Both Rings Which Form The Spiro Are Hetero Rings Patents (Class 548/409)
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Publication number: 20110059545Abstract: The present invention relates to a time temperature indicator for indicating a temperature change over time comprising one dimeric or trimeric spiropyran indicator of the formula I or II wherein R1-R4 independently of one another is hydrogen, —C1C6 alkoxy, halogen, CF3, —C1C6 alkyl or —NO2, R5 is hydrogen, halogen, —C1-C6 alkoxy, —COOH, —COO—C1-C6 alkyl, —CF3 or phenyl; R11 is hydrogen or R11 and R5 form together a phenyl ring; Ra is —C1-C6 alkyl Rb is —C1-C6 alkyl, or together with Ra form a 5-6 membered ring L is a divalent linker; L? is a trivalent linker.Type: ApplicationFiled: January 14, 2008Publication date: March 10, 2011Applicant: FRESHPOINT HOLDINGS SAInventors: Husein Salman, Elena Tenetov, Leonhard Feiler, Thomas Raimann
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Patent number: 7855218Abstract: Compounds of formula (I) wherein the variables are defined herein, pharmaceutical compositions thereof and methods for treatment using the same.Type: GrantFiled: October 6, 2006Date of Patent: December 21, 2010Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, Daniele Andreotti, Markus Bergauer, Riccardo Giovannini, Agostino Marasco
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Publication number: 20100311734Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.Type: ApplicationFiled: July 24, 2008Publication date: December 9, 2010Inventors: Maurizio Botta, Emiliano Castiglioni, Romano Di Fabio, Raffaella Spinosa, Andrea Togninelli
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Patent number: 7803833Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.Type: GrantFiled: October 6, 2006Date of Patent: September 28, 2010Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20100228025Abstract: A structured organic film with an added functionality comprising a plurality of segments and a plurality of linkers arranged as a covalent organic framework, wherein the structured organic film may be a multi-segment thick structured organic film.Type: ApplicationFiled: March 3, 2010Publication date: September 9, 2010Applicant: XEROX CORPORATIONInventors: Adrien Pierre COTE, Matthew A. HEUFT
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Publication number: 20100224867Abstract: An electronic device comprising a structured organic film with an added functionality comprising a plurality of segments and a plurality of linkers arranged as a covalent organic framework, wherein the structured organic film may be a multi-segment thick structured organic film.Type: ApplicationFiled: March 3, 2010Publication date: September 9, 2010Applicant: XEROX CORPORATIONInventors: Matthew A. HEUFT, Adrien Pierre CÔTÉ
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Publication number: 20100204224Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.Type: ApplicationFiled: July 7, 2006Publication date: August 12, 2010Applicant: VERNALIS R & D LIMITEDInventors: Richard Hamlyn, Glyn Addison, Christopher Geoffrey Earnshaw, Harry Finch, Mike Huckstep, Rosemary Lynch, Sarah Mellor
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Publication number: 20100190688Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.Type: ApplicationFiled: July 12, 2005Publication date: July 29, 2010Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
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Patent number: 7700641Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: GrantFiled: April 11, 2006Date of Patent: April 20, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100034961Abstract: The present invention relates to time-temperature indicator (TTI) systems comprising spiropyran indicator of formula (I) wherein R1 is hydrogen, —C1-C6 alkoxy, halogen, —C1-C6 alkyl or —NO2, R2 is hydrogen or —C1-C6 alkoxy; R3 is NO2 halogen; R4 is hydrogen, —C1-C6 alkoxy or halogen; R5 is hydrogen, halogen, —C1-C6 alkoxy, —COOH, —COO—C1-C6alkyl, —CF3 or phenyl; R11 hydrogen or R11 and R5 form together a phenyl ring; Y is phenyl, naphthyl, anthracen-9-yl, 9H-fluoren-9-yl or a residue Formula (A) wherein R6 is hydrogen, halogen, —C1-C6 alkoxy, —NO2, —CF3, —O—CF3, —CN, —COO—C1-C6alkyl, phenyl or biphenyl, 9H-fluoren-9-yl; R7 is hydrogen, halogen, —CN,—C1-C6 alkoxy or R7 and R6 form together a phenyl ring; R8 is hydrogen, halogen, —CN, or —C1-C6 alkoxy; R9 is hydrogen or halogen or CN. R10 is hydrogen or halogen or CN. Ra is —(CH2)n- with n=1-6 or —CH2—CH?CH—. With the proviso that Formula (B) and Formula (C) are excluded.Type: ApplicationFiled: December 28, 2007Publication date: February 11, 2010Applicant: FRESHPOINT HOLDINGS SAInventors: Elena Tenetov, Husein Salman, Julien Assous, Leonhard Feiler, Thomas Raimann
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Patent number: 7655686Abstract: The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.Type: GrantFiled: June 26, 2007Date of Patent: February 2, 2010Assignee: Novartis AGInventors: Yves Auberson, Ralf Glatthar, Rhys Salter, Oliver Simic, Marina Tintelnot-Blomley
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Publication number: 20090298808Abstract: 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: January 6, 2009Publication date: December 3, 2009Inventors: Wenqing Yao, Chunhong He, Jingcong Zhuo
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Publication number: 20090280060Abstract: The present invention provides photochromic compounds and derivatives thereof as shown in claim 1 and methods of use of these compounds and derivatives. The present invention also provides photochromic optical probes capable of undergoing light directed reversible transition between a first state and a second state. The invention also teaches methods of determining and controlling reversible optical biomolecular interactions, for example binding of calcium in a subject.Type: ApplicationFiled: December 5, 2008Publication date: November 12, 2009Inventors: Gerard J. D. Marriott, Tomoyo Sakata, Yuling Yan
