Chalcogen Or Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/379.4)
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Patent number: 7608718Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: November 3, 2005Date of Patent: October 27, 2009Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnoldus H. J. Herremans
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Publication number: 20090215624Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: October 20, 2006Publication date: August 27, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen
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Patent number: 7528162Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: September 17, 2002Date of Patent: May 5, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Jacobus Tipker, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
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Publication number: 20090082396Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Inventors: Josephus H.M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Publication number: 20090042966Abstract: The present invention relates to fluorinated dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: April 3, 2006Publication date: February 12, 2009Inventors: Paul J. Coleman, Christopher D. Cox
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Patent number: 7482470Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: GrantFiled: May 7, 2007Date of Patent: January 27, 2009Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert John Chorvat
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Publication number: 20080312276Abstract: The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: June 11, 2008Publication date: December 18, 2008Inventors: Josephus H.M. Lange, Hendrik C. Wals, Bernard J. Vliet Van, Mahmut Yildirim
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Patent number: 7465809Abstract: The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: October 25, 2005Date of Patent: December 16, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Xiaojie Li, Zhihua Sui
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Publication number: 20080249095Abstract: Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: July 18, 2006Publication date: October 9, 2008Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
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Publication number: 20080207637Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: ApplicationFiled: February 14, 2005Publication date: August 28, 2008Inventors: Rosa Cuberes Altisen, Bonifacio Gutierrez Silva, Jordi Frigola- Constansa
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Publication number: 20080194582Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: March 10, 2006Publication date: August 14, 2008Inventors: Paul J. Coleman, Christopher D. Cox, George D. Hartman
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Publication number: 20080188442Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: July 17, 2006Publication date: August 7, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Clemens Lamberth, Camilla Corsi, Josef Ehrenfreund, Hans Tobler, Harald Walter
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Patent number: 7407972Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: December 20, 2004Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Jeremy John Edmunds
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Patent number: 7320995Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.Type: GrantFiled: July 31, 2003Date of Patent: January 22, 2008Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Jose Eugenio De Diego Gomez, Alfonso De Dios, Chafiq Hamdouchi Hamdouchi, Tiecho Li, Beatriz Lopez De Uralde Garmendia, Michal Vieth, Jeremy Schulenberg York, Robert Dean Dally, Miriam Filadelfa Del Prado Catalina, Carlos Jaramillo Aguado, Luisa Maria Martin-Cabrejas, Carlos Montero Salgado, Sheila Pleite Selgas, Concepcion Sanchez-Martinez, Timothy Alan Shepherd, James Howard Wikel
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Publication number: 20080015198Abstract: The present invention relates to substitute pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: February 16, 2005Publication date: January 17, 2008Applicant: LABORATORIOS DEL DR.ESTEVE S.A.Inventor: Rosa Cuberes Altisen
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Publication number: 20070259934Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: May 7, 2007Publication date: November 8, 2007Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert John Chorvat
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Patent number: 7262223Abstract: The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound.Type: GrantFiled: January 23, 2004Date of Patent: August 28, 2007Assignee: Neurochem (International) LimitedInventors: Xianqi Kong, Xinfu Wu, David Migneault
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Patent number: 6974810Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification.Type: GrantFiled: September 17, 2002Date of Patent: December 13, 2005Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnoldus H. J. Herremans
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Patent number: 6965032Abstract: This invention relates to a compound of Formula I, a method for its preparation and its use in the preparation of a compound of Formula II wherein R1, R2, R3, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R6, R7, R8 and n are as defined in the disclosure. Also disclosed are certain intermediates of Formula 4 for the preparation of compounds of Formula I wherein X is N and R2, R3 and n are as defined in the disclosure.Type: GrantFiled: August 13, 2002Date of Patent: November 15, 2005Assignee: E. I. du Pont de Nemours and CompanyInventor: John Herbert Freudenberger
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Patent number: 6958403Abstract: Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (?)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chType: GrantFiled: December 8, 2004Date of Patent: October 25, 2005Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Montserrat Alcon-Marrugat, Miguel Angel Pericas-Brondo, Maria Rosa Cuberes-Altisen, Jordi Frigola-Constansa
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Patent number: 6852750Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnostic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.Type: GrantFiled: June 21, 2002Date of Patent: February 8, 2005Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Takashi Tsukamoto, Barbara S. Slusher, Eric Wang
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Patent number: 6846935Abstract: Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomeric ally pure compounds (?)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl cType: GrantFiled: June 6, 2002Date of Patent: January 25, 2005Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Montserrat Alcon-Marruga, Miguel Angel Pericas-Brondo, Maria Rosa Cuberes-Altisen, Jordi Frigola-Constansa
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Publication number: 20040248944Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazo, derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: ApplicationFiled: March 22, 2004Publication date: December 9, 2004Inventors: Cornelis G Kruse, Josephus H. M. Lange, Jacobus Tipker, Arnoldus H.J. Herremans, Herman H. Van Stuivenberg
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Publication number: 20040106800Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: ApplicationFiled: September 24, 2003Publication date: June 3, 2004Inventors: Josephus H.M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnolds H.J. Herremans
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Publication number: 20040102496Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.Type: ApplicationFiled: November 5, 2003Publication date: May 27, 2004Inventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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Publication number: 20040067983Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators.Type: ApplicationFiled: July 2, 2003Publication date: April 8, 2004Inventors: Terrance D. Barrett, J. Guy Breitenbucher, Laurent Gomez, Michael D. Hack, Liming Huang, Kelly J. McClure, Magda F. Morton, Clark A. Sehon, Nigel P. Shankley
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Publication number: 20040014801Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.Type: ApplicationFiled: May 8, 2003Publication date: January 22, 2004Applicant: The Regents of the University of CaliforniaInventors: Fred E. Cohen, Xiaohui Du, Chun Guo, James H. McKerrow
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Patent number: 6573287Abstract: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where n is 0 or 1; X is H or CN; Y is N, NH or O; Z is CH2 when Y is O or N—H, with Y—Z forming a single bond, and Z is CH when Y is N, with Y—Z forming a double bond; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.Type: GrantFiled: March 26, 2002Date of Patent: June 3, 2003Assignee: Bristo-Myers Squibb CompanyInventors: Richard B. Sulsky, Jeffrey A. Robl
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Publication number: 20030100585Abstract: The present invention is directed to a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.Type: ApplicationFiled: June 12, 2002Publication date: May 29, 2003Inventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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Patent number: 6476060Abstract: The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor. The compounds have the formula (I) wherein R and R1 are the same or different and represent unsubstituted or substituted phenyl, thienyl, or pyridyl, or naphthyl. naphthyl R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v) as defined herein, Bb represents sulfonyl or carbonyl, and R3 represents benzyl, phenyl, thienyl or pyridyl, each of which is unsubstituted or substituted, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphthyl.Type: GrantFiled: March 23, 2001Date of Patent: November 5, 2002Assignee: Solvay Pharmaceuticals, B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Bernard J. Van Vliet
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Publication number: 20020115860Abstract: Compositions and methods are described for hydrating terminal alkynes catalytically in anti-Markovnikov fashion. The compositions comprise a transition metal complex including at least one organic ligand having at least two heteroatoms, wherein the heteroatoms are directly bonded or located one atom away. Preferably, at least one of the heteroatoms is nitrogen, which is typically provided as part of a heterocyclic ring. Other preferred heteroatoms include S, P, N, As or Se. A particularly preferred catalyst employs a P-linked imidazole ligand bound to Ru. Such complexes have a controlled adaptable proton transfer ability and/or a hydrogen bonding ability making them particularly useful as chemical reaction facilitators.Type: ApplicationFiled: February 16, 2001Publication date: August 22, 2002Applicant: San Diego State University FoundationInventor: Douglas Byran Grotjahn
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Publication number: 20020103381Abstract: The present invention provides a method for the synthesis of compounds of Formula I: 1Type: ApplicationFiled: November 30, 2000Publication date: August 1, 2002Inventor: Armen M. Boldi
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Patent number: 6353117Abstract: The present invention relates to new pyazoline derivatives of formula and to physiologically acceptable salts thereof, to the method for their preparation and to their application as medicaments.Type: GrantFiled: November 28, 2000Date of Patent: March 5, 2002Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: María Rosa Cuberes-Altisent, Juana María Berrocal-Romero, María Montserrat Contijoch-Llobet, Jordi Frigola-Constansa
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Patent number: 6242609Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.Type: GrantFiled: April 7, 1999Date of Patent: June 5, 2001Assignee: Konica CorporationInventor: Fumio Ishii
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Publication number: 20010000179Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: 1Type: ApplicationFiled: December 1, 2000Publication date: April 5, 2001Inventor: Donald J. Pinto
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Patent number: 6184243Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked ureas and carbamates of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: October 2, 1998Date of Patent: February 6, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li, Wei Huang
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Patent number: RE38963Abstract: The present invention relates to new pyazoline derivatives of formula and to physiologically acceptable salts thereof, to the method for their preparation and to their application as medicaments.Type: GrantFiled: May 27, 1999Date of Patent: January 31, 2006Assignee: Laboratorios del Dr. EsteveInventors: Maria Rosa Cuberes-Altisent, Juana Maria Berrocal-Romero, Maria Montserrat-Contijoch-Llobet, Jordi Frigola-Constansa