Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/371.4)
  • Publication number: 20100273841
    Abstract: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): 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: Application
    Filed: April 23, 2010
    Publication date: October 28, 2010
    Applicant: Shionogi & Co., Ltd.
    Inventors: Takayuki OKUNO, Masahiro SAKAGAMI
  • Publication number: 20100249191
    Abstract: Novel isoxazolines of the formula (I) wherein A represents C or N; R represents haloalkyl; X represents halogen or haloalkyl; l represents 0, 1 or 2; Y represents halogen, alkyl, alkoxy, haloalkyl, cyano, nitro, amino, acylamino, alkoxycarbonylamino, haloalkoxycarbonyl-amino or alkylsulfonylamino; m represents 0, 1 or 2; and G represents any one selected from heterocyclic groups described in the specification; and intermediates, and a use thereof as insecticides and/or for controlling animal parasites.
    Type: Application
    Filed: August 1, 2007
    Publication date: September 30, 2010
    Applicant: Bayer Cropscience SA
    Inventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Philippe Desbordes, Pierre Genix, Benoit Hartmann, Amos Mattes, Klaus Kunz, Rudiger Fischer, Oliver Gaertzen, Oswald Ort, Darren Mansfield, Alain Villier
  • Publication number: 20100190777
    Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.
    Type: Application
    Filed: July 16, 2008
    Publication date: July 29, 2010
    Applicant: PLEXXIKON INC.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Patent number: 7759382
    Abstract: This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity, and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: July 20, 2010
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jay S. Tung, Lee H. Latimer, Jing Wu, Albert Garofalo, Michael A. Pleiss, Darren Dressen, Ashley Guinn, Scott A. Jenkins, Jennifer Sealy, John Tucker, David W. G. Wone
  • Patent number: 7737151
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: June 15, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Julian M. C. Golec
  • Publication number: 20100099681
    Abstract: The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases.
    Type: Application
    Filed: August 13, 2009
    Publication date: April 22, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Bärfacker, Raimund Kast, Nils Griebenow, Heinrich Meier, Peter Kolkhof, Barbara Albrecht-Küpper, Adam Nitsche, Nicole Teusch, Johannes-Peter Stasch, Dirk Schneider
  • Patent number: 7687533
    Abstract: The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R1-R5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: March 30, 2010
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Douglas James Critcher, Nigel Derek Arthur Walshe, Christelle Lauret
  • Patent number: 7671072
    Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereof in the treatment of, inter alia, conditions, diseases, and symptoms including, inter alia, Alzheimer's Disease, cancer, dementia, depression, diabetes, hair loss, schizophrenia, and stroke.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: March 2, 2010
    Assignee: Pfizer Inc.
    Inventors: John W. Benbow, Daniel W. Kung
  • Publication number: 20100041720
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein Y, X1, X2, X3, R1, and R2 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: August 11, 2009
    Publication date: February 18, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Steven P. Latshaw, Bo Liu, Meena V. Patel, Arturo Perez-Medrano, Xueqing Wang
  • Publication number: 20090239841
    Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
    Type: Application
    Filed: October 24, 2005
    Publication date: September 24, 2009
    Inventors: Alan J. Hutchison, Jun Yuan
  • Publication number: 20090227648
    Abstract: This invention relates to novel compounds having the formula and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
    Type: Application
    Filed: April 20, 2005
    Publication date: September 10, 2009
    Inventors: Paul Lyne, Bin Wang
  • Publication number: 20090221838
    Abstract: The invention relates to an alternative process for the preparation of substituted 5-amino-pyrazoles, in which a carbonyl compound is reacted with a hydrazine derivative and cyanogen chloride to give an N-cyanohydrazone which is cyclized in the presence of a strong base.
    Type: Application
    Filed: August 18, 2006
    Publication date: September 3, 2009
    Inventors: Meinrad Brenner, Hans Williner
  • Patent number: 7538135
    Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
    Type: Grant
    Filed: July 7, 2004
    Date of Patent: May 26, 2009
    Assignee: Novartis AG
    Inventor: Thalaththani Ralalage Vedananda
  • Patent number: 7479357
    Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.
    Type: Grant
    Filed: September 13, 2002
    Date of Patent: January 20, 2009
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
  • Publication number: 20090012075
    Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 8, 2007
    Publication date: January 8, 2009
    Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Patent number: 7455698
    Abstract: 4-(Pyrazol-4-ylimino)-2,5-cyclohexadienylidene-ammonium salts of the general formula(I) and colorants comprising these compounds for keratin fibres.
    Type: Grant
    Filed: April 4, 2005
    Date of Patent: November 25, 2008
    Assignee: Wella AG
    Inventors: Laurent Chassot, Laurence Descloux, Sylviane Oberson, Gisela Umbricht, Hans-Juergen Braun
  • Publication number: 20080280874
    Abstract: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.
    Type: Application
    Filed: October 11, 2005
    Publication date: November 13, 2008
    Inventors: Craig Johnstone, Darren Mckerrecher, Kurt Gordon Pike, Michael James Waring
  • Patent number: 7439366
    Abstract: The present invention relates to a phenacylamine derivative of the formula (I) or a salt thereof: wherein A is alkyl, cycloalkyl, phenyl which may be substituted by Y, pyridyl which may be substituted by Y, or pyrazolyl which may be substituted by Y, R1 and R2 are each alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbocycle, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl or COR4, X is halogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkenyloxy, haloalkenyloxy, alkynyloxy, haloalkynyloxy, alkylthio, haloalkylthio, alkenylthio, haloalkenylthio, alkynylthio, haloalkynylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, dialkylaminosulfonyl, nitro, cyano, phenyl which may be substituted by Y, phenoxy which may be substituted by Y, benzyloxy which may be substituted by Y, or pyridyloxy which may be substituted by Y, and n is an integer of from 0 to 5.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: October 21, 2008
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Yuji Nakamura, Masayuki Morita, Kenji Izakura
  • Publication number: 20080249154
    Abstract: A compound represented by formula (I) (wherein ring A is a nitrogen-containing ring which may have a substituent(s), E is a binding bond or a spacer of which main chain has an atom number of 1-8, Q is a hydrogen atom, a hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s).), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. Since the compounds of the present invention represented by formula (I), a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof have the affinity to MBR, they are useful for the prevention and/or treatment for disease caused by stress.
    Type: Application
    Filed: December 24, 2004
    Publication date: October 9, 2008
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki Ohmoto, Masashi Kato, Seishi Katsumata, Junichiro Manako
  • Patent number: 7335779
    Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: February 26, 2008
    Assignee: Quonova, LLC
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20080036373
    Abstract: A platinum complex represented by the general formula (1) below, useful as a phosphorescence emission material, a tetradentate ligand useful for synthesizing the platinum complex, and a light-emitting device containing at least one of the platinum complex. wherein ring B represents a nitrogen-containing aromatic heterocyclic ring; rings A, C and D each independently represent an aromatic or aromatic heterocyclic ring, while either of the rings C and D represents five-membered ring, the other represents a five- or six-membered ring; RA, RB, RC, and RD respectively represent substituents on the rings A, B, C, and D; two of XA, XB, XC, and XD represent a nitrogen atom that may be bound with the platinum atom by a coordinate bond, the others each independently represent a carbon atom or nitrogen atom that may be bound with the platinum atom by a covalent bond; Q represents a bivalent atom or atomic group bridging the rings B and C; and YC and YD each independently represent a carbon atom or nitrogen atom.
    Type: Application
    Filed: August 8, 2007
    Publication date: February 14, 2008
    Inventors: Hisanori Itoh, Takeshi Iwata, Yoshimasa Matsushima
  • Patent number: 7317024
    Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: January 8, 2008
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Bingwei V. Yang
  • Patent number: 7307097
    Abstract: Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: December 11, 2007
    Assignee: SmithKline Beechman Corporation
    Inventors: Jerry Leroy Adams, Jiri Kasparec, Domingos J. Silva
  • Patent number: 7303592
    Abstract: Hair dyeing compositions are provided which comprise at least one coupler selected from N-aryl-m-phenylenediamine derivatives, 2-substituted N-aryl-m-phenylenediamine derivatives, and N-aryl-m-diaminopyridine derivatives, in combination with and at least one diaminopyrazole primary intermediate.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: December 4, 2007
    Assignee: The Procter & Gamble Company
    Inventors: Mu'lll Lim, Guiru Zhang, Bryan Patrick Murphy
  • Patent number: 7268235
    Abstract: A method for the preparation of N-pyrazolylamidoximes of the general formula I R1 and R2 independently represent an alkyl, aryl, or heteroaryl group, comprises reacting a 5-(?-ketoalkyl)-3-substituted-1,2,4-oxadiazoles of the general formula II with hydrazine.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: September 11, 2007
    Assignee: Eastman Kodak Company
    Inventors: Francesco DeBellis, Alice J. Kim, legal representative, Chang-Kyu Kim, deceased
  • Patent number: 7262223
    Abstract: 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: Grant
    Filed: January 23, 2004
    Date of Patent: August 28, 2007
    Assignee: Neurochem (International) Limited
    Inventors: Xianqi Kong, Xinfu Wu, David Migneault
  • Patent number: 7183306
    Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: February 27, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
  • Patent number: 7037880
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: May 2, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 6989402
    Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: January 24, 2006
    Assignee: Karo Bio AB
    Inventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
  • Patent number: 6974829
    Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Grant
    Filed: May 7, 2003
    Date of Patent: December 13, 2005
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
  • Patent number: 6956055
    Abstract: The invention relates to substituted ?-lactone compounds, to methods for the production thereof, to medicaments containing these compounds and to the use of these compounds for producing medicaments.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: October 18, 2005
    Assignee: Grunenthal GmbH
    Inventors: Corinna Sundermann, Michael Przewosny, Werner Englberger
  • Patent number: 6949578
    Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.
    Type: Grant
    Filed: July 14, 2004
    Date of Patent: September 27, 2005
    Assignee: Pharmacia Corporation
    Inventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
  • Patent number: 6894173
    Abstract: 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: Grant
    Filed: February 10, 2003
    Date of Patent: May 17, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • Patent number: 6887280
    Abstract: Novel compositions for use in oxidative hair coloring compositions are provided. The compositions comprise one or more oxidative hair coloring N-aryl-m-phenyldiamine derivatives as couplers and one or more diaminopyrazole primary intermediates in combination.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: May 3, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan, Sabina Burdzovic
  • Patent number: 6858639
    Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): ? (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: February 22, 2005
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
  • Patent number: 6818775
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: December 9, 2003
    Date of Patent: November 16, 2004
    Assignee: Allergan, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Publication number: 20040220232
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Application
    Filed: February 14, 2004
    Publication date: November 4, 2004
    Inventors: David L. Brown, Matthew J. Graneto, Susan J. Hartmann, Suzanne Metz, Michael A. Stealey, John J. Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu
  • Publication number: 20040127526
    Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1
    Type: Application
    Filed: December 10, 2003
    Publication date: July 1, 2004
    Applicant: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: 6706920
    Abstract: An antistatic composition comprises (a) at least one ionic salt consisting of a nonpolymeric nitrogen onium cation and a weakly coordinating fluoroorganic anion, the conjugate acid of the anion being a superacid; and (b) at least one thermoplastic polymer. The composition exhibits good antistatic performance over a wide range of humidity levels.
    Type: Grant
    Filed: December 28, 2001
    Date of Patent: March 16, 2004
    Assignee: 3M Innovative Properties Company
    Inventors: William M. Lamanna, Thomas P. Klun, Kathleen A. Hachey, Alan D. Fanta
  • Patent number: 6686318
    Abstract: The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R1, R2, R3, R4 and Z have the meanings given in the description, to a process for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: February 3, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Kurt Findeisen, Joachim Kluth, Karl-Heinz Linker, Klaus-Helmut Müller, Otto Schallner, Markus Dollinger
  • Publication number: 20040010023
    Abstract: The invention relates to novel biphenyl derivatives of the general formula (I), wherein R4 represents an aromatic heterocycle, and to the physiologically acceptable salts or solvates thereof. The inventive compounds are integrin inhibitors and are used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections and restenosis following angioplasty or for pathological processes that are maintained or propagated by angiogenesis.
    Type: Application
    Filed: February 21, 2003
    Publication date: January 15, 2004
    Inventors: Wolfgang Stahle, Gunter Holzemann, Simon Goodman
  • Patent number: 6673956
    Abstract: The present invention relates to processes for the preparation of a compound of the formula wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: January 6, 2004
    Assignee: Aventis Agriculture Ltd.
    Inventor: Jean-Erick Ancel
  • Patent number: 6664247
    Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: December 16, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • Patent number: 6660046
    Abstract: The invention concerns novel pyrazole derivatives comprising at least a cationic group Z, Z being selected among the quaternized aliphatic chains, aliphatic chains comprising at least a saturated quaternized cycle, and aliphatic chains comprising at least an unsaturated quaternized cycle, their use as oxidation base for dyeing keratin fibres, dyeing compositions containing them, and dyeing methods using them.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 9, 2003
    Assignee: L'Oreal S.A.
    Inventors: Eric Terranova, Alain Lagrange
  • Patent number: 6653483
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: November 25, 2003
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 6653300
    Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
  • Patent number: 6645258
    Abstract: The invention relates to novel compositions for the oxidation dyeing of keratin fibers, comprising at least one specific diaminopyrazole derivative, to the dyeing process using this composition, to novel diaminopyrazole derivatives and to a process for their preparation.
    Type: Grant
    Filed: October 18, 2001
    Date of Patent: November 11, 2003
    Assignee: L'Oreal, S.A.
    Inventors: Laurent Vidal, Agnès Burande, Gérard Malle, Michel Hocquaux
  • Publication number: 20030187235
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: December 9, 2002
    Publication date: October 2, 2003
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Publication number: 20030186982
    Abstract: Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): 1
    Type: Application
    Filed: November 6, 2002
    Publication date: October 2, 2003
    Inventors: Jollie Duaine Godfrey, John Hynes, Alaric J. Dyckman, Katerina Leftheris, Zhongping Shi, Stephen T. Wrobleski, Wendel William Doubleday, John A. Grosso
  • Patent number: 6617342
    Abstract: This invention provides compounds and their pharmaceutically acceptable salts, pharmaceutical formulation of said compounds and methods for treating hyperglycemia associated with non-insulin dependant diabetes and for treating hyperlipidemia.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: September 9, 2003
    Assignee: Eli Lilly and Company
    Inventor: Samuel James Dominianni