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Publication number: 20090215795Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.Type: ApplicationFiled: July 17, 2008Publication date: August 27, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
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Publication number: 20090162420Abstract: The invention relates to a salt of an ACE inhibitor dicarboxylic acid with an organic amine and/or an alkali compound, a transdermal therapeutic system comprising the salt, and a method of producing the transdermal therapeutic system.Type: ApplicationFiled: December 5, 2006Publication date: June 25, 2009Inventors: Karin Klokkers, Michael Helfrich, Jörg Nink
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Patent number: 7534790Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: GrantFiled: November 21, 2007Date of Patent: May 19, 2009Assignee: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Patent number: 7524856Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, p, X, Y, R3, R4, t and, R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 20, 2004Date of Patent: April 28, 2009Assignee: AstraZeneca ABInventors: Nafizal Hossain, Svetlana Ivanova
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Publication number: 20090105289Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 ?-hydroxy-Steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: October 12, 2005Publication date: April 23, 2009Applicant: Novo Nordisk A/SInventors: John Paul Kilburn, Henrik Sune Anderson, Gita Camilla Tejlgaard Kampen
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Publication number: 20090082393Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.Type: ApplicationFiled: September 17, 2008Publication date: March 26, 2009Applicant: LES LABORATOIRES SERVIERInventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Jean-Gilles Parmentier, Alain Benoist, Tony Verbeuren, Alain Rupin, Christine Courchay, Serge Simonet
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Patent number: 7504506Abstract: Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.Type: GrantFiled: November 4, 2004Date of Patent: March 17, 2009Assignee: Elixir Pharmaceuticals, Inc.Inventors: Peter Distefano, Andrew Napper, Rory Curtis, Jay Luly, Manuel A. Navia, Russell J. Thomas, Jean-Francois Pons, Jeffrey O. Saunders
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Patent number: 7498338Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, t, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 15, 2004Date of Patent: March 3, 2009Assignee: AstraZeneca ABInventors: Andrew Baxter, Nafizal Hossain, Svetlana Ivanova, Marguerite Mensonides-Harsema, Austen Pimm, James Reuberson
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Patent number: 7482372Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: March 30, 2005Date of Patent: January 27, 2009Assignee: Bristol-Myers Squibb CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Publication number: 20090022689Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: July 9, 2008Publication date: January 22, 2009Inventors: Yat Sun Or, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 7476688Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.Type: GrantFiled: April 19, 2002Date of Patent: January 13, 2009Assignee: EISAI R&D Management Co., Ltd.Inventors: Shuichi Suzuki, Masanobu Shinoda, Motoji Kogushi, Hiroko Kobayashi
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Publication number: 20080311495Abstract: An image forming medium includes a substrate and an imaging layer coated on or impregnated into said substrate, where the imaging layer includes as a photochromic material a spiropyran compound having a conjugated pathway, dispersed in a polymeric binder, wherein the photochromic material exhibits a reversible transition between a colorless state and a colored state in response to heat and light.Type: ApplicationFiled: June 13, 2007Publication date: December 18, 2008Applicant: XEROX CORPORATIONInventors: Tyler B. NORSTEN, Gabriel IFTIME, Peter M. KAZMAIER
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Publication number: 20080293678Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 17, 2006Publication date: November 27, 2008Applicant: NitroMed, Inc.Inventor: David S. Garvey
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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: 20080221322Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.Type: ApplicationFiled: October 31, 2007Publication date: September 11, 2008Applicant: AstraZeneca ABInventors: Euan Alexander Arnott, John Crosby, Mathew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
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Patent number: 7393858Abstract: The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: March 4, 2004Date of Patent: July 1, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Olivier Dirat, Jason Matthew Elliott, Ian Thomas Huscroft, Richard Alexander Jelley, Janusz Jozef Kulagowski, Piotr Antoni Raubo, Duncan Edward Shaw, Francine Sternfeld, Christopher John Swain
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Publication number: 20080125430Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: August 30, 2007Publication date: May 29, 2008Applicant: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jiangyong Chen, Shanghai Yu
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Publication number: 20080108632Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.Type: ApplicationFiled: November 2, 2007Publication date: May 8, 2008Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Chu-chung Lin, Pei-chin Cheng, Yo-chin Liu, Chen-fu Liu, Chi-Hsin Richard King
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Patent number: 7173048Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.Type: GrantFiled: April 27, 2005Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Narendra Panday, Hasane Ratni, Tanja Schulz-Gasch, Matthew Blake Wright
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Patent number: 6906053Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 12, 2004Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6890915Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 23, 2002Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6890938Abstract: Compound with an indole linked through an aliphatic ring system to an aromatic moiety are useful in treating conditions associated with enhanced P38? kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: May 10, 2005Assignee: Scios, Inc.Inventors: Gregory Luedtke, Richland Tester, Sundeep Dugar, Qing Lu, John Perumattam, Xuefei Tan
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Patent number: 6887869Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
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Patent number: 6835744Abstract: This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to C(CH3)2, C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt tType: GrantFiled: April 24, 2002Date of Patent: December 28, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6803471Abstract: The present invention provides indolinospiropyran compounds and methods for their manufacture, which compounds are useful as photochromic compounds. The compounds of the invention are substituted on the indole ring with succinimide, which substitution permits ring opening of the succinimide and modulation of the bulk and photochromic properties of the compounds. The compounds may be conveniently prepared using the solid phase organic synthesis of the invention.Type: GrantFiled: January 28, 2002Date of Patent: October 12, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Erick M. Carreira, Weili Zhao
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Publication number: 20030232872Abstract: Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.Type: ApplicationFiled: May 6, 2003Publication date: December 18, 2003Inventors: Richard Glennon, Richard Westkaemper
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Publication number: 20030228984Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1Type: ApplicationFiled: April 1, 2003Publication date: December 11, 2003Inventors: Hermann Hagemann, Reiner Fischer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Udo Schneider, Wolfram Andersch
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Patent number: 6608068Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: December 11, 2001Date of Patent: August 19, 2003Assignees: Wyeth, Ligand PharmaceuticalsInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030105327Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.Type: ApplicationFiled: November 18, 2002Publication date: June 5, 2003Applicant: KANEKA CORPORATIONInventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
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Publication number: 20030099910Abstract: The present invention relates to a photochromic spirobenzopyran compound of the formula (1) and its derivatives, a spirobenzopyran group having unsaturated terminal groups, a polymer prepared therefrom, a method for the production thereof, a composition comprising said spirobenzopyran or said spirobenzopyran group-containing polymer and a photochromic switch film using the same: 1Type: ApplicationFiled: August 24, 1999Publication date: May 29, 2003Inventors: EUN-KYOUNG KIM, YUN-KI CHOI, SAM-ROK KEUM
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Patent number: 6562857Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB, RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoType: GrantFiled: January 9, 2002Date of Patent: May 13, 2003Assignee: WyethInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030064995Abstract: Amide and urea derivatives of the formula IType: ApplicationFiled: September 10, 2002Publication date: April 3, 2003Applicant: MERCK PATENT GMBHInventors: Christoph Van Amsterdam, Hartmut Greiner, Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Lisa Matzen, Wilfried Rautenberg
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Patent number: 6541635Abstract: The present invention discloses a method for producing angiotensin converting enzyme inhibitor of the following formula (I) and pharmaceutically acceptable salts thereof, in which a compound of the following formula (II), wherein R and R1 are defined as in the specification, is subjected to a de-protective reaction of silyl group in non-aqueous medium. This reaction is easily carried out only in the non-aqueous medium, so that by-product is minimized and the yield is high.Type: GrantFiled: June 25, 2002Date of Patent: April 1, 2003Assignee: Everlight USA, Inc.Inventors: Mong-Jong Tien, Yu-Liang Liu
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Publication number: 20030008909Abstract: This invention provides compounds of the formula I: 1Type: ApplicationFiled: April 24, 2002Publication date: January 9, 2003Applicant: WYETHInventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20020198188Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.Type: ApplicationFiled: January 10, 2002Publication date: December 26, 2002Applicant: Children's Medical Center CorporationInventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Publication number: 20020091115Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1Type: ApplicationFiled: June 26, 2001Publication date: July 11, 2002Inventors: Alexey B. Dyatkin, Bruce E. Maryanoff, William J. Hoekstra, Wei He, William A. Kinney
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Publication number: 20020087007Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.Type: ApplicationFiled: November 21, 2001Publication date: July 4, 2002Applicant: Kaneka CorporationInventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse