Thiophene Ring (including Hydrogenated) Patents (Class 544/146)
  • Patent number: 10308667
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
    Type: Grant
    Filed: May 9, 2018
    Date of Patent: June 4, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Cédrickx Godbout, Thomas Trieselmann, Viktor Vintonyak
  • Patent number: 9994591
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: June 12, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Cédrickx Godbout, Thomas Trieselmann, Viktor Vintonyak
  • Patent number: 9238639
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: January 19, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150133657
    Abstract: The present invention provides processes for the preparation of rivaroxaban. The present invention also provides an intermediate for the preparation of rivaroxaban.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 14, 2015
    Inventors: Pankaj Kumar Singh, Mukesh Kumar Sharma, Chandra Has Khanduri
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Patent number: 8927589
    Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Publication number: 20140364421
    Abstract: [Problem] A compound which is useful as an IK1 channel activator is provided. [Means for Solution] As a result of studies on the IK1 channel activator, the present inventors have found that a benzothiophene compound shows effectiveness on visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia, thereby completing the invention. A compound of the invention has an IK1 channel activation effect, and can also be used as an agent for preventing and/or treating visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia. In addition, the IK1 channel activator can be used as an agent for preventing and/or treating inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tsukasa ISHIHARA, Kazuhiro IKEGAI, Ikumi KURIWAKI, Hiroyuki HISAMICHI, Nobuaki TAKESHITA, Ryuichi TAKEZAWA
  • Publication number: 20140329802
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20140256712
    Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Publication number: 20140235629
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, 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: September 26, 2012
    Publication date: August 21, 2014
    Inventors: Michael D. Bartberger, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Brian M. Fox, Jiasheng Fu, Ana Gonzalez Buenrostro, Felix Gonzalez Lopez De Turiso, Darin J. Gustin, Julie A. Heath, Michael G. Johnson, Frank Kayser, David John Kopecky, Yihong Li, Zhihong Li, Zhihua Ma, Joel Micintosh, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Michael J. Schmitt, Daqing Sun, Xiaodong Wang, Malgorzata Wanska, Christine Weathers, Xuelei Yan
  • Patent number: 8796268
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Patent number: 8729068
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: May 20, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20140073584
    Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.
    Type: Application
    Filed: September 30, 2013
    Publication date: March 13, 2014
    Applicant: SIGNALRX PHARMACEUTICALS, INC.
    Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
  • Publication number: 20140065103
    Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 14, 2013
    Publication date: March 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Patent number: 8648189
    Abstract: The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: February 11, 2014
    Assignee: Sandoz AG
    Inventors: Hubert Sturm, Dominic De Souza, Kerstin Knepper, Martin Albert
  • Publication number: 20130331387
    Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: February 22, 2012
    Publication date: December 12, 2013
    Applicant: Lupin Limited
    Inventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8592413
    Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: November 26, 2013
    Assignee: Allergan, Inc.
    Inventors: Todd Gac, David W. Old
  • Patent number: 8557807
    Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as P1-3 kinase.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: October 15, 2013
    Assignee: Signal Rx Pharmaceuticals, Inc.
    Inventors: Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
  • Publication number: 20130245255
    Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.
    Type: Application
    Filed: May 2, 2013
    Publication date: September 19, 2013
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Taito NISHINO, Shunsuke IWAMOTO, Katsuaki MIYAJI
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20130196984
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.
    Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
  • Publication number: 20130190289
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Publication number: 20130184457
    Abstract: The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.
    Type: Application
    Filed: February 10, 2011
    Publication date: July 18, 2013
    Applicant: SANDOZ AG
    Inventors: Hubert Sturm, Dominic De Souza, Kerstin Knepper, Martin Albert
  • Patent number: 8487091
    Abstract: Disclosed herein are compounds represented by the formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: July 16, 2013
    Assignee: Allergan, Inc.
    Inventors: Mark Holoboski, Robert M. Burk, Mari Posner, Yariv Donde, David W. Old
  • Publication number: 20130172339
    Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
    Type: Application
    Filed: September 19, 2011
    Publication date: July 4, 2013
    Applicant: KANCERA AB
    Inventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
  • Publication number: 20130158022
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Application
    Filed: May 14, 2010
    Publication date: June 20, 2013
    Applicant: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunlun He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
  • Publication number: 20130123252
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: NOVARTIS AG
    Inventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
  • Publication number: 20130116247
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 9, 2013
    Applicant: MANNKIND CORPORATION
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Publication number: 20130053369
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130029973
    Abstract: A compound has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating hyperphosphatemia, preventing hyperphosphatemia, or both. The compound is a tetrahydrobenzothiophene compound. A pharmaceutical composition for treating hyperphosphatemia includes the compound or salt thereof. A method of treating hyperphosphatemia includes administering to a subject an effective amount of the compound or salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: January 31, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20130005962
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-5-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu HAN, Kai GERLACH, Dhileepkumar KRISHNAMURTHY, Burkhard MATTHES, Herbert NAR, Roland PFAU, Henning PRIEPKE, Annette SCHULER-METZ, Chris H. SENANAYAKE, Peter SIEGER, Wenjun TANG, Wolfgang WIENEN, Yibo XU, Nathan K. YEE
  • Patent number: 8324204
    Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: December 4, 2012
    Assignee: UCB Pharma SA
    Inventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
  • Publication number: 20120302562
    Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
    Type: Application
    Filed: May 23, 2012
    Publication date: November 29, 2012
    Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
  • Patent number: 8313978
    Abstract: An exemplary organic semiconductor copolymer includes a polymeric repeat structure having a polythiophene structure and an electron accepting unit. The electron accepting unit has at least one electron-accepting heteroaromatic structure with at least one electron-withdrawing imine nitrogen in the heteroaromatic structure or a thiophene-arylene comprising a C2-30 heteroaromatic structure. Methods of synthesis and electronic devices incorporating the disclosed organic semiconductors, e.g., as a channel layer, are also disclosed.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 20, 2012
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Bang Lin Lee, Kook Min Han, Jung Han Shin, Sang Yoon Lee, Eun Jeong Jeong
  • Patent number: 8299068
    Abstract: Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: October 30, 2012
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 8288380
    Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1—W2 represents CH—CH, or Y represents a single bond and W1—W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: October 16, 2012
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20120258965
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Applicants: The Johns Hopkins University, Cardioxyl Pharmaceuticals
    Inventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20120252801
    Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
  • Publication number: 20120214794
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: October 13, 2011
    Publication date: August 23, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20120178723
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 12, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu