Tricyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.03)
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Publication number: 20140023614Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.Type: ApplicationFiled: March 21, 2012Publication date: January 23, 2014Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
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Publication number: 20140018354Abstract: The present invention provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response.Type: ApplicationFiled: July 23, 2010Publication date: January 16, 2014Inventors: Nathaniel Moorman, Thomas Shenk
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Publication number: 20140005163Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: ApplicationFiled: May 24, 2013Publication date: January 2, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frederic Stauffer
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Publication number: 20130338117Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 27, 2013Publication date: December 19, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: Robert P. RICCIARDI
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as Axl inhibitors
Patent number: 8609650Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: July 26, 2011Date of Patent: December 17, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Patent number: 8598178Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: GrantFiled: October 31, 2007Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
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Patent number: 8598154Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: GrantFiled: August 26, 2011Date of Patent: December 3, 2013Assignee: Corcept Therapeutics, Inc.Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
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Publication number: 20130310374Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of the present invention and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammation and angiogenesis related disorders.Type: ApplicationFiled: December 5, 2011Publication date: November 21, 2013Applicant: PIRAMAL ENTERPRISES LIMITED`Inventors: Sanjay Kumar, Rajiv Sharma, Vijaykumar Bhagwan Deore, Nilambari Nilkanth Yewalkar, Veena R. Agarwal, Nilesh Dagia, Nishigandha Naik
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Patent number: 8580792Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.Type: GrantFiled: February 1, 2012Date of Patent: November 12, 2013Assignee: Critical Outcome Technologies Inc.Inventor: Wayne R. Danter
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Publication number: 20130289029Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: ApplicationFiled: August 18, 2011Publication date: October 31, 2013Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
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Publication number: 20130274258Abstract: Compounds of general formula (I), wherein A, Y, R1 and R2 are defined herein are useful in the treatment or prevention of proliferative diseases including cancer or infectious or parasitic diseases.Type: ApplicationFiled: November 3, 2011Publication date: October 17, 2013Applicant: PHILIP MORRIS PRODUCTS S.A.Inventors: Stephane Demotz, Gerhard Lang, Damian McHugh, Axel Teichert, Fernando Goffman, Paul M. Doyle, Paul M. Blaney, Raymond Fisher, Andrew Smith, Emma L. Blaney, Simon Foster
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Publication number: 20130261104Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.Type: ApplicationFiled: May 9, 2013Publication date: October 3, 2013Applicant: Genentech, Inc.Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
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Publication number: 20130225551Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: ApplicationFiled: April 30, 2012Publication date: August 29, 2013Inventors: Ashok V. Purandare, James W. Grebinski, Amy Hart, Jennifer Inghrim, Gretchen Schroeder, Honghe Wan
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Publication number: 20130225555Abstract: The present invention provides compounds of formula (I) wherein Ra, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 14, 2013Publication date: August 29, 2013Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca ABInventors: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
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Publication number: 20130225553Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: ApplicationFiled: March 7, 2013Publication date: August 29, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
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Patent number: 8507494Abstract: The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: April 25, 2011Date of Patent: August 13, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk
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Publication number: 20130203746Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: November 16, 2012Publication date: August 8, 2013Inventor: Medivation Technologies Inc.
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Publication number: 20130203769Abstract: Methods for targeting adaptive responses to chemotherapy are described. In various embodiments, a method comprises administering at least one compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC, in association with administration of at least one antagonist of PPAR?, PPAR?, or PGC1?. In various embodiments, the compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC is rapamycin, everolimus, temsirolimus, or imatinib. The antagonist of PPAR?, PPAR?, or PGC1? can be GW7647, GW6471, GW501516, GSK3787, or GSK0660.Type: ApplicationFiled: February 7, 2013Publication date: August 8, 2013Applicant: UNIVERSITY OF CINCINNATIInventor: UNIVERSITY OF CINCINNATI
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Patent number: 8501741Abstract: Anti-infection levorotatory optically active compound (S-configuration) of prulifloxacin represented by the following formula (1) and preparation method thereof are disclosed. Said method utilizes levorotatory ulifloxacin as the raw material and the reaction is conducted in organic solvent in the presence of alkaline materials, wherein the reaction temperature is ?20° C.˜60° C. and the reaction time is 15 minutes to 24 hours.Type: GrantFiled: October 22, 2010Date of Patent: August 6, 2013Assignee: Hainan Hualon Pharmaceutical Co., Ltd.Inventors: Jun Ying, Feng Peng, Yuping Wang, Suiwei An, Jinqiang Liang, Beimei Liang, Qingchun Ni, Cheng Luo
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Patent number: 8497262Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: November 18, 2010Date of Patent: July 30, 2013Assignee: Dart NeuroScience (Cayman) LtdInventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
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Publication number: 20130190322Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. 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: March 8, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130190323Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: March 8, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130190304Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: March 12, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130184252Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.Type: ApplicationFiled: March 6, 2013Publication date: July 18, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITED
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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: 20130178479Abstract: The present invention relates to a pharmaceutical combination which comprises (a) an mTOR catalytic inhibitor, such as a catalytic phosphatidylinositol-3-kinase (PI3K) and mTOR inhibitor compound which is an imidazoquinoline derivative and (b) at least one allosteric mTOR inhibitor compound, and optionally, at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the treatment of an mammalian target of rapamycin (mTOR) kinase dependent proliferative diseases; and the uses of such a combination in the treatment of mTOR kinase dependent proliferative diseases; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.Type: ApplicationFiled: October 3, 2011Publication date: July 11, 2013Applicant: NOVARTIS AGInventors: Yan Chen, Xizhong Huang, Leon Murphy, Beat Nyfeller
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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: 20130165449Abstract: The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: ApplicationFiled: February 19, 2013Publication date: June 27, 2013Applicant: CRITICAL OUTCOME TECHNOLOGIES INC.Inventor: CRITICAL OUTCOME TECHNOLOGIES INC.
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Patent number: 8470826Abstract: The present invention relates to an episomal structure expressing a functional oncogene, whereby said oncogene is a fusion gene of two chromosomal gene fragments. More specifically, the invention relates to a NUP214-ABL1 fusion product, important in the development of T-cell acute lymphoblastic leukemia, to methods to detect the fusion and to methods to prevent the oncogenic activity of said fusion product.Type: GrantFiled: June 15, 2010Date of Patent: June 25, 2013Assignees: VIB VZW, K.U. Leuven Research and DevelopmentInventors: Jan Cools, Anne Hagemeijer, Peter Marynen
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Publication number: 20130150359Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.Type: ApplicationFiled: June 24, 2011Publication date: June 13, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Publication number: 20130143893Abstract: The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.Type: ApplicationFiled: January 30, 2013Publication date: June 6, 2013Applicant: MERCK SERONO SAInventors: Sharad Magar, Andreas Goutopoulos, Yihua Liao, Matthias Schwarz, Russell J. Thomas
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Publication number: 20130131077Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical-compositions comprising the compounds and 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: December 21, 2012Publication date: May 23, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130131054Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-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: December 21, 2012Publication date: May 23, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130116262Abstract: Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130116235Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130116245Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130109699Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.Type: ApplicationFiled: July 5, 2011Publication date: May 2, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
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Publication number: 20130096132Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.Type: ApplicationFiled: October 16, 2012Publication date: April 18, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Patent number: 8420643Abstract: The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: GrantFiled: December 2, 2011Date of Patent: April 16, 2013Assignee: Critical Outcome Technologies Inc.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20130079352Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: November 16, 2012Publication date: March 28, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130079337Abstract: The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 26, 2011Publication date: March 28, 2013Applicant: SANOFIInventors: ALEXANDRE BENAZET, OLIVIER DUCLOS, NATHALIE GUILLO, GILBERT LASSALLE, KARIM MACARY, VALÉRIE VIN
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Publication number: 20130072485Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical ResearchInventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
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Patent number: 8399449Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: GrantFiled: February 25, 2009Date of Patent: March 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Patent number: 8394789Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: February 6, 2009Date of Patent: March 12, 2013Assignee: MSD Oss B.V.Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
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Patent number: 8383629Abstract: This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD 1 in mammals. Formula (I).Type: GrantFiled: February 26, 2009Date of Patent: February 26, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Wei He, Wei Zhao, Robert D. Simpson
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Patent number: 8377957Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: November 29, 2011Date of Patent: February 19, 2013Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Publication number: 20130040959Abstract: The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: April 25, 2011Publication date: February 14, 2013Inventors: Douglas C. Beshore, Scott D. Kuduk
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Patent number: 8367675Abstract: The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: GrantFiled: July 25, 2011Date of Patent: February 5, 2013Assignee: Critical Outcome Technologies Inc.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20130023521Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: January 17, 2011Publication date: January 24, 2013Applicant: HYBRIGENICS SAInventors: Roman Lopez, Frederic Colland
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Publication number: 20130012505Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.Type: ApplicationFiled: February 28, 2011Publication date: January 10, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann