Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
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Publication number: 20090105257Abstract: The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.Type: ApplicationFiled: November 15, 2004Publication date: April 23, 2009Inventors: David Francis Corbett, Kate Anna Dwornik, Dulce Maria Garrido, Stephen Carl McKeown, Wendy Yoon Mills, Andrew James Peat, Terrence Lee Smalley, JR.
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Patent number: 7517880Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 1, 2002Date of Patent: April 14, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20090093483Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: ApplicationFiled: December 17, 2007Publication date: April 9, 2009Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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Patent number: 7501414Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: December 21, 2005Date of Patent: March 10, 2009Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
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Publication number: 20090062286Abstract: The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.Type: ApplicationFiled: May 5, 2008Publication date: March 5, 2009Inventors: Kenneth William Foreman, Frances E. Park, Lee Arnold
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Publication number: 20090048258Abstract: The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: January 31, 2006Publication date: February 19, 2009Inventors: Masaki Ogino, Yoshihisa Nakada, Mitsuyuki Shimada, Kouhei Asano, Norikazu Tamura, Minori Masago
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20080306054Abstract: The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; C1-5 hydrocarbyl and C1-5 hydrocarbyloxy; wherein the C1-5 hydrocarbyl and C1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C1-2 alkoxy, amino, mono- and di-C1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C1-5 hydrocarbyl-amino, wherein the acyclic C1-5 hydrocarbyl group and the mono and di-C1-5 hydrocarbylamino moieties in each instance are optionally substitType: ApplicationFiled: April 13, 2006Publication date: December 11, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead
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Publication number: 20080293722Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.Type: ApplicationFiled: March 15, 2005Publication date: November 27, 2008Applicant: WyethInventors: Robert Zelle, Christopher Todd Baker, Paul Will, Vincent P. Galullo
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Patent number: 7452891Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Publication number: 20080275028Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.Type: ApplicationFiled: July 19, 2005Publication date: November 6, 2008Inventors: Giovanni Gaviraghi, Chiara Ghiron, Hendrik Bothmann, Renza Roncarati, Georg Christian Terstappenn
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Publication number: 20080269220Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.Type: ApplicationFiled: March 14, 2005Publication date: October 30, 2008Inventors: Tsuneo Yasuma, Nobuyuki Negoro, Shinobu Sasaki
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Publication number: 20080261982Abstract: Stilbene derivatives exhibit killing and suppression of growth activity against a variety of cancer cells, and are effective at suppressing tumor growth in vivo. The stilbene derivatives may be used in the treatment of diseases characterized by cell hyperproliferation including human malignancies and non-malignant diseases such as liver cirrhosis. Stilbenes may also disrupt abnormal vessels in tumor to achieve vascular disrupting effect to suppress tumor growth. Water soluble pro-drug forms of stilbene derivatives are particularly useful in suppressing tumor growth in vivo.Type: ApplicationFiled: April 23, 2007Publication date: October 23, 2008Inventors: Ruey-min Lee, Daniele Simoni
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Patent number: 7427618Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 30, 2004Date of Patent: September 23, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz, Christoph van Amsterdam
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Publication number: 20080196176Abstract: This invention relates to unsubstituted and polymeric leuco colorants for use as consumer product additives to indicate a product function by color change, to make attractive or distinctive visual effects, or to provide latent or delayed color generation. The colorants may be present in a stable, colorless state and may be transformed to an intense colored state upon exposure to certain physical or chemical changes. Alternatively, the colorants may be transformed from one color to another color upon exposure to certain physical or chemical changes. The colored form of the unsubstituted or polymeric leuco colorant may be transient, since the colorant can revert back to its colorless form or its original color after the physical or chemical activation has been removed or changed. Polymeric leuco colorants are typically comprised of at least two components: at least one leuco chromophore component and at least one polymeric component.Type: ApplicationFiled: February 6, 2008Publication date: August 21, 2008Inventors: Eduardo Torres, Patrick D. Moore, Joe Clark
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Publication number: 20080196177Abstract: This invention relates to unsubstituted and polymeric leuco colorants for use as consumer product additives to indicate a product function by color change, to make attractive or distinctive visual effects, or to provide latent or delayed color generation. The colorants may be present in a stable, colorless state and may be transformed to an intense colored state upon exposure to certain physical or chemical changes. Alternatively, the colorants may be transformed from one color to another color upon exposure to certain physical or chemical changes. The colored form of the unsubstituted or polymeric leuco colorant may be transient, since the colorant can revert back to its colorless form or its original color after the physical or chemical activation has been removed or changed. Polymeric leuco colorants are typically comprised of at least two components: at least one leuco chromophore component and at least one polymeric component.Type: ApplicationFiled: February 6, 2008Publication date: August 21, 2008Inventors: Patrick D. Moore, Eduardo Torres
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Publication number: 20080021126Abstract: The invention relates to novel photoinitiators of formula (I) wherein each of the substituents is given the definition as set forth in the Specification and the claims. The photoinitiators can be used to prepare multifunctional photoinitiators.Type: ApplicationFiled: January 24, 2005Publication date: January 24, 2008Inventors: Kurt Dietliker, Rinaldo Husler, Jean-Luc Birbaum, Jean-Pierre Wolf
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Patent number: 7314872Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula I: wherein Q is morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.Type: GrantFiled: August 18, 2004Date of Patent: January 1, 2008Assignee: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Patent number: 7166601Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 26, 2006Date of Patent: January 23, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7157457Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.Type: GrantFiled: September 28, 2001Date of Patent: January 2, 2007Assignee: Glaxo Group LimitedInventors: Rachael Anne Ancliff, Caroline Mary Cook, Colin David Eldred, Paul Martin Gore, Lee Andrew Harrison, Simon Teanby Hodgson, Duncan Bruce Judd, Suzanne Elaine Keeling, Xiao Qing Lewell, Graeme Michael Robertson, Stephen Swanson
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Patent number: 7125991Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: December 13, 2004Date of Patent: October 24, 2006Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 7112586Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: February 25, 2005Date of Patent: September 26, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7105662Abstract: The present invention relates to a process for the preparation of N-substituted 2,6-dialkylmorpholines of the formula I in which R1 and R2, independently of one another, are hydrogen, alkyl or cycloalkyl, or R1 and R2 together with the carbon atom to which they are bonded are a 5- to 14-membered carbocycle, and R3 and R4, independently of one another, are alkyl or cycloalkyl, by reacting at least one carbonyl compound of the formula II in which R1 and R2 have the meanings given above, with at least one morpholine of the formula III in which R3 and R4 have the meanings given above, in the presence of hydrogen and at least one metal-containing catalyst, wherein the active component of the catalyst consists essentially of platinum group metals.Type: GrantFiled: March 15, 2002Date of Patent: September 12, 2006Assignee: BASF AkteingesellschaftInventors: Michael Henningsen, Andreas Kusche, Michael Hüllmann, Lothar Rüb, Stefan Käshammer, Till Gerlach
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Patent number: 7071201Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 2, 2001Date of Patent: July 4, 2006Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 7070630Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R1 and R2 are each independently selected from hydrogen atoms, a C1 to C5 alkyl or hydroxyalkyl group, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 member cyclic ring optionally containing one or more additional atoms selected from O, N or S atoms, and n is equal to 1 or 2, with the proviso that when n is equal to 2 only one of R1 and R2 may be hydrogen.Type: GrantFiled: May 3, 2004Date of Patent: July 4, 2006Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6967199Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: November 8, 2002Date of Patent: November 22, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 6964963Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.Type: GrantFiled: August 27, 2002Date of Patent: November 15, 2005Assignee: Bayer AktiengesellschaftInventors: Joachim Komoschinski, Herbert Diehl
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Patent number: 6900243Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: February 20, 2001Date of Patent: May 31, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
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Patent number: 6875764Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.Type: GrantFiled: October 27, 2000Date of Patent: April 5, 2005Assignee: New Pharma Research Sweden ABInventors: Sabrina Muzi, Shoaá Abdul Rahman
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Patent number: 6849733Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.Type: GrantFiled: August 22, 1997Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
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Patent number: 6838561Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1, and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group; phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.Type: GrantFiled: January 18, 2002Date of Patent: January 4, 2005Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Publication number: 20040242576Abstract: The present invention relates to compounds of formula I 1Type: ApplicationFiled: May 26, 2004Publication date: December 2, 2004Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Publication number: 20040162287Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.Type: ApplicationFiled: November 10, 2003Publication date: August 19, 2004Applicant: GRUENENTHAL GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
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Patent number: 6765009Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: April 10, 2002Date of Patent: July 20, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
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Patent number: 6750339Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R1 and R2 are each independently selected from hydrogen atoms, a C1 to C5 alkyl or hydroxyalkyl group, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 member cyclic ring optionally containing one or more additional atoms selected from O, N or S atoms, and n is equal to 1 or 2, with the proviso that when n is equal to 2 only one of R1 and R2 may be hydrogen.Type: GrantFiled: January 18, 2002Date of Patent: June 15, 2004Assignee: The Procter and Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Patent number: 6743790Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 6, 2001Date of Patent: June 1, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Publication number: 20040077857Abstract: The present invention relates to a process for the preparation of N-substituted 2,6-dialkylmorpholines of the formula I 1Type: ApplicationFiled: September 11, 2003Publication date: April 22, 2004Inventors: Michael Henningsen, Andreas Kusche, Michael Hullmann, Lothar Rub, Stefan Kashammer, Till Gerlach
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040072802Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: 1Type: ApplicationFiled: October 9, 2002Publication date: April 15, 2004Inventors: Jingwu Duan, Bryan W. King, Carl Decicco, Thomas P. Maduskuie, Mathew E. Voss
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Patent number: 6720332Abstract: Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: February 27, 2003Date of Patent: April 13, 2004Assignee: SmithKline Beecham CorporationInventors: Scott Howard Dickerson, David Harold Drewry, James Andrew Linn
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Patent number: 6716839Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: February 26, 2003Date of Patent: April 6, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Piñeiro-Núñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6699990Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing said compounds and used for oxidative dyeing of fibers.Type: GrantFiled: October 21, 2002Date of Patent: March 2, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6667309Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 12, 2002Date of Patent: December 23, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6602869Abstract: This invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.Type: GrantFiled: November 21, 2001Date of Patent: August 5, 2003Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton