Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/561)
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Publication number: 20030153508Abstract: An N-containing five-membered ring compound of formula (I) 1Type: ApplicationFiled: July 23, 2002Publication date: August 14, 2003Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Publication number: 20030153596Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: July 9, 2002Publication date: August 14, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
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Publication number: 20030149083Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents for various diseases concerning &agr; 4 integrin.Type: ApplicationFiled: May 20, 2002Publication date: August 7, 2003Applicant: AJINOMOTO CO. INCInventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Publication number: 20030130520Abstract: A method of producing a compound of formula 1Type: ApplicationFiled: August 22, 2002Publication date: July 10, 2003Inventor: Peter Maienfisch
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Publication number: 20030130322Abstract: The present invention relates to a method of treating alcoholism or alcohol dependence in a mammal, including a human, by administering to the mammal a monoamine reuptake inhibitor in combination with an opioid antagonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a monoamine reuptake inhibitor and an opioid antagonist.Type: ApplicationFiled: May 22, 2002Publication date: July 10, 2003Applicant: Pfizer Inc.Inventor: Harry R. Howard
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Publication number: 20030125563Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.Type: ApplicationFiled: October 15, 2002Publication date: July 3, 2003Inventors: Stephen L. Buchwald, Daniel H. Appella, Yasunori Moritani, Ryo Shintani, Valdas Jurkauskas
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Patent number: 6583182Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.Type: GrantFiled: November 30, 2001Date of Patent: June 24, 2003Assignee: Chelator LLCInventors: Harry S Winchell, Joseph Y Klein, Elliot D Simhon, Rosa L Cyjon, Ofer Klein, Haim Zaklad
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Publication number: 20030114496Abstract: Novel sulphones of formula I are disclosed: 1Type: ApplicationFiled: August 20, 2002Publication date: June 19, 2003Inventors: Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams, Brian John Williams
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Publication number: 20030092747Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: June 13, 2002Publication date: May 15, 2003Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Publication number: 20030087939Abstract: Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): 1Type: ApplicationFiled: October 23, 2002Publication date: May 8, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Eugene Richard Hickey, Weimin Liu, David S.. Thomson
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Publication number: 20030087945Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 13, 2002Publication date: May 8, 2003Applicant: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6555711Abstract: Disclosed is a process comprising reacting an N-allylimino nitrobenzene compound with a diaminodinucleophile to form an &agr;-amino-N-allylamidino nitrobenzene compound and the compound itself.Type: GrantFiled: September 18, 2002Date of Patent: April 29, 2003Assignee: Eastman Kodak CompanyInventors: Robert J. Niger, William B. Vreeland
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Patent number: 6545153Abstract: An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.Type: GrantFiled: July 18, 2002Date of Patent: April 8, 2003Assignee: Warner-Lambert CompanyInventors: Donald Eugene Butler, Randall Lee Dejong, Jade Douglas Nelson, Michael Gerard Pamment, Timothy Lee Stuk
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Patent number: 6541632Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.Type: GrantFiled: June 19, 2002Date of Patent: April 1, 2003Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
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Patent number: 6538016Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Publication number: 20030045726Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: ApplicationFiled: September 13, 2002Publication date: March 6, 2003Inventors: George W. Muller, Mary Shire
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Publication number: 20030040625Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstitutedpropanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: ApplicationFiled: August 29, 2002Publication date: February 27, 2003Inventor: Ibert Clifton Wells
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Publication number: 20030036660Abstract: A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound N-2-bromoethylpyrrole.Type: ApplicationFiled: September 3, 2002Publication date: February 20, 2003Inventors: Douglas C. Caskey, John R. Duchek, Henry J. Buehler
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Patent number: 6521626Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates theType: GrantFiled: March 23, 1999Date of Patent: February 18, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Patent number: 6521787Abstract: The non-hydrated gabapentin polymorph is prepared by drying an aqueous solution of gabapentin by spray drying or turbo-drying and it is used for the preparation of pharmaceutical grade gabapentin by subjecting the polymorph to crystallisation from solvents.Type: GrantFiled: November 21, 2000Date of Patent: February 18, 2003Assignee: Medichem, S.A.Inventors: Jordi Bosch Lladó, Rafael García Cruz, Elias Molins Grau, Maria del Carmen Onrubia Miguel
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6518429Abstract: The present invention relates to novel imidazole derivatives which show an inhibitory activity against farnesyl transferase, pharmaceutically acceptable salts or isomers thereof and pharmaceutical compositions comprising such imidazole derivatives. More particularly, the present invention relates to intermediate compounds which are used in the preparation of the imidazole derivatives of the invention. Related processes also are disclosed.Type: GrantFiled: March 20, 2001Date of Patent: February 11, 2003Assignee: LG Chemical, Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6512121Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 11, 2001Date of Patent: January 28, 2003Assignee: G.D. Searle & Co.Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20030018057Abstract: Novel thiol derivatives of formula I 1Type: ApplicationFiled: June 13, 2002Publication date: January 23, 2003Inventors: Cynthia Anne Fink, Faribroz Firooznia
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Publication number: 20030018203Abstract: Novel calcilytic compounds and methods of using them are provided.Type: ApplicationFiled: July 17, 2002Publication date: January 23, 2003Inventors: Maria Amparo Largo, James Francis Callahan, Pradip Kumar Bhatnagar, Eric G. Del Mar, William M. Bryan, Joelle L. Burgess
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Publication number: 20030008996Abstract: A radical polymerizable compound comprising a structure represented by the following formula (I), (II) or (III): 1Type: ApplicationFiled: March 14, 2002Publication date: January 9, 2003Inventor: Kazuto Kunita
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Patent number: 6492394Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.Type: GrantFiled: December 22, 1999Date of Patent: December 10, 2002Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
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Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020137945Abstract: A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound N-2-bromoethylpyrrole.Type: ApplicationFiled: February 5, 2002Publication date: September 26, 2002Inventors: Douglas C. Caskey, John R. Duchek, Henry J. Buehler
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Patent number: 6441177Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.Type: GrantFiled: December 16, 1999Date of Patent: August 27, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
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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: 6426355Abstract: Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: September 27, 2000Date of Patent: July 30, 2002Assignee: American Home ProductsInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
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Patent number: 6420427Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6417372Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.Type: GrantFiled: April 2, 2001Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
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Publication number: 20020077486Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 2, 2001Publication date: June 20, 2002Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6380358Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.Type: GrantFiled: December 1, 1999Date of Patent: April 30, 2002Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Konrad Feichtinger, Todd T. Romoff
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Patent number: 6380429Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.Type: GrantFiled: September 15, 2000Date of Patent: April 30, 2002Assignee: E. I. du Pont Nemours and CompanyInventor: Eric Maurice Smith
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Publication number: 20020049338Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.Type: ApplicationFiled: September 20, 2001Publication date: April 25, 2002Applicant: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6376681Abstract: This invention relates to the drug, ketorolac and the synthesis of compounds useful in the manufacture of ketorolac. Ketorolac tromethamine is a pharmaceutical compound useful as an analgesic.Type: GrantFiled: December 6, 2000Date of Patent: April 23, 2002Assignee: Mallinckodt Inc.Inventors: John R. Duchek, Henry J. Buehler, Douglas C. Caskey
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Patent number: 6362230Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: November 21, 2000Date of Patent: March 26, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Publication number: 20020028945Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: June 11, 2001Publication date: March 7, 2002Inventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffrey S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6353017Abstract: N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.Type: GrantFiled: August 22, 2000Date of Patent: March 5, 2002Assignee: Novartis AGInventors: Eva Altmann, Claudia Betschart, Keigo Gohda, Miyuki Horiuchi, Rene Lattmann, Martin Missbach, Junichi Sakaki, Michihiro Takai, Naoki Teno, Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry van Duzer
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Publication number: 20020019422Abstract: The present invention relates to novel cycloalkylalkanecarboxamides of the formula I 1Type: ApplicationFiled: May 31, 2001Publication date: February 14, 2002Inventors: Frank Wetterich, Karl Eicken, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Ingo Rose
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Patent number: 6331640Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 29, 1999Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6320059Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acrid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: March 7, 2000Date of Patent: November 20, 2001Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6319939Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkType: GrantFiled: June 1, 2000Date of Patent: November 20, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Publication number: 20010041709Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: January 26, 2001Publication date: November 15, 2001Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson