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: June 29, 2010Publication date: January 27, 2011Inventor: Roland Joseph Billedeau
-
Publication number: 20110021511Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: ApplicationFiled: December 21, 2007Publication date: January 27, 2011Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
-
Publication number: 20110009381Abstract: Provided herein are novel sirtuin-modulating compounds Structural Formula (I): and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 7, 2008Publication date: January 13, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Jeremy S. Disch, Bruce Szczepankiewicz, Giovanna Gualtieri, Rebecca L. Casaubon
-
Publication number: 20110003790Abstract: The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Qiang Ding, Yahua Liu, Xu Wu, Qihui Jin, Jianwei Che, S. Frank Yan
-
Publication number: 20100331319Abstract: A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Inventors: Christel Jeanne Marie MENET, Koen Kurt SMITS
-
Patent number: 7851468Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: GrantFiled: May 14, 2007Date of Patent: December 14, 2010Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
-
Publication number: 20100311729Abstract: The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.Type: ApplicationFiled: May 9, 2008Publication date: December 9, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet, Jiong Lan, Sabrina Pecchi, Joseph Schoepfer
-
Publication number: 20100311693Abstract: This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.Type: ApplicationFiled: June 4, 2010Publication date: December 9, 2010Applicant: CEPHALON, INC.Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
-
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
-
Publication number: 20100305114Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: August 9, 2010Publication date: December 2, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
-
Publication number: 20100305113Abstract: The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.Type: ApplicationFiled: May 7, 2008Publication date: December 2, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet
-
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
-
Publication number: 20100280021Abstract: The present invention comprises pyridopyrimidinediamine compounds of the general formula I: The compounds of the present invention are potent inhibitors of PTP1B. Accordingly, the invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.Type: ApplicationFiled: July 16, 2010Publication date: November 4, 2010Inventors: Steven Joseph Berthel, Adrian Wai-Hing Cheung, Kyungjin Kim, Shiming Li, Kshitij Chhabilbhai Thakkar, Weiya Yun
-
Publication number: 20100273786Abstract: Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitors, wherein the substituents of formula (I) are defined as same as the description.Type: ApplicationFiled: November 27, 2008Publication date: October 28, 2010Inventors: Peng Cho Tang, Fanglong Yang, Jiang Fan, Hu Feng, Yang Wang, Tao Yang