The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
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Patent number: 7375219Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: April 13, 2006Date of Patent: May 20, 2008Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20080064691Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.Type: ApplicationFiled: August 4, 2004Publication date: March 13, 2008Applicant: AstraZeneca ABInventors: Alan Martin Birch, Stuart Norman Lile Bennett, Andrew Duncan Campbell, Iain Simpson, Paul Robert Owen Whittamore, David Paul Whalley, Linda Godfrey
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Patent number: 7342041Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 11, 2008Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
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Patent number: 7256188Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity.Type: GrantFiled: May 8, 2002Date of Patent: August 14, 2007Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20070173500Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: January 23, 2007Publication date: July 26, 2007Applicant: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
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Patent number: 7208491Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.Type: GrantFiled: February 3, 2004Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 7205330Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: April 17, 2007Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Patent number: 7192957Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 20, 2007Assignee: Schering CorporationInventors: Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanli Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7176200Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain themType: GrantFiled: September 3, 2004Date of Patent: February 13, 2007Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 7173027Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.Type: GrantFiled: January 29, 2002Date of Patent: February 6, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Hongfeng Deng
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7173057Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: February 6, 2007Assignee: Schering CorporationInventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7141568Abstract: Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: July 1, 2004Date of Patent: November 28, 2006Assignee: Pfizer Italia S.r.l.Inventors: Daniele Fancelli, Barbara Forte, Jürgen Moll, Mario Varasi, Paola Vianello
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Patent number: 7105516Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.Type: GrantFiled: September 15, 2003Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
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Patent number: 7101877Abstract: 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: September 29, 2003Date of Patent: September 5, 2006Assignee: 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: 7091220Abstract: The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same.Type: GrantFiled: December 20, 2000Date of Patent: August 15, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Patent number: 7049314Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.Type: GrantFiled: September 15, 2003Date of Patent: May 23, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, Jeffrey A. Deskus, John E. Macor, Ronald J. Mattson, Zhaoxing Meng, Charles P. Sloan
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Patent number: 7041235Abstract: The present invention relates to fluorescent diketopyrrolopyrrole analogues of the general formula (I), wherein A1 and A2 are C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, C5–C8cycloalkyl, C5–C8cycloalkenyl, aryl or heteroaryl, A3 and A4 are independently of each other C1–C18alkyl, Ar3, —CR30R31—(CH2)m—Ar3, or Y—R32, wherein R30 and R31 independently of each other stand for hydrogen or C1–C4alkyl, or phenyl which can be substituted up to three times with C1–C3alkyl, Ar3 stands for aryl, in particular phenyl or 1- or 2-naphthyl, C5–C8cycloalkyl, in particular cyclohexyl, or heteroaryl, which can be substituted one to three times with C1–C8alkyl, C1–C8alkoxy, halogen or phenyl, which can be substituted with C1–C8alkyl or C1–C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, Y is C(O)— or SO2— and R32 is C1–C18alkyl, Ar3, or aralkyl and A3 can additionally be hydrogen, C1–C8alkyloxycarbonyl, such as tertbutoxycarbonyl, or aralkyloxycarbonyl, such as benzyloxycarbonyl, a process for their preparation andType: GrantFiled: August 1, 2002Date of Patent: May 9, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Colin Morton, David Macdonald Smith, Abul Iqbal
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Patent number: 6849622Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Publication number: 20040266762Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.Type: ApplicationFiled: June 2, 2004Publication date: December 30, 2004Inventor: Matthias Gerlach
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Publication number: 20040235833Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: March 12, 2004Publication date: November 25, 2004Applicant: Pfizer IncInventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
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Publication number: 20040220183Abstract: The invention relates to new hydroxyindoles of the Formula, 1Type: ApplicationFiled: May 27, 2004Publication date: November 4, 2004Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Publication number: 20040214820Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.Type: ApplicationFiled: December 31, 2003Publication date: October 28, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GmbHInventors: Heinz-Werner Kleemann, Jean-Christophe Carry, Pascal Desmazeau, Serge Mignani, Jean Bouoquerel, Arielle Genevois-Borella, Baptiste Ronan
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Patent number: 6809098Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: GrantFiled: August 21, 2002Date of Patent: October 26, 2004Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20040209867Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: ApplicationFiled: April 20, 2004Publication date: October 21, 2004Applicant: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Publication number: 20040204407Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: March 8, 2004Publication date: October 14, 2004Applicant: SUGEN Inc.Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
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Patent number: 6797708Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 28, 2004Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Publication number: 20040180888Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.Type: ApplicationFiled: March 22, 2004Publication date: September 16, 2004Applicant: IDENIX PHARMACEUTICALS INC.Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
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Publication number: 20040173777Abstract: The present invention relates to fluorescent diketopyrrolopyrrole analogues of the general formula (I), wherein A1 and A2 are C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C5-C8cycloalkyl, C5-C8cycloalkenyl, aryl or heteroaryl, A3 and A4 are independently of each other C1-C18alkyl, Ar3, —CR30R31—(CH2)m—Ar3, or Y-R32, wherein R30 and R31 independently of each other stand for hydrogen or C1-C4alkyl, or phenyl which can be substituted up to three times with C1-C3alkyl, Ar3 stands for aryl, in particular phenyl or 1- or 2-naphthyl, C5-C8cycloalkyl, in particular cyclohexyl, or heteroaryl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, halogen or phenyl, which can be substituted with C1-C8alkyl or C1-C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, Y is C(O)— or SO2— and R32 is C1-C18alkyl, Ar3, or aralkyl and A3 can additionally be hydrogen, C1-C8alkyloxycarbonyl, such as tertbutoxycarbonyl, or aralkyloxycarbonyl, such as benzyloxycarbonyl, a proType: ApplicationFiled: February 4, 2004Publication date: September 9, 2004Inventors: Colin Morton, David MacDonald Smith, Abdul Iqbal
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Patent number: 6787651Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.Type: GrantFiled: October 9, 2001Date of Patent: September 7, 2004Assignee: SmithKline Beecham CorporationInventors: Andreas Stolle, Jacques P. Dumas, William Carley, Philip D. G. Coish, Steven R. Magnuson, Yamin Wang, Dhanapalan Nagarathnam, Derek B. Lowe, Ning Su, William H. Bullock, Ann-Marie Campbell, Ning Qi, Jeremy L. Baryza, James H. Cook
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Publication number: 20040157841Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1Type: ApplicationFiled: February 3, 2004Publication date: August 12, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 6774233Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: August 10, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6759428Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 2, 2003Date of Patent: July 6, 2004Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
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Patent number: 6753327Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.Type: GrantFiled: October 11, 2000Date of Patent: June 22, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Publication number: 20040087584Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs.Type: ApplicationFiled: July 18, 2003Publication date: May 6, 2004Applicant: MEMORY PHARMACEUTICALS CORP.Inventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
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Patent number: 6730671Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.Type: GrantFiled: February 13, 2003Date of Patent: May 4, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20040077851Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.Type: ApplicationFiled: July 25, 2003Publication date: April 22, 2004Inventors: Alexandros Makriyannis, Hongfeng Deng
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Publication number: 20040067939Abstract: The present invention provides glucokinase activators of formula I: 1Type: ApplicationFiled: September 30, 2003Publication date: April 8, 2004Inventor: Wendy Lea Corbett
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Patent number: 6716837Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c aType: GrantFiled: November 13, 2000Date of Patent: April 6, 2004Assignee: NPS Allelix Biopharmaceuticals, Inc.Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
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Publication number: 20040063939Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventors: Hans-Joachim Jansch, Helge Hartenhauer, Hans Stange, Norbert Hofgen, Jurgen Schafer
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Patent number: 6710068Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.Type: GrantFiled: April 11, 2002Date of Patent: March 23, 2004Assignee: Idenix Pharmaceuticals, Inc.Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
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Patent number: 6706709Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: June 4, 2001Date of Patent: March 16, 2004Assignee: Sugen, Inc.Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
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Publication number: 20040048858Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula 1Type: ApplicationFiled: December 19, 2002Publication date: March 11, 2004Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten, Kimberly J. Worsencroft, Liming Ni
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Patent number: 6699862Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&mType: GrantFiled: March 24, 2000Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
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Publication number: 20040030131Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.Type: ApplicationFiled: September 3, 2003Publication date: February 12, 2004Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
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Publication number: 20040029858Abstract: 2-(III-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.Type: ApplicationFiled: July 10, 2003Publication date: February 12, 2004Inventors: Ernesto Menta, Nicoletta Pescalli
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Publication number: 20040019207Abstract: The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitrType: ApplicationFiled: July 17, 2003Publication date: January 29, 2004Applicant: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldback Nielsen, Elsebet Ostergaard Nielsen
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Publication number: 20040002495Abstract: A compound of formula I 1Type: ApplicationFiled: May 19, 2003Publication date: January 1, 2004Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth