Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The 1,3-diazole Diazole Ring By Nonionic Bonding Patents (Class 546/274.7)
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Patent number: 9969695Abstract: The present invention relates to an N-substituted imidazole carboxylic ester chiral compound containing an ether side chain and to its preparation and application. The structure of this compound is represented by Formula (I). This compound can induce a rapid and reversible general anesthesia effect. Animal experiments show that this compound has rapid and short-acting pharmacological characteristics, so that it can be used as a rapid and short-acting general anesthesia medicine. Compared with etomidate, this compound can reduce the inhibition on the synthesis of adrenal cortical hormone, with an advantage of rapid and full recovery of the post-operative patient. The only chiral carbon in the compound structure belongs to the R form.Type: GrantFiled: October 30, 2014Date of Patent: May 15, 2018Assignee: WEST CHINA HOSPITAL, SICHUAN UNIVERSITYInventors: Wensheng Zhang, Jun Yang, Jin Liu, Lei Tang, Bowen Ke
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Patent number: 9475794Abstract: A process for the preparation of a Form I crystalline polymorph of imidacloprid, including: (i) dissolving imidacloprid in an appropriate amount of aqueous solvent or mixture of solvents to obtain an aqueous solution; (ii) cooling the aqueous solution slowly, thereby forming crystals of polymorph Form I of imidacloprid; (iii) isolating the crystals. A process for the preparation of a Form II crystalline polymorph of imidacloprid, comprising: dissolving imidacloprid in an appropriate amount of non-aqueous solvent or mixture of non-aqueous solvents to obtain a non-aqueous solution; (ii) cooling the solution rapidly, thereby forming crystals of polymorph Form II of imidacloprid; (iii) isolating the crystals.Type: GrantFiled: November 12, 2015Date of Patent: October 25, 2016Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITEDInventors: James Timothy Bristow, Yifan Wu
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Patent number: 9212162Abstract: A process for the preparation of a Form I crystalline polymorph of imidacloprid, including: (i) dissolving imidacloprid in an appropriate amount of aqueous solvent or mixture of solvents to obtain an aqueous solution; (ii) cooling the aqueous solution slowly, thereby forming crystals of polymorph Form I of imidacloprid; (iii) isolating the crystals. A process for the preparation of a Form II crystalline polymorph of imidacloprid, comprising: dissolving imidacloprid in an appropriate amount of non-aqueous solvent or mixture of non-aqueous solvents to obtain a non-aqueous solution; (ii) cooling the solution rapidly, thereby forming crystals of polymorph Form II of imidacloprid; (iii) isolating the crystals.Type: GrantFiled: June 24, 2014Date of Patent: December 15, 2015Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY, LTDInventors: James Timothy Bristow, Yifan Wu
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Patent number: 9029352Abstract: The present invention is directed to a process for the preparation of heterocyclic derivatives of formula I wherein J, X, Z, and R2 are as defined herein. Such compounds are useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.Type: GrantFiled: August 5, 2013Date of Patent: May 12, 2015Assignee: Janssen Pharmaceutica NVInventors: Krzysztof Kolodziejczyk, Alfred Elisabeth Stappers, Christopher A. Teleha, Koen Johan Herman Weerts
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Patent number: 9006269Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: GrantFiled: April 19, 2013Date of Patent: April 14, 2015Assignee: Vernalis (R&D) Ltd.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Patent number: 8937184Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.Type: GrantFiled: February 14, 2006Date of Patent: January 20, 2015Assignee: Abbvie B.V.Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
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Publication number: 20140378457Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: September 9, 2014Publication date: December 25, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
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Patent number: 8883180Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: August 29, 2013Date of Patent: November 11, 2014Assignee: Bayer Intellectual Property GmbHInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140228340Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: August 13, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
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Publication number: 20140228367Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.Type: ApplicationFiled: February 5, 2014Publication date: August 14, 2014Inventor: Gary A. Flynn
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Publication number: 20140206701Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptor.Type: ApplicationFiled: March 20, 2014Publication date: July 24, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, KEN CHOW, TODD M. HEIDELBAUGH, SANTOSH C. SINHA, PHONG X. NGUYEN, SMITA S. BHAT, WENKUI K. FANG
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Patent number: 8771665Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: GrantFiled: December 16, 2011Date of Patent: July 8, 2014Assignee: Cocrystal Discovery, Inc.Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Patent number: 8759254Abstract: The present invention relates to a product for use with new plants comprising a package which is optionally degradable, wherein said package forms an enclosed space is provided. At least one plant enhancer at least one pesticide, and/or at least one pesticide is located in the enclosed space formed by the package. The invention further is directed to method for treating a plant and to method for reducing shock to a plant.Type: GrantFiled: May 5, 2009Date of Patent: June 24, 2014Assignee: Bayer Cropscience LPInventors: Rui Luiz Correa Picanco, Guillaume Huchet, Charles William Boyd, Stephanie Darnell, Kenneth James Essig, Raymond L. Cheek
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Publication number: 20140155407Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.Type: ApplicationFiled: October 21, 2011Publication date: June 5, 2014Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
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Publication number: 20140148448Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: January 30, 2014Publication date: May 29, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Renee Louise DESJARLAIS, Sanath K. MEEGALLA, Mark WALL, Kenneth WILSON
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Patent number: 8729271Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.Type: GrantFiled: September 16, 2011Date of Patent: May 20, 2014Assignee: Taisho Pharmaceutical Co., LtdInventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
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Publication number: 20140045778Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: ApplicationFiled: January 3, 2013Publication date: February 13, 2014Applicants: THE KITASATO INSTITUTE, MEIJI SEIKA PHARMA CO., LTD.Inventors: MEIJI SEIKA PHARMA CO., LTD., THE KITASATO INSTITUTE
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Publication number: 20140045789Abstract: The present invention is directed to a process for the preparation of heterocyclic derivatives of formula I wherein J, X, Z, and R2 are as defined herein. Such compounds are useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.Type: ApplicationFiled: August 5, 2013Publication date: February 13, 2014Applicant: Janssen Pharmaceutica NVInventors: Krzysztof KOLODZIEJCZYK, Alfred Elisabeth Stappers, Christopher A. Teleha, Koen Johan Herman Weerts
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Patent number: 8598217Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: GrantFiled: April 30, 2010Date of Patent: December 3, 2013Assignees: Astex Therapeutics Ltd., Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
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Publication number: 20130303572Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lõrincz, György Dormán, Anikó Görbe
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Publication number: 20130211079Abstract: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventor: Alexander DOEMLING
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Patent number: 8497376Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: October 16, 2008Date of Patent: July 30, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Carl R. Illig, Jinsheng Chen, Sanath K. Meegalia, Mark J. Wall
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Publication number: 20130184460Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.Type: ApplicationFiled: September 16, 2011Publication date: July 18, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
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Patent number: 8481548Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognititve disorders and memory deficits, as well as chronic and acute pain.Type: GrantFiled: October 31, 2007Date of Patent: July 9, 2013Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20130165472Abstract: This invention provides compounds of formula IA: and also provides compounds of formula IIA, IIIA, IVA, or VA: wherein HY, R1, R2, R3, R14, G1, G2, G3, and G4, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: MILLENNIUM PHARMACEUTICALS, INC.
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Publication number: 20130143927Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: June 8, 2012Publication date: June 6, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Patent number: 8455398Abstract: Amide compounds, preparation methods and uses thereof. The structure of the compounds is represented as the general formula (I), in which the definitions of substituents are illuminated as description. The present amide compounds have broad spectrum activity of killing pests and are effective on lepidopteran pests including ostrinia nubilalis, sugarcane borer, adoxophyes orana fischer von reslerstamm, apple fruit borer, grapholitha inopinata, lymantri dispar l., cnaphalocrocis medinalis, ostrinia furnacalis, helicoverpa assulta, grapholitha inopinata, plutella xylostella, spodoptera exigua, prodenia litura etc., especially for plutella xylostella, spodoptera exigua. The present amide compounds can obtain good effect at very low dosage. At the same time, some compounds have good fungicidal activity which can be used to prevent rice blast, phytophthora infestans, cucumber downy mildew or grey mold of vegetables.Type: GrantFiled: June 3, 2009Date of Patent: June 4, 2013Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.Inventors: Changling Liu, Baoshan Chai, Hong Zhang, Jichun Yang, Zhinian Li, Yongwu Peng, Junfeng Wang, Jiao Wu, Shicun Ma, Miao Li
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Patent number: 8450346Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: GrantFiled: February 27, 2009Date of Patent: May 28, 2013Assignee: Vernalis (R&D) Ltd.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Publication number: 20130085272Abstract: A procedure for using thermolabile groups to protect a hydroxyl function, above all in nucleosides, nucleotides, oligomers, nucleic acids during the reactions of organic synthesis. Various new compounds that can be used to implement the procedure. The way of using thermolabile groups to protect hydroxyl functions consists in a primary, secondary and tertiary hydroxyl group converting into a groups during the reaction between a compound and a compound whose hydroxyl group is to be blocked. The blocking reaction is carried out by means of widely known methods appropriate for that purpose in the presence of a chemically basic catalyst. The obtained product has its hydroxyl group blocked. Then the compound with the group blocked can be used for the purposes of various chemical processes. After their completion, the hydroxyl group is unblocked by dissolving it in a solvent at a temperature of 50-95° C.Type: ApplicationFiled: June 1, 2011Publication date: April 4, 2013Applicant: INSTYTUT CHEMII BIOORGANICZNEJ POLSKIEJ AKADEMII NAUKInventor: Marcin Krzysztof Chmielewski
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Patent number: 8362022Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein, having the structure: are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.Type: GrantFiled: January 14, 2009Date of Patent: January 29, 2013Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
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Publication number: 20120316170Abstract: To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Daiichi Sankyo Company LimitedInventors: Nobuo Machinaga, Jun Chiba, Fumihito Muro, Hiroshi Yuita, Jun Watanabe
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Publication number: 20120302608Abstract: The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.Type: ApplicationFiled: May 10, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Norman Earle Hughes, Bryan Hurst Norman, Timothy Andrew Woods
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Publication number: 20120214849Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: November 17, 2011Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
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Publication number: 20120214799Abstract: 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: ApplicationFiled: April 9, 2012Publication date: August 23, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Guy Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Patent number: 8168627Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: GrantFiled: March 16, 2010Date of Patent: May 1, 2012Assignee: Endorecherche, Inc.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, Rene Maltais
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Publication number: 20120101064Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: ApplicationFiled: April 30, 2010Publication date: April 26, 2012Applicants: Astex Therapeutics Limited, Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
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Patent number: 8101772Abstract: The present invention relates to novel active compound combinations comprising a known oxime ether derivative (trifloxystrobin) and imidacloprid, which combinations are highly suitable for controlling phytopathogenic fungi and insects.Type: GrantFiled: August 5, 2002Date of Patent: January 24, 2012Assignee: Bayer Cropscience AGInventors: Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Hirohisa Ohtake
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Publication number: 20110313167Abstract: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.Type: ApplicationFiled: June 21, 2011Publication date: December 22, 2011Inventor: Alexander Doemling
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Publication number: 20110269800Abstract: There is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, including all tautomers thereof, compositions comprising the same, use of said compound and compositions for treatment, in particular for the treatment of asthma and COPD, and processes for the preparation of said compound.Type: ApplicationFiled: October 2, 2009Publication date: November 3, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Peter John Murray, Catherine Elisabeth Charron
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Patent number: 8030339Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: October 12, 2006Date of Patent: October 4, 2011Assignee: Neurosearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
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Publication number: 20110237576Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.Type: ApplicationFiled: October 22, 2009Publication date: September 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Shuji Yonezawa, Yuusuke Tamura, Yuuji Kooriyama, Gaku Sakaguchi
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Publication number: 20110172276Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.Type: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Patent number: 7964620Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.Type: GrantFiled: September 17, 2008Date of Patent: June 21, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20110142856Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoidarthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: February 15, 2011Publication date: June 16, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20110136874Abstract: The present invention relates to fungicide N-(2-pyridylpropyl)carboxamide derivative and its oxa, aza and thia analogues of formula (I), their process of preparation and intermediate compound for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. wherein A, T, W, X, n and Z3 to Z7 represent various substituents.Type: ApplicationFiled: August 6, 2009Publication date: June 9, 2011Inventors: Samir Bennabi, Pierre-Yves Coqueron, Philippe Desbordes, Stéphanie Gary, Rachel Rama, Philippe Rinolfi, Jürgen Benting, Peter Dahmen
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Patent number: 7943803Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: GrantFiled: May 4, 2010Date of Patent: May 17, 2011Assignee: Nippon Soda Co., Ltd.Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20110077237Abstract: 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: ApplicationFiled: April 1, 2010Publication date: March 31, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Guy W. Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
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Patent number: 7812026Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: GrantFiled: December 21, 2006Date of Patent: October 12, 2010Assignee: AstraZeneca ABInventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20100249132Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: September 9, 2008Publication date: September 30, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober