Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
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Publication number: 20020099207Abstract: The invention relates to compounds of the formula 1Type: ApplicationFiled: October 15, 2001Publication date: July 25, 2002Inventor: Heinz Stadler
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Patent number: 6410482Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.Type: GrantFiled: May 13, 1997Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6410483Abstract: Compounds of the formula (I) and salts thereof in which R1-R9, W and A are as defined in formula (I) of claim 1 are suitable as herbicides and plant growth regulators. They can be prepared by processes according to claim 5 via intermediates according to claim 9, some of which are novel.Type: GrantFiled: January 21, 1998Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6403582Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.Type: GrantFiled: January 12, 2001Date of Patent: June 11, 2002Assignee: Schering CorporationInventors: Gregory A. Reichard, Neng-Yang Shih, Dasong Wang
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Patent number: 6395897Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: November 5, 1999Date of Patent: May 28, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Leah L. Frye, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6380387Abstract: Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: November 21, 2000Date of Patent: April 30, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6372741Abstract: The present invention is to the novel use of a cytokine inhibitor, which cytokine is inhibited by the inhibition of the kinase CSBP/p38/RK, for the treatment of chronic diseases which are caused by excessive, undesired or inappropriate angiogenesis.Type: GrantFiled: September 8, 1998Date of Patent: April 16, 2002Assignee: SmithKline Beecham CorporationInventors: Jeffrey R. Jackson, James D. Winkler
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Patent number: 6331506Abstract: Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which R1 to R6, W, X, Y, Z are as defined in claim 1 and the group R2R3C is a carbon atom which is subsituted by at least one electron-withdrawing radical R2 or R3 are suitable as herbicides and plant growth regulators. They can be prepared in accordance with known processes via intermediates, some of which are novel.Type: GrantFiled: September 16, 1998Date of Patent: December 18, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6294535Abstract: The invention relates to novel uracil derivatives having excellent inhibiting effects on human derived thymidine phosphorylates and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators and antitumor agents containing such novel compounds, and a process for their preparation and use are described.Type: GrantFiled: December 9, 1999Date of Patent: September 25, 2001Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shingo Yano, Yukio Tada, Hideki Kazuno, Tsutomu Sato, Junichi Yamashita, Norihiko Suzuki, Tomohiro Emura, Masakazu Fukushima, Tetsuji Asao
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Patent number: 6294542Abstract: The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.Type: GrantFiled: December 20, 1999Date of Patent: September 25, 2001Assignee: Boryung Pharmaceutical Co. Ltd.Inventors: Jae-hyoung Lee, Kyung-jin Jang, Byoung-wug Yoo, Ji-han Kim, Jae-seog Kang, Sang-lin Kim
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Patent number: 6218376Abstract: Compounds of formula I or salts thereof where for example Y is a group of the formula (i) and R1 is a group of formula (ii) are provided along with compositions containing them and processes for their preparation. The compounds are P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists, and are useful in the treatment of inflammatory conditions.Type: GrantFiled: December 9, 1998Date of Patent: April 17, 2001Assignee: AstraZeneca UK LimitedInventors: Nicholas Kindon, Premji Meghani, Stephen Thom
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Patent number: 6218537Abstract: 1,4,5,-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: May 13, 1998Date of Patent: April 17, 2001Assignee: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Timothy Francis Gallagher, Joseph Sisko, Irennegbe Kelly Osifo, Jeffrey Charles Boehm
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Patent number: 6204265Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.Type: GrantFiled: December 21, 1999Date of Patent: March 20, 2001Assignee: Schering CorporationInventors: Gregory A. Reichard, Neng-Yang Shih, Dasong Wang
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6165942Abstract: A compound represented by the general formula (I) and a salt thereof: ##STR1## wherein: Rf represents a (C.sub.1 -C.sub.4)haloalkyl group; X.about.Y represents N.dbd.N or CH.dbd.N or the like; A represents a nitrogen atom or CH; Z represents an oxygen or sulfur atom; Rg represents a hydrogen or halogen atom and the like; R1, R2, R3, R4 and R5 are each independently represent a hydrogen or halogen atom or a nitro or cyano group or the like.Type: GrantFiled: April 1, 1999Date of Patent: December 26, 2000Assignee: Nissan Chemical Industries, Ltd.Inventors: Jun Satow, Yoshihiro Kudo, Eitatsu Ikeda, Tsutomu Nawamaki, Chiaki Kawaguchi
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Patent number: 6159969Abstract: The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described.Type: GrantFiled: January 12, 1998Date of Patent: December 12, 2000Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shingo Yano, Yukio Tada, Hideki Kazuno, Tsutomu Sato, Junichi Yamashita, Norihiko Suzuki, Tomohiro Emura, Masakazu Fukushima, Tetsuji Asao
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Patent number: 6136971Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.Type: GrantFiled: July 15, 1999Date of Patent: October 24, 2000Assignee: Roche Colorado CorporationInventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 6133442Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.Type: GrantFiled: March 5, 1999Date of Patent: October 17, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 6124306Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: September 21, 1998Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
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Patent number: 6100257Abstract: Novel pyrimidin-4-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl optionally substituted with halogen; R.sup.3 is alkyl optionally substituted with halogen, alkenyl, or alkynyl; and Q is substituted phenyl. Also provided are intermediates for their production and processes for producing these intermediates.Type: GrantFiled: February 10, 1998Date of Patent: August 8, 2000Assignee: Sumitomo Chemical Company, Ltd.Inventors: Masayuki Enomoto, Hisayuki Hoshi, Yuzuru Sanemitsu
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Patent number: 6096753Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 4, 1997Date of Patent: August 1, 2000Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
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Patent number: 6087368Abstract: Novel quinazolinone compounds, methods of using such compounds in the treatment of cGMP-associated conditions such as erectile dysfunction, and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 28, 1999Date of Patent: July 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: John E. Macor, David P. Rotella, Harold N. Weller, III, David W. Cushman, Joseph P. Yevich
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Patent number: 6083945Abstract: Disclosed are cyclic urea-containing compounds that are useful as antiarrhythmic and/or antifibrillatory agents. These compounds have the following structure: ##STR1## where X and Y are each independently selected from various cyclic moieties; R.sub.5 is a substituted or unsubstituted C.sub.2 alkyl (thus providing a 6-membered cyclic urea); and R.sub.1, R.sub.2, R.sub.3, R.sub.4, L, and A are as defined in the specification. Also disclosed are compositions containing the compounds and methods of treating humans or other mammals afflicted with cardiac arrhythmias and/or cardiac fibrillation by administration of the compounds/compositions.Type: GrantFiled: September 10, 1997Date of Patent: July 4, 2000Assignee: The Procter & Gamble CompanyInventors: Stanford Salvatore Pelosi, Jr., Chia-Nien Yu
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Patent number: 6080738Abstract: A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and a pharmaceutical use thereof. The heterocyclic amide compound and a pharmacologically acceptable salt thereof of the present invention have superior inhibitory action on chymase group in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be used for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.Type: GrantFiled: April 22, 1999Date of Patent: June 27, 2000Assignee: Yoshitomi Pharmaceuticals Industries, Ltd.Inventors: Fumihiko Akahoshi, Atsuyuki Ashimori, Takuya Yoshimura, Masahiro Eda, Hiroshi Sakashita, Masahide Nakajima, Teruaki Imada
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Patent number: 5990150Abstract: Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.Type: GrantFiled: March 19, 1997Date of Patent: November 23, 1999Assignee: Sankyo Company, Ltd.Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura, Katsuo Wada
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Patent number: 5981537Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: May 9, 1996Date of Patent: November 9, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 5962682Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.Type: GrantFiled: August 18, 1997Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 5948785Abstract: Heterocyclic amide compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.Type: GrantFiled: October 27, 1997Date of Patent: September 7, 1999Assignee: The Green Cross CorporationInventors: Fumihiko Akahoshi, Takuya Yoshimura, Masahiro Eda, Atsuyuki Ashimori, Hajime Fukuyama, Masahide Nakajima, Teruaki Imada, Hideki Okunishi, Mizuo Miyazaki
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Patent number: 5922646Abstract: Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators. Compounds of the formula (I) and salts thereof ##STR1## in which W.sup.1, W.sup.2, R, n, R.sup.1, R.sup.2, R.sup.4, X, Y and Z are as defined in claim 1 and R.sup.3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.Type: GrantFiled: August 4, 1997Date of Patent: July 13, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5922645Abstract: Compounds of the formula (I) and salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties.They can be prepared by processes analogous to known processes (cf. claim 5), in some cases via novel intermediate products (cf.Type: GrantFiled: November 22, 1995Date of Patent: July 13, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 5883092Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## ?wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient.Type: GrantFiled: March 4, 1998Date of Patent: March 16, 1999Assignee: Kowa Co., Ltd.Inventors: Mitsuteru Hirata, Takeo Deushi, Yoshio Takahashi, Masahiro Tamura, Takeshi Ohshima, Toshiaki Oda, Tetsuya Ishikawa, Hiroyuki Sonoki, Masami Shiratsuchi
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Patent number: 5877312Abstract: This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.Type: GrantFiled: December 31, 1996Date of Patent: March 2, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Prabhakar Kondaji Jadhav, George Clautice Emmett, Michael Ernest Pierce
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Patent number: 5869476Abstract: The invention relates to pyrimidinone derivatives and the pharmaceutically acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, and thus useful in treating cardiovascular diseases caused by angiotensin II.Type: GrantFiled: April 25, 1997Date of Patent: February 9, 1999Assignee: Boryung Pharmaceutical Co., Ltd.Inventors: Woo Hyun Paik, Ji Han Kim, Jae Hyoung Lee, Kyung Jin Jang, Kwang Jae Cho, Jae Seog Kang, Byoung Wug Yoo, Je Bum Park, Kyung Jin Kim, Kun Ja Lee
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Patent number: 5866583Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.Type: GrantFiled: April 24, 1997Date of Patent: February 2, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Guerry, Henri Stalder, Pierre-Charles Wyss
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Patent number: 5864036Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: April 17, 1998Date of Patent: January 26, 1999Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm, Dennis Lee
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Patent number: 5856484Abstract: Compounds of formula I: ##STR1## are disclosed. The compounds inhibit the binding of endothelin to its receptors.Type: GrantFiled: October 7, 1996Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
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Patent number: 5854179Abstract: Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) and salts thereof ##STR1## in which R*, R.sup.1, R.sup.2, R.sup.3, X, Y, Z, W, n and m are defined as in claim 1, and specifically R* is a formyl equivalent of the formula CHO, --CH.dbd.NR or CH(X.sup.1 R')(X.sup.2 R"), are suitable as herbicides and plant growth regulators. They are prepared analogously to known methods, in some cases using novel intermediate products of the formula (XVII) ##STR2## in which U*.dbd.NH.sub.2, Cl or (substituted) amino.Type: GrantFiled: November 3, 1995Date of Patent: December 29, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 5852019Abstract: The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.Type: GrantFiled: February 4, 1998Date of Patent: December 22, 1998Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Akio Ejima, Masamichi Sugimori, Ikuo Mitsui
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Patent number: 5849666Abstract: N-substituted hydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) or salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, Q, X, Y and Z are defined as in formula (I) as claimed in claim 1, are suitable as herbicides and plant growth regulators.The compounds (I) are prepared by processes analogous to known processes (cf.Type: GrantFiled: November 22, 1995Date of Patent: December 15, 1998Assignee: Hoechst Schering Agrevo GmbHInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 5837708Abstract: Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.Type: GrantFiled: October 15, 1996Date of Patent: November 17, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
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Patent number: 5814631Abstract: A chymase inhibitor containing as its effective ingredient a quinazoline derivative, or a pharmaceutically acceptable salt thereof, having the formula (1): ##STR1## and a pharmaceutical preparation for the prevention of cardiac and circulatory system diseases derived from abnormal exacerbation of Ang II production containing the same as its effective ingredient.Type: GrantFiled: May 28, 1997Date of Patent: September 29, 1998Assignee: Suntory LimitedInventors: Harukazu Fukami, Akiko Ito, Shinjiro Niwata, Saki Kakutani, Motoo Sumida, Yoshinobu Kiso
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Patent number: 5811549Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: November 21, 1997Date of Patent: September 22, 1998Assignee: SmithKline BeechamInventors: Jerry L. Adams, Jeffrey C. Boehm
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Patent number: 5763448Abstract: A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia ##STR1##Type: GrantFiled: March 18, 1996Date of Patent: June 9, 1998Assignee: Merck, Sharp & Dohme LimitedInventors: William Robert Carling, Ian James Collins, Michael Rowley, Paul David Leeson
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Patent number: 5747421Abstract: Formylaminophenylsulfonylureas; processes for their preparation, and their use as herbicides and plant growth regulatorsCompounds of the formula (I) ##STR1## in which R.sup.1 is H, a substituted or unsubstituted hydrocarbon radical or an unsubstituted or substituted heterocyclic radical,R.sup.2 is H, (C.sub.1 -C.sub.6)-alkyl or (C.sub.1 -C.sub.6)-alkoxy,R.sup.3 is halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, (C.sub.1 -C.sub.6)-haloalkyl, (C.sub.1 -C.sub.6)-haloalkoxy, NO.sub.2, CN, NH.sub.2, (C.sub.1 -C.sub.4) -mono- or dialkylamino, each independently of other radicals R.sup.3 if n is 2 or 3,n is 0, 1, 2 or 3,W is an oxygen atom or a sulfur atom,X and Y independently of one another are halogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, (C.sub.1 -C.sub.4)-alkoxy and (C.sub.1 -C.sub.Type: GrantFiled: May 30, 1995Date of Patent: May 5, 1998Assignee: Hoechst Schering Agrevo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 5739333Abstract: Novel sulfonamide derivatives of the formula ?I!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is --0--, --S-- or --NH--, Alk is lower alkylene or alkenylene, Z is --O-- or --NH --, R is substituted or unsubstituted aromatic heterocyclic or aryl, R.sup.1 is H, substituted or unsubstituted amino, substituted or unsubstituted lower alkyl, alkenyl, alkynyl, substituted or unsubstituted lower alkylthio, or alkoxy, or substituted or unsubstituted heterocyclic or aryl, or pharmaceutically acceptable salts thereof, which are useful in the prophylaxis or treatment of disorders associated with endothelin activities such as hypertension, pulmonary hypertension, renal hypertension, Raynaud disease, bronchial asthma, gastric ulcer, chronic heart failure, etc.Type: GrantFiled: May 9, 1996Date of Patent: April 14, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
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Patent number: 5728706Abstract: A benzenesulfonamide derivative of the formula ?I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.Type: GrantFiled: April 24, 1996Date of Patent: March 17, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
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Patent number: 5726173Abstract: N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12);R.sup.Type: GrantFiled: December 12, 1996Date of Patent: March 10, 1998Assignee: Berlex Laboratories, Inc.Inventors: Raju Mohan, Michael M. Morrissey
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Patent number: 5723409Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.Type: GrantFiled: April 28, 1995Date of Patent: March 3, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5721341Abstract: The invention relates to derivatives of nucleosides, processes for the production of these derivatives of nucleosides, as well as specific polyclonal and monoclonal antibodies of the aforementioned derivatives.These derivatives comply with the following chemical formula: ##STR1## in which n is equal to 1, R.sup.1 stands for H or a linear mono-, di- or tri-phosphoric acid, R.sup.2 stands for a hydroxyl group, alkyl group, aryl group, a protein containing a free amino site, an aminoalkyl polystyrene or a silica grafted with an alkyl amine chain and R.sup.3 represents a substituted base chosen from among uracil, thymine, cytosine, guanine or adenine.Type: GrantFiled: June 5, 1996Date of Patent: February 24, 1998Assignees: Commissariat a l'Energie Atomique, Centre National d'Etudes SpatialesInventors: Didier Molko, Jean Cadet, Isabelle Cimaz
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Patent number: 5716955Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: January 10, 1997Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm