Carbocyclic Ring Containing Patents (Class 544/321)
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Patent number: 6156772Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 14, 1999Date of Patent: December 5, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
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Patent number: 6153619Abstract: There are provided compositions and methods comprising compounds of formula I: ##STR1## wherein R.sup.1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.Type: GrantFiled: March 22, 1999Date of Patent: November 28, 2000Assignee: American Cyanamid CompanyInventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
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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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Patent number: 6111102Abstract: Compounds of the formula I or salts thereof, in whichX is oxygen, --O--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, and Y is N or CH,R.sup.1 is (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or (C.sub.2 -C.sub.6)alkynyl, which are in each case optionally substituted, or, in the case where X=oxygen, also (subst.) phenyl,R.sup.2 is H, (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or -alkynyl or (C.sub.3 -C.sub.6)cycloalkyl,R.sup.3 and R.sup.4 are H, (subst.) (C.sub.1 -C.sub.4)alkyl or (subst.) (C.sub.1 -C.sub.4)alkoxy or halogen, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)-alkylamino or di[(C.sub.1 -C.sub.4)alkyl]-amino,R.sup.5 is H or (C.sub.1 -C.sub.4)alkyl and R.sup.6 is hydrogen,may be prepared by reacting compounds of the formula II,R.sup.1 --X--R.sup.7 (II)with compounds of the formulae III, IV and VR.sup.8 --OCN (III)SO.sub.2 Cl.sub.2 (IV) ##STR1## where R.sup.7 and R.sup.8 are H, a quarternary ammonium ion or one equivalent of a metal cation.Type: GrantFiled: March 2, 1999Date of Patent: August 29, 2000Assignee: Hoechst AktiengesellschaftInventor: Gunter Schlegel
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Patent number: 6110925Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.Type: GrantFiled: August 6, 1998Date of Patent: August 29, 2000Assignee: Research Corporation Technologies, Inc.Inventors: Robert M. Williams, Chenguang Yuan
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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: 6093718Abstract: This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.Type: GrantFiled: February 12, 1999Date of Patent: July 25, 2000Assignee: Zeneca LimitedInventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Nicholas John Newcombe
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Patent number: 6057325Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.Type: GrantFiled: November 9, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutia, N.V.Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 6048866Abstract: Compounds of formula (1) are described: ##STR1## and the salts, solvates, hydrates and N-oxides thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.Type: GrantFiled: March 13, 1998Date of Patent: April 11, 2000Assignee: Celltech Therapeutics, LimitedInventors: Martin Clive Hutchings, Peter David Davis, David Festus Charles Moffat
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Patent number: 6040315Abstract: Herein is disclosed how to make and to use a nonmetallic antacid composition which is the product of the co-polymerization of guanidine and polyethylenimine. The resultant polymer is useful as an antacid.Type: GrantFiled: October 29, 1998Date of Patent: March 21, 2000Inventor: Charles E. Day
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Patent number: 6028073Abstract: N-substitued 3-azabicyclo[3.2.0]heptane derivatives of formula (I) ##STR1## in which R.sup.1, R.sup.2, A, X, Y and Z have the meanings given in the description, their method of preparation and their use as pharmacological agents.Type: GrantFiled: September 18, 1998Date of Patent: February 22, 2000Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Thomas Hoger, Liliane Unger, Hans-Jurgen Teschendorf
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Patent number: 6013651Abstract: The present invention is directed to compounds of the formula ##STR1## and pharmaceutically acceptable salts and isomers thereof.Type: GrantFiled: March 4, 1998Date of Patent: January 11, 2000Assignee: G. D. Searle & Co.Inventors: Thomas E. Rogers, Peter G. Ruminski
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Patent number: 6008351Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: December 18, 1995Date of Patent: December 28, 1999Assignee: Corvas International, Inc.Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck, Marguerita S. L. Lim-Wilby, Ruth F. Nutt, Matthew M. Abelman
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Patent number: 5972949Abstract: There are disclosed novel ether compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or the like; A is a group of the general formula: ##STR2## B is a group of the general formula: ##STR3## and X is oxygen or sulfur; and harmful-organism controlling agents containing them as active ingredients.Type: GrantFiled: October 16, 1998Date of Patent: October 26, 1999Assignee: Sumito Chemical Co., Ltd.Inventors: Akira Shuto, Hirosi Kisida, Toru Tsuchiya, Yoji Takada, Hiroaki Fujimoto
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Patent number: 5958934Abstract: The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in whichn is 1, 2, or 3;R.sup.6 and R.sup.7 are hydrogen or lower alkyl;R.sup.8 is hydrogen or lower alkyl; andR.sup.9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl;R.sup.3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl, --(CH.sub.2).sub.m NR.sup.10 R.sup.Type: GrantFiled: November 21, 1997Date of Patent: September 28, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
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Patent number: 5945427Abstract: The present invention is directed to derivatives of 5-thia- and 5-selenopyrimidinone are useful as inhibitors of the enzyme glycimide ribonucleotide formyl transferase (GARFT) and amino imidozole carboxamide ribonucleotide formyl transferase (AICARFT), pharmaceutical compositions containing these derivatives, and methods of using these derivatives. The present invention is also directed to intermediates useful for preparing these derivatives and methods of preparing these intermediates.Type: GrantFiled: January 6, 1998Date of Patent: August 31, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Patent number: 5945426Abstract: A pharmaceutical composition comprising a compound of the following general formula ?I! or its salt. ##STR1## wherein R.sup.1 represents aryl or a heteroaromatic group. R.sup.2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R.sup.3 and R.sup.4 independently represent hydrogen or alkyl or R.sup.3 and R.sup.4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents C.sub.2-10 alkylene. W represents O, S, or (CH).sub.n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.Type: GrantFiled: March 7, 1997Date of Patent: August 31, 1999Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shoichi Chokai, Yojiro Ukai, Tomiyoshi Aoki, Kyoichi Ideguchi
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Patent number: 5936085Abstract: Disclosed and claimed is a process for the preparation of a carbamate (IV)Ar--O--CO--NR--B (IV)by reaction of a saltM.sup..sym. .crclbar.NR--B (II-S)with a diaryl carbonate(ArO).sub.2 CO (III).The carbamate can be reacted, without any necessity of intermediate isolation, with a sulfonamide A--SO.sub.2 NH.sub.2 (V) to give a sulfonylurea (I) or salts thereofA--SO.sub.2 --NH--CO--NR--B (I).And thus, disclosed and claimed too is a process for the preparation of sulfonylurea (I) by (i) contacting a salt (II-S) with a diaryl carbonate (III) to form a carbamate (IV), and (ii) contacting carbamate (IV) from step (i) with or without intermediate isolation, with a sulfonamide (V). These processes avoid the use of alkali metal hydrides as a base. And, these processes can additionally include the preparation of salt (II-S) from a compound H--NR--B (II) and base M.sup..sym. Base.sup..crclbar..Type: GrantFiled: July 11, 1996Date of Patent: August 10, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Harald Knorr, Klemens Minn, Jan Vermehren
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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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: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5912350Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: October 8, 1997Date of Patent: June 15, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 5912252Abstract: The subject invention concerns compounds of formula (I): whereinn=1 or 2;R.sup.1 is H, NH.sub.2 or halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 represents the group CR.sup.6 R.sup.7 R.sup.8 where R.sup.6, R.sup.7 and R.sup.8 are the same or different and are each H, C.sub.1-6 alkyl or C.sub.1-6 haloalkyl;R.sup.4 and R.sup.5 are the same or different and are selected from the group consisting of H, CO.sub.2 H, CO.sub.2 C.sub.1-6, NHSO.sub.2 CF.sub.3, tetrazole and (CR.sup.9 R.sup.10).sub.p (Y).sub.q (CR.sup.9 R.sup.10).sub.t Z where (CR.sup.9 R.sup.10), or (CR.sup.9 R.sup.10).sub.t is straight or branched chain bearing the substituents R.sup.9 and R.sup.10 when p or t>1;R.sup.9 and R.sup.10 are the same or different and are each C.sub.0-6 alkyl-Z;p=1-3;q=0 or 1;t=0-4, provided that t>0 when q=1;Y=O, NH or S(O).sub.m where m=0-2; andZ is selected from a group consisting of H, CN, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3 tetrazole, triazole, CONH.sub.2, CON(C.sub.1-6 alkyl).sub.2, CONH(C.sub.Type: GrantFiled: May 19, 1997Date of Patent: June 15, 1999Assignee: Darwin Discovery LimitedInventors: Steven Colin Beasley, John Gary Montana
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Patent number: 5908844Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel ompounds are suitable for controlling diseases.Type: GrantFiled: May 6, 1996Date of Patent: June 1, 1999Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
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Patent number: 5886176Abstract: The invention relates to a novel process for preparing herbicidal sulphonylurea salts of the formula (I) ##STR1## in which M.sup.+ represents an alkali metal ion or an alkaline earth metal ion equivalent,Z represents N, CH or C-halogen,R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,(where R.sup.2, X and Y have the meanings given in the description).Type: GrantFiled: March 1, 1993Date of Patent: March 23, 1999Assignee: Bayer AktiengesellschaftInventor: Klaus-Helmut Muller
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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: 5869428Abstract: A pyridonesulfonylurea compound of the formula (I) or its salt: ##STR1## wherein Q is ##STR2## for use as a herbicide, wherein the variables are hereinbelow defined.Type: GrantFiled: March 4, 1996Date of Patent: February 9, 1999Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Yasuo Morishima, Shigeo Murai, Yoshiyuki Aoyama, Hiroshi Sasaki, Hiroshi Kikugawa, Soichiro Nagayama, Makiko Mitani
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Patent number: 5863924Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.Type: GrantFiled: May 20, 1997Date of Patent: January 26, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
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Patent number: 5863923Abstract: Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH--(b) or --CH.dbd.CH--C(Cl)=CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.Type: GrantFiled: May 1, 1997Date of Patent: January 26, 1999Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Henri Paul Van Daele, Jean-Paul Rene Marie Andre Bosmans, Willy Joannes Carolus Van Laerhoven
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Patent number: 5859020Abstract: The invention relates to substituted 4-alkoxypyrimidines of the formula ##STR1## in which R.sup.1 is hydrogen, halogen, alkyl or cycloalkyl, R.sup.2 is hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted alkylthio, alkylamino or dialkylamino, R.sup.3 is hydrogen, alkyl, alkoxy, haloalkoxy, halogen, alkylthio, amino, alkylamino or dialkylamino, and R.sup.4 is hydrogen, alkyl, cycloalkyl or haloalkyl, where R.sup.2 and R.sup.3 together with the carbon atoms to which they are attached can also form a ring, and Q is as defined in the description.The invention furthermore relates to a process for their preparation, to agents containing them, and to their use as pesticides.Type: GrantFiled: January 15, 1997Date of Patent: January 12, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Preuss, Gerhard Salbeck, deceased, Wolfgang Schaper, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
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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: 5824624Abstract: New herbicidal pyridine and pyrimidine derivatives of general formula (I), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.2 or each R.sup.2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.Type: GrantFiled: December 6, 1996Date of Patent: October 20, 1998Assignee: American Cyanamid CompanyInventors: Axel Kleeman, Helmut Siegfried Baltruschat, Thelka Hulsen
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Patent number: 5807863Abstract: This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.3-6 cycloalkyl, or di-C.sub.1-4 alkylamino,R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, or di-C.sub.1-4 alkyl-amino,R.sub.3 is hydrogen or methyl,R.sub.4 is aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or heteroaryl-C.sub.1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; andX is CH or nitrogen;the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.Type: GrantFiled: September 19, 1996Date of Patent: September 15, 1998Assignee: Novartis CorporationInventors: Martin Eberle, Clemens Lamberth, Fritz Schaub
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Patent number: 5783576Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.Type: GrantFiled: August 9, 1996Date of Patent: July 21, 1998Assignee: Boehringer Ingelheim KGInventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
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Patent number: 5780473Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.Type: GrantFiled: July 25, 1996Date of Patent: July 14, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
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Patent number: 5760038Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.Type: GrantFiled: February 6, 1995Date of Patent: June 2, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
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Patent number: 5753668Abstract: The present invention provides certain novel nitro or nitroso substituted benzyloxy pyrimidines useful as AGT inactivators. An example of such a pyrimidine is a compound of the formula ##STR1## wherein R.sub.1, is NO.sub.2 or NO, and R.sub.2 is hydrogen, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl, thiol, C.sub.1 -C.sub.4 alkythio, trifluoromethoxy, oxymethanesulfonyl, oxytrifluoromethanesulfonyl, or C.sub.1 -C.sub.4 oxyacyl. The present invention further provides pharmaceutical compositions comprising these compounds, and a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.Type: GrantFiled: June 11, 1996Date of Patent: May 19, 1998Assignees: The United States of America as represented by the Department of Health and Human Services, Penn State Research Foundation, Arch Development CorporationInventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
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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: 5739134Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: April 14, 1998Assignee: Janssen Pharmacetuica N.V.Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
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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: 5726312Abstract: Intermediates for preparing derivatives of 5-thia- and 5-selenopyrimidinone, ##STR1## which are useful as inhibitors of the enzymes glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). The present invention is also directed to methods of preparing these intermediates.Type: GrantFiled: May 24, 1995Date of Patent: March 10, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Patent number: 5723473Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.Type: GrantFiled: April 11, 1995Date of Patent: March 3, 1998Assignee: Zeneca LimitedInventor: Brian Leslie Pilkington
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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: 5721192Abstract: Aminosulfonyl ureas having general formula (I): ##STR1## The aminosulfonyl ureas having general formula (I) have a high herbicidal activity.Type: GrantFiled: October 16, 1996Date of Patent: February 24, 1998Assignee: Isagro Ricerca S.r.l.Inventors: Giovanni Meazza, Giampaolo Zanardi, Sergio Massimini, Piero La Porta, Ernesto Signorini
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Patent number: 5716993Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.Type: GrantFiled: September 14, 1995Date of Patent: February 10, 1998Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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Patent number: 5696053Abstract: Salts of the formula (I) ##STR1## in which n is 0, 1, 2 or 3,R is halogen, alkyl or alkoxy, mainly in each case independently of other substituents R in the event that n is greater than 1,R.sup.1 is a substituted or unsubstituted hydrocarbon radical or a substituted or unsubstituted heterocyclic radical,R.sup.2 is an acyl radical,R.sup.3 is hydrogen or C.sub.1 -C.sub.5 -alkyl,M.sym. is a metal or ammonium ion,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.4 -alkylthio, or are C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkynyloxy, mono- or di(C.sub.1 -C.sub.Type: GrantFiled: May 30, 1995Date of Patent: December 9, 1997Assignee: Hoechst AktiengesellschaftInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer