Chalcogen Attached Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/58)
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Publication number: 20100222389Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 13, 2008Publication date: September 2, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Harald Walter, Daniel Stierli, Hans Tobler
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Patent number: 7776922Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.Type: GrantFiled: November 17, 2005Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulf Brüggemeier, Petros Gatsios, Mark Meininghaus, Leila Telan, Elisabeth Woltering, Martina Wuttke, Hartmut Beck, Nils Griebenow, Frank Süβmeier, Niels Svenstrup, Axel Kretschmer, Marcus Bauser, Johannes Köbberling, Wahed Moradi, Siegfried Zaiss, Claudia Hirth-Dietrich, Barbara Albrecht
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Patent number: 7772238Abstract: The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 14, 2006Date of Patent: August 10, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jed Lee Hubbs, Sam Kattar, Joey Methot, Thomas Miller, Phieng Siliphaivanh, Matthew Stanton, Kevin Wilson, David J. Witter
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Publication number: 20100190831Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20100163852Abstract: The present invention provides a light emitting device material which enables a light emitting device having high efficiency and excellent chromatic purity and durability using a light emitting device material containing a pyrene compound represented by formula (1), wherein any one of R1 to R10 is a group represented by formula (2), or 1 to 4 substituents is/are group(s) represented by formula (3), and a light emitting device using the same.Type: ApplicationFiled: June 8, 2007Publication date: July 1, 2010Inventors: Kazumasa Nagao, Seiichiro Murase
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Publication number: 20100166881Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Publication number: 20100160632Abstract: The present invention relates to zinc amide bases of the general formula (I) (R1R2N)2—Zn.aMgX12.bLiX2??(I) wherein R1 and R2 are each independently selected from substituted or unsubstituted, linear or branched alkyl, alkenyl, alkynyl or silyl derivatives thereof, and substituted or unsubstituted aryl or heteroaryl, and wherein R1 and R2 can form together a ring structure, or R1 and/or R2 can be part of a polymer structure; X12 is a divalent anion or two monovalent anions that are independent from each other; X2 is a monovalent anion; a is >0; and b is >0. The zinc amide bases can be used, amongst other things, for deprotonation and metallization of aromatics.Type: ApplicationFiled: May 14, 2008Publication date: June 24, 2010Inventors: Paul Knochel, Stefan Wunderlich
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Publication number: 20100130570Abstract: The present invention relates N-5-membered, fused, heteroaryl-methylene-N-cycloalkyl-carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3; W1 to W5; Y1 to Y3 and p represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: May 27, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
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Patent number: 7705034Abstract: The invention is concerned with novel vinylogous acid derivatives of formula I: wherein A and R1 to R5 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as chymase inhibitors.Type: GrantFiled: September 24, 2007Date of Patent: April 27, 2010Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Hans Hilpert, Bernd Kuhn, Harald Mauser
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Patent number: 7705022Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: GrantFiled: October 27, 2006Date of Patent: April 27, 2010Assignee: Lankenau Institute for Medical ResearchInventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Publication number: 20100094025Abstract: The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.Type: ApplicationFiled: December 20, 2007Publication date: April 15, 2010Applicants: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kousuke Komenoi, Atsushi Nakamura, Makoto Kasai, Masakazu Imamura, Ryota Shiraki, Keita Nakanishi
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Patent number: 7683185Abstract: The present invention provides histone deacetylase inhibitors of general formula (I), process for the preparation of such compounds and uses of the compounds in medicine.Type: GrantFiled: November 18, 2003Date of Patent: March 23, 2010Assignee: Queen Mary & Westfield CollegeInventors: Simon Joel, Charles Marson, Pascal Savy
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Patent number: 7652063Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein the dashed line represents the presence or absence of a double bond; J is C?O or CHOH; A is —(CH2)6—, or cis —CH2CH?CH—(CH2)3—, wherein 1 or 2 carbons may be substituted with S or O; B is CO2H, or CO2R, CONR2, CONHCH2CH2OH, CON(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl; D is —(CH2)n—, —X(CH2)n, or —(CH2)nX—, wherein n is from 0 to 3 and X is S or O; and E is an aromatic or heteroaromatic moiety having from 0 to 4 substituents, said substituents each comprising from 1 to 6 non-hydrogen atoms is disclosed herein. Methods, compositions, and medicaments related thereto, as well as experimental results showing prostaglandin EP4 selective agonist activity for certain compounds disclosed herein, are also disclosed.Type: GrantFiled: September 15, 2006Date of Patent: January 26, 2010Assignee: Allergan, Inc.Inventor: Yariv Donde
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Publication number: 20100004466Abstract: The present invention is related to benzothiophen-2-carbonylguanidine derivatives, a preparation method thereof, and pharmaceutical compositions containing the same. The derivatives have potent inhibitory effect on the sodium/hydrogen exchanger NHE-I, improve the functional recovery of ischemia/reperfusion-induced heart injury in isolated ischemic heart models, and significantly reduce the myocardiac infarct size in in vivo ischemic animal models, thereby showing excellent cardioprotective effects. Also, the derivatives are protective of both neuronal cells and the brain as proven by their protective effects on neuronal cells from necrosis and apoptosis and by their ability to significantly reduce cerebral infarct sizes in in vivo ischemic brain models.Type: ApplicationFiled: December 27, 2005Publication date: January 7, 2010Inventors: Kyu Yang Yi, SunKyung Lee, Jee Hee Suh, Nak Jeong Kim, Hyunsuk Lee, Byung-Ho Lee, Sung-eun Yoo, Kyung-Hee Lee, Yong Oh Lee
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Patent number: 7632846Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: GrantFiled: April 6, 2005Date of Patent: December 15, 2009Assignee: Merck Patent Gesellschaft mit beschrankterInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gèrard Ferrand, Yves Bonhomme
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Publication number: 20090299074Abstract: The invention provides benzo[b]thiophene derivatives useful as production intermediates for chymase inhibitors, and a process for their production. The invention relates to benzo[b]thiophene derivatives represented by the following formula, and a process for their production.Type: ApplicationFiled: October 27, 2006Publication date: December 3, 2009Applicant: TEIJIN PHARMA LIMITEDInventors: Naoki Yajima, Yaoshinori Sato, Hiroshi Yoshino, Tatsuya Koizumi, Yasuhiro Hiroki
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Publication number: 20090286996Abstract: Process for preparing a compound of formula (I), or a salt thereof, comprising reacting of a compound of formula (II) wherein X and R are as herein defined; with a compound of formula (III) NH2OZ??(III) wherein Z is a hydroxy protecting group, in presence of a catalyst, to obtain a compound of formula (IV), or a salt thereof, removing the hydroxyl protecting group to obtain a compound of formula (V), or a salt thereof; converting a compound of formula (V), or a salt thereof, into a compound of formula (I), or a salt thereof; and, if desired, converting a compound of formula (I) into a salt thereof, or vice versa.Type: ApplicationFiled: April 14, 2009Publication date: November 19, 2009Applicant: Dipharma Francis S.r.I.Inventors: Emanuele ATTOLINA, Gianmaria Dell'Anna, Roberto Rossi, Pietro Allegrini, Gabriele Razzetti
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Publication number: 20090264663Abstract: The invention provides 3-hydroxymethylbenzo[b]thiophene derivatives useful as production intermediates for chymase inhibitors, and a process for their production. The invention relates to 3-hydroxymethylbenzo[b]thiophene derivatives represented by the following formula (II), and a process for their production.Type: ApplicationFiled: October 27, 2006Publication date: October 22, 2009Applicant: TEIJEN PHARMA LIMITEDInventors: Naoki Yajima, Yasuhiro Hiroki, Hiroshi Yoshino, Tatsuya Koizumi
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Publication number: 20090261300Abstract: There are provided a heteroacene derivative having an excellent oxidation resistance and capable of forming a semiconductor active phase by a coating process, and an oxidation-resistant organic semiconductor material using the same, as well as an organic thin film.Type: ApplicationFiled: August 28, 2007Publication date: October 22, 2009Applicant: TOSOH CORPORATIONInventor: Makoto Watanabe
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Publication number: 20090221654Abstract: A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.Type: ApplicationFiled: November 14, 2008Publication date: September 3, 2009Applicant: CAYMAN CHEMICAL COMPANYInventors: Nancy S. Barta, Stephen D. Barrett, Gregory W. Endres, Andrei M. Kornilov, Kirk M. Maxey, Adam Uzieblo
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Patent number: 7576122Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: August 27, 2004Date of Patent: August 18, 2009Assignee: Merck & Co. Inc.Inventors: Dong-Ming Shen, James B. Doherty
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Publication number: 20090176996Abstract: The present invention is directed to novel processes for the preparation of sulfamide derivatves, useful in the treatment of epilepsy and related disorders.Type: ApplicationFiled: January 7, 2009Publication date: July 9, 2009Inventors: Ahmed Abdel-Magid, Steven J Mehrman, Caterina Ferraro
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Publication number: 20090176995Abstract: Disclosed are soluble diarylmethanofullerene derivatives that are effective as acceptors for organic thin-film solar batteries. They help to constitute effective organic thin-film solar batteries.Type: ApplicationFiled: November 28, 2008Publication date: July 9, 2009Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA INSTITUTE OF TECHNOLOGYInventors: Takeshi Toru, Norio Shibata, Shuichi Nakamura, Tetsuo Soga, Yasuhiko Hayashi, Surya Prakash Singh
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Publication number: 20090131400Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: ApplicationFiled: July 25, 2008Publication date: May 21, 2009Applicant: IRM LLCInventors: Yuan Mi, Shifeng Pan, Nathanael Schiander Gray, Wenqi Gao, Yi Fan, Tao Jiang
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090105308Abstract: The present invention relates to novel benzoheterocyclylethylcarboxamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, methods for the control of phytopathogenic fungi of plants using these compounds or their compositions:Type: ApplicationFiled: July 6, 2006Publication date: April 23, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090054235Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of 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.Type: ApplicationFiled: July 6, 2006Publication date: February 26, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Patent number: 7488833Abstract: A process for the enantioselective preparation of amino alcohols of formula I by enantioselective hydrogenation of amino ketones of the formula II in the presence of a non-racemic catalyst. The catalyst is a transition-metal complex in which the transition metal is complexed to a chiral diphosphine ligand.Type: GrantFiled: August 1, 2003Date of Patent: February 10, 2009Assignee: Merck Patent GmbHInventors: Joachim Kralik, Kai Fabian, Christoph Mürmann, Norbert Schweickert
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Publication number: 20090030006Abstract: The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(?O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical coType: ApplicationFiled: January 27, 2006Publication date: January 29, 2009Inventors: Takamitsu Kobayashi, Tsutomu Sato, Masahiro Nishimoto
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Publication number: 20090009061Abstract: The object of the present invention is to provide a composition for conductive materials from which a conductive layer having a high carrier transport ability can be made, a conductive material formed of the composition and having a high carrier transport ability, a conductive layer formed using the conductive material as a main material, an electronic device provided with the conductive layer and having high reliability, and electronic equipment provided with the electronic device.Type: ApplicationFiled: July 27, 2005Publication date: January 8, 2009Inventors: Yuji Shinohara, Koichi Terao, Takashi Shinohara
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Publication number: 20090005434Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.Type: ApplicationFiled: June 27, 2008Publication date: January 1, 2009Applicant: Novo Nordisk A/SInventors: Preben Houlberg Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
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Publication number: 20080319047Abstract: The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.Type: ApplicationFiled: July 27, 2005Publication date: December 25, 2008Inventors: Hiroharu Matsuoka, Tsutomu Sato, Masahiro Nishimoto, Yasuharu Kato, Masahiro Sakaitani, Sang-Hak Lee
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Publication number: 20080293909Abstract: The present invention provide a covered heteroaromatic ring compound whose hetero ring effectively is covered and that is suitable for electronic materials and the like. For example, following Scheme 1 below, first, a thiophene monomer unit (1T) is synthesized, and then oligomers (2T) to (16T) are synthesized by repeating oxidative polymerization. The hetero ring is not limited to thiophene, and may be furan or pyrrole, for example. Also, substituents on silicon are not limited to those in Scheme 1, and any substituents may be used. The degree of polymerization and the synthesis method are not limited to those in Scheme 1. In the compound of the present invention, ? electronic conjugation effectively is kept as shown in the ultraviolet and visible absorption spectrum in FIG. 1, for example.Type: ApplicationFiled: March 2, 2006Publication date: November 27, 2008Applicants: OSAKA UNIVERSITY, JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Yoshio Aso, Yutaka Ie, Aihong Han
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Publication number: 20080287489Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: ApplicationFiled: July 23, 2008Publication date: November 20, 2008Inventors: Dong-Ming Shen, James B. Doherty
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Patent number: 7442793Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 11, 2003Date of Patent: October 28, 2008Assignee: SmithKline Beecham CorporationInventors: Jinhwa Lee, Siegfried B. Christensen, IV
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Patent number: 7425631Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 12, 2004Date of Patent: September 16, 2008Assignees: Amgen Inc., Array BioPharma Inc.Inventors: Robert D. Groneberg, Benny C. Askew, Jr., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Patent number: 7419986Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: September 2, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080194539Abstract: The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen. The compounds are suitable for medical use.Type: ApplicationFiled: December 27, 2005Publication date: August 14, 2008Applicant: Schwarz Pharma AGInventors: Peter Gmeiner, Harald Hubner, Karin Schlotter
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Publication number: 20080194637Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: November 2, 2007Publication date: August 14, 2008Applicants: Curis, Inc., WyethInventors: Shirley Ann Brunton, Oivin M. Guicherit, Simon N. Haydar, Lawrence I. Kruse, Dane Springer
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Publication number: 20080171786Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.Type: ApplicationFiled: November 17, 2005Publication date: July 17, 2008Inventors: Ulf Bruggemeier, Petros Gatsios, Mark Meininghaus, Leila Telan, Elisabeth Woltering, Martina Wuttke, Hartmut Beck, Nils Griebenow, Frank Sussmeier, Niels Svenstrup, Axel Kretschmer, Marcus Bauser, Johannes Kobberling, Wahed Moradi, Siegfried Zaiss, Claudia Hirth-Dietrich, Barbara Albrecht
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Publication number: 20080153802Abstract: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.Type: ApplicationFiled: December 21, 2006Publication date: June 26, 2008Applicant: THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCHInventors: Guillaume Laurent Lessene, Jonathan Baell
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Publication number: 20080145698Abstract: The invention relates to the improvement of organic electroluminescent devices, especially blue-emitting devices, by using compounds of formula (1) as dopants in the emitting layer.Type: ApplicationFiled: June 22, 2005Publication date: June 19, 2008Applicant: Merck Patent GmbHInventors: Holger Heil, Philipp Stossel, Horst Vestweber
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Publication number: 20080132543Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of a carbohydrate; or said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: October 24, 2005Publication date: June 5, 2008Inventors: Wha Bin Im, Yariv Donde, Mark Holoboski, David W. Old, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Robert M. Burk, Todd Gac
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Patent number: 7381734Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: July 22, 2005Date of Patent: June 3, 2008Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Publication number: 20080119490Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Marc-Andre POUPART, Pierre Louis BEAULIEU, Jean RANCOURT
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Patent number: 7335666Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: February 26, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080027096Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.Type: ApplicationFiled: March 4, 2005Publication date: January 31, 2008Inventors: Neeraj Garg, Eva Kristina Kock, Henrik Per Hakan Jernstedt, Mikael Johan Gillner
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Publication number: 20080027014Abstract: Novel compounds of formula (A) or a pharmaceutically acceptable salt thereof: wherein symbols are as defined in claims, which are useful as SGLT inhibitors and for treatment of diabetes and related diseases.Type: ApplicationFiled: July 26, 2007Publication date: January 31, 2008Inventors: Sumihiro Nomura, Mitsuya Hongu