Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
  • Pyrazolo Piperidine Derivatives as NADPH Oxidase Inhibitors
    Publication number: 20120316380
    Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: GENKYOTEX SA
    Inventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
  • HETEROCYCLIC SULFONAMIDE DERIVATIVES
    Publication number: 20120316149
    Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Inventors: Ramulu PODDUTOORI, Can WANG, Xianglin ZHAO
  • METHODS OF TREATING MESOTHELIOMA WITH A PI3K INHIBITOR COMPOUND
    Publication number: 20120308562
    Abstract: Methods are provided for treating mesothelioma patients with a dual PI3K/mTOR inhibitor, GDC-0980: (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, and having the structure:
    Type: Application
    Filed: June 1, 2012
    Publication date: December 6, 2012
    Inventors: Mika K. Derynck, Jennifer O'Hara Lauchle
  • AKT / PKB INHIBITORS
    Publication number: 20120309739
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Application
    Filed: November 3, 2010
    Publication date: December 6, 2012
    Applicant: ALMAC DISCOVERY LIMITED
    Inventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
  • NOVEL COMPOUNDS
    Publication number: 20120309755
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, Ra, Rb have meanings given in the description.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 6, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
  • BICYCLIC HETEROARYL DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE
    Publication number: 20120302567
    Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.
    Type: Application
    Filed: January 28, 2011
    Publication date: November 29, 2012
    Applicants: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, HANMI PHARM. CO. LTD.
    Inventors: Seung Hyun Jung, Young Hee Jung, Wha Il Choi, Jung Beom Son, Eun Ju Jeon, In Ho Yang, Tae Hun Song, Mi Kyoung Lee, Myoung Sil Ko, Young Gil Ahn, Maeng Sup Kim, Young Jin Ham, Tae Bo Sim, Hwan Geun Choi, Jung Mi Han, Dong-sik Park, Hwan Kim
  • 1,3,4-OXADIAZOLE-2-CARBOXAMIDE COMPOUND
    Publication number: 20120302524
    Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
    Type: Application
    Filed: December 28, 2010
    Publication date: November 29, 2012
    Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTURE
    Inventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
  • Organic compounds
    Patent number: 8318750
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • COMPOUNDS
    Publication number: 20120295883
    Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.
    Type: Application
    Filed: September 21, 2011
    Publication date: November 22, 2012
    Applicants: GENENTECH, INC., MEDICAL RESEARCH COUNCIL TECHNOLOGY
    Inventors: Bryan K. CHAN, Huifen CHEN, Anthony ESTRADA, Daniel SHORE, Zachary SWEENEY, Edward Giles MCIVER
  • COMBINATION OF KINASE INHIBITORS AND USES THEREOF
    Publication number: 20120294930
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
    Type: Application
    Filed: February 23, 2012
    Publication date: November 22, 2012
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • NOVEL PYRIMIDINE COMPOUNDS AS mTOR AND PI3K INHIBITORS
    Publication number: 20120288492
    Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
    Type: Application
    Filed: December 27, 2010
    Publication date: November 15, 2012
    Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
  • FUSED PYRIDINE DERIVATIVES
    Publication number: 20120289497
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Application
    Filed: January 17, 2011
    Publication date: November 15, 2012
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
    Publication number: 20120289496
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: May 4, 2012
    Publication date: November 15, 2012
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20120289493
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: November 15, 2012
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Morpholinopurine derivatives
    Patent number: 8309546
    Abstract: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: November 13, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Kiyoshi Nakayama, Kazuyuki Sugita, Masaki Setoguchi, Yuichi Tominaga, Masanori Saitou, Takashi Odagiri
  • 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    Publication number: 20120283239
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 8, 2012
    Applicant: MSD OSS B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20120283257
    Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Application
    Filed: July 19, 2012
    Publication date: November 8, 2012
    Applicant: F. HOFFMANN-LA ROCHE AG
    Inventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohal
  • UREA DERIVATIVES, METHODS FOR THEIR MANUFACTURE, AND USES THEREFOR
    Publication number: 20120283255
    Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: June 27, 2012
    Publication date: November 8, 2012
    Inventors: Pierre DEPREZ, Hélène Jary, Taoues Temal
  • PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
    Publication number: 20120277209
    Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: June 22, 2012
    Publication date: November 1, 2012
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
  • NOVEL PYRIDOPYRAZINE DERIVATIVES, PROCESS OF MANUFACTURING AND USES THEREOF
    Publication number: 20120277219
    Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
    Type: Application
    Filed: July 5, 2012
    Publication date: November 1, 2012
    Applicant: Aeterna Zentaris GmbH
    Inventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
  • 5 OXO-5,8-DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATIVES AS CAMKII KINASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES
    Publication number: 20120277220
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives, to their preparation and to their therapeutic use.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Applicant: SANOFI
    Inventors: Philippe BEAUVERGER, Guillaume BEGIS, Sandrine BISCARRAT, Olivier DUCLOS, Gary MCCORT
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20120277225
    Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
    Type: Application
    Filed: July 6, 2012
    Publication date: November 1, 2012
    Applicant: Pharmacyclics, Inc.
    Inventors: Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
  • Methods for treating drug resistant cancer
    Patent number: 8299081
    Abstract: A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, wherein the patient is a cancer patient with drug-resistant cancer, wherein the compound of Formula I is as defined in the application.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: October 30, 2012
    Assignee: Novartis AG
    Inventors: Glenn C. Michelson, Vivien W. Chan, Carla C. Heise, Marion Wiesmann, Timothy D. Dawes
  • METHODS FOR TREATING ALZHEIMER'S DISEASE
    Publication number: 20120270844
    Abstract: Provided herein arc PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Alzheimer's disease.
    Type: Application
    Filed: October 8, 2010
    Publication date: October 25, 2012
    Applicant: aFRAXis, Inc.
    Inventors: Jay Lichter, Benedikt Vollrath, David Campbell, Sergio G. Durón
  • 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
    Publication number: 20120270866
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Application
    Filed: October 8, 2010
    Publication date: October 25, 2012
    Applicant: aFRAXis Inc.
    Inventors: Benedikt Vollrath, Daivd Campbell, Sergio G. Durón, Warren Wade
  • Indazole and Pyrazolopyridine Compounds As CCR1 Receptor Antagonists
    Publication number: 20120270870
    Abstract: Diclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1, X and G are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
    Type: Application
    Filed: October 19, 2010
    Publication date: October 25, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Daniel Kuzmich, Can Mao, Hossein Razavi
  • SUBSTITUTED PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES AND THERAPEUTIC USES THEREOF
    Publication number: 20120269831
    Abstract: Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 25, 2012
    Applicant: TEMPLE UNIVERSITY- OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: E. Premkumar Reddy, M.V. Ramana Reddy
  • Purine compounds selective for PI3K P110 delta, and methods of use
    Patent number: 8293736
    Abstract: The invention provides compounds having the general formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and n are defined herein, compositions including the compounds and method of using the compounds to treat a disease or disorder mediated by the p110 delta isoform of PI3 kinase selected from immune disorders, cancer, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: October 23, 2012
    Assignee: F. Hoffmann la Roche AG
    Inventors: Jun Li, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
  • Thienopyrimidine derivatives as P13K inhibitors
    Patent number: 8293735
    Abstract: Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110? isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: October 23, 2012
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Timothy Colin Hancox, Neil Anthony Pegg, Alan John Nadin, Stephen Price
  • Heterocyclic Modulators of Lipid Synthesis
    Publication number: 20120264737
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Application
    Filed: March 8, 2012
    Publication date: October 18, 2012
    Applicant: 3-V BIOSCIENCES, INC.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • PYRROLOPYRAZOLES, POTENT KINASE INHIBITORS
    Publication number: 20120264751
    Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.
    Type: Application
    Filed: October 6, 2011
    Publication date: October 18, 2012
    Inventors: Junhu ZHANG, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
  • CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
    Publication number: 20120264739
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Application
    Filed: December 30, 2010
    Publication date: October 18, 2012
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • N-9 substituted purine compounds, compositions and methods of use
    Patent number: 8288381
    Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: October 16, 2012
    Assignee: Genentech, Inc.
    Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Kevin Hon Luen Lau, Wendy Lee, Kirk D. Robarge
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20120258966
    Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus 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 disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Application
    Filed: March 8, 2012
    Publication date: October 11, 2012
    Applicants: F. HOFFMAN-LA ROCHE AG, PIRAMED LIMITED
    Inventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
  • PYRIDOPYRAZINE DERIVATIVES AND THEIR USE
    Publication number: 20120259151
    Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
    Type: Application
    Filed: April 4, 2012
    Publication date: October 11, 2012
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Matthias GERLACH, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
  • NOVEL ANTIPLATELET AGENT
    Publication number: 20120258951
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: December 17, 2010
    Publication date: October 11, 2012
    Applicant: Mitsubishi Tanage Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • PYRIDOPYRAZINE DERIVATIVES AND THEIR USE
    Publication number: 20120258080
    Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
    Type: Application
    Filed: April 4, 2012
    Publication date: October 11, 2012
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Matthias GERLACH, Irene SEIPELT, Lars BLUMENSTEIN, Gilbert MUELLER, Eckhard GUENTHER, Tilmann SCHUSTER, Michael TEIFEL
  • THIAZOLE DERIVATIVES FOR THE TREATMENT OF DISEASES SUCH AS CANCER
    Publication number: 20120252759
    Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: November 9, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKER HAFTING
    Inventors: Timo Heinrich, Hannes Koolman
  • HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
    Publication number: 20120252779
    Abstract: The invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: October 19, 2010
    Publication date: October 4, 2012
    Inventors: Nigel Ramsden, Richard John Harrison, Sally Oxenford, Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe
  • Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions
    Publication number: 20120252782
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, 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: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • NOVEL PYRIDOPYRAZINES AND THEIR USE AS MODULATORS OF KINASES
    Publication number: 20120252760
    Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: ZENTARIS GmbH
    Inventors: Eckhard Claus, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Michael Czech, Tilmann Schuster
  • Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
    Publication number: 20120252783
    Abstract: 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: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • BENZPYRAZOLE DERIVATIVES AS INHIBITORS OF PI3 KINASES
    Publication number: 20120245171
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: December 3, 2010
    Publication date: September 27, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Paul Spencer Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT
    Publication number: 20120245170
    Abstract: The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent.
    Type: Application
    Filed: October 13, 2010
    Publication date: September 27, 2012
    Applicant: Pierre Fabre Medicament
    Inventors: Karim Bedjeguelal, Rémi Rabot, El Bachir Kaloun, Patrice Mayer, Arnaud Marchand, Nicolas Rahier, Philippe Schambel, Hugues Bienayme
  • Composition, Synthesis, and Use of New Substituted Pyran and Pterin Compounds
    Publication number: 20120245168
    Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.
    Type: Application
    Filed: March 25, 2011
    Publication date: September 27, 2012
    Applicant: DUQUESNE UNIVERSITY OF THE HOLY GHOST
    Inventors: Partha Basu, Igor Pimkov
  • MODULATORS OF TOLL-LIKE RECEPTOR 7
    Publication number: 20120244121
    Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
    Publication number: 20120245169
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: January 13, 2012
    Publication date: September 27, 2012
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES
    Publication number: 20120245138
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: May 2, 2012
    Publication date: September 27, 2012
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use
    Publication number: 20120238568
    Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.
    Type: Application
    Filed: April 28, 2012
    Publication date: September 20, 2012
    Applicants: Institute of Cancer Research: Royal Cancer Hospital (The), CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
  • SELECTIVE ANTIBACTERIALS FOR CLOSTRIDIUM DIFFICILE INFECTIONS
    Publication number: 20120232077
    Abstract: The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again Clostridium difficile-associated diseases.
    Type: Application
    Filed: September 10, 2010
    Publication date: September 13, 2012
    Inventors: George E. Wright, Wei-Chu Xu