Halogen Patents (Class 562/456)
-
Publication number: 20090264469Abstract: The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.Type: ApplicationFiled: October 18, 2005Publication date: October 22, 2009Applicants: BIO-PROJET, SUN PHARMACEUTICAL INDUSTRIES LTD.Inventors: Marc Capet, Nicolas Levoin, Isabelle Berrebi-Bertrand, Olivia Poupardin, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Thennati Rajamannar, Ranjan Kumar Pal, Biswajit Samanta, Jignesh K. Jivani, Bhavesh M. Panchal, Isha H. Bhatt, Jayraj D. Aradhye
-
Publication number: 20090247638Abstract: The invention provides a method of treating an angiogenesis-mediated ocular disorder, e.g. ocular neovascularisation, retinal neovascularisation, including neovascularisation following injury or infection, retrolental fibroplasias, and neovascular glaucoma, age-related macular degeneration, diabetic retinopathy, pathologic myopia, ocular histoplasmosis, neovascular glaucoma, retinopathy of prematurity, the after effects of corneal transplantation, control of postsurgical ocular inflammation (e.g. after cataract surgery), cystoid macular edema (CME), herpes keratitis, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor of formula I wherein R, R1, R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug esters thereof.Type: ApplicationFiled: June 10, 2009Publication date: October 1, 2009Inventors: Romulus Kimbro Brazzell, George N. Lambrou, Elisabeth Latour, Anna Ottiecz, Jeanette Marjorie Wood
-
Publication number: 20090215899Abstract: A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, cyano group, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and phenyl group, X represents a single bond or oxygen atom, Z represents a phenylene group or a substituted phenylene group, m represents 0 or 1.Type: ApplicationFiled: October 11, 2007Publication date: August 27, 2009Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Youichi YAMAGUCHI, Takeshi YANASE, Susumu MUTO, Akiko ITAI
-
Publication number: 20090163588Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: February 25, 2009Publication date: June 25, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
-
Publication number: 20090149543Abstract: A method of treating a cyclooxygenase-2 dependent disorder or condition comprising administering 5-methyl-2-(2?-chloro-6?-fluoroanilino)phenylacetic acid in an amount effective to treat such a disorder or condition for about 24 hours, comprising administering orally once a day to a human in need of such treatment one or more immediate release pharmaceutical compositions comprising 5-methyl-2-(2?-chloro-6?-fluoroanilino)phenylacetic acid, and compositions suitable for use in such methods.Type: ApplicationFiled: February 6, 2009Publication date: June 11, 2009Inventors: Anees Abdulquadar Karnachi, Maha Y. Khaled, Jurij Holinej, Yatindra Joshi
-
Publication number: 20090131527Abstract: The present invention relates to novel anthranilic acid derivatives represented by Chemical Formula I, and a chloride channel blocking agent containing the anthranilic acid derivative or its pharmacologically acceptable salts as an active ingredient. In another aspect, the present invention relates to a method of accurately and efficiently detecting the intracellular chloride channel inhibition and method of screening a chloride channel blocking agent.Type: ApplicationFiled: January 30, 2008Publication date: May 21, 2009Applicant: Korea Institute of Science and TechnologyInventors: Changjoon Justin Lee, Eun-Joo Roh, Soo-Jin Oh, Jung-Hwan Park, Jae-Kyun Lee
-
Publication number: 20090105300Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.Type: ApplicationFiled: October 17, 2008Publication date: April 23, 2009Inventor: Chih Yung HO
-
Publication number: 20090082452Abstract: The present application describes deuterium-enriched lumiracoxib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Patent number: 7495126Abstract: This invention relates to a method for preparing tetrafluorobenzyl-5-aminosalicylic acid derivative and its pharmaceutically acceptable salt compounds. In particular, this invention relates to a method for preparing tetrafluorobenzyl-5-aminosalicylic acid derivative and its pharmaceutically acceptable salts by using tetrafluorobenzilidine-5-aminosalicylic acid derivative as an intermediate.Type: GrantFiled: May 25, 2006Date of Patent: February 24, 2009Assignee: Choongwae Pharma CorporationInventors: Tae-Seop Hwang, Hyun-Gyu Kim
-
Publication number: 20090018145Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas.Type: ApplicationFiled: October 18, 2005Publication date: January 15, 2009Applicant: Compass Pharmaceuticals LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
-
Publication number: 20090017003Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.Type: ApplicationFiled: March 1, 2007Publication date: January 15, 2009Applicant: SULFIDRIS S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
-
Publication number: 20080249318Abstract: A process for the production of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug ester thereof, comprising cleaving a lactam of formula II wherein the symbols are as defined, with a base; and precursors therefor and processes for the preparation of the precursors. The compounds of Formula I are pharmaceutically active compounds which are selective inhibitors of Cyclooxygenase II.Type: ApplicationFiled: August 16, 2007Publication date: October 9, 2008Inventors: Murat Acemoglu, Thomas Allmendinger, John Vincent Calienni, Jacques Cercus, Olivier Loiseleur, Gottfried Sedelmeier, David Xu
-
Publication number: 20080249175Abstract: A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, cyano group, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and phenyl group, X represents a single bond or oxygen atom, Z represents a phenylene group or a substituted phenylene group, m represents 0 or 1.Type: ApplicationFiled: October 11, 2007Publication date: October 9, 2008Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Youichi YAMAGUCHI, Takeshi YANASE, Susumu MUTO, Akiko ITAI
-
Publication number: 20080234381Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.Type: ApplicationFiled: May 23, 2006Publication date: September 25, 2008Applicant: Novo Nordisk A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Anders Klarskov Petersen, Flemming Elmelund Nielsen, Birgit Sehested Hansen
-
Patent number: 7408078Abstract: The present invention provides pharmaceutical compositions useful in treating hepatitis C infection. The present invention also provides methods of treating hepatitis C infection by administering to a mammal the pharmaceutical compositions of the present invention.Type: GrantFiled: October 8, 2003Date of Patent: August 5, 2008Assignees: Wyeth, ViroPharma IncorporatedInventors: Jonathan D. Bloom, Thomas R. Bailey
-
Patent number: 7378546Abstract: A method for producing 2-amino-5-iodobenzoic acid which comprises bringing 2-aminobenzoic acid (A) and molecular iodine (B) into reaction with each other in the liquid phase in the presence of an oxidizing agent. Hydrogen peroxide is preferable as the oxidizing agent. This method does not require a step for purifying 2-amino-5-iodobenzoic acid or a step for recovering iodine, and 2-amino-5-iodobenzoic acid having excellent quality can be produced economically advantageously with a great yield. The product can be advantageously used as an intermediate for drugs, an agricultural chemical and a raw material for functional chemicals.Type: GrantFiled: August 3, 2005Date of Patent: May 27, 2008Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Kazuhiro Yamada, Norio Fushimi
-
Patent number: 7371867Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: November 6, 2006Date of Patent: May 13, 2008Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
-
Patent number: 7321044Abstract: The invention relates to intermediate products and a new process for the production of benzocycloheptene C. The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.Type: GrantFiled: October 15, 2002Date of Patent: January 22, 2008Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Wolfgang Beckmann, Jens Geisler, Holger Kirstein, Ulrich Niedballa, Eckhard Ottow, Sigmar Radau, Claudia Schulz, Thomas Wessa
-
Patent number: 7202364Abstract: Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3–C6)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted ?-naphthyl, bicyclic heterocyclic aryl, (C3–C6)cycloalkyl-monocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.Type: GrantFiled: November 25, 2003Date of Patent: April 10, 2007Assignee: Novartis, AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Lauren G. Monovich, Benjamin B. Mugrage, David T. Parker, John H. VanDuzer, Sompong Wattanasin
-
Patent number: 7132559Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: February 25, 2002Date of Patent: November 7, 2006Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
-
Patent number: 7115662Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: December 4, 2003Date of Patent: October 3, 2006Assignee: Novartis AGInventors: Roger A Fujimoto, Leslie W McQuire, Benjamin B Mugrage, John H Van Duzer, Daqiang Xu
-
Patent number: 7087778Abstract: Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereofType: GrantFiled: August 23, 2004Date of Patent: August 8, 2006Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kouji Sato, Yoshihiro Takayanagi, Katsuhiko Okano, Keiji Nakayama, Akihiro Imura, Mikihiro Itoh, Tsutomu Yagi, Yukinari Kobayashi, Tomoyuki Nagai
-
Patent number: 7019033Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: December 10, 2002Date of Patent: March 28, 2006Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
-
Patent number: 7015349Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.Type: GrantFiled: March 26, 2003Date of Patent: March 21, 2006Assignee: The Gillette CompanyInventors: Anwar Jardien, Roman Rariy, Gurpreet S. Ahluwalia, Douglas Shander
-
Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
-
Patent number: 6974595Abstract: New pharmaceutical compositions for oral use containing Diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to Diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other side effects; in particular, these formulations permit to obtain in human patients higher Cmax of the active principle and shorter Tmax together with a lower coefficient of variation.Type: GrantFiled: March 14, 2000Date of Patent: December 13, 2005Assignee: ProEthic Pharmaceuticals, Inc.Inventors: Alberto Reiner, Giorgio Reiner
-
Patent number: 6900244Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.Type: GrantFiled: May 23, 2003Date of Patent: May 31, 2005Assignee: Pharmacia CorporationInventors: Jennifer Ann Van Camp, James W. Malecha, Julie M. Miyashiro, Gary A. DeCrescenzo, Joe T. Collins, Monica J. Kalman
-
Patent number: 6831102Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: December 6, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jon J. Hangeland
-
Patent number: 6727281Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: July 23, 2002Date of Patent: April 27, 2004Assignee: Novartis AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
-
Patent number: 6727250Abstract: Carboxylic acid amides of general formula which inhibit telomerase and are useful for treating tumor diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are: (1) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-phenyl)-amide, and, (2) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-4,5-dimethoxy-phenyl)-amide.Type: GrantFiled: January 3, 2002Date of Patent: April 27, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Norbert Hauel, Henning Priepke, Klaus Damm, Andreas Schnapp
-
Patent number: 6686499Abstract: The present invention relates to a method for making 2-N-phenylamino)benzoic acids by coupling a benzoic acid and an aniline using an alkaline metal hexamethyldisilazide as a base.Type: GrantFiled: August 20, 2001Date of Patent: February 3, 2004Assignee: Warner-Lambert CompanyInventors: Michael Huai Gu Chen, Javier Magano
-
Patent number: 6677479Abstract: Compounds of the formula (I) and also process for preparing them where substituents X1, X2, Y and Z are defined as follows: X1 is H or F X2 is H or F Y is CI, Br, or I Z is CHO or COOH or CN n is 0 or 1 and also their use as starting material for preparing agrochemicals, electronics materials and pharmaceuticals.Type: GrantFiled: November 12, 2002Date of Patent: January 13, 2004Assignee: Clariant Finance LBVI LimitedInventors: Wolfgang Schmidt, Rainer Wingen
-
Publication number: 20030162974Abstract: The invention relates to intermediate products and a new process for the production of benzocycloheptene C.Type: ApplicationFiled: October 15, 2002Publication date: August 28, 2003Applicant: Schering AGInventors: Johannes Platzek, Wolfgang Beckmann, Jens Geisler, Holger Kirstein, Ulrich Niedballa, Eckhard Ottow, Sigmar Radau, Claudia Schulz, Thomas Wessa
-
Patent number: 6573252Abstract: The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable of being salified with nitric acid.Type: GrantFiled: January 19, 2001Date of Patent: June 3, 2003Assignee: Nicox, S.A.Inventor: Piero Del Soldato
-
Publication number: 20030009060Abstract: This invention relates to 1,2-di(4-hydroxyaryl)tetrafluoroethanes of the general formula (I) 1Type: ApplicationFiled: May 29, 2002Publication date: January 9, 2003Inventors: Albrecht Marhold, Kathe Baumann
-
Patent number: 6504052Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: November 16, 2001Date of Patent: January 7, 2003Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
-
Patent number: 6451858Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: September 13, 2001Date of Patent: September 17, 2002Assignee: Novartis AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
-
Patent number: 6380256Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 30, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
-
Patent number: 6369270Abstract: Compound of the formula are useful as intermediates to new 4-benzoylisoxazoles.Type: GrantFiled: October 19, 1999Date of Patent: April 9, 2002Assignee: Rhone Poulenc Agriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
-
Patent number: 6310099Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: November 27, 2000Date of Patent: October 30, 2001Assignee: Novartis AgInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
-
Patent number: 6274762Abstract: The invention provides an improved process for the preparation of a compound containing a 2,4,6-triiodinated benzene ring, said process comprising reacting a 2,4,6-unsubstituted 5-amino-benzoic acid or derivative there of with an iodine halide iodinating agent in an aqueous reaction medium, characterised in that the iodinating agent is added to an aqueous medium containing the 5-amino-benzoic acid or derivative at two different temperature ranges: (A) one or more primary portions of the agent are added at a temperature in the range 40 to 70° C. and then one or more secondary portions of the agent are added at a temperature in the range 75 to 95° C. or (B) one or more primary portions of the agent are added at a temperature in the range 75 to 95° C. and then one or more secondary portions of the agent are added at a temperature of 60 to 70° C.Type: GrantFiled: November 12, 1999Date of Patent: August 14, 2001Assignee: Nycomed Imaging ASInventors: Dick Malthe-Sorenssen, Ole Magne Homestad, Britt Sterud
-
Patent number: 6258982Abstract: The present invention relates to a hydrogenation process for the preparation of aromatic amino compounds containing directly on the aryl ring or in a side chain one or more entities that may also undergo hydrogenation, such as carbon multiple bonds, nitrile groups, imino groups or carbonyl groups. The preparation is carried out by catalytic hydrogenation of the corresponding aromatic nitro compounds in the presence of a phosphorus-modified noble metal catalyst. The invention relates also to the use of modified noble metal catalysts for the hydrogenation of aromatic nitro compounds containing carbon multiple bonds and/or substituted by nitrile, imino or carbonyl groups.Type: GrantFiled: March 10, 1999Date of Patent: July 10, 2001Assignee: Novartis AGInventors: Peter Baumeister, Urs Siegrist, Martin Studer
-
Patent number: 6172058Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.Type: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
-
Patent number: 6168913Abstract: The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching “tags” that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.Type: GrantFiled: October 14, 1997Date of Patent: January 2, 2001Assignee: Abbott LaboratoriesInventors: Jill Edie Hochlowski, Thomas J. Sowin, Daniel W. Norbeck, Warren S. Wade, David N. Whittern
-
Patent number: 6137003Abstract: The present invention relates to bis(haloethyl)aminobenzene derivatives featured by having carboxyl-containing moiety and one other moiety at the ortho position with respect to the bis(haloethyl)amino substituent of the benzene ring. The moiety at the ortho position can be alkyl, cycloalkyl, heterocycloalkyl, aryl heteroaryl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), alkyl(heteroaryl), alkyl(aryl), --(--O-alkyl).sub.2-5 or --Y.sup.1 --Y.sup.2 in which Y.sup.1 is O, S, or N(R.sup.5) wherein R.sup.5 is hydrogen or alkyl, and Y.sup.2 is alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroacryl, alkyl(cycloalkyl), alkyl(hetero-cycloalkyl), alkyl(aryl), or alkyl(heteroaryl).Type: GrantFiled: October 28, 1998Date of Patent: October 24, 2000Assignee: Shionogi BioResearchInventors: Mitsunori Ono, Keizo Koya, Lijun Sun, Wojciech Wrona, Sylvia Holden, Noriaki Tatsuta
-
Patent number: 6127392Abstract: Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: October 3, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
-
Patent number: 6114386Abstract: A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HANBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.Type: GrantFiled: October 14, 1997Date of Patent: September 5, 2000Assignee: University of AlabamaInventors: Ming Luo, Clinton L. White
-
Patent number: 6096921Abstract: The invention relates to novel o-aminophenolcarboxylic acids, and o-aminothiophenolcarboxylic acids of the following structure: ##STR1## where A.sup.1 to A.sup.7 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.3 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: September 1, 1999Date of Patent: August 1, 2000Assignee: Siemens AktiengesellschaftInventors: Recai Sezi, Michael Keitmann
-
Patent number: 5945556Abstract: A process for preparing N-carboxymethylene-4-chloroanthranilic acid, and its dialkyl esters. The invention relates to a process for preparing N-carboxymethylene-4-chloroanthranilic acid and its dialkyl esters, which comprises reacting 2,4-dichlorobenzoic acid in the presence of a base, of a solvent and of a catalyst with glycine to give N-carboxymethylene-4-chloroanthranilic acid and, where appropriate, reacting the latter in the presence of a base and of a solvent with a dialkyl sulfate, dialkyl carbonate or alkyl halide to give the dialkyl ester.Type: GrantFiled: April 14, 1998Date of Patent: August 31, 1999Assignee: Clariant GmbHInventors: Theodor Papenfuhs, Ralf Pfirmann, Stefan Krause, Doris Neumann-Grimm
-
Patent number: 5916922Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: November 24, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron