Chalcogen Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 514/238.2)
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Patent number: 7803800Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.Type: GrantFiled: September 30, 2005Date of Patent: September 28, 2010Assignee: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Patent number: 7795304Abstract: The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: GrantFiled: August 22, 2005Date of Patent: September 14, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Patent number: 7781613Abstract: Disclosed are compounds of the general formula (I), with the definitions of the substituents R1 to R5, A and X being detailed in the text, and to their physiologically tolerated salts, to processes for preparing these compounds and to the use thereof as inhibitors of hormone-sensitive lipase (HSL).Type: GrantFiled: June 25, 2007Date of Patent: August 24, 2010Assignee: Sanofi-AventisInventors: Karl Schoenafinger, Stefan Petry, Guenter Mueller, Karl-Heinz Baringhaus
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Publication number: 20100210603Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: September 11, 2009Publication date: August 19, 2010Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Publication number: 20100168112Abstract: The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine mediated conditions.Type: ApplicationFiled: July 15, 2009Publication date: July 1, 2010Inventors: Michael G. KELLY, John Kincaid, Satyanarayana Janagani
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Publication number: 20100160289Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventors: Mark J. Macielag, James J. McNally
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Patent number: 7723328Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.Type: GrantFiled: April 3, 2006Date of Patent: May 25, 2010Assignees: The University of North Carolina at Chapel Hill, The Regents of the University of California, The United States of America as represented by the Department of Veterans AffairsInventors: Frank M. Longo, Stephen M. Massa
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Patent number: 7713961Abstract: The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1—X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: GrantFiled: March 30, 2006Date of Patent: May 11, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Stefan Peters, Klaus Fuchs, Niklas Heine, Sandra Handschuh, Cornelia Dorner-Ciossek, Klaus Klinder, Marcus Kostka
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Publication number: 20100113449Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Publication number: 20100105687Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of the following formula, Formula (2), wherein the variables have the meaning defined in the specification.Type: ApplicationFiled: February 26, 2008Publication date: April 29, 2010Applicant: ALLERGAN, INC.Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Patent number: 7696205Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: October 16, 2007Date of Patent: April 13, 2010Assignee: Bristol-Myers Squibb CompanyInventor: Robert J. Cherney
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Publication number: 20100087438Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, R4, R5, X1, and j are defined herein. The compounds are useful as potassium ion channel inhibitors.Type: ApplicationFiled: August 31, 2009Publication date: April 8, 2010Applicant: Xention LimitedInventors: Richard John HAMLYN, Mushtaq Mulla, Derek Edward John, Simon Mark Jones, Basil Hartzoulakis, David Madge, John Ford
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Patent number: 7691849Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions comprising the same, and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: GrantFiled: October 30, 2007Date of Patent: April 6, 2010Assignee: CytRx CorporationInventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
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Publication number: 20100063027Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n— wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.Type: ApplicationFiled: April 25, 2007Publication date: March 11, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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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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Publication number: 20100041658Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.Type: ApplicationFiled: April 16, 2007Publication date: February 18, 2010Inventors: Alexis Denis, Vincent Gerusz, Yannick Bonvin
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Publication number: 20090215775Abstract: Compounds of formula (I) are disclosed for treatment of cancer.Type: ApplicationFiled: May 16, 2006Publication date: August 27, 2009Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
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Publication number: 20090203666Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: May 4, 2007Publication date: August 13, 2009Applicant: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
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Publication number: 20090143386Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
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Publication number: 20090137593Abstract: A 4-amino-2,6-dimethylphenol compound having the formula given in the description, acid-addition salts thereof, a process for preparing them, pharmaceutical composition comprising them and its use as anti-pyretic and anti-nociceptive agents.Type: ApplicationFiled: March 30, 2007Publication date: May 28, 2009Applicant: AZIEN CHIM RIUNITE ANGEL FRANC A.C.R.A.F. S.P.A.Inventor: Beatrice GARRONE
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Publication number: 20090118291Abstract: This invention relates to hydroxamic acid derivatives having a carbamate linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.Type: ApplicationFiled: August 22, 2005Publication date: May 7, 2009Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
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Publication number: 20090105259Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors.Type: ApplicationFiled: September 8, 2006Publication date: April 23, 2009Inventors: Jae U. Jeong, Robert W. Marquis
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Publication number: 20090054439Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R, R? and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.Type: ApplicationFiled: July 31, 2008Publication date: February 26, 2009Applicant: SANOFI-AVENTISInventors: Gilles COURTEMANCHE, Pierre DESPEYROUX, Evelyne FONTAINE, Pierrick ROCHARD, Claudine SERRADEIL-LE GAL, Erich Von Roedern
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Publication number: 20090023735Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is selected from a group consisting of dialkylamino, NO2, CN, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, oxazol-2-yl, oxazolylaminocarbonyl, aryl, aroyl, aryl-CH(OH)—, arylaminocarbonyl, furanyl, where the aryl, aroyl and furanyl moieties may be substituted, guanidinyl-(CH2)z—N(R?)—, Het-(CH2)z—N(R?)—, Het-CO—N(R?)—, Het-CH(OH)— and Het-CO—, where Het is an optionally substituted 4-6-membered heterocyclic ring containing one or more heteroatoms sleeted from N, S and O, R? is hydrogen or alkyl, and z is an integer 1 to 5; RA is a group of formula (A), (B), (C) or (D) as defined in the claims; and RB is hydrogen, alkyl, alkanoyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminoalkyl, mono- or dialkylaminoalkyl or Het-alkyl, where Het is as defined above.Type: ApplicationFiled: September 15, 2006Publication date: January 22, 2009Inventors: Jyrki Heino, Mark Johnson, Jarmo Kapyla, Anne Marjamaki, Tommi Nyronen, Marika Ojala, Olli Pentikainen, Marjo Pihlavisto, Liisa Nissinen
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Publication number: 20090023736Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 28, 2008Publication date: January 22, 2009Applicant: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Weiwen Ying, Teresa Przewloka, Lijun Sun
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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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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Publication number: 20080287442Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: ApplicationFiled: January 11, 2007Publication date: November 20, 2008Applicant: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Publication number: 20080207620Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: February 22, 2008Publication date: August 28, 2008Inventors: Manoj C. Desai, Allen Y. Hong, Hon C. Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20080161307Abstract: A method for the treatment of delayed gastric emptying, in a patient in need of such treatment, which comprises administering an effective amount of a 5-HT4 agonist, e.g. tegaserod or salts or hydrates thereof, to the patient.Type: ApplicationFiled: January 27, 2006Publication date: July 3, 2008Inventors: David Lewis Earnest, Mikhail Rojavin, Gervais Tougas
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Patent number: 7361655Abstract: The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.Type: GrantFiled: July 12, 2004Date of Patent: April 22, 2008Assignee: CytRx CorporationInventors: Zita Jegesné Csákai, Ede Márványos, László Ürögdi, Magdolna Bathóné Török, László Dénes
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Patent number: 7348324Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Type: GrantFiled: October 18, 2002Date of Patent: March 25, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Imamura, Shohei Hashiguchi, Taeko Hattori, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba, Yoshihiro Sugihara
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Patent number: 7345095Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: October 6, 2006Date of Patent: March 18, 2008Assignee: Pfizer IncInventors: Michael A. Brodney, Karen J. Coffman
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Patent number: 7265220Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.Type: GrantFiled: February 17, 2003Date of Patent: September 4, 2007Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7169783Abstract: The invention relates to an antagonist of one or more of Rho family members having ability to elicit neurite outgrowth from cultured neurons in an assay method which includes culturing neurons on a substrate that incorporates a growth-inhibiting amount of Rho family member and exposing the cultured neurons to a candidate Rho family member antagonist agent to permit neuron growth. Candidates which elicit neurite outgrowth from the cultured neurons are thus identified as Rho family antagonists.Type: GrantFiled: December 17, 2001Date of Patent: January 30, 2007Assignee: Universite de MontrealInventors: Lisa McKerracher, Maxime Lehmann
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Patent number: 7163942Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: January 16, 2007Assignee: Pfizer Inc.Inventors: Michael A. Brodney, Karen J. Coffman
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Patent number: 7045521Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: November 12, 2003Date of Patent: May 16, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Robert Cherney
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Patent number: 7045551Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said aryl hydroxyethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: May 16, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Qiang Sun, Huan He, Alexandre L'Heureux
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Patent number: 6998400Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or tobacco products, seasonal affective disorder, chronic fatigue, narcolepsy or cognitive impairment using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: February 14, 2006Assignee: Smithkline Beecham CorporationInventors: John A. Ascher, Joseph Andrews Johnston, Susan Marie Learned-Coughlin, Alan Bye
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Patent number: 6995283Abstract: The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.Type: GrantFiled: February 28, 2002Date of Patent: February 7, 2006Assignee: SmithKline Beecham CorporationInventor: Joseph Howing Chan
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Patent number: 6953797Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: February 20, 2001Date of Patent: October 11, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Ian Millichip
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Patent number: 6887903Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.Type: GrantFiled: October 14, 1999Date of Patent: May 3, 2005Assignee: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
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Patent number: 6875765Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.Type: GrantFiled: May 10, 2002Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
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Patent number: 6875764Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.Type: GrantFiled: October 27, 2000Date of Patent: April 5, 2005Assignee: New Pharma Research Sweden ABInventors: Sabrina Muzi, Shoaá Abdul Rahman
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Patent number: 6869951Abstract: The present invention provides a matrix metalloproteinase inhibiting compound having structure (VIII) or a salt, an enantiomer, a diastereomer, a racemate, or a tautomer thereof. In other embodiments, the present invention provides a method of changing the conformation of a matrix metalloproteinase, a method of inhibiting a matrix metal metalloproteinase, and a method of treating osteoarthritis.Type: GrantFiled: July 12, 2000Date of Patent: March 22, 2005Assignee: Pharmacia CorporationInventors: William C. Stallings, Huey S. Shieh, Susan C. Howard, Gary A. DeCrescenzo, Joseph J. McDonald
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Patent number: 6818765Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.Type: GrantFiled: October 16, 2001Date of Patent: November 16, 2004Assignee: Universite de LiegeInventors: Jacques Delarge, Jean-Michel Dogne, Bernard Masereel
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Patent number: RE39593Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 17, 2003Date of Patent: April 24, 2007Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs