Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/426)
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Publication number: 20110253934Abstract: The invention relates to mesogenic tetrahydropyran compounds having at least four rings, of the formula I in which R1, A1, A2, X1, L1, L2, m and n have the meanings indicated in Claim 1, and to a process for the preparation thereof, to the use thereof in liquid-crystalline media, to liquid-crystalline media comprising at least one compound of the formula I, and to electro-optical displays containing a liquid-crystalline medium of this type.Type: ApplicationFiled: July 17, 2007Publication date: October 20, 2011Inventors: Lars Lietzau, Markus Czanta, Atsutaka Manabe
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Publication number: 20110257226Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.Type: ApplicationFiled: December 24, 2009Publication date: October 20, 2011Inventor: Hiromasa Mitsudera
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Patent number: 7998968Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=—CR3; X1=—CR2 or —NR2; and X2=—CR5 or —NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.Type: GrantFiled: November 25, 2009Date of Patent: August 16, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
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Publication number: 20110160300Abstract: Disclosed are aspartic protease inhibitors represented by the following Formula: wherein R1, R2, R3, R4, R5, R6, R7a, R7b and n are as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods for treating an aspartic protease mediated disorder using the same.Type: ApplicationFiled: June 18, 2009Publication date: June 30, 2011Inventors: Marlys Hammond, Patrick Stoy
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Publication number: 20110144197Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 and R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
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Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
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Patent number: 7935709Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein s, T, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of p38 mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: July 16, 2007Date of Patent: May 3, 2011Assignee: Amgen Inc.Inventors: Fang-Tsao Hong, Kelvin K. C. Sham, Seifu Tadesse, Andrew Tasker
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Patent number: 7928123Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 13, 2007Date of Patent: April 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Publication number: 20110077251Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2010Publication date: March 31, 2011Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
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Patent number: 7915433Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.Type: GrantFiled: April 15, 2005Date of Patent: March 29, 2011Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20110039853Abstract: 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 19, 2008Publication date: February 17, 2011Inventor: Soren Ebdrup
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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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Publication number: 20100311989Abstract: Disclosed is a process for the preparation of tetrahydropyran-di-amine represented by Structural Formula (I): wherein R1 is H or alkyl and E is H or an amine protecting group.Type: ApplicationFiled: September 17, 2008Publication date: December 9, 2010Inventors: Marlys Hammond, Patrick Stoy, Scott K. Thompson
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Publication number: 20100311976Abstract: The invention relates to a novel process for preparing enantiomerically enriched or pure tetrahydroquinoline derivatives by reacting a chiral dihydropyran-methylamine C with a aldehyde B and an aniline A in a multicomponent one pot synthesis in the presence of a protonic acid or Lewis acid with a suitable solvent. A, B, C have the meaning as described in the specification.Type: ApplicationFiled: November 20, 2008Publication date: December 9, 2010Applicant: MERCK PATENT GESELLSCHAFTInventors: Ulrich Emde, Oliver Block, Kai Schiemann
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Publication number: 20100256400Abstract: Disclosed is a process for the preparation of a tetrahydropyran-di-amine represented by Structural Formula (I): wherein R1 is H or alkyl and E is H or an amine protecting group.Type: ApplicationFiled: September 17, 2008Publication date: October 7, 2010Inventors: Paul G. Spoors, Lara S. Kallander, David A. Claremon
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Patent number: 7795315Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
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Publication number: 20100160424Abstract: Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: June 20, 2008Publication date: June 24, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing yuan, Wei Zhao
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Patent number: 7674807Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.Type: GrantFiled: March 1, 2005Date of Patent: March 9, 2010Assignee: Bayer CropScience AGInventors: Katsuaki Wada, Takuya Gombuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Norihiko Nakakura, Rüdiger Fischer, Tetsuya Murata, Eiichi Shimojo
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Publication number: 20100056528Abstract: The invention provides sulfonamide compounds of formula (I) as defined herein, pharmaceutical compositions containing the same and methods of treatment using such compounds and pharmaceutical compositions. These compounds have a common wide range of beneficial therapeutic indications, in particular as analgesic and anti-inflammatory agents.Type: ApplicationFiled: December 19, 2007Publication date: March 4, 2010Inventors: Avihai Yacovan, Iris Alroy, Alexander Aizikovich, Sima Mirilashvili, Flavio Gryszpan
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Patent number: 7662849Abstract: 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: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Patent number: 7651742Abstract: The present invention relates to a liquid-crystalline medium comprising 1,2-difluoroethene compounds of the general formula I, in which R1, ring A, Z1, Z2, m, X and L1-6 are as defined in claim 1. The invention also relates to the use of the medium for electro-optical purposes and to displays containing this medium. Novel 1,2-difluoroethene compounds having 3 or more rings are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: January 26, 2010Assignee: Merck Patent GmbHInventors: Michael Wittek, Markus Czanta, Harald Hirschmann, Volker Reiffenrath
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Patent number: 7645797Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: GrantFiled: May 28, 2008Date of Patent: January 12, 2010Assignee: XenoPort, Inc.Inventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Publication number: 20100000865Abstract: A convenient, rapid, and highly sensitive protein detection method is provided. According to the present invention, an easily water-soluble compound of formula I is provided: [wherein, R1 and R2 are same or different, each of which is an aryl or heteroaryl group substituted with one or more anionic substituents].Type: ApplicationFiled: June 26, 2009Publication date: January 7, 2010Applicants: NATIONAL INSTIT OF ADVANCE INDUST SCIENCE AND TECH, Kanto Kagaku Kabushiki KaishaInventors: Yoshio SUZUKI, Kenji Yokoyama, Nobuyuki Takagi, Tomoyuki Chimuro, Atsushi Shinohara
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Publication number: 20090318501Abstract: The present invention is directed to aspartic protease inhibitors represented by the following structural formula; or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.Type: ApplicationFiled: September 17, 2007Publication date: December 24, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
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Publication number: 20090312369Abstract: The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.Type: ApplicationFiled: September 18, 2007Publication date: December 17, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Lanqi Jia, Patrick T. Flaherty
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Patent number: 7618996Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R1, R2, R3, R4, R5, and R6 are described herein.Type: GrantFiled: September 10, 2007Date of Patent: November 17, 2009Assignee: Pfizer Inc.Inventors: Roger B. Ruggeri, George T. Magnus-Aryitey
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Patent number: 7615651Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R, R1, R2a, R2b, R3, R4, V, R6, R7, R8, R9, W and X are described herein.Type: GrantFiled: November 13, 2007Date of Patent: November 10, 2009Assignee: Pfizer Inc.Inventors: Roger B. Ruggeri, George T. Magnus-Aryitey, Benjamin A. Thuma
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Publication number: 20090275651Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.Type: ApplicationFiled: September 14, 2006Publication date: November 5, 2009Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
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Publication number: 20090229670Abstract: An organic photoelectric conversion material for a photoelectric conversion element is provided, the organic photoelectric conversion material represented by formula 1 and having a molecular weight of 250 or greater but not greater than 800: wherein, A represents an electron withdrawing atomic group; R1, R2 and R3 each independently represents a hydrogen atom or a substituent; L represents a divalent TC conjugated substituent; D represents an electron donating aromatic substituent; and X represents O, S, or N—Ra in which Ra represents a hydrogen atom or a substituent.Type: ApplicationFiled: March 11, 2009Publication date: September 17, 2009Applicant: FUJIFILM CorporationInventors: Tetsu KITAMURA, Kimiatsu Nomura, Tetsuro Mitsui
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Patent number: 7582749Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.Type: GrantFiled: October 26, 2007Date of Patent: September 1, 2009Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, Meng He, Terry A. Kellar, II, Forrest R. Blackburn
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Patent number: 7579487Abstract: This invention relates to a process for preparing optically active ?-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.Type: GrantFiled: May 6, 2005Date of Patent: August 25, 2009Assignee: Merck & Co., Inc.Inventors: Spencer D. Dreher, Norihiro Ikemoto, C. Scott Shultz, J. Michael Williams
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Publication number: 20090209770Abstract: Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds. (wherein, R1, R2 and R3 are as defined in the specification.Type: ApplicationFiled: October 1, 2008Publication date: August 20, 2009Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Yong Seo CHO, You Seung KIM, Jae Kyun LEE, Hyunah CHOO, Ae Nim PAE
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Patent number: 7576129Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.Type: GrantFiled: February 6, 2004Date of Patent: August 18, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaki Asada, Kaoru Kobayashi, Masami Narita, Kazutoyo Sato, Atsushi Kinoshita, Toshihiko Nagase, Ken Yoshikawa
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Patent number: 7569601Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.Type: GrantFiled: May 14, 2007Date of Patent: August 4, 2009Assignee: SmithKline Beecham CorporationInventors: Jing Fang, Dennis Heyer, Aaron Bayne Miller, Frank Navas, III, Terrence Lee Smalley, Jr., William J. Zuercher, Subba Reddy Katamreddy
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Publication number: 20090137601Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: November 22, 2006Publication date: May 28, 2009Applicant: ASTRAZENECA ABInventors: Simon Thomas Barry, Jason Grant Kettle, David Alan Rudge
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Publication number: 20090082423Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: September 10, 2008Publication date: March 26, 2009Inventors: Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090012153Abstract: The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—CONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical.Type: ApplicationFiled: June 26, 2008Publication date: January 8, 2009Applicant: PharmaleadsInventors: Bernard Roques, Marie-Claude Fournie-Zaluski
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Patent number: 7420002Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: GrantFiled: June 11, 2002Date of Patent: September 2, 2008Assignee: XenoportInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Patent number: 7417059Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.Type: GrantFiled: March 31, 2005Date of Patent: August 26, 2008Assignee: Takeda Pharmacetical Company LimitedInventors: Norikazu Tamura, Takashi Ichikawa, Masayuki Ii
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Publication number: 20080167371Abstract: Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R, R1, R2a, R2b, R3, R4, V, R6, R7, R8, R9, W and X are described herein.Type: ApplicationFiled: November 13, 2007Publication date: July 10, 2008Inventors: Roger B. Ruggeri, George T. Magnus-Aryitey, Benjamin Aaron Thuma
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Patent number: 7364804Abstract: A light-emitting compound that has excellent carrier transportation properties and that can exhibit long wavelength light is disclosed. Further, a method for manufacturing the light-emitting compound in a high yield is disclosed. The disclosed light-emitting compound is a pyran derivative as represented by general formula 1: wherein A1 and A2 are individually a ?-conjugated system group having 6 to 16 conjugating carbon atoms; X1 is a dialkylamino group; and Y1 is a diarylamino group or an alkylarylamino group.Type: GrantFiled: August 13, 2004Date of Patent: April 29, 2008Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Sachiko Yamagata, Ryoji Nomura, Satoshi Seo
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Patent number: 7361388Abstract: The invention relates to liquid-crystalline compounds of formula (I), wherein R11, X11, Z11, Z12, Z13, L11, L12, L13, L14, L15 and L16 have the meanings as cited in Claim 1, and to a method for the production thereof, their use in liquid-crystalline media, liquid-crystalline media containing at least one compound of formula (I), and to electro-optical displays containing a liquid-crystalline medium of this typeType: GrantFiled: May 24, 2004Date of Patent: April 22, 2008Assignee: Merck Patent GmbHInventors: Peer Kirsch, Eike Poetsch, Atsutaka Manabe
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Patent number: 7314943Abstract: The invention relates to pyran derivatives of formula I and processes and intermediates for their preparation and derivatisation, and the use thereof in liquid-crystalline media.Type: GrantFiled: May 25, 2004Date of Patent: January 1, 2008Assignee: Merck Patent GmbHInventors: Eike Poetsch, Volker Meyer, Werner Binder, Michael Heckmeier, Georg Luessem, Stephan Guertler
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Patent number: 7300953Abstract: The present invention discloses a process for preparing a nitrile compound, a carboxylic acid compound or a carboxylic acid ester compound represented by the formula (2): wherein R represents a cyano group, a carboxyl group or an ester group, R1 and R2 each represent a group which does not participate in the reaction, which may have a substituent, and R1 and R2 may be combined to each other to form a ring, which comprises subjecting an acetic acid compound represented by the formula (1): wherein R, R1 and R2 have the same meanings as defined above, to decarboxylation in the presence of a metal catalyst.Type: GrantFiled: September 17, 2004Date of Patent: November 27, 2007Assignee: Ube Industries, LtdInventors: Shigeyoshi Nishino, Kenji Hirotsu, Hidetaka Shima, Keiji Iwamoto, Takashi Harada
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Patent number: 7217465Abstract: A light-emitting compound that can be easily applied to vacuum vapor deposition and exhibit long wavelength light is disclosed. Further, a light-emitting element without inferior luminescence properties due to the carbonization of a light-emitting compound during vapor deposition; and a light-emitting device that is composed of the light-emitting elements are also disclosed. A pyran derivative is represented by the following general formula 1: wherein R1 is a hydrogen element or an alkoxy group.Type: GrantFiled: October 19, 2004Date of Patent: May 15, 2007Assignee: Semicondutor Energy Laboratory Co., Ltd.Inventors: Sachiko Yamagata, Hiroko Abe, Nobuharu Ohsawa, Ryoji Nomura, Satoshi Seo
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Patent number: 7196209Abstract: The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein R1, R3, R4, R5, R6 and X are as herein defined. The present invention is further directed to a continuous process for the preparation of Topiramate.Type: GrantFiled: October 23, 2003Date of Patent: March 27, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Thomas W. Adkins, Charles F. Cicco, Penina Feibush, Donald A. Koch, Cynthia Maryanoff, Walter E. Stalzer
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Patent number: 7157589Abstract: The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein X, R1, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: March 1, 2004Date of Patent: January 2, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Joachim Ernst Berkner, Scott Duncan, John Mills
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Patent number: 6916948Abstract: Derivatives of bis-(1,3-dihydroxy-prop-2-yl)amine are disclosed, together with the use of such derivatives and of bis(1,3-dihydroxy-prop-2-yl)amine itself in the preparation of polymers, in particular dendrimers. Some of the derivatives may be useful as non-ionic surfactants.Type: GrantFiled: September 12, 2001Date of Patent: July 12, 2005Assignee: Isis Innovation LimitedInventors: George W. J. Fleet, David Scott, Malcolm Finn, Thomas Krūlle
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Patent number: 6905786Abstract: A compound represented by the following formula (I): wherein R1, R2 and R3each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group and at least one of the aryl group and heterocyclic group contains a group represented by formula (II), R1, R2 and R3 may be linked to each other to form a ring, wherein R4, R5 and R6, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2,RX3 each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.Type: GrantFiled: December 3, 2002Date of Patent: June 14, 2005Assignee: Fuji Photo Film., Ltd.Inventor: Kazumi Nii