Sulfur In Substituent Q Patents (Class 564/162)
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Publication number: 20120101053Abstract: The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.Type: ApplicationFiled: June 16, 2010Publication date: April 26, 2012Inventors: Cameron Black, Christian Beaulieu
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Patent number: 8143447Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.Type: GrantFiled: September 5, 2007Date of Patent: March 27, 2012Assignee: BiPar Sciences, Inc.Inventors: Jerome Moore, Bruce Keyt, John Burnier, Barry M. Sherman, Max Totrov, Valeria S. Ossovskaya
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Patent number: 8124807Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.Type: GrantFiled: December 16, 2008Date of Patent: February 28, 2012Assignee: MSD K.K.Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
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Patent number: 8119842Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1 E, E?, D, Z and L are as defined herein.Type: GrantFiled: December 14, 2009Date of Patent: February 21, 2012Assignee: Roche Palo Alto LLPInventors: Kieran Durkin, Lawrence Emerson Fisher, Arthur Meili, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
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Publication number: 20120041036Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.Type: ApplicationFiled: February 8, 2010Publication date: February 16, 2012Inventors: Isao Kinoyama, Yohei Koganemaru, Takehiro Miyazaki, Takuya Washio
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Patent number: 8110703Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumors, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumors, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.Type: GrantFiled: May 31, 2009Date of Patent: February 7, 2012Assignees: Anhui Medical University, Anhui New Star Pharmaceutical Development Co., Ltd.Inventors: Feihu Chen, Jingbo Shi, Yuan Wang, Jun Li, Juan Shen, Jingjing Ruan, Fanrong Wu
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Patent number: 8110329Abstract: A charge controlling agent is provided as a compound in which an amide group is introduced together with a sulfonic group or a derivative thereof. The charge controlling agent is characterized by including at least one compound represented by the chemical formula (2) in which an amide group is introduced together with at least one of a sulfonic group, a sulfonic acid ester, a sulfonic acid salt, and a sulfonic acid halide.Type: GrantFiled: November 8, 2006Date of Patent: February 7, 2012Assignee: Canon Kabushiki KaishaInventors: Akiko Tominaga, Tatsuki Fukui, Takashi Kenmoku, Ako Kusakari, Masato Minami, Tetsuya Yano, Takeshi Ikeda, Norikazu Fujimoto, Atsushi Tani
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Patent number: 8101665Abstract: Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula j wherein m is from 1 to 5 and X is halo, with Z2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula k wherein n is from 1 to 5, provided that n is less than or equal to m.Type: GrantFiled: December 17, 2008Date of Patent: January 24, 2012Assignee: Roche Palo Alto LLCInventors: Mohammand R. Masjedizadeh, Shao-Yong Wu
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Publication number: 20120014905Abstract: Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.Type: ApplicationFiled: March 4, 2010Publication date: January 19, 2012Inventors: Antony Robert Godwin, Stephen James Brocchini
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Publication number: 20110306670Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: ApplicationFiled: August 25, 2011Publication date: December 15, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventor: Heinz-Werner KLEEMANN
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Publication number: 20110301235Abstract: Provided herein are organoselenium compounds and pharmaceutical compositions thereof. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders using the compounds and pharmaceutical compositions provided herein.Type: ApplicationFiled: December 2, 2010Publication date: December 8, 2011Applicant: Alquest Therapeutics, Inc.Inventors: Daniel A. Erlanson, Stig K. Hansen
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Patent number: 8067592Abstract: Fungicidal compounds of the general formula (1), wherein Ar is a group of the formula (A), (B1), (B2) or (C), or Ar is a 5- or 6-linked group of the formula (D1) or (D2); and R1, R2, R3, R4, R5, n, A1, A2, A3, A4, A5, Ka, Kb, L, M, V, W, X, Y and Z have the definitions given in claim 1.Type: GrantFiled: May 28, 2004Date of Patent: November 29, 2011Assignee: Syngenta LimitedInventors: Patrick Jelf Crowley, Roger Salmon, Olivia Anabelle Sageot, David Philip Bacon, David William Langton
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Publication number: 20110245262Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 20, 2007Publication date: October 6, 2011Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
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Publication number: 20110236395Abstract: Inhibitors of matrix metalloproteinase 2 are used to treat or prevent a fibrotic disorder of the posterior capsule of the eye, for example posterior capsule opacification (PCO), or of a tissue or structure of the eye other than the lens or capsular bag.Type: ApplicationFiled: September 9, 2009Publication date: September 29, 2011Applicant: UNIVERSITY OF EAST ANGLIAInventors: Ian Michael Wormstone, Lucy Dawes, Julie Ann Eldred, Dylan Edwards, Lisa Hodgkinson
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Publication number: 20110207654Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.Type: ApplicationFiled: February 24, 2011Publication date: August 25, 2011Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
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Publication number: 20110207605Abstract: What is described are 3-aminocarbonyl-substituted benzoylcyclohexanediones of the formula (I) as herbicides. In this formula (I), R1 to R5 are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. X is alkylene.Type: ApplicationFiled: February 17, 2011Publication date: August 25, 2011Applicant: BAYER CROPSCIENCE AGInventors: Chieko UENO, Simon DÖRNER-RIEPING, Andreas VAN ALMSICK, Christopher Hugh ROSINGER, Jan DITTGEN, Dieter FEUCHT, Isolde HÄUSER-HAHN
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Publication number: 20110166366Abstract: Provided are chalcogenoxanthylium compounds which can effectively be used as sensitizers in photodynamic therapy, virucides in photodynamic antimicrobial chemotherapy and reversal agents of Pgp function in cancer cells. Further provided is a general method for the preparation of chalcogenoxanthylium compounds.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Inventors: Michael R. Detty, David J. Donnelly, Stephen J. Wagner
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Patent number: 7960586Abstract: The invention encompasses processes for obtaining pure armodafinil substantially free of disulfide impurities that is suitable for use on an industrial scale. In particular, a processes for purifying armodafinil from bis(diphenylmethyl)disulfide comprising: dissolving crude armodafinil in ethanol to form a solution; adding a solvent selected from the group consisting of linear or branched C5-C8 alkyl, linear or branched C5-C8 ether, and mixtures thereof to the solution to form a reaction mixture; cooling the reaction mixture; and isolating pure armodafinil from the reaction mixture.Type: GrantFiled: August 18, 2008Date of Patent: June 14, 2011Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Boaz Gome
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Publication number: 20110136723Abstract: A compound of the general formula X-[Q-W—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.Type: ApplicationFiled: July 17, 2009Publication date: June 9, 2011Applicant: POLYTHERICS LIMITEDInventor: Antony Godwin
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Publication number: 20110098505Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein Ar, Y, R1 are as defined in claim 1.Type: ApplicationFiled: January 4, 2011Publication date: April 28, 2011Applicant: CEPHALON FRANCEInventors: Laurence Prat, Olivier Neckebrock, Dominique Schweizer, Philippe Louvet
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Patent number: 7915449Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein n, Y, R1, R1a, R2 and R2a are as defined.Type: GrantFiled: March 18, 2008Date of Patent: March 29, 2011Assignee: Cephalon FranceInventors: François Rebiere, Gérard Duret, Laurence Prat
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Publication number: 20110065196Abstract: The present invention provides a method of forming an ion of formula (I) comprising the steps of: (i) reacting a compound of the formula (IIa); with a biopolymer, BP, having at least one group capable of reacting with M to form a covalent linkage, to provide a biopolymer derivative of the formula (IIIa); and (ii) cleaving the C—X bond between X and the ?-carbon atom of the derivative of formula (IIIa) to form the ion of formula (I); where: (IV) is a carbon atom bearing a single positive charge or a single negative charge; and X is a group comprising a thioether sulphur atom bound directly to the ?-carbon which is capable of being cleaved from the ?-carbon atom to form an ion of formula (I). The biopolymer derivatives of the invention have enhanced ionisability with respect to free biopolymer (BP) enabling improved analysis of the biopolymer using mass spectrometry.Type: ApplicationFiled: June 16, 2006Publication date: March 17, 2011Inventors: Mikhail Shchepinov, Pablo Bernad
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Publication number: 20110065681Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: February 27, 2009Publication date: March 17, 2011Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
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Publication number: 20110065799Abstract: The invention relates to novel inhibitors of urokinase and to their preparation and use for the therapy, prophylaxis and diagnosis of a tumor, in particular for reducing the formation of tumor metastases.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz
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Patent number: 7902372Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.Type: GrantFiled: April 2, 2008Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Patent number: 7893111Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I). wherein Ar, Y, R1 are as defined in claim 1.Type: GrantFiled: March 13, 2006Date of Patent: February 22, 2011Assignee: Cephalon FranceInventors: Laurence Prat, Olivier Neckebrock
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Patent number: 7893093Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: March 22, 2006Date of Patent: February 22, 2011Assignee: ViroBay, Inc.Inventor: Craig J. Mossman
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003852Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: February 18, 2008Publication date: January 6, 2011Inventor: Soren Ebdrup
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Patent number: 7838560Abstract: The invention relates to novel inhibitors of urokinase and to their preparation and use for the therapy, prophylaxis and diagnosis of a tumor, in particular for reducing the formation of tumor metastases.Type: GrantFiled: March 11, 2003Date of Patent: November 23, 2010Assignee: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz
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Publication number: 20100286109Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100286125Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: March 28, 2008Publication date: November 11, 2010Inventors: Alan T. Johnson, Seongjin Kim
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Patent number: 7812193Abstract: The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I); wherein n, Y, R1, R1a, R2 and R2a are as defined herein.Type: GrantFiled: October 30, 2007Date of Patent: October 12, 2010Assignee: Cephalon FranceInventors: Francois Rebiere, Gerard Duret, Laurence Prat
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Publication number: 20100249147Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.Type: ApplicationFiled: December 16, 2008Publication date: September 30, 2010Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
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Publication number: 20100234468Abstract: The present invention relates to a process for the preparation of polymorphic forms of the R- and S-enantiomers of modafinil, R-(?)-2-benzhydrylsulfinylacetamide and S-(+)-2-benzhydrylsulfinylacetamide respectively.Type: ApplicationFiled: May 30, 2008Publication date: September 16, 2010Inventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Dattatrey Kokane
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Patent number: 7786171Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: GrantFiled: March 26, 2009Date of Patent: August 31, 2010Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100210631Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.Type: ApplicationFiled: May 14, 2008Publication date: August 19, 2010Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
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Publication number: 20100210731Abstract: Polymorphs and solvates of racemic, enantiomerically pure, and enantiomerically mixed modafinil are formed and discussed. In addition, said forms are described as useful for the treatment of many conditions including, but not limited to, narcolepsy.Type: ApplicationFiled: February 19, 2010Publication date: August 19, 2010Applicant: Cephalon, Inc.Inventors: Magali Bourghol Hickey, Matthew Peterson, Orn Almarsson, Mark Oliveira
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Publication number: 20100197794Abstract: There is provided a fluorine-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein G represents an oxygen atom or a sulfur atom; R2 represents a C1-C4 chain hydrocarbon group which is optionally substituted with a halogen atom, etc.; R3 and R4 independently represent a C1-C4 chain hydrocarbon group or a hydrogen atom; R represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom; R6 represents a halogen atom, a cyano group, a nitro group or a -(G)q-R8 group; R7 represents an amino group etc.; R8 represents a C1-C4 chain hydrocarbon group which is optionally substituted with a halogen atom; m represents an integer of 0 to 5; n represents an integer of 0 to 2; p represents 0 or 1; q represents 0 or 1; and G1 represents an oxygen atom etc.Type: ApplicationFiled: July 25, 2008Publication date: August 5, 2010Inventors: Koji Kumamoto, Hiroyuki Miyazaki
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Patent number: 7763661Abstract: This invention relates to novel substituted pentafluorosulfanylbenzenes of the formula I: and/or salts thereof as claimed, for use as a synthetic intermediates for preparing medicaments, diagnostic aids, liquid crystals, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides, arthropodicides and polymers.Type: GrantFiled: March 9, 2007Date of Patent: July 27, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Heinz-Werner Kleemann, Remo Weck
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Publication number: 20100160682Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1 E, E?, D, Z and L are as defined herein.Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Inventors: Kieran Durkin, Lawrence Emerson Fisher, Arthur Meili, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
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Publication number: 20100137401Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: February 2, 2010Publication date: June 3, 2010Applicant: Incyte CorporationInventors: Wenqing Yao, Colin Zhang, Jincong Zhuo, Meizhong Xu, Konstantinos Agrios, Brian Metcalf
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Patent number: 7700655Abstract: A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represeType: GrantFiled: April 9, 2007Date of Patent: April 20, 2010Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Akiko Itai
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Patent number: 7687665Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: June 23, 2005Date of Patent: March 30, 2010Assignee: Incyte CorporationInventors: Wenqing Yao, Colin Zhang, Jincong Zhuo, Meizhong Xu, Konstantinos Agrios, Brian Metcalf
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Publication number: 20100063144Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.Type: ApplicationFiled: October 24, 2007Publication date: March 11, 2010Applicant: IMPERIAL INNOVATIONS LTDInventors: Eric Ofori Aboagye, David Michael Vigushin, Wendy Vigushin
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Publication number: 20100048718Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 5.23, 5.03, 4.22 and 4.10 ?, and a process for the preparation thereof.Type: ApplicationFiled: July 22, 2009Publication date: February 25, 2010Applicant: Cephalon FranceInventors: Olivier Neckebrock, Laurent Courvoisier, Stephanie Graf, Gilles Serrure, Gerard Francois Coquerel, Sebastien Rose, Christine Besselievre, Franck Patrick Mallet, Adriaan Jan Van Langevelde
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Publication number: 20100048720Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 14.14, 10.66, 7.80 and 4.02 ?, and a process for the preparation thereof.Type: ApplicationFiled: July 22, 2009Publication date: February 25, 2010Applicant: Cephalon FranceInventors: Olivier Neckebrock, Laurent Courvoisier, Stéphanie Graf, Gilles Serrure, Gérard Fransois Coquerel, Sébastien Rose, Christine Besselievre, Franck Patrick Mallet, Adriaan Jan Van Langevelde
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Publication number: 20100048719Abstract: The invention relates to a polymorphic form of (?)-modafinil that produces a powder X-ray diffraction spectrum comprising intensity peaks corresponding to interplanar spacings of about 12.31, 8.54, 7.27 and 3.62 ?, and a process for the preparation thereof.Type: ApplicationFiled: July 22, 2009Publication date: February 25, 2010Applicant: Cephalon FranceInventors: Olivier Neckebrock, Laurent Courvoisier, Stephanie Graf, Gilles Serrure, Gerard Francois Coquerel, Sebastien Rose, Christine Besselievre, Franck Patrick Mallet, Adriaan Jan Van Langevelde
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Publication number: 20100041657Abstract: The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.Type: ApplicationFiled: May 11, 2006Publication date: February 18, 2010Applicant: NOVO NORDICK A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Flemming Elmelund Nielsen, Anders Klarskov Petersen