Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 546/113)
  • Publication number: 20120277207
    Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: November 17, 2010
    Publication date: November 1, 2012
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
  • Patent number: 8299252
    Abstract: It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents —(O)n—R; R represents a C1-C6 alkyl group or the like; n represents 0 or 1; X represents O or the like; R2, R3 and R4 are independently selected from a hydrogen atom or C1-C3 alkyl; or R2 and R3 may join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: October 30, 2012
    Assignees: Chugai Seiyaku Kabushiki Kaisha, The University of Tokyo
    Inventors: Sawako Ozawa, Nobuhiro Oikawa, Eisaku Mizuguchi, Hirosato Ebiike, Fumio Watanabe, Kenji Morikami, Nobuo Shimma, Nobuya Ishii, Toshiyuki Tsukaguchi
  • Publication number: 20120270879
    Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Daniel Kuzmich
  • Patent number: 8293769
    Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
  • Patent number: 8293897
    Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter—and/or intra—cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: October 23, 2012
    Assignees: Sunshine Lake Pharma Co., Ltd.
    Inventor: Ning Xi
  • Patent number: 8288393
    Abstract: The present invention relates to a nitrogen-containing heterocyclic compound or salt thereof, represented by the following formula (I), and a pest control agent containing the compound or salt thereof, as an active ingredient of the pest control agent: (wherein, R0 represents a halogen atom, or the like; Z represents an unsubstituted or substituted aryl group, or the like; Y represents a nitro group, or the like; n represents an integer of 0 to 3; D represents a 5-membered to 8-membered hydrocarbon ring group or heterocyclic group; X represents a functional group represented by the following formula (II)-1 or formula (II)-2: (wherein, in the formula (II)-1, the dotted line represents a single bond or double bond, and R1 and R2 respectively and independently represent a hydrogen atom, nitro group, hydroxyl group, mercapto group, unsubstituted or substituted amino group, or organic group; and, in the formula (II-2), W represents an oxygen atom or sulfur atom; and, R11 represents a hydrogen atom, hydrox
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: October 16, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jyun Iwata, Masahiro Kawaguchi
  • Patent number: 8288376
    Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: October 16, 2012
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
  • Publication number: 20120258969
    Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Inventors: Steven S. Bondy, David A. Oare, Gerhard Puerstinger
  • Publication number: 20120252807
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 4, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
  • Publication number: 20120252780
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 29, 2010
    Publication date: October 4, 2012
    Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
  • Publication number: 20120245347
    Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.
    Type: Application
    Filed: March 23, 2012
    Publication date: September 27, 2012
    Applicant: SOUTHERN METHODIST UNIVERSITY
    Inventors: Edward A. Biehl, Haribabu Ankati, Sukanta Kamila
  • Publication number: 20120245199
    Abstract: The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 27, 2012
    Applicant: SANOFI
    Inventors: Yong Mi CHOI-SLEDESKI, Thaddeus R. NIEDUZAK, Gregory B. POLI, Patrick Wai-Kwok SHUM, Gregory T. STOKLOSA, Zhicheng ZHAO
  • Publication number: 20120245344
    Abstract: A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH?CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.
    Type: Application
    Filed: August 30, 2010
    Publication date: September 27, 2012
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Tsuyoshi Endo, Hiroto Tanaka, Toshihiro Takahashi, Toshihiro Kunigami
  • Publication number: 20120245174
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
  • Publication number: 20120238752
    Abstract: Provided is a colored photosensitive curing composition useful for color filters in primary colors, including blue, green, and red, having a high molar absorption coefficient and allowing a reduction in film thickness and superior color purity and fastness. A colored photosensitive curing composition, comprising, as its colorant, a dipyrromethene-based metal complex compound obtained from a metal or metal compound and a dipyrromethene-based compound represented by the following Formula (I): wherein in Formula (I), R1 to R6 each independently represent a hydrogen atom or a substituent group; and R7 represents a hydrogen or halogen atom, or an alkyl, aryl or heterocyclic group.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 20, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Yuki MIZUKAWA, Ryoji GOTO, Hideki TAKAKUWA, Masashi OGIYAMA, Toru FUJIMORI
  • Publication number: 20120238588
    Abstract: Derivatives of pyrrolo[2,3-b]pyridine which are useful as SGK-1 kinase inhibitors are described herein. The invention described herein also describes pharmaceutical compositions containing derivatives of pyrrolo[2,3-b]pyridine and methods of using pyrrolo[2,3-b]pyridine derivatives and pharmaceutical compositions thereof in the treatment of diseases mediated by SGK-1.
    Type: Application
    Filed: March 27, 2012
    Publication date: September 20, 2012
    Inventors: James S. Frazee, Marlys Hammond, Sharada Manns, Scott Kevin Thompson, David G. Washburn, Kazuya Kano, Hiroko Nakamura
  • Publication number: 20120238559
    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 20, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Patent number: 8268857
    Abstract: This invention provides compounds that are useful for treating patients having a TGF-?-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH?CH, CH?N, or N?CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: September 18, 2012
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Anjali Pandey, Meenakshi S. Venkatraman
  • Patent number: 8268814
    Abstract: Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds for treating and/or inhibiting pain or other conditions at least partly mediated by the bradykinin 1 receptor.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: September 18, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Ellen Klegraf, Stefan Oberboersch, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Engels
  • Patent number: 8268859
    Abstract: Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 18, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Harcken, Rajashekhar Betageri, Todd Bosanac, Michael Jason Burke, Soojin Kim, Daniel Kuzmich, Thomas Wai-ho Lee, Zhibin Li, Pingrong Liu, John Lord, Hossein Razavi, Jonathan Timothy Reeves, David Thomson
  • Patent number: 8268858
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: September 18, 2012
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Wayne Spevak, Songyuan Shi, Hanna Cho, Prabha N. Ibrahim, Chao Zhang, Shenghua Shi, Yong Zhou, Dean Artis, Jiazhong Zhang
  • Patent number: 8263612
    Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: September 11, 2012
    Assignees: Gilead Sciences, Inc., K.U. Leuven Research & Development
    Inventors: Steven S. Bondy, David A. Oare, Gerhard Puerstinger
  • Publication number: 20120225874
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.
    Type: Application
    Filed: May 17, 2012
    Publication date: September 6, 2012
    Applicant: NOVARTIS AG
    Inventors: Masashi KISHIDA, Naoko MATSUURA, Hidetomo IMASE, Yuki IWAKI, Ichiro UMEMURA, Osamu OHMORI, Eiji KAWAHARA
  • Patent number: 8258152
    Abstract: The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: September 4, 2012
    Assignee: Genentech, Inc.
    Inventors: Hazel Joan Dyke, Stephen Price, Karen Williams
  • Publication number: 20120220622
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Application
    Filed: November 2, 2010
    Publication date: August 30, 2012
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Publication number: 20120220561
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: August 12, 2011
    Publication date: August 30, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
  • Publication number: 20120220587
    Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 6, 2010
    Publication date: August 30, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
  • Publication number: 20120220570
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 30, 2012
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Sasaki, Yuta Tanaka
  • Publication number: 20120220569
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 30, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tomohiro Ohashi, Zenyu Shiokawa, Yuta Tanaka, Satoshi Sasaki
  • Patent number: 8252930
    Abstract: Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: August 28, 2012
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20120214815
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 23, 2012
    Applicant: UCB Pharma, S.A.
    Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
  • Publication number: 20120214783
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: May 3, 2012
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pierre L. BEAULIEU, Pasquale FORGIONE, Alexandre GAGNON, Cedrickx GODBOUT, Marc-Andre JOLY, Montse LLINAS-BRUNET, Julie NAUD, Martin POIRIER, Jean RANCOURT
  • Publication number: 20120214790
    Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.
    Type: Application
    Filed: March 11, 2011
    Publication date: August 23, 2012
    Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
  • Patent number: 8247556
    Abstract: The invention encompasses a method for preparing 6-susbtituted-7-aza-indoles.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: August 21, 2012
    Assignee: Amgen Inc.
    Inventor: Thomas Storz
  • Publication number: 20120208811
    Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.
    Type: Application
    Filed: August 5, 2010
    Publication date: August 16, 2012
    Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
  • Publication number: 20120208837
    Abstract: This invention relates to novel substituted azaindoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing selective inhibitory activity of oncogenic B-RafV600E protein kinase.
    Type: Application
    Filed: September 13, 2011
    Publication date: August 16, 2012
    Inventor: Roger Tung
  • Publication number: 20120208827
    Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.
    Type: Application
    Filed: October 27, 2010
    Publication date: August 16, 2012
    Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
  • Publication number: 20120208794
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 16, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Satoshi Sasaki, Yuta Tanaka
  • Publication number: 20120208819
    Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.
    Type: Application
    Filed: October 5, 2010
    Publication date: August 16, 2012
    Inventors: Joseph Arndt, Timothy Chan, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Daniel Scott, Lihong Sun, Jermaine Thomas, Kurt van Vloten, Deping Wang, Lei Zhang, Daniel Erlanson
  • Patent number: 8242124
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: August 14, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, Nicholas A. Meanwell, David J. Carini, Wenying Li
  • Publication number: 20120202784
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: January 13, 2012
    Publication date: August 9, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
  • Publication number: 20120202783
    Abstract: Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: October 21, 2010
    Publication date: August 9, 2012
    Inventors: Bryan James Branstetter, Michael A. Letavic, Kiev S. Ly, Dale A. Rudolph, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman
  • Publication number: 20120202690
    Abstract: The present invention relates to substituted heterobicyclic carboxylic acid derivatives, as well as N-oxides and agriculturally acceptable salts thereof, and their use in controlling plant growth, particularly undesirable plant growth, in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredients and/or a safener.
    Type: Application
    Filed: October 8, 2010
    Publication date: August 9, 2012
    Applicant: SYNGENTA LIMITED
    Inventors: William Guy Whittingham, Caroline Louise Winn, Julie Evelyne Blanc, Shuji Hachisu, Matthew Brian Hotson, Harry Glithro
  • Patent number: 8236817
    Abstract: Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy -4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater ability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprises the steps of: a) suspending 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating the product which is separated, (form A) and, additionally, e), reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.5% and 0.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: August 7, 2012
    Assignee: Chemi S.p.A.
    Inventors: Stefano Turchetta, Pietro Massardo, Valentina Aromatario
  • Publication number: 20120196866
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • Publication number: 20120196856
    Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 26, 2010
    Publication date: August 2, 2012
    Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
  • Publication number: 20120190707
    Abstract: The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to prevent and treat cancer and other conditions.
    Type: Application
    Filed: January 24, 2012
    Publication date: July 26, 2012
    Inventors: Ze'ev Ronai, Maurizio Pellecchia, Gary Chiang
  • Publication number: 20120190700
    Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.
    Type: Application
    Filed: January 17, 2012
    Publication date: July 26, 2012
    Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120184530
    Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
    Type: Application
    Filed: March 27, 2012
    Publication date: July 19, 2012
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventor: Stephen M. CONDON