Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
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Patent number: 8530489Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 22, 2012Date of Patent: September 10, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
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Patent number: 8530480Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: GrantFiled: September 3, 2008Date of Patent: September 10, 2013Assignee: The Scripps Research InstituteInventors: Theodore Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
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Patent number: 8530492Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.Type: GrantFiled: April 19, 2010Date of Patent: September 10, 2013Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Publication number: 20130231519Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 12, 2011Publication date: September 5, 2013Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Patent number: 8524709Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: GrantFiled: January 12, 2012Date of Patent: September 3, 2013Assignee: Tyrogenex, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Patent number: 8524728Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: February 15, 2011Date of Patent: September 3, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Gustaaf Celine Verdonck, Patrick René Angibaud, Bruno Roux, Isabelle Noëlle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen
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Publication number: 20130225601Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE
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Publication number: 20130225591Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.Type: ApplicationFiled: September 14, 2010Publication date: August 29, 2013Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
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Publication number: 20130225581Abstract: The present invention provides a nitrogen-containing aromatic heterocyclic derivative represented by formula (I): [wherein W represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like, R4 represents a hydrogen atom or the like, R5 represents a hydrogen atom or the like, R9 represents substituted imidazolyl, R12 and R13 may be the same or different, each represent a hydrogen atom or the like, R22 and R23 may be the same or different, each represent a hydrogen atom or the like, R24 represents a hydrogen atom or the like, Y represents C—R25 (wherein R25 represents a hydrogen atom or the like) or the like] or a pharmaceutically acceptable salt thereof and a FGFR inhibitor comprising, as an active ingredient, the nitrogen-containing aromatic heterocyclic derivative or the pharmaceutically acceptable salt thereof, or the like.Type: ApplicationFiled: July 15, 2011Publication date: August 29, 2013Applicant: KYOWA HAKKO KIRIN CO., LTDInventors: Takayuki Furuta, Kazuo Kubo, Toshiyuki Atsumi, Maasa Yamanouchi
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Publication number: 20130225579Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.Type: ApplicationFiled: June 8, 2011Publication date: August 29, 2013Applicant: Tianjin Hemay Bio-Tech Co., Ltd.Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
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Patent number: 8518944Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: October 25, 2010Date of Patent: August 27, 2013Assignee: Pfizer Inc.Inventors: Chakrapani Subramanyam, Travis T. Wager
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Patent number: 8518950Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: January 25, 2006Date of Patent: August 27, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
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Publication number: 20130214258Abstract: A compound of the invention is represented by a formula (1) below. In the formula (1), at least one of A1 and A2 represents a substituted or unsubstituted nitrogen-containing aromatic heterocyclic group. A material for an organic electroluminescence device contains the compound represented by the formula (1). The material for an organic electroluminescence device includes an organic thin-film layer between an anode and a cathode, in which the organic thin-film layer contains the compound represented by the formula (1).Type: ApplicationFiled: February 1, 2013Publication date: August 22, 2013Applicant: IDEMITSU KOSAN CO., LTD.Inventor: IDEMITSU KOSAN CO., LTD.
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Publication number: 20130217664Abstract: Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, 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, allergic or 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 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.Type: ApplicationFiled: February 7, 2013Publication date: August 22, 2013Inventors: Christel Jeanne Marie MENET, Benoit Antoine SCHMITT, Raphael Jean Joel GENEY, Kevin James DOYLE, Joanne PEACH, Nicholas John PALMER, Graham Peter JONES, David HARDY, James Edward Stewart DUFFY
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Patent number: 8513256Abstract: The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(?) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.Type: GrantFiled: February 8, 2012Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Hans Michael Bürger, Paul William Manley, Michael Mutz
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Patent number: 8513272Abstract: Alternative chemical and/or solid state forms of Compound I, processes to reproducibly make them and methods of treating patients using them.Type: GrantFiled: May 11, 2011Date of Patent: August 20, 2013Assignee: Cephalon, Inc.Inventors: Stephen Bierlmaier, Raymond Scott Field, R. Curtis Haltiwanger, Martin J. Jacobs, Robert E. McKean, Mehran Yazdanian, Veronique Courvoisier
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Publication number: 20130210809Abstract: The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 12, 2011Publication date: August 15, 2013Inventors: Christelle Boléa, Sylvain Celanire, Cédric Boudou, Lam Tang, Jean-Philippe Rocher, Nigel John Liverton
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Publication number: 20130210847Abstract: The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 15, 2012Publication date: August 15, 2013Applicant: Natco Pharma LimitedInventors: Amala Kompella, Adibhatla Kali Satya Bhujanga Rao, Sreenivas Rachakonda, Venugopala Krishna Gampa, Venkaiah Chowdary Nannapaneni
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Publication number: 20130210816Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.Type: ApplicationFiled: July 28, 2011Publication date: August 15, 2013Inventors: Tin-Yau Chan, Henry M. Vaccaro
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Publication number: 20130210774Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.Type: ApplicationFiled: August 26, 2011Publication date: August 15, 2013Applicants: EMORY UNIVERSITY, RFS PHARMA, LLCInventors: Steven J. Coats, Franck Amblard, Hongwang Zhang, Longhu Zhou, Richard Anthony Whitaker, Tamara Rosario McBrayer, Raymond F. Schinazi, Junxing Shi
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Publication number: 20130210800Abstract: The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11, R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2011Publication date: August 15, 2013Applicant: PFIZER INC.Inventors: Sajiv Krishnan Nair, Simon Paul Planken
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Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
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Publication number: 20130210807Abstract: The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3? are —H or methyl, or R3 and R3 taken together form a double bond, or R3? is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.Type: ApplicationFiled: July 9, 2011Publication date: August 15, 2013Inventors: Nigel J Liverton, Christelle Boléa, Sylvain Celanire, Yunfu Luo
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Patent number: 8507485Abstract: A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X represents R1 and R2 independently represent a hydrogen atom, an alkyl, an aryl or an aromatic heterocyclic; R3 represents a hydrogen atom, a halogen atom, a hydroxy, an alkoxy, an aryloxy, an alkyl, an aryl, an amino, an alkylamino, a cycloalkylamino, an arylamino, an alkylcarbonylamino, an arylcarbonylamino, a mercapto, an alkylthio, an arylthio, an alkylsulfinyl or a nonaromatic heterocyclic; A1 represents a sulfur atom, a sulfinyl or a sulfonyl; and A2 represents an alkylene.Type: GrantFiled: January 24, 2011Date of Patent: August 13, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto
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Patent number: 8507491Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: GrantFiled: August 24, 2009Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Patent number: 8507514Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: GrantFiled: February 5, 2010Date of Patent: August 13, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20130200359Abstract: The present invention relates to compounds of the formula (1) and (2) which are suitable for use in electronic devices, in particular organic electroluminescent devices.Type: ApplicationFiled: September 16, 2011Publication date: August 8, 2013Applicant: Merck Patent GmbHInventors: Philipp Stoessel, Dominik Joosten, Arne Besing
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Publication number: 20130203755Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: May 24, 2011Publication date: August 8, 2013Applicant: UNIVERSITY OF ROCHESTERInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
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Publication number: 20130203786Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: May 16, 2011Publication date: August 8, 2013Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
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Patent number: 8501758Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.Type: GrantFiled: August 27, 2010Date of Patent: August 6, 2013Assignees: IRM LLC, Novartis AGInventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
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Patent number: 8501760Abstract: A pharmaceutical composition, especially capsules, comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process.Type: GrantFiled: September 21, 2012Date of Patent: August 6, 2013Assignee: Novartis AGInventor: Nathalie Bruneau
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130196967Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET 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: ApplicationFiled: January 29, 2013Publication date: August 1, 2013Inventors: Alessandra BARTOLOZZI, Zhidong CHEN, Jonathon Alan DINES, Ho Yin LO, Pui Leng LOKE, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20130197059Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.Type: ApplicationFiled: January 24, 2013Publication date: August 1, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130196985Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.Type: ApplicationFiled: June 3, 2011Publication date: August 1, 2013Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of SciencesInventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng
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Patent number: 8497278Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. Many of the compounds disclosed herein may be represented by the following generic formula: in which Y is a direct bond or heteroatom and A3 is usually a nitrogenous heterocycle.Type: GrantFiled: May 19, 2009Date of Patent: July 30, 2013Assignee: Sunovion Pharmaceuticals Inc.Inventors: Qun Kevin Fang, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
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Publication number: 20130190339Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: December 10, 2012Publication date: July 25, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents of the University of Texas System
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Publication number: 20130190293Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: July 25, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130190302Abstract: The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: January 25, 2013Publication date: July 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffman-La Roche Inc.
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Publication number: 20130190307Abstract: Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.Type: ApplicationFiled: September 15, 2011Publication date: July 25, 2013Inventors: Weiguo Su, Weihan Zhang, Haibin Yang
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Publication number: 20130184284Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
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Publication number: 20130178459Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.Type: ApplicationFiled: March 29, 2011Publication date: July 11, 2013Applicant: Oncotherapy Science, Inc.Inventors: Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
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Publication number: 20130178470Abstract: The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.Type: ApplicationFiled: September 9, 2011Publication date: July 11, 2013Applicant: HANGZHOU BENSHENG PHARACEUTICALS CO., LTD.Inventors: Rongzhen Xu, Fuwen Xie, Hongxi Lai, Frank Rong
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Publication number: 20130172330Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.Type: ApplicationFiled: November 15, 2012Publication date: July 4, 2013Applicant: ALTIRIS THERAPEUTICS, INC.Inventor: Altiris Therapeutics, Inc
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Publication number: 20130172549Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: January 29, 2013Publication date: July 4, 2013Applicant: H. Lundbeck A/SInventor: H. Lundbeck A/S
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Publication number: 20130172310Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: September 12, 2012Publication date: July 4, 2013Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Publication number: 20130172354Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.Type: ApplicationFiled: February 21, 2013Publication date: July 4, 2013Applicant: NOVARTIS AGInventor: Novartis AG
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Publication number: 20130172351Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 26, 2012Publication date: July 4, 2013Applicant: MERCK PATENT GMBHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos