Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding Patents (Class 548/364.1)
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Publication number: 20080064698Abstract: The invention relates to 1-(2,4,6-trisubstituted-phenyl)-5-amino-4-substituted-pyrazole derivatives of formula (I) or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: ApplicationFiled: February 25, 2005Publication date: March 13, 2008Applicant: Bayer CropScience S.A.Inventors: Stefan Schnatterer, David Teh-Wei Chou, Werner Knauf, Daniela Jans, Karl Seeger
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Patent number: 7332518Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH?CHR2, CH?C?CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7cycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: GrantFiled: January 24, 2002Date of Patent: February 19, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Stephan Trah
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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: 20070281973Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: Josephus H.M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
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Patent number: 7300950Abstract: The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.Type: GrantFiled: April 13, 2005Date of Patent: November 27, 2007Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
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Publication number: 20070244177Abstract: There is dislosed herein compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.Type: ApplicationFiled: April 12, 2007Publication date: October 18, 2007Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Almstetter, Andreas Treml
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Patent number: 7282516Abstract: The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).Type: GrantFiled: December 22, 2005Date of Patent: October 16, 2007Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Serge Martinez, Murielle Rinaldi-Carmona
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Patent number: 7279476Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: January 5, 2005Date of Patent: October 9, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Oing Tang, Francois Maltais, James Walter Janetka, Michael Robin Hale
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Publication number: 20070225280Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: March 14, 2007Publication date: September 27, 2007Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
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Publication number: 20070213302Abstract: 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: March 9, 2007Publication date: September 13, 2007Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat
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Patent number: 7253290Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: August 19, 2003Date of Patent: August 7, 2007Assignee: AstraZeneca ABInventors: Thomas Geoffrey Bird, Mickael Louis Pierre Maudet
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Patent number: 7247734Abstract: The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3 is independently: a C5-20aryl group, and is optionally substituted; Ar4 is independently: a C5-20aryl group, and is optionally substituted; R5 is independently: hydrogen; halo; hydroxyl; ether; formyl; acyl; carboxy; ester; acyloxy; oxycarbonyloxy; amido; acylamido; aminocarbonyloxy; tetrazolyl; amino; nitro; cyano; azido; sulfhydryl; thioether; sulfonamide; C1-7alkyl; C3-20heterocycyl; or C5-20aryl; R<SP>N</SP> is independently: —H; C1-7alkyl; C3-20heterocycyl; or, C5-20aryl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: GrantFiled: December 19, 2002Date of Patent: July 24, 2007Assignees: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., Institute of Cancer Research of Royal Cancer HospitalInventors: Martin James Drysdale, Brian William Dymock, Xavier Barril-Alonso, Paul Workman, Laurence Harris Pearl, Chrisostomos Prodromou, Edward McDonald
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Patent number: 7244739Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.Type: GrantFiled: May 14, 2004Date of Patent: July 17, 2007Assignee: Torreypines Therapeutics, Inc.Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
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Patent number: 7238722Abstract: The present invention relates to pyrazolyalkines and to their use, to a process for preparing them and also to intermediates.Type: GrantFiled: January 5, 2004Date of Patent: July 3, 2007Assignee: LANXESS Deutschland GmbHInventors: Wolfgang Ebenbeck, Florian Rampf, Albrecht Marhold
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Patent number: 7230025Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: September 23, 2003Date of Patent: June 12, 2007Assignee: Pfizer, Inc.Inventors: Oscar Barba, Lyn Howard Jones
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Patent number: 7230116Abstract: The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to their use as pesticides, microbicides and herbicides.Type: GrantFiled: October 21, 2002Date of Patent: June 12, 2007Assignee: Bayer CropScience, AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Mark Wilhelm Drewes, Christoph Erdelen, deceased
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Patent number: 7208169Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: April 16, 2003Date of Patent: April 24, 2007Assignee: Bayer CropScience LPInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
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Patent number: 7205323Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.Type: GrantFiled: October 12, 2005Date of Patent: April 17, 2007Assignee: Glenmark Pharmaceuticals S.A.Inventors: Abraham Thomas, Gopalan Balasubramanian, V. S. Prasada Rao Lingam, Daisy Manish Shah
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Patent number: 7189755Abstract: Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.Type: GrantFiled: February 10, 2004Date of Patent: March 13, 2007Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
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Patent number: 7186843Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: April 29, 2004Date of Patent: March 6, 2007Assignee: Daiichi Pharmaceutical Co. Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Patent number: 7186741Abstract: The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.Type: GrantFiled: March 17, 2003Date of Patent: March 6, 2007Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Josephus H. M. Lange, Maria L. Pras-Raves, Cornelis G. Kruse, Herman H. van Stuivenberg, Tinka Tuinstra, Hiskias Keizer
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Patent number: 7186738Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: March 6, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7183307Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: May 3, 2004Date of Patent: February 27, 2007Assignee: Vertex Pharmaceuticals IncroporatedInventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
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Patent number: 7179835Abstract: The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.Type: GrantFiled: November 13, 2002Date of Patent: February 20, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Matthew Campbell, Chuen Chan, Henry Anderson Kelly, Nigel Paul King, Savvas Kleanthous, Andrew McMurtrie Mason, Stefan Senger, Paul William Smith, Nigel Stephen Watson, Robert John Young
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Patent number: 7157482Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: January 2, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7151113Abstract: The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5, R6 and m are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: May 3, 2004Date of Patent: December 19, 2006Assignee: Bristol Myers Squibb CompanyInventors: Alaric J. Dyckman, Jagabandhu Das, Katerina Leftheris, Chunjian Liu, Robert V. Moquin, Stephen T. Wrobleski
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Patent number: 7148069Abstract: The present invention provides a method for the analysis of a compound with amino group (e.g., an amino acid or peptide) contained in a sample and convenient manner with a high sensitivity. The compound with amino group in a sample containing the compound with amino group is labeled with a specific carbamate compound such as p-trimethylammonium anilyl-N-hydroxysuccinimidyl carbamate iodide to enhance the selectivity and sensitivity. The present invention is preferably used in conjunction with mass spectrometry such as MS/MS method to facilitate quantitative analysis. The present invention further provides labeling reagents for mass spectrometry.Type: GrantFiled: August 16, 2004Date of Patent: December 12, 2006Assignee: Ajinomoto Co., Inc.Inventors: Hiroshi Miyano, Akihisa Yahashi, Kazutaka Shimbo, Masakazu Nakazawa, Kazuo Hirayama
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Patent number: 7144910Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.Type: GrantFiled: October 29, 2003Date of Patent: December 5, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Andrew Madin, Mark Peter Ridgill
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Patent number: 7138361Abstract: Compounds of Formula (1), their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein A, R1, R2a, R2b, W, Y, and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (1).Type: GrantFiled: November 20, 2001Date of Patent: November 21, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Clifford Daniel Cotterman, Chi-Ping Tseng
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Patent number: 7132534Abstract: The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions. The present invention makes it possible in particular to obtain a chromatic, strong, relatively unselective and resistant coloration of keratin fibers.Type: GrantFiled: July 7, 2003Date of Patent: November 7, 2006Assignee: L'OrealInventors: Stéphane Sabelle, Laure Ramos, Madeleine LeDuc
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7109228Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: April 5, 2002Date of Patent: September 19, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7091350Abstract: The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR?, SR, SOR, SO2R, COOR, CONRR?, PO(OH)2, SO3X, NHCONRR, a non-cationic heterocycle, an aryl, a halogen. R2 and R3 are different from H and represent, independently of each other, an alkyl or alkenyl group; R2 and R3, together with the nitrogen atom to which they are attached, can form a heterocycle possibly comprising at least one other heteroatom selected from among N, O and S; R2 and R3 or the heterocycle that they form with the nitrogen to which they are attached can be substituted by at least one substituent defined above.Type: GrantFiled: February 14, 2002Date of Patent: August 15, 2006Assignee: L'OrealInventors: Thilo Fessmann, Eric Terranova
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Patent number: 7060822Abstract: Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.Type: GrantFiled: July 24, 2000Date of Patent: June 13, 2006Assignee: Abbott GmbH & Co. KGInventors: Lee Arnold, Marina Moran Moset, Jose Maria Castellano Berlanga, Isabel Fernandez, David J. Calderwood, Paul Rafferty
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Patent number: 7057049Abstract: This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I): wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4, and Y5 are as defined in the specification.Type: GrantFiled: April 1, 2003Date of Patent: June 6, 2006Assignee: Pharmacia CorporationInventors: Kimberley C. Allen, Dennis K. Anderson, John E. Baldus, Todd Boehlow, Jerry D. Clark, Dan R. Dukesherer, Albert D. Edney, Tom Fevig, Sastry Kunda, Jon P. Lawson, Patrick H. Lau, Lisa L. McDermott, Michael K. Mao, Jodi L. Moe, Partha Mudipalli, Win Naing, Shaun R. Selness, Christine B. Seymour, Tobin C. Schilke, Shekhar Viswanath, John K. Walker, Gopichand Yalamanchili
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Patent number: 7041687Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: January 23, 2003Date of Patent: May 9, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Guy Brenchley, Julian M. C. Golec, Ronald Knegtel, Michael Mortimore, Sanjay Patel, Alistair Rutherford
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Patent number: 7030141Abstract: 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: October 23, 2002Date of Patent: April 18, 2006Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Patent number: 7026346Abstract: Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-smalll cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including hormone-refractory prostate cancer. Further provided are methods of treating cancer in a subject in need of such treatment using the compounds of the present invention. Further provided are methods for using the compounds of the present invention to treat, inhibit, or delay the onset of cancer in a subject. Further provided are methods of inducing apoptosis in rapidly proliferating cells, particularly, though not necessarily cancer cells, using the compounds of the present invention.Type: GrantFiled: April 8, 2003Date of Patent: April 11, 2006Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Xueqin Song, Ho-Pi Lin
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Patent number: 7009056Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.Type: GrantFiled: February 5, 2001Date of Patent: March 7, 2006Assignee: University College LondonInventors: Giti Garthwaite, David Selwood, Marcel Kling, Grant Wishart
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Patent number: 6998415Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: January 12, 2004Date of Patent: February 14, 2006Assignee: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Kathy L. Rogers, legal representative, Hwang-Fun Lu, David L. Brown, Roland S. Rogers, deceased
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6995182Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: March 26, 2003Date of Patent: February 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Vincent Mutel, Juergen Wichmann
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Patent number: 6984651Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: August 7, 2003Date of Patent: January 10, 2006Assignee: Bristol-Myers Squibb Pharma, CompanyInventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
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Patent number: 6958339Abstract: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.Type: GrantFiled: February 2, 2001Date of Patent: October 25, 2005Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Jun Ishikawa, Makoto Takeuchi
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Patent number: 6951874Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: February 23, 2001Date of Patent: October 4, 2005Assignee: AstraZeneca ABInventors: Peter Hansen, Lars Pettersson
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Patent number: 6949546Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: July 10, 2003Date of Patent: September 27, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
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Patent number: 6949578Abstract: 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: GrantFiled: July 14, 2004Date of Patent: September 27, 2005Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
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Patent number: 6927217Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: GrantFiled: October 16, 2002Date of Patent: August 9, 2005Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait