Carbonyl Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/329)
-
Publication number: 20090088322Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: October 1, 2008Publication date: April 2, 2009Applicant: Dow AgroSciences LLCInventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, James M. Ruiz, Carla N. Yerkes, Thomas L. Siddall, Willuam C. Lo
-
Patent number: 7501407Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: November 18, 2004Date of Patent: March 10, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
-
Publication number: 20090062125Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.Type: ApplicationFiled: August 29, 2008Publication date: March 5, 2009Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Katherine A. Guenthenspberger, William C. Lo, Thomas L. Siddall
-
Publication number: 20090048109Abstract: 2-(2-Fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidine-carboxylic acid and its derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: July 30, 2008Publication date: February 19, 2009Applicant: Dow AgroSciences LLCInventors: Jeffrey B. Epp, William C. Lo, Paul R. Schmitzer, Carla N. Yerkes
-
Publication number: 20090043098Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety.Type: ApplicationFiled: April 28, 2006Publication date: February 12, 2009Inventor: Rafael Shapiro
-
Publication number: 20090005391Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: November 3, 2006Publication date: January 1, 2009Inventors: Matthew Colin Thor Fyfe, Martin James Procter
-
Patent number: 7449470Abstract: The invention provides a compound of formula (I) wherein R and R? are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R? and R?? are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.Type: GrantFiled: October 1, 2004Date of Patent: November 11, 2008Assignee: Universiteit LeidenInventors: Lisa Chung Wai Chang, Adriaan P. Ijzerman, Johannes Brussee
-
Publication number: 20080275064Abstract: Compounds of formula (I), including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof as antagonists of adenosine receptors, in particular antagonists of the A2A adenosine receptor subtype.Type: ApplicationFiled: April 11, 2006Publication date: November 6, 2008Inventors: Deborah Slee, Marion Lanier, Binh G. Vong, Yongsheng Chen, Xiaohu Zhang, Emily Lin, Manisha Moorjani, Julio Cesar Castro Palomino Laria
-
Publication number: 20080275062Abstract: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consistinType: ApplicationFiled: January 28, 2005Publication date: November 6, 2008Inventors: David Harold Drewry, David Kendall Jung, James Andrew Linn, Robert Neil Hunter, Dennis Lee, Robert A. Stavenger, Clark Sehon
-
Publication number: 20080261990Abstract: The present invention relates to novel pyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular diseases, in particular dyslipidemias, arteriosclerosis, coronary heart disease, thrombosis and metabolic syndrome.Type: ApplicationFiled: September 10, 2005Publication date: October 23, 2008Applicant: Bayer healthCare AGInventors: Elke Dittrich-Wengenroth, Lars Barfacker, Axel Kretschmer, Claudia Hirth-Dietrich, Peter Ellinghaus, Martin Raabe, Hilmar Bischoff, Christian Pilger, Ulrich Rosentreter, Stephan Bartel, Klemens Lustig, Armin Kern, Dieter Lang, Marcus Bauser
-
Patent number: 7439240Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.Type: GrantFiled: June 23, 2003Date of Patent: October 21, 2008Assignee: AstraZeneca ABInventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
-
Publication number: 20080255095Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.Type: ApplicationFiled: June 18, 2007Publication date: October 16, 2008Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
-
Patent number: 7419984Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor-cells.Type: GrantFiled: September 24, 2003Date of Patent: September 2, 2008Assignee: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A Jenkins, J Peter Klein, Cory T Kohm, John Tulinsky
-
Patent number: 7375108Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents R1 to R3 and L are as defined in the description and R4 corresponds to one of the formulae in which Ra, X and Rb are as defined in the description; and also to processes for preparing these compounds, to pesticidal compositions comprising these compounds and to their use as pesticides.Type: GrantFiled: July 15, 2004Date of Patent: May 20, 2008Assignee: BASF AktiengesellschaftInventors: Anja Schwögler, Markus Gewehr, Bernd Müller, Thomas Grote, Wassilios Grammenos, Jordi Tormo i Blasco, Andreas Gypser, Joachim Rheinheimer, Carsten Blettner, Peter Schäfer, Frank Schieweck, Oliver Wagner, Reinhard Stierl, Ulrich Schöfl, Siegfried Strathmann, Maria Scherer
-
Patent number: 7332491Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Christian Eickmeier, Gisela Schnapp, Norbert Redemann, Flavio Solca, Jens Juergen Quant
-
Patent number: 7326705Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl group, R1, R2, R3 and R4 are as defined herein, and where X is N, R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: January 31, 2005Date of Patent: February 5, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
-
Publication number: 20070299076Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: ApplicationFiled: June 18, 2007Publication date: December 27, 2007Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
-
Patent number: 7312359Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: December 21, 2005Date of Patent: December 25, 2007Assignee: Roche Palo Alto LLCInventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
-
Patent number: 7300907Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 12, 2007Date of Patent: November 27, 2007Assignee: Dow Agrosciences LLCInventors: Jeffrey B. Epp, James M. Ruiz, Paul R. Schmitzer, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
-
Patent number: 7294627Abstract: Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.Type: GrantFiled: December 9, 2002Date of Patent: November 13, 2007Assignee: Eli Lilly and CompanyInventors: Steven Douglas Hiscock, Stuart Donald Jones, Daniel Jon Sall, Stephen Clinton Young, Michael Robert Wiley
-
Patent number: 7253174Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 12, 2006Date of Patent: August 7, 2007Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
-
Patent number: 7129239Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.Type: GrantFiled: October 20, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventor: David A. Griffith
-
Patent number: 7125997Abstract: The invention is directed to novel biaryl derivatives, to the uses of these compounds in various medicinal applications, including the treatment, prevention and control of proliferative diseases such as tumors, and to pharmaceutical compositions comprising these compounds. Compounds of the invention can be used to treat or prevent diseases or disorders that involve the activity of MIF-1 and/or adenosine kinase.Type: GrantFiled: December 18, 2003Date of Patent: October 24, 2006Assignee: IRM LLCInventors: Jason Chyba, Quinn Devereax, Garret Hampton, Fred King
-
Patent number: 7112589Abstract: The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g.Type: GrantFiled: August 29, 2002Date of Patent: September 26, 2006Assignee: Novartis AGInventors: Eva Altmann, Kenji Hayakawa, Genji Iwasaki
-
Patent number: 7053089Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: February 20, 2002Date of Patent: May 30, 2006Assignee: Merck & Co., Inc.Inventors: Christopher F. Claiborne, John W. Butcher, David A. Claremon, Brian E. Libby, Nigel J. Liverton, Peter M. Munson, Kevin T. Nguyen, Brian Phillips, Wayne Thompson, John A. McCauley
-
Patent number: 7041670Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: GrantFiled: April 8, 2003Date of Patent: May 9, 2006Assignee: Schering-Plough Animal Health CorporationInventors: Constantine G. Boojamra, Lee S. Chong, Scott J. Hecker, Tomasz W. Glinka, Dale E. Shuster
-
Patent number: 7034019Abstract: The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(?O)—R8; —S(?O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formulaType: GrantFiled: May 3, 2001Date of Patent: April 25, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc René de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief
-
Patent number: 7005433Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: December 29, 2003Date of Patent: February 28, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
-
Patent number: 6992187Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as in the specification.Type: GrantFiled: August 29, 2001Date of Patent: January 31, 2006Assignee: Aventis Pharma Deutschland GmbHInventors: Anuschirwan Peyman, Gerrit Schubert
-
Patent number: 6953802Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 20, 2001Date of Patent: October 11, 2005Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
-
Patent number: 6916804Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
-
Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
-
Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
-
Patent number: 6838464Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: February 26, 2001Date of Patent: January 4, 2005Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
-
Patent number: 6838128Abstract: The invention relates to chiral nonracemic liquid crystal compounds which are useful as components in liquid crystal compositions to impart high polarization to the mixture. The materials of this invention can be combined with liquid crystal host materials to impart improved properties to mixtures. Chiral nonracemic compounds of this invention can function as additives or dopants in host materials to impart chirality into an LC material.Type: GrantFiled: February 5, 2002Date of Patent: January 4, 2005Assignee: Displaytech, Inc.Inventors: Michael Wand, Xin Hua Chen
-
Publication number: 20040254185Abstract: Selective anthranilamide pyridinamides as VEGFR-2 and VEGFR-3 inhibitors, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, such as, e.g.Type: ApplicationFiled: June 23, 2004Publication date: December 16, 2004Inventors: Alexander Ernst, Andreas Huth, Martin Kruger, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey
-
Publication number: 20040242568Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising the formula: 1Type: ApplicationFiled: March 24, 2004Publication date: December 2, 2004Applicant: Syrrx, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Publication number: 20040242613Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: January 27, 2004Publication date: December 2, 2004Applicants: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Mario G. Cardozo, Derek Cogan, Charles Lawrence Cywin, Georg Dahmann, Darren DiSalvo, John David Ginn, Anthony S. Prokopowicz, Denice M. Spero, Erick Young
-
Publication number: 20040235876Abstract: Pyrimidines of formla (1) are described: 1Type: ApplicationFiled: June 22, 2004Publication date: November 25, 2004Applicant: Celltech R&D LimitedInventors: Jeremy Martin Davis, David Festus Charles Moffat
-
Patent number: 6797714Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: GrantFiled: August 21, 2002Date of Patent: September 28, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza
-
Publication number: 20040152134Abstract: Melanocortin receptor-specific bicyclic compounds having the structure: 1Type: ApplicationFiled: January 21, 2004Publication date: August 5, 2004Applicant: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
-
Patent number: 6756380Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rinType: GrantFiled: May 22, 2000Date of Patent: June 29, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
-
Patent number: 6734187Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.Type: GrantFiled: July 23, 2002Date of Patent: May 11, 2004Assignee: Mitsubishi Chemical CorporationInventors: Toshihiko Tanaka, Eiichirou Iwashita, Akiko Tarao, Akira Amenomori, Yuya Ono
-
Patent number: 6716850Abstract: Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CHR8)n-—D—(CHR8)m—; D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl; R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularType: GrantFiled: March 5, 2002Date of Patent: April 6, 2004Assignee: Medivir ABInventors: Stefan Lindström, Christer Sahlberg, Hans Wallberg, Genaidy Kalyanov, Lourdes Salvador Odén, Lotta Naeslund
-
Patent number: 6680385Abstract: A method for the preparation of aryl methyl ketones converts a variety of ethyl arenas to the corresponding aryl methyl ketones using a dioxygen-containing gas as the oxidant. The catalyst used for the reaction is a metal complex bearing general formulas as disclosed.Type: GrantFiled: January 25, 2002Date of Patent: January 20, 2004Assignees: The Hong Kong Polytechnic University, Sichuan UniversityInventors: Albert Sun-Chi Chan, Jian-Ying Qi, Cheng-Chao Pai, Xian-Jun Li, Li-Sheng Deng, Wen-Zao Li, Bin Sun, Jia-Yuan Hu
-
Patent number: 6657060Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.Type: GrantFiled: November 8, 2001Date of Patent: December 2, 2003Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Patrizio Mattei, Werner Neidhart, Philippe Pflieger
-
Patent number: 6645968Abstract: Compounds of formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.Type: GrantFiled: February 5, 2001Date of Patent: November 11, 2003Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Hao Bai, Jorge D. Brioni, William A. Carroll, Murali Gopalakrishnan, Robert J. Gregg, Mark W. Holladay, Peggy P. Huang, John F. Kincaid, Michael E. Kort, Philip R. Kym, John K. Lynch, Arturo Perez-Medrano, Henry Q. Zhang
-
Patent number: 6635766Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.Type: GrantFiled: March 28, 1997Date of Patent: October 21, 2003Assignee: Lonza AGInventors: Jean-Paul Roduit, Georges Kalbermatten
-
Patent number: 6632820Abstract: A pyrimidine derivative of formula (I) wherein, for example, R1 is-(1-6C)alkyl or (3-5C)alkenyl [optionally substituted by a phenyl substituent]; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bears one substituent of formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH-link]; wherein, for example, X is CH2, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH2, (1-4C)alkoxy, (1-4C)alkylthio, —NH(1-4C)alkyl, —N[(1-4C)alkyl]2 or —NH-(3-8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may each optionally bear other substituents selected from halogeno, (1-6C)alkyl, cyano and (2-4C)alkenyl, or a pharmaceutically-acceptable salt, or in-vivo-hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are describeType: GrantFiled: February 26, 2001Date of Patent: October 14, 2003Assignee: AstraZeneca ABInventors: Gloria Anne Breault, Philip John Jewsbury, Janet Elizabeth Pease
-
Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman