Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/309)
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Patent number: 8822462Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: GrantFiled: January 28, 2010Date of Patent: September 2, 2014Assignee: Emory UniversityInventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
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Publication number: 20140243335Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Publication number: 20140243337Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Publication number: 20140234939Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.Type: ApplicationFiled: December 23, 2013Publication date: August 21, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
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Publication number: 20140234245Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.Type: ApplicationFiled: November 5, 2012Publication date: August 21, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Cédric Poinsard
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Patent number: 8809544Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: GrantFiled: February 7, 2014Date of Patent: August 19, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Koichi Kutose, Hiroki Inoue, Shiro Tsubokura
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Publication number: 20140228408Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: August 14, 2014Applicant: AMAKEM NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre, Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140219960Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.Type: ApplicationFiled: April 23, 2012Publication date: August 7, 2014Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventor: Jong-Won Oh
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Publication number: 20140221435Abstract: The invention relates to amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.Type: ApplicationFiled: January 29, 2014Publication date: August 7, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
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Patent number: 8796269Abstract: The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.Type: GrantFiled: August 25, 2010Date of Patent: August 5, 2014Assignee: Nerre Therapeutics LimitedInventors: Andrew Simon Craig, Salima Zarah Ismail, Ronnie Maxwell Lawrence
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Publication number: 20140213791Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].Type: ApplicationFiled: August 24, 2012Publication date: July 31, 2014Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
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Publication number: 20140213786Abstract: The present invention provides a novel method for producing a compound represented by general formula (VII) below or a pharmaceutically acceptable salt thereof or a synthetic intermediate thereof: wherein R2 represents a hydrogen atom or a halogen atom, Rc represents a C1-6 alkyl group, X represents a group selected from a heteroaryl group etc., R11 represents an atom or group selected from a hydrogen atom, a halogen atom, a C1-6 alkyl group, etc., R16 and R17 each independently represent an atom or group selected from a hydrogen atom, a C1-6 alkyl group, etc., and R15 represents a hydrogen atom or a C1-6 alkyl group.Type: ApplicationFiled: September 5, 2012Publication date: July 31, 2014Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Masatoshi Murakata, Takuma Ikeda, Takahiro Ichige
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Patent number: 8778939Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.Type: GrantFiled: September 27, 2010Date of Patent: July 15, 2014Assignee: Glaxo Group LimitedInventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Publication number: 20140194629Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: ApplicationFiled: February 7, 2014Publication date: July 10, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Koichi KUTOSE, Hiroki INOUE, Shiro TSUBOKURA
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Publication number: 20140187555Abstract: The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.Type: ApplicationFiled: August 9, 2012Publication date: July 3, 2014Applicant: AMAKEM NVInventors: Dirk Leysen, Olivier Defert, Sandro Boland
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Publication number: 20140186923Abstract: Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.Type: ApplicationFiled: March 14, 2013Publication date: July 3, 2014Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20140187586Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, 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: ApplicationFiled: March 12, 2014Publication date: July 3, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Zhiqiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Publication number: 20140171651Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: ApplicationFiled: February 7, 2014Publication date: June 19, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Koichi KUTOSE, Hiroki INOUE, Shiro TSUBOKURA
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Publication number: 20140170058Abstract: Residual palladium is removed and recovered from 4-amino-3-halo-5-fluoro-6-(aryl)pyridine-2-carboxylates and 4-amino-3-halo-6-(aryl)pyridine-2-carboxylates by treatment with an aqueous solution containing from about 20 to about 50% of an alkali metal bisulfite at a temperature from about 60 to about 90° C. and a pH from about 3.8 to about 7.0.Type: ApplicationFiled: March 14, 2013Publication date: June 19, 2014Applicant: DOW AGROSCIENCES LLCInventors: Jossian Oppenheimer, Mark V. M. Emonds
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Publication number: 20140163235Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: ApplicationFiled: February 7, 2014Publication date: June 12, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Koichi KUTOSE, Hiroki INOUE, Shiro TSUBOKURA
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Publication number: 20140155436Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: ApplicationFiled: November 4, 2013Publication date: June 5, 2014Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIEInventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
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Publication number: 20140155616Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Koichi KUTOSE, Hiroki INOUE, Shiro TSUBOKURA
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Publication number: 20140155615Abstract: Disclosed is a compound containing a pyridine ring that can be synthesized in an industrially advantageous manner, and is useful as an intermediate for producing tetrazolyloxime derivatives that exhibit fungicidal activity (wherein R0 represents a C1-6 alkoxy group, C1-6 alkoxy-C1-6 alkoxy group or the like, R1 represents a C1-2 alkoxycarbonyl group, acetyl group or the like, Z represents a halogen atom, cyano group or the like, X represents a halogen atom, and n represents an integer of 0 to 3), and industrially advantageous production methods for producing 2-substituted amino-6-halomethylpyridine derivatives and tetrazolyloxime derivatives.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Hidekazu Miyazaki, Satoru Yanaka, Shiro Tsubokura, Tadashi Sugiura, Kaoru Noda, Kengo Suzuki
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Publication number: 20140155613Abstract: Disclosed is a compound containing a pyridine ring that can be synthesized in an industrially advantageous manner, and is useful as an intermediate for producing tetrazolyloxime derivatives that exhibit fungicidal activity (wherein R0 represents a C1-6 alkoxy group, C1-6 alkoxy-C1-6 alkoxy group or the like, R1 represents a C1-2 alkoxycarbonyl group, acetyl group or the like, Z represents a halogen atom, cyano group or the like, X represents a halogen atom, and n represents an integer of 0 to 3), and industrially advantageous production methods for producing 2-substituted amino-6-halomethylpyridine derivatives and tetrazolyloxime derivatives.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Hidekazu Miyazaki, Satoru Yanaka, Shiro Tsubokura, Tadashi Sugiura, Kaoru Noda, Kengo Suzuki
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Patent number: 8729107Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.Type: GrantFiled: September 9, 2010Date of Patent: May 20, 2014Assignee: Purdue Research FoundationInventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
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Publication number: 20140135496Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y ia halogen atm, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Applicant: Nissan Chemical Industries, Ltd.Inventors: Takeshi MITA, Yuki FURUKAWA, Ken-ichi TOYAMA, Manabu YAOSAKA, Eitatsu IKEDA, Yoshihide MASUZAWA, Mitsuaki KOMODA
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Patent number: 8710234Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: GrantFiled: September 20, 2013Date of Patent: April 29, 2014Assignee: Mitsui Chemicals, Inc.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8710233Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: GrantFiled: October 19, 2006Date of Patent: April 29, 2014Assignee: Gruenenthal GmbHInventors: Jeewoo Lee, Hyung Chul Ryu, Robert Frank, Gregor Bahrenberg, Jean De Vry, Thomas Christoph, Derek John Saunders, Klaus Schiene, Bernd Sundermann
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Patent number: 8703959Abstract: There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m?4.Type: GrantFiled: March 28, 2011Date of Patent: April 22, 2014Assignee: Nippon Soda Co., LtdInventors: Koichi Kutose, Hiroki Inoue, Shiro Tsubokura
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Patent number: 8691847Abstract: 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: GrantFiled: September 12, 2012Date of Patent: April 8, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song
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Patent number: 8691996Abstract: Disclosed is a compound containing a pyridine ring that can be synthesized in an industrially advantageous manner, and is useful as an intermediate for producing tetrazolyloxime derivatives that exhibit fungicidal activity (wherein R0 represents a C1-6 alkoxy group, C1-6 alkoxy-C1-6 alkoxy group or the like, R1 represents a C1-2 alkoxycarbonyl group, acetyl group or the like, Z represents a halogen atom, cyano group or the like, X represents a halogen atom, and n represents an integer of 0 to 3), and industrially advantageous production methods for producing 2-substituted amino-6-halomethylpyridine derivatives and tetrazolyloxime derivatives.Type: GrantFiled: March 11, 2011Date of Patent: April 8, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Hidekazu Miyazaki, Satoru Yanaka, Shiro Tsubokura, Tadashi Sugiura, Kaoru Noda, Kengo Suzuki
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Publication number: 20140094455Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Patent number: 8686157Abstract: The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.Type: GrantFiled: August 24, 2011Date of Patent: April 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: John R. Snoonian, Patricia Ann Oliver-Shaffer
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Patent number: 8686154Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: June 10, 2009Date of Patent: April 1, 2014Assignee: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
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Patent number: 8653086Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: GrantFiled: October 21, 2009Date of Patent: February 18, 2014Assignee: Oregon Health & Science UniversityInventors: Xiangshu Xiao, Bingbing Li
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Publication number: 20140046071Abstract: Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, James P. Kanter, Keiko Sujino, Sharique Sami Zuberi
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Patent number: 8648100Abstract: The invention relates to the use of Roflumilast, Roflumilast N-Oxide or a pharmaceutically acceptable salt of either for the treatment of pulmonary hypertension. The invention additionally relates to the use of Roflumilast, Roflumilast N-oxide or a pharmaceutically acceptable salt of either in combination with a PDE5 inhibitor or a pharmaceutically acceptable salt thereof for the treatment of pulmonary hypertension.Type: GrantFiled: April 12, 2006Date of Patent: February 11, 2014Assignee: Takeda GmbHInventors: Rolf Beume, Armin Hatzelmann, Degenhard Marx, Christian Schudt, Hermann Tenor, Saadia Eddahibi, Serge Adnot
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Publication number: 20140038960Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Patent number: 8642510Abstract: The invention describes a compound having the formula (I), wherein X is F, Cl, Br, or I; R1 is CH3, C2H5, C2H4R3, C2H3R3R4, C3H7, C3H6R or C3H5R3R4; R is H, CH3, C2H5, C2H4R3 or C2H3R3R4; and R3 and R4 are, independently, X, OH or NH2 for the treatment of plants, for increasing plant growth.Type: GrantFiled: March 3, 2009Date of Patent: February 4, 2014Assignee: GMI-Gregor Mendel-Institut fuer Molekulare Pflanzenbiologie GmbHInventors: Claudia Jonak, Wilfried Rozhon
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20140011275Abstract: The present invention relates to a composition for suppressing the death of stem cells during suspension culturing, a composition for mass culturing of stem cells, and a method for suppressing cell death of stem cells during suspension culturing. The composition of the present invention can be usefully used for effective single suspension culturing of stem cells, particularly, mesenchymal stem cells, or used for mass suspension culturing under the circumstances in which cell aggregation does not occur.Type: ApplicationFiled: December 27, 2011Publication date: January 9, 2014Applicant: SEOUL NATIONAL UNIVERSITY HOSPITALInventors: Eun Ju Lee, Hyo Soo Kim
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Publication number: 20140004044Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including for the treatment of demyelinating diseases and/or in vivo imaging of the central nervous system to diagnose and/or assess the progression of MS or other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: The University of ChicagoInventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum
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Publication number: 20140005212Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, R1b, R2a, R2b, R2c, A1, A2, and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: December 21, 2011Publication date: January 2, 2014Applicant: Purdue Pharma L.P.Inventors: Chiyou Ni, Minnie Park, Bin Shao, Laykea Tafesse, Jiangchao Yao, Mark Youngman, Xiaoming Zhou
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Publication number: 20130327251Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.Type: ApplicationFiled: March 7, 2013Publication date: December 12, 2013Applicant: THE UNIVERSITY OF HOUSTON SYSTEMInventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
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Publication number: 20130324412Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.Type: ApplicationFiled: August 8, 2013Publication date: December 5, 2013Applicant: DOW AGROSCIENCES LLCInventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
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Publication number: 20130317020Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20130310347Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.Type: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130303526Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 16, 2011Publication date: November 14, 2013Applicant: Purdue Pharma L.P.Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
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Publication number: 20130303549Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: ApplicationFiled: July 10, 2013Publication date: November 14, 2013Inventors: Jean-Guy BOITEAU, Laurence CLARY, Corinne Millois BARBUIS