At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Patent number: 6245763Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: January 14, 2000Date of Patent: June 12, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6235746Abstract: Compounds of general formula (1) are described: wherein R1 is a hydrogen or halogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group or a group selected from hydroxyl (—OH), substituted hydroxyl, thiol (—SH), substituted thiol, amino (—NH2), or substituted amino; R2 and R3, which may be the same or different, is each an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R4 is a hydrogen atom or a straight or branched chain alkyl group; R5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R6 is a hydrogen or halogen atom or an amino (—NH2), substituted amino, nitro, carboxyl (—CO2H) or esterified carboxyl group or a group —X1—R6a where X1 is a direct bond or a linker atom or group and R6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom orType: GrantFiled: February 16, 1999Date of Patent: May 22, 2001Assignee: Celltech Therapeutics, LimitedInventors: Peter David Davis, David Festus Charles Moffat, Jeremy Martin Davis, Martin Clive Hutchings
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Patent number: 6200977Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: February 12, 1999Date of Patent: March 13, 2001Assignee: Tularik Inc.Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Patent number: 6200984Abstract: A compound of the general formula I: is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions, processes for preparing the compounds and methods of treatment are also disclosed.Type: GrantFiled: October 5, 1998Date of Patent: March 13, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Allen B. Reitz, James J. McNally, Pauline Sanfilippo
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Patent number: 6197779Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 orType: GrantFiled: March 25, 1999Date of Patent: March 6, 2001Assignee: Janssen Pharmaceutica, Inc.Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc RenĂ© De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, 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, cancer, 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 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6172005Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and Q, W, X, Y, Z, and R1 through R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.Type: GrantFiled: September 1, 1999Date of Patent: January 9, 2001Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas P. Selby
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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: 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: 6080750Abstract: A pyrimidine compound of the formula [I] ##STR1## wherein R1 is H, C.sub.1 -C.sub.4 lower alkyl, halogen atom, --OH, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.6 hydroxy(lower)alkoxy or --NH.sub.2 ; R2 is H, --NH.sub.2 or --NHCOCH.sub.3 ; R3 is --NR5(CH.sub.2)i--CH.sub.2 OH; R4 is H, halogen atom, --NH.sub.2, --CN, --CHO, --CH.sub.2 OH, --COOH, --CH.sub.2 NH.sub.2, --CONH.sub.2 or --CH.dbd.N--A wherein A is --OH, C.sub.1 -C.sub.4 lower alkyl or C.sub.1 -C.sub.4 lower alkoxy; R5 is H or C.sub.1 -C.sub.4 lower alkyl; and i is an integer of 1 to 4, and an anti-rotavirus agent comprising, as an active ingredient, a compound of the formula [I] wherein R3 is a group selected from the following: ##STR2## The novel pyrimidine compound of the present invention and related derivatives thereof have superior anti-rotavirus action and are useful for the prophylaxis and treatment of rotaviral diseases.Type: GrantFiled: May 6, 1997Date of Patent: June 27, 2000Assignee: Nippon Shoji Kaisha Ltd.Inventors: Masakatsu Hisaki, Yoichiro Ohta, Kenji Kawanishi, Yasuko Ichigobara, Fuzuki Iwakura, Masanobu Azuma, Tatsuo Suzutani, Manabu Node, Kiyoharu Nishide
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Patent number: 6030976Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.Type: GrantFiled: June 3, 1998Date of Patent: February 29, 2000Assignee: Hoffman-La Roche Inc.Inventors: Michael Bos, Thierry Godel, Claus Riemer, Andrew Sleight
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Patent number: 6001844Abstract: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: March 11, 1998Date of Patent: December 14, 1999Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Soumya P Sahoo, Richard L. Tolman
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Patent number: 5990311Abstract: The present invention relates to a process for preparation of 5,6-dimethyl-2-(4-fluorophenyl-amino)-4-(1-methyl-1,2,3,4-tetrahydroisoqui nolin-2-yl)pyrimidine represented by the following formula (I), ##STR1## and its acid addition salts by reacting a pyrimidine derivative represented by the formula (II-A), ##STR2## in which Hal represents a halogen, with 1-methyl-1,2,3,4-tetrahydroisoquinoline represented by the formula (III), ##STR3##Type: GrantFiled: October 21, 1998Date of Patent: November 23, 1999Assignee: Uhan CorporationInventors: You Wha Hong, Young Nam Lee, Hong Bae Kim
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Patent number: 5965559Abstract: The invention concerns compounds of formula (I), wherein each of G.sup.1, G.sup.2 and G.sup.6 is CH or n; m is 1 or 2; R.sup.1 includes hydrogen, halogeno and (1-4C)alkyl; M.sup.1 is a group of formula: NR.sup.2 -L.sup.1 -T.sup.1 R.sup.3, in which R.sup.2 and R.sup.3 together form a (1-4C)alkylene group, L.sup.1 includes (1-4C)alkylene, and T.sup.1 is CH or N; A may be a direct link; M.sup.2 is a group of the formula: (T.sup.2 R.sup.4).sub.r -L.sup.2 T.sup.3 R.sup.5 in which R is 0 or 1, each of T.sup.2 and T.sup.3 is CH or N, each of R.sup.4 and R.sup.5 is hydrogen or (1-4C)alkyl, or R.sup.4 and R.sup.5 together form a (1-4C)alkylene group, and L.sup.2 includes (1-4C)alkylene; M.sup.3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocycle moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.Type: GrantFiled: March 26, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
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Patent number: 5958935Abstract: 2-Anilinopyrimidines, processes for their preparation, pharmaceutical compositions containing them, their use in medicine. In a preferred embodiment, the compounds have the general formula (1): ##STR1## wherein R.sup.1 is preferably methoxy; R.sup.2 and R.sup.3 are preferably methyl; R.sup.4 is preferably a hydrogen atom; R.sup.5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.6 is a hydrogen or halogen atom or an amino (--NH.sub.2), substituted amino, nitro, carboxyl (--CO.sub.2 H), esterified carboxyl or --X.sup.1 R.sup.6a where X.sup.1 is a direct bond or a linker atom or group and R.sup.6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; and R.sup.7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group.Type: GrantFiled: November 19, 1996Date of Patent: September 28, 1999Assignee: Celltech Therapeutics LimitedInventors: Peter David Davis, David Festus Charles Moffat, Jeremy Martin Davis, Martin Clive Hutchings
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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: 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: 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: 5917041Abstract: The present invention is related to a process of making of 2,6-diaminopurines wherein the 6-amino group is substituted by R.sup.4 and R.sup.5, by reacting a compound of formula (VI) ##STR1## with an excess of amine NHR.sup.4 R.sup.5.Type: GrantFiled: October 24, 1997Date of Patent: June 29, 1999Assignee: Glaxo Wellcome Inc.Inventors: Susan Mary Daluge, Michael Tolar Martin
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Patent number: 5914319Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: June 22, 1999Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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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: 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: 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: 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: 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: 5747473Type: GrantFiled: August 18, 1995Date of Patent: May 5, 1998Assignee: Medivir ABInventors: Bjorn Olof Classon, Bengt Bertil Samuelsson, Ingemar Sven-Anders Kvarnstrom, Lars Goran Svansson, Stefan Carl Tore Svensson
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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: 5726159Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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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: 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: 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: 5710130Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5703086Abstract: The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.Type: GrantFiled: June 6, 1995Date of Patent: December 30, 1997Assignee: The Picower Institute for Medical ResearchInventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich
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Patent number: 5700295Abstract: The invention relates to compounds of formula ##STR1## wherein the variables have the meanings given in the claims. The compounds are suitable for use as UV absorbers for the photochemical stabilisation of undyed, dyed or printed textile fiber materials and for enhancing the sun protection factor thereof.Type: GrantFiled: October 11, 1995Date of Patent: December 23, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Francesco Fuso, Gerhard Reinert
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Patent number: 5696259Abstract: This invention describes 2,4-diamino-5-iodopyrimidines II where R, R1, R2, and R3 are independently selected from hydrogen, alkyl, cycloalkyl, alkoxyalkyl, alkoxyalkoxyalkyl, and arylalkyl; or, R1 and R2, and R3 and R, each independently, when taken together with pentylene or 3-oxapentylene, form piperidine and morpholine ring systems respectively; and R4 is hydrogen or lower alkyl. These compounds are useful intermediates in the preparation of insecticides I where U is an optionally substituted alkenylene.Type: GrantFiled: July 22, 1996Date of Patent: December 9, 1997Assignee: FMC CorporationInventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, Mary E. Brown, John W. Buser
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Patent number: 5693808Abstract: Di-, tri- and tetrachromophoric perylene-3,4:9,10-tetracarboxylic acid imides of the formula I ##STR1## in which A is, for example, 1,4-phenylene,R is 1-hexylheptyl andm is 2,are readily accessible by reaction of a perylene-3,4:9,10-tetracarboxylic acid monoanhydride monoimide with 1,4-diaminobenzene-bisformamide. The preparation process and also a specific process for the preparation of monochromic perylene-3,4:9, 10-tetracarboxylic acid bisimides are also claimed. These processes are particularly suitable for reaction of highly electron-rich aromatic amines, which cannot be reacted under conventional condensation conditions.Type: GrantFiled: November 6, 1995Date of Patent: December 2, 1997Assignee: Ciba Specialty Chemicals CorporationInventor: Heinz Langhals
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Patent number: 5677310Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl-S-, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.Type: GrantFiled: February 5, 1996Date of Patent: October 14, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
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Patent number: 5658854Abstract: Acylated aminophenylureas, preparation and use as herbicides and plant growth regulatorsThe compounds of the formula I or their salts ##STR1## in which G is a radical G1, G2 or G3 ##STR2## R.sup.1 is H or alkyl, R.sup.2 is COOH, CSOH or a derivative of the carboxyl or thiocarboxyl group, of 1 to 20 carbon atoms, or acyl of the type CO-R.degree. of 1-12 carbon atoms, or an imino, hydrazone or oxime derivative of the group CO-R.degree., and R.degree. , R.sup.3a, R.sup.4a, R.sup.3b, R.sup.4b, W, X, Y and Z are as defined in claim 1, are suitable as selective herbicides and plant growth regulators in crops.The preparation is carried out in analogy to known processes (see claim 5) by way of intermediates, some of which are new, from the group consisting of benzene-sulfonamides (II), benzenesulfonyl isocyanates (IV) and benzesulfonyl chlorides (VI) and heterocyclically substituted carbamates (III), amines (V) and/or (thio)-isocyanates (XIX).Type: GrantFiled: June 30, 1994Date of Patent: August 19, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5648490Abstract: Disclosed is a process for the preparation of 5-formylaminopyrimidines of the general formula: ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and signify H, OH, SH, NH.sub.2, alkylamino, halogen, O-alkyl, S-alkyl or alkyl, as well as aryl, and alkyl is an aliphatic radical containing up to 4 carbon atoms, from the corresponding 5-nitrosopyrimidines of the general formula: ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the same meanings as above, wherein the starting compound is subjected to a reductive formylation in the presence of a noble metal catalyst, as well as of formic acid and of a salt thereof.Type: GrantFiled: March 28, 1995Date of Patent: July 15, 1997Assignee: SKW Trostberg AktiengesellschaftInventors: Franz Thalhammer, Jurgen Graefe
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Patent number: 5648315Abstract: Compounds of the formula (I) and their salts as defined below, ##STR1## in which R.sup.1 is CO--Q--R.sup.8, where R.sup.8 .dbd.H or RR.sup.2 and R.sup.3 are H or (C.sub.1 -C.sub.4)alkyl,R.sup.4 is H, R, RO, OH, RCO, RSO.sub.2, PhSO.sub.2R.sup.5 is RSO.sub.2, PhSO.sub.2, PhCO, RNHSO.sub.2, R.sub.2 NSO.sub.2, RCO, CHO, COCOR', CW--T--R.sup.9, CW--NR.sup.10 R.sup.11, CW--N(R.sup.12).sub.2 orR.sup.4 and R.sup.5 together are the chain (CH.sub.2).sub.m B or --B.sup.1 --(CH.sub.2).sub.m1 B-- where B.dbd.SO.sub.2, CO; m=3, 4; m.sup.1 =2, 3;T and W.dbd.O, S; Q.dbd.O, S, NR.sup.13 where R.sup.13 .dbd.H, R;R.sup.6 .dbd.H, R, RO, RCO, ROCO, Hal, NO.sub.2, CN;R.sup.7 .dbd.H, CH.sub.3 ; R.sup.9 .dbd.R; R.sup.10, R.sup.11 .dbd.H, R; N(R.sup.12).sub.2 =heterocycleA=pyrimidinyl and triazinyl radical or an analog thereof,where R=(substituted) aliphatic hydrocarbon radical, are suitable as selective herbicides. They are prepared by analogous processes via sulfonamides.Type: GrantFiled: October 13, 1994Date of Patent: July 15, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5622954Abstract: 5-Substituted-2,4-diaminopyrimidines, and agriculturally acceptable salts thereof, when present in insecticidally or acaricidally effective amounts, and with a suitable agricultural carrier, are useful as active ingredients in novel insecticidal and acaricidal compositions. These pyrimidines may be represented by the following formula: ##STR1## wherein Ar is ##STR2## and wherein U is an alkenylene or alkynylene moiety, and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, V, W, X, Y, Z and n are as defined herein; also disclosed and claimed are novel intermediates thereof.Type: GrantFiled: March 2, 1995Date of Patent: April 22, 1997Assignee: FMC CorporationInventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, Mary E. Brown, John W. Buser
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Patent number: 5610300Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.Type: GrantFiled: June 6, 1995Date of Patent: March 11, 1997Assignee: Ciba-Geigy CorporationInventors: Karl-Heinz Altmann, Ren e Imwinkelried, Albert Eschenmoser
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Patent number: 5599793Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: February 4, 1997Assignee: Eli Lilly and CompanyInventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5597779Abstract: N-Phenylsulfonyl-N'-pyrimidinylureas and -thioureas of formula I ##STR1## in which X is oxygen, sulfur, SO or SO.sub.2 ; W is oxygen or sulfur; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, fluorine, chlorine, bromine, iodine, (X).sub.n R.sub.3, NO.sub.2, NR.sub.4 R.sub.5, ##STR2## or cyano; n is the number 0 or 1; R.sub.3 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl which is substituted by 1-4 halogen atoms, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio; or C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkenyl which is substituted by 1-4 halogen atoms; R.sub.4 is hydrogen, CH.sub.3 O, CH.sub.3 CH.sub.2 O or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.6 is hydrogen, methyl or ethyl; R.sub.7 is hydrogen or methyl; Z is ##STR3## E is methine; R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.2 -C.sub.5 alkoxyalkyl, C.Type: GrantFiled: April 10, 1995Date of Patent: January 28, 1997Assignee: Ciba-Geigy CorporationInventor: Willy Meyer
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Patent number: 5585381Abstract: A pyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or --NHR.sup.11 group; R.sup.2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, --(CH.sub.2).sub.m C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.12, --NH(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH(CH.sub.2).sub.p C.sub.6 H.sub.4 --OR.sup.13, --N(R.sup.14)(CH.sub.2).sub.q C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.15, --NHC(.dbd.O)(CH.sub.2).sub.r C.sub.6 H.sub.5, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --OR.sup.16, or --O(CH.sub.2).sub.s C.sub.6 H.sub.5 group; R.sup.3 is --COOH, --COOR.sup.17, hydroxyl, --OR.sup.18, --NH.sub.2, --N(R.sup.19).sub.2, --NHR.sup.20, azole, or sulfonic acid group; R.sup.11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, and R.sup.Type: GrantFiled: May 31, 1995Date of Patent: December 17, 1996Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Michihito Ise