Plural Double Bonds Between The Ring Members Of The Oxazole Ring Patents (Class 548/235)
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Patent number: 6380213Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: November 17, 2000Date of Patent: April 30, 2002Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
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Patent number: 6372915Abstract: The present invention relates to a method for producing a compound of the formula [7] wherein R1 is an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted heterocyclic group, R2 is a lower alkyl or a halogenated lower alkyl and R3 is a halogen atom or a hydrogen atom. The method of the present invention includes reacting compound [1] with thionyl chloride to give compound [2] and obtaining the objective compound [7] at a high yield via intermediate [5], and is utilizable for industrial production.Type: GrantFiled: March 2, 2001Date of Patent: April 16, 2002Assignee: Japan Tobacco Inc.Inventors: Koji Matsuda, Katsuyoshi Hara, Minoru Akamatsu
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Patent number: 6372895Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: July 7, 2000Date of Patent: April 16, 2002Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Publication number: 20020042520Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) 1Type: ApplicationFiled: May 22, 2001Publication date: April 11, 2002Inventors: Yijun Deng, Dennis Hlasta
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Biphenylsulfonyl cyanamides, method for the production thereof and their utilization as a medicament
Patent number: 6369069Abstract: The invention relates to compounds of the formula (I), in which the symbols have the following meaning: R(1) is 1. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; 2. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, in which one to all hydrogen atoms are replaced by fluorine; 3. alkenyl having 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 carbon atoms; or 4. —CnH2n−nn—Y, nn is zero or 2; and n is zero, 1, 2, 3 or 4; where n is unequal to zero or 1 if nn is equal to 2; 5. —CnH2n−nn—Y, nn is zero or 2; and n is 1, 2, 3 or 4; where n is unequal to 1 if nn is equal to 2.Type: GrantFiled: August 4, 2000Date of Patent: April 9, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Sabine Faber, Hans-Willi Jansen, Stefan Petry -
Patent number: 6365738Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.Type: GrantFiled: June 29, 1999Date of Patent: April 2, 2002Assignee: Reilly Industries, Inc.Inventors: Ramiah Murugan, Eric F. V. Scriven
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Patent number: 6362166Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: October 13, 2000Date of Patent: March 26, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Siegfried H. Reich, Thomas L. Little, Jr., Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine, Ted M. Bleckman
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Patent number: 6362209Abstract: A heterocyclic aromatic oxazole compound of the formula (I) wherein Z is an oxygen atom; one of R and R1 is a group of the formula wherein R3 is lower alkyl, amino or lower alkylamino, and R4, R5, R6 and R7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R4, R5, R6 and R7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 17, 1999Date of Patent: March 26, 2002Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Publication number: 20020035265Abstract: A 5-(2-substituted-4-nitrophenyl)-oxazole is prepared by decarboxylating a 5-(2-substituted-4-nitrophenyl)-4-oxazolecarboxylic acid in an aprotic amide solvent containing a protic compound. A 5-(2-substituted-4-nitrophenyl)-oxazolecarboxylic acid and a 5-(2-substituted-4-nitrophenyl)-carboalkoxyoxazole, which are novel compounds, are provided.Type: ApplicationFiled: December 26, 2000Publication date: March 21, 2002Applicant: THE NIPPON SYNTHETIC CHEMICAL INDUSTRY CO., LTD.Inventors: Akio Katsuura, Azusa Yonezawa, Keisuke Tsuzuki, Kazumasa Hirata
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Publication number: 20020032226Abstract: This invention is directed to an amorphous 5-(4-aminosulfonyl-3-fluorophenyl)-4-cyclohexyl-2-methyloxazole compound, substantially free of crystals, methods for preparing the compound and pharmaceutical compositions containing the compound.Type: ApplicationFiled: May 25, 2001Publication date: March 14, 2002Inventors: Thomas W. Schultz, Daniel Korey
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Patent number: 6355662Abstract: Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.Type: GrantFiled: October 26, 1999Date of Patent: March 12, 2002Assignee: Pfizer IncInventors: Allen Jacob Duplantier, Anthony John Milici, Louis Stanley Chupak
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Patent number: 6340694Abstract: The diarylbenzopyran derivatives represented by formula I, and the pharmaceutically acceptable salts thereof, are disclosed. The composition comprising the compound of formula I, or a pharmaceutically acceptable salt thereof, shows an excellent selective inhibition of cyclooxygenase-2.Type: GrantFiled: February 20, 2001Date of Patent: January 22, 2002Assignee: Pacific CorporationInventors: Yung Hyup Joo, Chang Hoon Lee, Min-Soo Noh, Jun-Yong Ha, Jin Kyu Choi, Kyung Min Lim, Jin Kwan Kim, Seon-Hwa Kang
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Patent number: 6333414Abstract: A process for the preparation of oxazoles of formula (II): by reaction of thiourea with the corresponding diketone ester.Type: GrantFiled: October 26, 2000Date of Patent: December 25, 2001Assignee: L'Oréal S.A.Inventors: Maria Dalko, Jacqueline Dumats
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Patent number: 6333416Abstract: An (oxazolin-4-yl)oxirane derivative of formula [IX] wherein R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl or an optionally substituted heteroarylalkyl, an enantiomer thereof or a salt thereof.Type: GrantFiled: April 17, 2001Date of Patent: December 25, 2001Assignees: Japan Tobacco Inc., Agouron Pharmaceuticals, Inc.Inventors: Takashi Inaba, Yasuki Yamada
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Publication number: 20010053774Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.Type: ApplicationFiled: December 14, 2000Publication date: December 20, 2001Applicant: GLAXO WELLCOME INC..Inventor: Timothy Mark Willson
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Patent number: 6331636Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.Type: GrantFiled: March 12, 1992Date of Patent: December 18, 2001Assignee: The Upjohn CompanyInventors: Arthur G. Romero, William H. Darlington
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Patent number: 6329371Abstract: A compound represented by the formula (I): wherein R1 is an optionally substituted heterocyclic group; R2 is optionally substituted aryl or heterocyclic group; R3 is hydrogen, alkyl, alkenyl, or alkynyl; R4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O)i wherein i is 0, 1, or 2, NR5 wherein R5 is hydrogen, alkyl, or acyl, —Q—N═C(R6)—, —B—C(R8)═N—, —CH═N—N═C(R9)—, or —CH═N—A—(CR10R11)m—; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.Type: GrantFiled: June 14, 2000Date of Patent: December 11, 2001Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
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Patent number: 6329408Abstract: Optically pure thiazolidinedione alcohols and ethers, and synthetic intermediates for preparing said alcohols and ethers. These compounds have utility as hypoglycemic and hypocholesterolemic agents.Type: GrantFiled: June 1, 1995Date of Patent: December 11, 2001Assignee: Pfizer Inc.Inventor: David A. Clark
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Patent number: 6329421Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: February 25, 1997Date of Patent: December 11, 2001Assignee: Merck Frosst Canada & Co.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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Publication number: 20010047019Abstract: The present invention describes compounds of formula I 1Type: ApplicationFiled: February 6, 2001Publication date: November 29, 2001Inventors: Mark E. Salvati, S. David Kimball
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Publication number: 20010041715Abstract: This invention provides substituted compounds of the general formulae: 1Type: ApplicationFiled: March 2, 2001Publication date: November 15, 2001Inventors: Michael S. Malamas, Richard E. McDevitt, Folake O. Adebayo
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Publication number: 20010039352Abstract: The present invention relates to a novel method for producing a compound of the formula [11] 1Type: ApplicationFiled: April 23, 2001Publication date: November 8, 2001Inventors: Koji Ando, Masanobu Suzuki
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Patent number: 6313308Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates therof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension, congestive heart failure and male erectile dysfunction.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Ambarish Singh, Chien-Kuang Chen, John A. Grosso, Edward J. Delaney, Xuebao Wang, Richard P. Polniaszek, John K. Thottathil
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Patent number: 6300357Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 9, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Patent number: 6300344Abstract: Heterocyclic compounds of the formula: wherein R1 is carboxy or protected carboxy, R2 is aryl which may have suitable substituent(s), R3 is aryl which may have suitable substituent(s), R4 is hydrogen, lower alkyl, hydroxy or aryl, A1 is lower alkylene, etc., etc. and n is 0 or 1, and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: July 20, 1999Date of Patent: October 9, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Kouji Hattori, Kazunori Tsubaki, Osamu Okitsu, Seiichiro Tabuchi
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Patent number: 6297267Abstract: A compound of the formula: wherein R1 is a hydrogen atom or a carboxy protective group, R2, R5, R6 and R7 are each a hydrogen atom or a hydroxy group, R3 and R4 are each a hydrogen atom, or are combined together to form an epoxy group or a single bond. R8 and R9 are each an optionally substituted aryl group, and X is a single bond or a methylene group, in addition to the above definitions. R2 and R3 may be combined together to form a single bond; provided that when R2, R5, R6 and R7 are each a hydrogen atom, then R3 and R4 are combined together to form an epoxy group; when R3 and R4 are combined together to form a single bond, then at least one of R2, R5, R6 and R7 is a hydroxy group and the others are hydrogen; and when R3 and R4 are each a hydrogen atom, then at least one of R2, R5, R6 and R7 is a hydroxy group and the others are hydrogen, and X is a methylene group, or its salt.Type: GrantFiled: April 26, 2000Date of Patent: October 2, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Naoaki Fujii, Akira Tanaka, Fujiko Takamura
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Patent number: 6271385Abstract: N-heterocyclicmethylpropylamine derivatives of formula (I): and acid addition salts thereof; wherein R1 represents hydrogen, halogen, alkyl, alkenyl, halogenated alkyl, alkoxy, halogenated alkoxy, hydroxyl, cyano, nitro, phenyl optionally having a substituent on a ring thereof or phenoxy; n represents an integer of 0-5; R2 represents a heterocycle containing at least one nitrogen atom as the hetero atom and optionally having a substituent on a ring thereof; and R3 represents hydrogen or C1-C5 alkyl.Type: GrantFiled: March 10, 2000Date of Patent: August 7, 2001Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Atsushi Ito, Satoru Kumazawa, Keiichi Sudo, Tsumoru Watanabe, Takayoshi Eizuka, Yoshitaka Niizeki
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Patent number: 6268313Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 7, 2000Date of Patent: July 31, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6268391Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.Type: GrantFiled: April 7, 2000Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal
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Patent number: 6255327Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: April 13, 1999Date of Patent: July 3, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Michael Brenner, Wolf-Dietrich Bechtel, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini
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Patent number: 6251926Abstract: This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.Type: GrantFiled: November 15, 1999Date of Patent: June 26, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Patent number: 6245790Abstract: Azole compounds of the formula: wherein R1 is lower alkyl substituted with carboxy, etc., R2 is hydrogen or lower alkyl, R3 is aryl, etc. R4 is aryl, etc. Q is etc., and X is O, NH or S, and its salt, which are useful as medicament.Type: GrantFiled: March 8, 2000Date of Patent: June 12, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Osamu Okitsu, Naoaki Fujii, Akira Tanaka, Kiyoshi Taniguchi, Satoshi Koyama, Mie Nishio
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Patent number: 6214799Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: January 7, 1999Date of Patent: April 10, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Siegfried H. Reich, Thomas L. Little, Jr., Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine, Ted M. Bleckman
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Patent number: 6211215Abstract: Heterocyclic compounds represented by the general formula (I) wherein R stands for an optionally substituted aromatic heterocyclic group; X stands for oxygen atom, an optionally oxidated sulfur atom, —C(═O)— or —CH(OH)—; Y stands for CH or N; m denotes an integer of 0 to 10: n denotes an integer of 1 to 5: cyclic group stands for an optionally substituted aromatic azole group; and ring A is optionally further substituted, or salts thereof. The compound (I) possesses action of inhibiting tyrosine kinase and useful as antitumor agents.Type: GrantFiled: November 18, 1998Date of Patent: April 3, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Etsuya Matsutani
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Patent number: 6194446Abstract: This invention provides compounds and their pharmaceutically-acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.Type: GrantFiled: December 18, 1998Date of Patent: February 27, 2001Assignee: Eli Lilly and CompanyInventors: Samuel James Dominianni, Margaret Mary Faul, Russell Dean Stucky, Leonard Larry Winneroski, Jr.
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Patent number: 6174883Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: June 7, 1995Date of Patent: January 16, 2001Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 6165944Abstract: 4-(3-Heterocyclyl-1-benzoyl)pyrazoles of the formula I ##STR1## where: R.sup.1 and R.sup.3 are each hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, N-alkylaminosulfonyl, N,N-dialkyl)aminosulfonyl, N-alkylsulfonylamino, N-haloalkylsulfonylamino, N-alkyl-N-alkylsulfonylamino or N-alkyl-N-haloalkylsulfonylamino;R.sup.2 is a 5- or 6-membered heterocyclyl radical with or without substitution which comprises 1 to 4 identical or different hetero atoms from the following group: oxygen, sulfur or nitrogen;R.sup.4 is hydrogen, halogen or alkyl;R.sup.5 is substituted pyrazole which is attached in position 4;and agriculturally useful salts thereof; processes for preparing the 4-(3-heterocyclyl-1-benzoyl)pyrazoles; compositions comprising them; and the use of these derivatives or these compositions comprising them for controlling undesirable plants.Type: GrantFiled: June 16, 1998Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Ernst Baumann, Stefan Engel, Guido Mayer, Joachim Rheinheimer, Matthias Witschel, Ulf Misslitz, Oliver Wagner, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6156748Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: October 6, 1997Date of Patent: December 5, 2000Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
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Patent number: 6150532Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: December 11, 1998Date of Patent: November 21, 2000Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Patent number: 6147220Abstract: This invention provides a process for the preparation of a 5-methylene-1,3-oxazoline from an alkyl ketone by reacting the alkyl ketone with an acetylating agent and an acid catalyst in an appropriate solvent and at an appropriate temperature. The resulting 5-methylene-1,3-oxazoline can be chlorinated and subsequently hydrolyzed to form an .alpha.-chloroketone which is useful as a fungicide.Type: GrantFiled: May 15, 1998Date of Patent: November 14, 2000Assignee: Rohm and Haas CompanyInventors: Renee Caroline Roemmele, Heather Lynnette Rayle
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Patent number: 6143790Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
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Patent number: 6133303Abstract: The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).Type: GrantFiled: August 2, 1999Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6118007Abstract: A process, as a substitute for hydrolysis, for preparing a nitroguanidine derivative represented by the following formula (2): ##STR1## wherein A represents a substituted or unsubstituted aromatic or non-aromatic hydrocarbon ring, a substituted or unsubstituted aromatic or non-aromatic heterocycle, a hydrogen atom or a substituted or unsubstituted alkyl, alkenyl or alkynyl group; and R.sub.2 represents a hydrogen atom, a substituted or unsubstituted C.sub.1-6 alkyl, alkenyl or alkynyl group, which comprises reacting a compound represented by the following formula (1): ##STR2## wherein R.sub.1 represents a substituted or unsubstituted, linear or cyclic C.sub.1-10 alkyl group and A and R.sub.2 have the same meanings as defined above, with ammonia, a primary amine or a secondary amine, or a salt thereof.Type: GrantFiled: March 24, 1998Date of Patent: September 12, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Koichi Ebihara, Tatsuo Kaiho, Michihiko Miyamoto, Daisuke Ura
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Patent number: 6096688Abstract: The novel compounds of formula I: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meaning given in claim 1, and herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: December 22, 1997Date of Patent: August 1, 2000Assignee: American Cyanamid CompanyInventors: Trevor Newton, Isabel Waldeck
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Patent number: 6090834Abstract: A class of substituted oxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R is selected from halo, mercapto, hydroxyl, lower carboxyalkylthio, lower haloalkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkoxy, aryloxy, lower alkylamino, aminocarbonyl, lower alkoxyalkyl, and lower carboxy(haloalkyl); wherein R.sup.2 is selected from lower alkyl and amino; and wherein R.sup.4 is selected from hydrido, lower alkyl, lower alkylamino, lower alkoxy and halo; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: December 1, 1998Date of Patent: July 18, 2000Assignee: G.D. Searle & Co.Inventors: John J Talley, Stephen R Bertenshaw, Donald J Rogier, Jr., Matthew J Graneto
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Patent number: 6077864Abstract: A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: June 17, 1999Date of Patent: June 20, 2000Assignee: Pfizer Inc.Inventors: Laurence Edward Burgess, James Patrick Rizzi
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Patent number: 6060606Abstract: An optical recording medium having at least a recording layer and a reflective layer on a substrates, the said recording layer contains a dipyrromethene metal chelate compound obtained from a dipyrromethene compound represented by the general formula (1) and a metal ion: ##STR1## wherein R.sup.1 to R.sup.7 are defined in the specification.Type: GrantFiled: April 14, 1999Date of Patent: May 9, 2000Assignees: Mitsui Chemicals, Inc., Yamamoto Chemicals, Inc.Inventors: Tsutami Misawa, Kenichi Sugimoto, Taizo Nishimoto, Hisashi Tsukahara, Takeshi Tsuda, Keisuke Takuma, Hideki Umehara
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Patent number: 6057347Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: September 16, 1997Date of Patent: May 2, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam