The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Tricyclo Ring System Patents (Class 544/126)
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Publication number: 20120220565Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: August 26, 2011Publication date: August 30, 2012Applicant: Corcept Therapeutics, Inc.Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
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Publication number: 20120208809Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers anType: ApplicationFiled: November 30, 2009Publication date: August 16, 2012Applicant: SANOFIInventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
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Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
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Publication number: 20120196854Abstract: A pharmaceutical composition comprising as an active ingredient, an aromatic heterocyclic compound represented by the formula (I): [wherein Q1 represents CR2 (wherein R2 represents a hydrogen atom or the like) or the like; Q2 represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like; Q3 represents a nitrogen atom or the like; R1 represents —C(?O)OR16 (wherein R16 represents a hydrogen atom or the like) or the like; R5 represents a hydrogen atom or the like; R6 represents optionally substituted cycloalkyl or the like; X and Y may be the same or different and each represent CH in which H may be substituted with a substituent or the like; and Z represents a nitrogen atom or the like] or the like is provided.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Chie Takada, Koji Saeki, Hirokazu Kawasaki, Miho Tagaya, Masato Komai, Toshihide Ikemura, Shinpei Yamaguchi, Kyoichiro Iida
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Publication number: 20120149703Abstract: A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].Type: ApplicationFiled: February 15, 2012Publication date: June 14, 2012Inventors: Makoto Jitsuoka, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20120121651Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
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Publication number: 20120071463Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: November 29, 2011Publication date: March 22, 2012Inventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Publication number: 20120040959Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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Publication number: 20120034250Abstract: [Problem] The present invention provides a condensed pyrrolopyridine derivative which is useful as an active ingredient for a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied a compound having a JAK inhibitory action, and as a result, they have found that a condensed pyrrolopyridine derivative which is the compound of the present invention has an excellent JAK inhibitory action, and is therefore useful as an agent for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction, thereby completing the present invention.Type: ApplicationFiled: April 13, 2010Publication date: February 9, 2012Applicant: Astellas Pharma Inc.Inventors: Shohei Shirakami, Yutaka Nakajima, Jun Maeda, Hiroaki Tominaga, Hiroaki Yamagishi, Takeshi Hondo, Masamichi Inami, Hiroki Morio, Takayuki Inoue, Tsuyoshi Mizutani, Hiroki Ishioka
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Publication number: 20120022060Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.Type: ApplicationFiled: December 3, 2009Publication date: January 26, 2012Applicant: MERCK PATENT GMBHInventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, JR., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
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Publication number: 20120022046Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: February 24, 2010Publication date: January 26, 2012Inventors: Chelsea M. Byrd, Dongcheng Dai, Robert Jordan, Dennis E. Hruby
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Patent number: 8101603Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: July 9, 2007Date of Patent: January 24, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
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Patent number: 8093389Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-CType: GrantFiled: January 8, 2008Date of Patent: January 10, 2012Assignees: Merck Sharp & Dohme Corp., MSD K.K.Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
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Patent number: 8088790Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: November 3, 2006Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Patent number: 8071587Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: May 25, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Publication number: 20110294799Abstract: The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: August 12, 2008Publication date: December 1, 2011Inventors: Samuel Hintermann, Konstanze Hurth, Joachim Nozulak, Marina Tintelnot-Blomley
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Publication number: 20110294800Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Applicant: The Trustees Of Columbia University in the City of New YorkInventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
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Publication number: 20110288091Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicants: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Jae Won Chang, Jianming Zhang, Carson C. Thoreen, Seong Woo Anthony Kang, David M. Sabatini, Qingsong Liu
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Publication number: 20110280808Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 18, 2011Publication date: November 17, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Publication number: 20110281862Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).Type: ApplicationFiled: August 27, 2009Publication date: November 17, 2011Applicants: Universita' Degli Studi di Milano - Bicocca, Universite' Claude Bernard de Lyon 1, Universite' de GeneveInventors: Carlo Gambacorti Passerini, Luca Mologni, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Benoit Joseph, Cedric Schneider, Pierre Garcia
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Publication number: 20110269705Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
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Publication number: 20110257169Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: May 19, 2011Publication date: October 20, 2011Applicant: NYCOMED GmbHInventor: Ulrich KAUTZ
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Publication number: 20110230471Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, D, Z, X, Y, m and p have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: November 5, 2009Publication date: September 22, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Wolfgang Staehle, Ingo Kober, Kai Schiemann, Melanie Schultz, Dirk Wienke
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Publication number: 20110223132Abstract: The invention provides compounds and salts of Formula I and Formula which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: March 14, 2011Publication date: September 15, 2011Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Barton James Bradbury, Milind Deshpande, Michael John Pucci, Qiuping Wang, Jason Allan Wiles, Monishing Song, Akihiro Hashimoto, Edlaine Lucien
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Patent number: 8017601Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 30, 2006Date of Patent: September 13, 2011Assignee: Amgen Inc.Inventors: Tae-Seong Kim, Jean-Christophe Harmange, Steven Bellon, Shon Booker, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Timothy S. Harvey, Joseph L. Kim, Matthew Lee, Longbin Liu, Vinod F. Patel, Andrew Tasker
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Publication number: 20110218193Abstract: The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.Type: ApplicationFiled: November 11, 2009Publication date: September 8, 2011Applicant: JE IL PHARMACEUTICAL CO., LTD.Inventors: Myung-Hwa Kim, Seung-Hyun Kim, Sae-Kwang Ku, Chun-Ho Park, Bo-Young Joe, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi, Dong-Kyu Ryu, Ji-Seon Park, Han-Chang Lee, Ji-So Choi, Young-Chul Kim
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Publication number: 20110212053Abstract: Provided are compounds according to Formula (I): or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.Type: ApplicationFiled: June 19, 2009Publication date: September 1, 2011Inventors: Dapeng QIAN, Amy Qi Han, Mark Hamilton, Eric Wang
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Publication number: 20110201593Abstract: The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.Type: ApplicationFiled: January 11, 2011Publication date: August 18, 2011Applicant: Genentech, Inc.Inventors: Srinivasan Babu, Phillippe Bergeron, Peter Dragovich, Hazel Joan Dyke, Paul Gibbons, Stefan Gradl, Emily Hanan, Christopher Hurley, Tony Johnson, Michael Koehler, Janusz Kulagowski, Sharada Labadie, Joseph Lyssikatos, Rohan Mendonca, Rebecca Pulk, Stuart Ward, Bohdan Waszkowycz, Mark Zak
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Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Publication number: 20110183938Abstract: 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: December 14, 2010Publication date: July 28, 2011Applicant: Genentech, Inc.Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams
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Publication number: 20110178053Abstract: The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF3; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C2-C7 alkenyl; optionally substituted linear or branched C2-C6 alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.Type: ApplicationFiled: June 11, 2009Publication date: July 21, 2011Applicant: SANOFI-AVENTISInventors: Christopher Arendt, Didier Babin, Olivier Bedel, Thierry Gouyon, Mikhail Levit, Ronghua Li, Serge Mignani, Neil Moorcroft, David Papin
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Publication number: 20110166346Abstract: The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of general formula 5 and 9, n-1-2, R=n-methylpiperazine or morpholine (Formula 9), wherein: n=2-3, m=2-3 and R=n-methylpiperazine or morpholine.Type: ApplicationFiled: March 3, 2009Publication date: July 7, 2011Inventors: Kamal Ahmed, Praveen Kumar Pogula
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Publication number: 20110160201Abstract: Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for preparing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.Type: ApplicationFiled: July 17, 2009Publication date: June 30, 2011Applicant: AZIENDE CHIMI. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Roberta Costi, Roberto Di Santo, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
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Publication number: 20110160183Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: March 11, 2011Publication date: June 30, 2011Applicant: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Publication number: 20110160198Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.Type: ApplicationFiled: June 29, 2010Publication date: June 30, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M.M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James Quada, Jennifer L.R. Freeman, Kalpathy Santhosh, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Stephen Thomas Davis, Thomas Scott Yokum
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Publication number: 20110144099Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: January 18, 2011Publication date: June 16, 2011Inventors: Kyle J. LINDSTROM, Hugues M. H. MARTIN, Bryon A. MERRILL, Michael J. RICE, Joshua R. WURST, Chad A. HARALDSON, Philip D. HEPPNER, Shri NIWAS, Matthew R. RADMER
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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
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Publication number: 20110136800Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
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Publication number: 20110136801Abstract: The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 2, 2010Publication date: June 9, 2011Applicants: Dainippon Sumitomo Pharma Co. Ltd., AstraZeneca ABInventors: Yoshiaki Isobe, Mai Kasai, Tomoaki Nakamura, Shingo Tojo, Hirotaka Kurebayashi
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Patent number: 7951821Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.Type: GrantFiled: March 1, 2007Date of Patent: May 31, 2011Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Benoit Marabout, Pierre Roger, Mireille Sevrin
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Patent number: 7947839Abstract: Bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) are described. Pharmaceutical compositions comprising an effective amount of a 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders are described. Methods are described for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a 1,8 bis-naphthalimide compound.Type: GrantFiled: January 30, 2006Date of Patent: May 24, 2011Assignee: Genentech, Inc.Inventors: Lewis J. Gazzard, Edward HyungSuk Ha, David Y. Jackson, Joann M. Um
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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
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Patent number: 7943610Abstract: Pyrazolopyridine-1,4-diamines and analogs thereof, e.g., pyrazolo[3,4-c]pyridine-1,4-diamines, pyrazolo[3,4-c]quinoline-1,4-diamines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinoline-1,4-diamines, and pyrazolo[3,4-c]naphthyridine-1,4-di-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: March 31, 2006Date of Patent: May 17, 2011Assignee: 3M Innovative Properties CompanyInventors: David S. Hays, Shri Niwas, Gregory D. Lundquist, Jr.
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Patent number: 7931975Abstract: An OLED device includes a cathode, an anode, and having there between a light-emitting layer, further including, between the cathode and the light emitting layer, a first layer having a thickness of 20 nm or less and containing a fluoranthene compound including one and only one fluoranthene nucleus and having no aromatic rings annulated to the fluoranthene nucleus, the fluoranthene nucleus having independently selected aromatic groups in the 7,10-positions and a phenanthroline group in the 8-or 9-position. The OLED device desirably includes a second layer containing an alkali metal or an alkali metal compound, located between the cathode and the first layer. The OLED device can also include a polycyclic aromatic compound in the first layer or in a third layer located between the first layer and the light-emitting layer. Devices of the invention provide improvement in features such as efficiency, drive voltage, and operational stability.Type: GrantFiled: November 7, 2008Date of Patent: April 26, 2011Assignee: Global OLED Technology LLCInventors: William J. Begley, Natasha Andrievsky
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Publication number: 20110092477Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Inventors: Doris Stoermer, Joseph F. Dellaria, JR., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
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Publication number: 20110081365Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is —CR4?CR5.Type: ApplicationFiled: February 27, 2009Publication date: April 7, 2011Applicants: IRM LLC, Novartis 35Inventors: Alex Cortez, Yongkai Li, Pranab Mishra, Manmohan Singh, David Skibinski, Nicholas Valiante, Tom Yao-Hsiang Wu, Xiaoyue Zhang, Yefen Zou
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Publication number: 20110065698Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate protein kinase CK2 activity, Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: August 26, 2010Publication date: March 17, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Fabrice PIERRE, Mustapha HADDACH, Collin F. REGAN, David M. RYCKMAN
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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