Divalent Chalcogen Double Bonded Directly To The Thiazine Ring Patents (Class 544/58.2)
  • CONDENSED PYRROLOPYRIDINE DERIVATIVE
    Publication number: 20120034250
    Abstract: [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: Application
    Filed: April 13, 2010
    Publication date: February 9, 2012
    Applicant: 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
  • NOVEL FUSED RING COMPOUND AND USE THEREOF
    Publication number: 20120035163
    Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: December 28, 2009
    Publication date: February 9, 2012
    Inventors: Tsuneo Yasuma, Nobuyuki Takakura, Yasufumi Miyamoto
  • HALOALKYLSULFONANILIDE DERIVATIVE
    Publication number: 20120029187
    Abstract: Novel herbicides are provided. A haloalkylsulfonanilide derivative represented by the formula (1) or an agrochemically acceptable salt thereof: the formula (1): wherein Z is —C(R9)(R10)— or —N(R11)—, A is an oxygen atom, a sulfur atom or —N(R12)—, W is an oxygen atom or a sulfur atom, m is an integer of from 0 to 3, n is an integer of from 0 to 3, m+n is from 1 to 3, R1 is halo C1-C6 alkyl, R2 is a hydrogen atom, C1-C6 alkyl or the like, each of R3 and R4 is independently a hydrogen atom, C1-C6 alkyl or the like, each of R5, R6, R7, R8, R9 and R10 is independently a hydrogen atom, a halogen, C1-C6 alkyl or the like, each of R11 and R12 is a hydrogen atom, C1-C6 alkyl, halo C1-C6 alkyl or the like, and X is independently a hydrogen atom, a halogen, C1-C6 alkyl, or the like.
    Type: Application
    Filed: April 14, 2010
    Publication date: February 2, 2012
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Masanori Kai, Takamasa Furuhashi, Yoshihide Masuzawa, Tetsuhiko Yano, Fumiyo Saito, Yoshihiko Nakaya
  • 5-ALKYNYL-PYRIMIDINES
    Publication number: 20120028952
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: January 24, 2011
    Publication date: February 2, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
  • 5-ALKYNYL-PYRIMIDINES
    Publication number: 20120028958
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: January 24, 2011
    Publication date: February 2, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
  • Organic compounds
    Patent number: 8097617
    Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: January 17, 2012
    Assignee: Novartis AG
    Inventors: Daniel Kaspar Baeschlin, Nils Ostermann, Francois Gessier, Finton Sirockin, Kenji Namoto
  • NOVEL ANELLATED PYRIDINE COMPOUNDS
    Publication number: 20120010201
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
    Type: Application
    Filed: June 29, 2011
    Publication date: January 12, 2012
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • 1-HYDROXYIMINO-3-PHENYL-PROPANES
    Publication number: 20120010190
    Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: July 12, 2011
    Publication date: January 12, 2012
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
  • COMPOUND, RESIN AND PHOTORESIST COMPOSITION
    Publication number: 20120009519
    Abstract: The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, a halogen atom or a C1-C6 alkyl group which may have one or more halogen atoms, A1 represents a divalent connecting group, X1 represents a C2-C36 heterocyclic group and one or more —CH2— in the C2-C36 heterocyclic group can be replaced by —CO— or —O—, R2 is independently in each occurrence a halogen atom, a hydroxyl group, a C1-C24 hydrocarbon group, a C1-C12 alkoxy group, a C2-C4 acyl group or a C2-C4 acyloxy group, and m represents an integer of 0 to 10.
    Type: Application
    Filed: July 1, 2011
    Publication date: January 12, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Hyungjoo KIM, Akira KAMABUCHI, Yuichi MUKAI
  • Biaryl Heterocyclic Compounds And Methods Of Making And Using The Same
    Publication number: 20120010200
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: September 22, 2011
    Publication date: January 12, 2012
    Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
  • NOVEL TETRAHYDRO-QUINOLINE DERIVATIVES
    Publication number: 20120004218
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.
    Type: Application
    Filed: June 27, 2011
    Publication date: January 5, 2012
    Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Yongfu Liu, Hongying Yun, Mingwei Zhou
  • Compound useful for the treatment of degenerative and inflammatory diseases
    Patent number: 8088764
    Abstract: A novel compound able to inhibit JAK is disclosed, that comprises a compound according to Formula I: or a pharmaceutically acceptable salt thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the 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: Grant
    Filed: June 25, 2010
    Date of Patent: January 3, 2012
    Assignee: Galapagos NV
    Inventors: Christel Jeanne Marie Menet, Koen Kurt Smits
  • PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
  • Heterocyclic Compounds Which Modulate The CB2 Receptor
    Publication number: 20110312944
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: February 16, 2010
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
  • CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
    Publication number: 20110312936
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • ANELLATED PYRIDINE COMPOUNDS
    Publication number: 20110313151
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • PHARMACEUTICAL USE OF SUBSTITUTED AMIDES
    Publication number: 20110312949
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • HETEROARYLOXYCARBOCYCLYL COMPOUNDS AS PDE10 INHIBITORS
    Publication number: 20110306591
    Abstract: Heteroaryloxycarbocyclyl compounds, 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, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 11, 2011
    Publication date: December 15, 2011
    Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
  • DIAMINOPYRIMIDINECARBOXAMIDE DERIVATIVE
    Publication number: 20110294749
    Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
    Type: Application
    Filed: June 28, 2011
    Publication date: December 1, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
  • BICYCLIC PYRAZOLE AND ISOXAZOLE DERIVATIVES AS ANTITUMOR AND ANTINEURODEGENERATIVE AGENTS
    Publication number: 20110294790
    Abstract: Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.
    Type: Application
    Filed: November 19, 2009
    Publication date: December 1, 2011
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
  • Pyrrolo[2,1-F] [1,2,4] Triazin-4-Ylamines IGF-1R Kinase Inhibitors for the Treatment of Cancer and Other Hyperproliferative Diseases
    Publication number: 20110294776
    Abstract: This invention relates to novel compounds of formula (I). Formula (I) in which the variable groups are as defined in the specification and claims, to pharmaceutical compositions containing them, and to a method of treatment using them for treatment of cancer.
    Type: Application
    Filed: November 2, 2006
    Publication date: December 1, 2011
    Applicant: BAYER HEALTHCARE AG
    Inventors: Stephen O'Connor, Jacques Dumas, Wendy Lee, Julie Dixon, David Cantin, David Gunn, Jennifer Burke, Barton Phillips, Derek Lowe, Tatiana Shelekhin, Gan Wang, Xin Ma, Shihong Ying, Andrea McClure, Furahi Achebe, Mario Lobell, Frederick Ehrgott, Christiana Iwuagwu, Kyle Parcella
  • BENZOTRIAZINE INHIBITORS OF KINASES
    Publication number: 20110294796
    Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
    Type: Application
    Filed: December 28, 2010
    Publication date: December 1, 2011
    Applicant: TargeGen, Inc.
    Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
  • NOVEL IMIDAZOPYRIDINES
    Publication number: 20110294779
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Application
    Filed: June 2, 2011
    Publication date: December 1, 2011
    Inventors: DANIELA ALBERATI, RUBÉN ALVAREZ SÁNCHEZ, KONRAD BLEICHER, ALEXANDER FLOHR, KATRIN GROEBKE ZBINDEN, MATTHIAS KOERNER, BERND KUHN, JENS-UWE PETERS, MARKUS RUDOLPH
  • Protein kinase inhibitors
    Patent number: 8067409
    Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 29, 2011
    Assignee: Abbott Laboratories
    Inventors: Nwe Y. Ba-Maung, Randy L. Bell, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Robert D. Hubbard, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
  • Pyrrolopyrazine Kinase Inhibitors
    Publication number: 20110288067
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Application
    Filed: May 18, 2011
    Publication date: November 24, 2011
    Inventors: Robert Than Hendricks, Johannes Hermann, Saul Jaime-Figueroa, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
  • RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
    Publication number: 20110287937
    Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
    Type: Application
    Filed: February 2, 2010
    Publication date: November 24, 2011
    Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.
    Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
  • PYRAZINOPYRAZINES AND DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20110288078
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: November 12, 2009
    Publication date: November 24, 2011
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: Wei-Sheng Huang, R. Mathew Thomas
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20110281851
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • 5-ALKYNYL-PYRIMIDINES
    Publication number: 20110281838
    Abstract: The present invention encompasses compounds of general Formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: July 28, 2009
    Publication date: November 17, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Tobias Wunberg, Ralph Brueckner, Dirk Kessler, Oliver Kraemer, Darryl McConnell, Siegfried Schneider, Lars van der Veen
  • INHIBITORS OF BACE1 AND METHODS FOR TREATING ALZHEIMER'S DISEASE
    Publication number: 20110275619
    Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 10, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • BICYCLIC PYRAZOLO-HETEROCYCLES
    Publication number: 20110275609
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Application
    Filed: January 14, 2010
    Publication date: November 10, 2011
    Applicant: CARA THERAPEUTICS, INC.
    Inventor: Robert Zhiyong Luo
  • NOVEL THIAZOLIDINEDIONE DERIVATIVE AND USE THEREOF
    Publication number: 20110269954
    Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.
    Type: Application
    Filed: December 30, 2009
    Publication date: November 3, 2011
    Inventors: Hoon Cho, Ying Wu, Cheol-Hee Choi
  • Fused Heteroaryl Diamide Compounds Useful as MMP-13 Inhibitors
    Publication number: 20110269668
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Application
    Filed: October 13, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alexander Heim-Riether, Shuang Liang, Sabine Schlyer
  • KINASE INHIBITORS
    Publication number: 20110269739
    Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.
    Type: Application
    Filed: October 29, 2010
    Publication date: November 3, 2011
    Applicants: Oscotec, Inc., Genosco
    Inventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
  • Nitrogen and Sulfur-Containing Heterocycle Derivatives
    Publication number: 20110269953
    Abstract: The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds herein described may also be useful in treating CNS disorders such as but not limited to Schizophrenia, Alzheimer's disease (AD).
    Type: Application
    Filed: March 1, 2011
    Publication date: November 3, 2011
    Inventor: Murty N. Armilli
  • FUSED TRICYCLIC COMPOUNDS AS SERINE-THREONINE PROTEIN KINASE AND PARP MODULATORS
    Publication number: 20110263581
    Abstract: 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 casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.
    Type: Application
    Filed: February 25, 2011
    Publication date: October 27, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
  • HETEROCYCLIC COMPOUND
    Publication number: 20110251187
    Abstract: The present invention relates to a compound represented by wherein each symbol is as defined in the specification, a salt thereof and the like.
    Type: Application
    Filed: May 29, 2009
    Publication date: October 13, 2011
    Inventors: Shizuo Kasai, Masahiro Kamaura, Nobuo Cho
  • Arylethynyl derivatives
    Publication number: 20110251169
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: April 5, 2011
    Publication date: October 13, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Modulators of indoleamine 2,3-dioxygenase and methods of using the same
    Patent number: 8034953
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: May 9, 2006
    Date of Patent: October 11, 2011
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • AMINOPYRIMIDINES AS SYK INHIBITORS
    Publication number: 20110245205
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 6, 2011
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • HETEROCYCLIC COMPOUNDS
    Publication number: 20110245223
    Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.
    Type: Application
    Filed: December 1, 2010
    Publication date: October 6, 2011
    Applicant: Japan Tobacco Inc.
    Inventors: Hiroshi Yamamoto, Yasuhiro Ohe, Hiroyuki Goto, Kazuhito Harada, Shinji Yata, Takashi Ito, Jun Nishiu, Makoto Kakutani, Shunsuke Fujii, Kota Asahina
  • FUSED, SPIROCYCLIC HETEROAROMATIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
    Publication number: 20110245224
    Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Application
    Filed: October 13, 2009
    Publication date: October 6, 2011
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • IMIDAZOPYRIMIDINE DERIVATIVES
    Publication number: 20110237564
    Abstract: The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R1, R2 and R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 29, 2011
    Inventors: Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP)
    Publication number: 20110237575
    Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: November 10, 2009
    Publication date: September 29, 2011
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
  • N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
    Publication number: 20110237573
    Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
    Type: Application
    Filed: March 1, 2010
    Publication date: September 29, 2011
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • AROMATIC COMPOUNDS WITH SULFUR CONTAINING LIGANDS
    Publication number: 20110237776
    Abstract: Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: where R1 is an aromatic backbone and R2 is a sulfur containing ligand.
    Type: Application
    Filed: March 25, 2010
    Publication date: September 29, 2011
    Inventors: BOYD E. HALEY, Niladrl Narayan Gupta
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • PURINE DERIVATIVES USEFUL AS P13 KINASE INHIBITORS
    Publication number: 20110230464
    Abstract: 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: Application
    Filed: October 27, 2008
    Publication date: September 22, 2011
    Inventors: Paul Goldsmith, Timothy Colin Hancox, Nei Anthony Pegg, Janusz Josef Kulagowski, Alan John Nadin, Stephen Price
  • Pyrrolopyrazine Kinase Inhibitors
    Publication number: 20110230462
    Abstract: 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: Application
    Filed: March 4, 2011
    Publication date: September 22, 2011
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • Substituted Isoquinolinones and Quinazolinones
    Publication number: 20110230457
    Abstract: The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: December 20, 2010
    Publication date: September 22, 2011
    Applicant: NOVARTIS AG
    Inventors: Joerg BERGHAUSEN, Nicole BUSCHMANN, Pascal FURET, François GESSIER, Joanna HERGOVICH LISZTWAN, Philipp HOLTZER, Edgar JACOBY, Joerg KALLEN, Keiichi MASUYA, Carole PISSOT SOLDERMANN, Haixia REN, Stefan STUTZ