The Benzene Ring Is Part Of A Substituent Which Contains Nitrogen Patents (Class 564/50)
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Patent number: 6864380Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: July 3, 2003Date of Patent: March 8, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Patent number: 6860928Abstract: Disclosed are compounds of the formulae wherein Z is a group of the formula —OR1, a group of the formula —SR1, or a group of the formula —NR1R2, Y is a group of the formula —OR3, a group of the formula —SR3, or a group of the formula —NR3R4, n is an integer representing the number of repeat —(CH2)— or —(CH2CH2O)— units, wherein, provided that at least one of R1, R2, R3, R4, R5, and R6 is a hydrogen atom, provided that at least one of R1, R2, R3, R4, R5, and R6 is other than a hydrogen atom, and provided that at least one Z or Y within the compound is a group of the formula —NR1R2 or a group of the formula —NR3R4, R1, R2, R3, R4, R5, R6, and R7 each, independently of the others, is (i) a hydrogen atom, (ii) an alkyl group, (iii) an aryl group, (iv) an arylalkyl group, or (v) an alkylaryl group, and wherein R7 can also be (vi) an alkoxy group, (vii) an aryloxy group, (Viii) an arylalkyloxy group, (ix) an alkylaryloxy group, (x) a polyalkyleneoxy group, (xi) a polyaryleneoxy group, (xii) a polyarylalkylenType: GrantFiled: September 4, 2002Date of Patent: March 1, 2005Assignee: Xerox CorporationInventors: Marcel P. Breton, Danielle C. Boils-Boissier, Jule W. Thomas, Jr., Donald R. Titterington, H. Bruce Goodbrand, Jeffrey H. Banning, James D. Wuest, Dominic Laliberte, Marie-Eve Perron
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Publication number: 20040224993Abstract: Compound of formula (I): 1Type: ApplicationFiled: June 7, 2004Publication date: November 11, 2004Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Publication number: 20040176446Abstract: The invention relates to compounds of formula (I), to salts and stereoisomers thereof, to their production and to their use for producing medicaments used for treating cardiovascular diseases.Type: ApplicationFiled: April 12, 2004Publication date: September 9, 2004Inventors: Cristina Alonso-Alija, Michael Harter, Michael Hahn, Josef Pernerstorfer, Stefan Weigand, Johannes-Peter Stasch, Frank Wunder
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Publication number: 20040167131Abstract: This invention discloses amino acid derivatives which display inhibitory effects on the serine protease factor Xa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, methods for the preparation of the compounds, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: ApplicationFiled: September 11, 2003Publication date: August 26, 2004Applicant: Pfizer Inc.Inventors: Gary Louis Bolton, Kevin James Filipski, Jeffrey Thomas Kohrt, Frances La, Daniele Marie Leonard
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Patent number: 6777561Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: June 1, 2000Date of Patent: August 17, 2004Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
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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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Publication number: 20040122063Abstract: The invention relates a compound represented by the formula (1):Type: ApplicationFiled: July 30, 2003Publication date: June 24, 2004Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
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Patent number: 6750253Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1Type: GrantFiled: February 22, 2002Date of Patent: June 15, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Publication number: 20040110832Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as antagonists, or more preferably, partial antagonist of factor IX and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds are useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX. Such diseases or disease states include stroke, myocardial infarction, aneurysm surgery, and deep vein thrombosis associated with surgical procedures, long periods of confinement, and acquired or inherited pro-coagulant states.Type: ApplicationFiled: August 8, 2003Publication date: June 10, 2004Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Xiao-Chuan Guo, Daniel Peter Christen, Devi Reddy Gohimmukkula, Guoxiang Huang, Robert Rothlein, Sameer Tyagi, Tripura Yaramasu, Christopher Behme
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Publication number: 20040102636Abstract: 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: ApplicationFiled: February 1, 2002Publication date: May 27, 2004Applicant: BAYER 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: 20040087491Abstract: A class of compounds is described which can be used for the treatment of viral infections.Type: ApplicationFiled: October 30, 2003Publication date: May 6, 2004Inventors: Daniel L. Flynn, Kenneth Williams, Susan L. Hockerman, Jeffrey Zablocki
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Publication number: 20040082625Abstract: The compounds of the invention are represented by the following general structure 1Type: ApplicationFiled: May 22, 2003Publication date: April 29, 2004Inventors: Michael G. Kelly, Shimin Xu, Ning Xi, Philip Miller, John F. Kincaid, Chiara Ghiron, Thomas Coulter
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Publication number: 20040075723Abstract: Disclosed are compounds of the formulae 1 2Type: ApplicationFiled: September 4, 2002Publication date: April 22, 2004Applicant: Xerox CorporationInventors: Marcel P. Breton, Danielle C. Boils-Boissier, Jule W. Thomas, Donald R. Titterington, H. Bruce Goodbrand, Jeffrey H. Banning, James D. Wuest, Dominic Laliberte, Marie-Eve Perron
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Publication number: 20040073043Abstract: The present invention provides stereoscopically-pure diastereomers of Formula I: 1Type: ApplicationFiled: October 9, 2003Publication date: April 15, 2004Inventors: Anthony Booth, James L. Caffrey
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Publication number: 20040067943Abstract: Compounds of the formula (I), in which M is a central building block selected from the group below in which Al, A2, K1 and K2 are as defined in the description, are novel effective tryptase inhibitors.Type: ApplicationFiled: August 18, 2003Publication date: April 8, 2004Inventor: Thomas Martin
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Publication number: 20040029913Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: ApplicationFiled: February 24, 2003Publication date: February 12, 2004Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
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Patent number: 6670400Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.Type: GrantFiled: April 8, 2002Date of Patent: December 30, 2003Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: 6630589Abstract: The invention features screening assays for compounds that are potentially useful for treating or preventing a proliferative disease. The assays are based on contacting a candidate compound with a cell containing a nucleic acid including a HER2 regulatory element and a reporter sequence. In addition, the invention features compounds identified by the assays of the invention. The invention further features compounds structurally related to those identified by the screening assays. Finally, the invention features methods of treating or preventing a proliferative disease using the compounds of the invention.Type: GrantFiled: March 26, 2002Date of Patent: October 7, 2003Assignee: Message PharmaceuticalsInventors: Anthony Giordano, Gordon Donald Powers, Michael Alan Sturgess, Ke Yang
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Publication number: 20030158226Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: August 21, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6608227Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.Type: GrantFiled: October 13, 2000Date of Patent: August 19, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Dean A Wacker, John V Duncia, Joseph B Santella, III, Daniel S Gardner
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Patent number: 6602302Abstract: New substituted 2,5-diamino-1-aminomethylbenzene compounds of formula (I), or physiologically compatible water-soluble salts thereof, are described as well as methods for preparing them. In addition, oxidation dye precursor compositions for dyeing keratin fibers, especially human hair, which each contain from 0.005 to 20 percent by weight of at least one of the new substituted 2,5-diamino-1-aminomethylbenzene compounds of formula (I), or their physiologically compatible water-soluble salts, are described. Methods for dyeing hair with ready-to-apply dye mixtures made by mixing these oxidation dye precursor compositions with an oxidizing agent, such as hydrogen peroxide solution, are also described.Type: GrantFiled: November 3, 2000Date of Patent: August 5, 2003Assignee: Wella AGInventors: Laurent Chassot, Hans-Juergen Braun
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Publication number: 20030114517Abstract: A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.Type: ApplicationFiled: March 12, 2002Publication date: June 19, 2003Inventors: William J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
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Publication number: 20030105332Abstract: The present invention provides stereoscopically-pure diastereomers of Formula I: 1Type: ApplicationFiled: March 25, 2002Publication date: June 5, 2003Inventors: Anthony Booth, James L. Caffrey
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Patent number: 6566554Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is anType: GrantFiled: February 22, 2002Date of Patent: May 20, 2003Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventor: Erik Rytter Ottosen
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Publication number: 20030065170Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 5, 2002Publication date: April 3, 2003Inventors: Katherine Louisa Widdowson, Qi Jin
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Publication number: 20030065188Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 6, 2002Publication date: April 3, 2003Inventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6525091Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.Type: GrantFiled: February 22, 2002Date of Patent: February 25, 2003Assignee: Telik, Inc.Inventors: Louise Robinson, Hugo O. Villar
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Publication number: 20020188027Abstract: Substituted diarylureas, pharmaceutical compositions containing them, and their use for stimulating Fas-mediated apoptosis. The compounds, as single stereoisomers or mixtures of stereoisomers, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful in methods of treating autoimmune diseases, infectious diseases, and malignancies.Type: ApplicationFiled: February 22, 2002Publication date: December 12, 2002Inventors: Louise Robinson, Hugo O. Villar
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Patent number: 6482804Abstract: A soluble ionic complex is formed by an aqueous mixture of a benzylammonium group-containing surfactant and a polynucleic acid sequence. When the mixture forms a vesicular complex, the sequence is packaged therein. This composition is useful in pharmaceutical compositions and in methods of delivering the polynucleic acid sequence (which preferably encodes a protein or peptide) to a cell for expression. Such methods are useful in therapy, as vaccines and as gene therapy agents.Type: GrantFiled: April 27, 2000Date of Patent: November 19, 2002Assignee: WyethInventors: Shankar Musunuri, Chandrasekhar Satishchandran
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Patent number: 6458998Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: May 25, 2000Date of Patent: October 1, 2002Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum
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Publication number: 20020137774Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: July 19, 2001Publication date: September 26, 2002Applicant: BAYER CORPORATIONInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Patent number: 6444691Abstract: The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80° C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.Type: GrantFiled: July 10, 2000Date of Patent: September 3, 2002Assignee: Solvakofarma, a.s.Inventors: Vladi{acute over (m)}ir Oremus, Vendelín {haeck over (S)}mahovský, Viera Fáberová, Ivan Kakalík, {haeck over (L)}udmila Schmidtová, Marián Zemánek
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Patent number: 6436999Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 18, 1997Date of Patent: August 20, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: 6372933Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.Type: GrantFiled: February 27, 2001Date of Patent: April 16, 2002Assignee: SmithKline Beecham CorporationInventors: Neil H. Baine, Ann Marie Eldridge, Marvin Sungwhan Yu
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Patent number: 6359061Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.Type: GrantFiled: March 19, 1999Date of Patent: March 19, 2002Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Edward Swayze, Peter William Davis
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Publication number: 20020028851Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: ApplicationFiled: April 3, 2001Publication date: March 7, 2002Inventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Publication number: 20020016350Abstract: This invention relates to a series of substitituted amino acids of Formula I 1Type: ApplicationFiled: August 10, 2001Publication date: February 7, 2002Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 6316478Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: March 3, 2000Date of Patent: November 13, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, Hong Nie
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Patent number: 6218389Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: July 31, 1998Date of Patent: April 17, 2001Assignee: The Procter & Gamble Co.Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
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Patent number: 6214880Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: September 21, 1999Date of Patent: April 10, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6180676Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: January 30, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6169206Abstract: 4-(N,N-Dialkylamino)aniline compounds of the following general formula (I): wherein R1 represents an alkyl group, an aryl group or a heterocyclic group, R2 to R5 each represent a hydrogen atom or a substituent, and R2 and R3, R1 and R2, or R4 and R5 may form a ring together; a processing composition for color photography, which contains at least one of these compounds; and a color image-forming method wherein at least one of these aniline compounds is used.Type: GrantFiled: January 24, 2000Date of Patent: January 2, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
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Patent number: 6136942Abstract: A one-component polyurethane composition is described that comprises a latent curing agent bonded to the prepolymer, from which curing agent aldehyde is liberated upon curing. Said aldehyde comprises two phenyl groups. By the specific design of the polyurethane composition, the application characteristics as well as the aging resistance of the cured polyurethane are improved.Type: GrantFiled: March 31, 1999Date of Patent: October 24, 2000Assignee: Sika AG, vorm. Kaspar Winkler & Co.Inventors: Ueli Pfenninger, Pierre-Andre Butikofer
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Patent number: 6121323Abstract: Bishydroxyureas are provided that inhibit the enzyme 5-lipoxygenase. These compounds have the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and M are defined herein. Also disclosed are pharmaceutical compositions containing such compounds and methods of inhibiting the enzyme 5-lipoxygenase using such compounds.Type: GrantFiled: December 3, 1997Date of Patent: September 19, 2000Assignee: 3M Innovative Properties CompanyInventor: Bryon A. Merrill
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Patent number: 6093742Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 27, 1997Date of Patent: July 25, 2000Assignee: Vertex Pharmaceuticals, Inc.Inventors: Francesco Gerald Salituro, Guy W. Bemis, Jeremy Green, James L. Kofron
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Patent number: 6063819Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.Type: GrantFiled: February 18, 1998Date of Patent: May 16, 2000Assignee: Cypros Pharmaceutical Corp.Inventors: Paul J. Marangos, Brian W. Sullivan, Torsten Wiemann, Anne M. Danks, Marina Sragovicz, Lewis R. Makings
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Patent number: 6028131Abstract: The invention relates to compounds of the formula I ##STR1## in which R is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl, --CH.sub.2 --A--R.sub.2 or a group of the formula II, ##STR2## R.sub.1 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula (II),R.sub.2 is C.sub.4 -C.sub.18 alkyl, --(CH.sub.2).sub.m --COOR.sub.5 or a group of the formula III, ##STR3## R.sub.3 is hydrogen, C.sub.5 -C.sub.8 cycloalkyl or C.sub.1 -C.sub.12 alkyl,R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula II or IV, ##STR4## A is S or SO, E is a direct bond, --CH.sub.2 --, --CH.sub.2 --O-- or --CH.sub.2 --NH--,G is --O-- or --NR.sub.3 --,Y is C.sub.1 -C.sub.18 alkyl, cyclohexyl, phenyl or alpha- or beta-naphthyl,R.sub.5 is C.sub.1 -C.sub.18 alkyl, andm is 1 or 2,with the provisos thateither at least one of the radicals R and R.sub.Type: GrantFiled: April 27, 1998Date of Patent: February 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Hans-Rudolf Meier, Gerrit Knobloch
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Patent number: 6005008Abstract: This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: August 15, 1997Date of Patent: December 21, 1999Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.