Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 546/17)
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Patent number: 7495007Abstract: The present invention relates to spiroindolinone derivatives of the formula and their enantiomers and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4, R5, R6, R7 and R8, are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: GrantFiled: August 29, 2007Date of Patent: February 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Qingjie Ding, Jin-Jun Liu, Song Yang, Zhuming Zhang
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Patent number: 7495008Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5?, X, Y and A are as defined in the specification.Type: GrantFiled: December 13, 2007Date of Patent: February 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20090042921Abstract: An insecticidal compound of formula (I), wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, R8 A1, A2, A3, A4, B1, B2, B3 and B4 are specified organic groups or salts or N-oxides thereof; compositions containing them and their using in controlling insects, acarines, nematodes or molluscs.Type: ApplicationFiled: December 9, 2004Publication date: February 12, 2009Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20080318990Abstract: The present invention relates to a compound of the following formula: where R1-R6, R10, Y, n, m, p, and q are as defined herein. Compounds and compositions of the present invention are useful for the treatment of diseases associated with the overexpression of CCR2.Type: ApplicationFiled: June 20, 2008Publication date: December 25, 2008Inventors: Hilary Schenck Eidam, Pamela A. Haile, Terry Vincent Hughes, Clark A. Sehon
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Publication number: 20080306086Abstract: The present invention relates to a compound of formula I wherein R2 R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: May 30, 2008Publication date: December 11, 2008Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20080306101Abstract: An insecticidal compound of formula I wherein X is O or NR11 where R11 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6 provided that p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof; compositions containing them and their using in controlling insects, acarines, nematodes or molluscs.Type: ApplicationFiled: December 9, 2004Publication date: December 11, 2008Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20080293685Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.Type: ApplicationFiled: May 22, 2008Publication date: November 27, 2008Applicant: Chevron U.S.A. Inc.Inventors: Deyuan Kong, Frederick W. Lam, Steven F. Sciamanna, Earl Shelton, Shenggao Liu, Robert M. Carlson
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Publication number: 20080287420Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.Type: ApplicationFiled: March 7, 2008Publication date: November 20, 2008Applicant: Infinity Discovery, Inc.Inventors: Alfredo Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
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Publication number: 20080281103Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: ApplicationFiled: December 20, 2007Publication date: November 13, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080280898Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5?, X, Y and A are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: November 13, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7449475Abstract: The invention provides compounds of formula (I) wherein m R1, n, R2, q, X, Y, Z, R3, R4, R5, R6, R7, R8, t, and R9 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: July 7, 2003Date of Patent: November 11, 2008Assignee: AstraZeneca ABInventors: Nafizal Hossain, Svetlana Ivanova, Marguerite Mensonides-Harsema
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Publication number: 20080269253Abstract: The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: October 9, 2006Publication date: October 30, 2008Applicant: Glenmark Pharmaceuticals, S.A.Inventors: Laxmikant Atmaram Gharat, Uday Mukund Joshi, Neelima Khairatkar Joshi
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Publication number: 20080255149Abstract: The invention relates to the use of carboxyamine compounds and salts thereof in the treatment of HDAC dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: September 25, 2006Publication date: October 16, 2008Inventors: Markus Rolf Dobler, Jonathan E. Grob, Arup Patnaik, Branko Radetich, Micheal Shultz, Yanyi Zhu
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Patent number: 7435816Abstract: The present invention relates to the chemical synthesis of solanum glycosides, in particular to the synthesis of solasonine as well as to novel ?-monosaccharide intermediate compounds, of Formula (2), where R1 is a benzylidene, 4-nitrobenzylidene or 4-methoxybenzylidine group, and each R2 independently is a benzoyl, acetyl or pivaloyl group:Type: GrantFiled: April 30, 2004Date of Patent: October 14, 2008Inventor: Mohammed Shahid
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Publication number: 20080234252Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2.Type: ApplicationFiled: May 8, 2006Publication date: September 25, 2008Inventors: Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
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Publication number: 20080233609Abstract: Spirolactam targeting compounds, related compounds, uses of such compounds, and methods of making such compounds are disclosed.Type: ApplicationFiled: February 29, 2008Publication date: September 25, 2008Inventors: Stephen C. Miller, Anjan K. Bhunia
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Publication number: 20080200491Abstract: The present invention relates to certain 1,2-dihydro-spiro[3H-indole-3,4?-piperidine]compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein G, R1, R2, R3, R4, R5, and Ar are as disclosed herein (“Compound(s) of the Invention”), which are useful, for example, as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.Type: ApplicationFiled: June 21, 2006Publication date: August 21, 2008Inventors: Thuy-Anh Tran, Sangdon Han, P. Douglas Boatman
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Publication number: 20080194610Abstract: In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R1 to R10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.Type: ApplicationFiled: January 7, 2008Publication date: August 14, 2008Inventors: Caterina Bissantz, Erwin Goetschi, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7410976Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.Type: GrantFiled: July 14, 2006Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
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Publication number: 20080188506Abstract: There are provided spiroindolinones of the formula and enantiomers and pharmaceutically acceptable salts and esters thereof which have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: January 31, 2008Publication date: August 7, 2008Inventors: Qingjie Ding, Jin-Jun Liu, Zhuming Zhang
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Publication number: 20080176883Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: ApplicationFiled: November 16, 2007Publication date: July 24, 2008Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Publication number: 20080171760Abstract: In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R1 to R10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.Type: ApplicationFiled: January 7, 2008Publication date: July 17, 2008Inventors: Caterina Bissantz, Erwin Goetschi, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080171761Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-CType: ApplicationFiled: January 8, 2008Publication date: July 17, 2008Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
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Publication number: 20080167332Abstract: Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.Type: ApplicationFiled: July 18, 2007Publication date: July 10, 2008Inventors: Scott Gibson, Barry Elkins, Mike Rogers, Ian Hassall, Hong Gu, Zhenyu Wang, Vinod Kumar, Synthana Suresh Kumar, Santosh Kavitake, Sidda Lingesha, Eric Merifield, David Ennis, John Pavey, Austen Pimm, James Reuberson, Bo-Goran Josefsson, Martin Hemmerling, Svetlana Ivanova, Marguerite Mensonides-Harsema, Hakan Schulz, John Mo, Tomas Eriksson, Per Strandberg
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Publication number: 20080167333Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5?, X, Y and A are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: July 10, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7396930Abstract: A process for producing cyclic thioether compounds and their synthetic intermediates. The process produces a compound represented by formula (5): wherein G1 is an alkylene group, R1 is a thiol protecting group, R2 is hydrogen or an amino protecting group, and Ar is an aryl group or a 5- to 7-membered heteroaryl group.Type: GrantFiled: December 6, 2004Date of Patent: July 8, 2008Assignee: Sankyo Company, LimitedInventors: Hiroshi Tomori, Keijiro Kobayashi, Fumihiko Toriyama
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Publication number: 20080161304Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5?, X, Y and A are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: July 3, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080161299Abstract: Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein R1 to R11 and X are as defined in the description.Type: ApplicationFiled: November 30, 2007Publication date: July 3, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080153861Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: June 26, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Roger-Evans, Patrick Schnider
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Publication number: 20080153863Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: June 26, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Roger-Evans, Patrick Schnider
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Publication number: 20080153862Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: ApplicationFiled: December 13, 2007Publication date: June 26, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7365067Abstract: The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: —CO—R4, —CO—O—R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).Type: GrantFiled: February 24, 2005Date of Patent: April 29, 2008Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Toshiyasu Takemoto, Takuya Ikeda, Kiyoshi Morimoto
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Patent number: 7354925Abstract: This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents a hydrogen atom, or the like; R4 represents a hydrogen atom or the like; represents one of the following or the like; R5 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.Type: GrantFiled: March 16, 2005Date of Patent: April 8, 2008Assignee: Pfizer Inc.Inventors: Yoshinobu Hashizume, Masako Hirota, Sachiko Mihara, Hisoshi Nakamura, Hiroki Koike, Yukari Matsumoto
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Patent number: 7351831Abstract: An intramolecular [3+2] cycloaddition reaction of a hydrazone is carried out under a mild condition with a high stereoselectivity and yield by reacting a hydrazone derivative in the presence of an asymmetric catalyst system obtained by mixing a zirconium alkoxide represented by the following formula (I): Zr(OR)4 ??(I) (wherein R is a hydrocarbon group which may have a substituent) with a binaphthol derivative represented by the following formula (II): (wherein Y1 and Y2 are each identical or different and denote a hydrogen atom or a halogen atom, and at least one of Y1 and Y2 denotes a halogen atom).Type: GrantFiled: March 11, 2003Date of Patent: April 1, 2008Assignee: Japan Science and Technology AgencyInventors: Shu Kobayashi, Yasuhiro Yamashita, Haruro Ishitani
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Patent number: 7351706Abstract: This invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiropiperidine-head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and to methods of preparation thereof.Type: GrantFiled: December 18, 2006Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7338962Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the ? opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other ? opioid receptor-mediated conditions.Type: GrantFiled: October 1, 2004Date of Patent: March 4, 2008Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Patent number: 7335665Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.Type: GrantFiled: July 3, 2003Date of Patent: February 26, 2008Assignee: H - Lundbeck A/SInventors: Mohammad R. Marzabadi, Yu Jiang, Kai Lu, Chien-An Chen, John E. De Leon, John Wetzel, Kim Andersen
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Patent number: 7332501Abstract: The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.Type: GrantFiled: July 10, 2006Date of Patent: February 19, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080039628Abstract: The present invention relates to the chemical synthesis of solanum glycosides, in particular to the synthesis of solasonine as well as to novel ?-monosaccharide intermediate compounds, of Formula (II), where each R1 is the same or different and independently represents a benzylidene, 4-nitrobenzylidene or 4-methoxybenzylidene group and each R2 is the same or different and independently represents a benzoyl, acetyl or pivaloyl group.Type: ApplicationFiled: April 30, 2004Publication date: February 14, 2008Inventor: Mohammed Shahid
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Patent number: 7329673Abstract: Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 31, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: Liangqin Guo, Shuwen He, Tianying Jian, Yingjie Lai, Jian Liu, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye, Jonathan R. Young
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Patent number: 7288613Abstract: The present invention relates to selected 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) said piperidine derivatives. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-2,2,6,6 tetramethyl piperidine, 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 dimethyl piperidine derivatives which are substituted in the 4 position by two oxygen atoms forming an open chain or cyclic ketal structure for controlled polymerization.Type: GrantFiled: February 28, 2006Date of Patent: October 30, 2007Assignee: Ciba Specialty Chemicals Corp.Inventors: Peter Nesvadba, Marie-Odile Zink, Wiebke Wunderlich
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Patent number: 7288559Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: October 30, 2007Assignee: Merck + Co, Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
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Patent number: 7279486Abstract: This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.Type: GrantFiled: March 29, 2005Date of Patent: October 9, 2007Assignee: Pfizer Inc.Inventors: Yoshinobu Hashizume, Masako Hirota, Sachiko Mihara, Hiroshi Nakamura, Hiroki Koike, Yukari Matsumoto
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Patent number: 7276511Abstract: The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor.Type: GrantFiled: August 2, 2004Date of Patent: October 2, 2007Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Nobuo Kawase, Nobuyuki Tanaka, Hideki Nakamura, Naoki Tsuzuike, Masakazu Murata
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Patent number: 7262212Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group —OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and —(CH2)nR2 may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): wherein R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 10, 2003Date of Patent: August 28, 2007Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Hideaki Kuroda, Motohiro Itotani, Takeshi Hasegawa, Yoshikazu Haraguchi, Takeshi Kuroda, Takayuki Matsuzaki, Kuninori Tai, Makoto Komatsu, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Yuji Seike, Masanori Kawasaki, Takumi Sumida, Shin Miyamura
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Patent number: 7247725Abstract: The present invention is directed to compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: October 24, 2003Date of Patent: July 24, 2007Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Alexander Pasternak, Lihu Yang, Changyou Zhou
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Patent number: 7217719Abstract: The present invention relates to 1,3,8-triara-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: June 16, 2005Date of Patent: May 15, 2007Assignee: Acadia Pharmaceuticals Inc.Inventor: Nathalie Schlienger
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Patent number: 7202251Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: April 10, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Cory R. Theberge, Xu-Fang Zhang, Craig Stump, C. Blair Zartman
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Patent number: 7115644Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.Type: GrantFiled: September 3, 2003Date of Patent: October 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
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Patent number: 7109207Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: June 26, 2003Date of Patent: September 19, 2006Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu, Thavalakulamgara K. Sasikumar, Martin S. Domalski