Plural 1,3-diazine Rings Patents (Class 544/296)
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Patent number: 5783580Abstract: This invention relates to compounds of formula I ##STR1## wherein R.sup.1 is C.sub.1-4 alkoxy or --NR.sup.8 R.sup.9 ;R.sup.2 is heteroaryl, heteroaryloxy or a group ##STR2## R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, cyano, nitro or halogen;R.sup.4 is hydrogen, halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl;R.sup.5 is hydrogen or methyl;R.sup.7 is hydrogen or methyl;R.sup.8 and R.sup.9 are independently C.sub.1-4 alkyl or together C.sub.3-6 alkylene;E is C.sub.1-3 alkylene;X is CH or nitrogen; andY is OCH.sub.3, NH.sub.2, NHCH.sub.3 or N(CH.sub.3).sub.2.Type: GrantFiled: May 23, 1996Date of Patent: July 21, 1998Assignee: Sandoz, Ltd.Inventors: Martin Eberle, Fritz Schaub, Gerald Wayne Craig
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Patent number: 5779934Abstract: A fluorine-containing optically active compound represented by the formula (1): ##STR1## wherein R.sub.1 is a saturated or unsaturated C.sub.3 -C.sub.20 alkyl group or a saturated or unsaturated C.sub.3 -C.sub.20 alkoxyalkyl group; A.sup.1, A.sup.2 and A.sup.3 independently represent one of the following groups: ##STR2## provided that, when A.sup.1 is a condensed ring group, a sum of p and q is 0 or 1 and A.sup.2 and A.sup.3 are both monocyclic groups, or when A.sup.1 is a monocyclic group, a sum of p and q is 1 or 2 with the proviso that when the sum of p and q is 2, A.sup.2 and A.sup.3 are both monocyclic groups; X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--; W is a fluorine atom or a hydrogen atom; n is an integer of 1 to 10; m, p and q are each 0 or 1; u and w are each an integer of 0 to 3; and * indicates an asymmetric carbon atom, which is useful as a component of a liquid crystal mixture.Type: GrantFiled: February 14, 1995Date of Patent: July 14, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Yukari Fujimoto, Tsutomu Matsumoto, Masayoshi Minai, Chizu Sekine, Kyoko Endo, Koichi Fujisawa
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Patent number: 5780629Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.Type: GrantFiled: June 6, 1996Date of Patent: July 14, 1998Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
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Patent number: 5773445Abstract: The application describes new 3-methoxy-2-phenyl-acrylic esters of the formula (I) ##STR1## in which R and Y have the meanings given in the description,a process for their preparation, and their use as pesticides.Type: GrantFiled: May 20, 1996Date of Patent: June 30, 1998Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Otto Schallner, Stefan Dutzmann, Heinz-Wilhelm Dehne, Gerd Hanssler
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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: 5760037Abstract: These compounds correspond to the following general formula: ##STR1## where: n is 0, 1, or 2,m is are 1, 2, or 3,R, R.sub.1, R.sub.2, and R.sub.3, whether identical or different, represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,R.sub.1 and R.sub.2, or R.sub.2 and R.sub.3 taken together can form a 5- or 6-group cycle,X and Y, whether identical or different, represent a nitrogenous aromatic heterocycle in position 2,Z.sub.1, Z.sub.2, and Z.sub.3, whether identical or different, represent an atom of hydrogen, a linear or branched alkyl radical at C.sub.1 -C.sub.4, the radical --OR.sub.4 or --NR.sub.4 R'.sub.4,R.sub.4 and R'.sub.4 represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,and the metallic salts and complexes thereof.Use in pharmaceutical and cosmetic compositions to protect the organism from oxidizing stress situations linked to certain pathological states.Type: GrantFiled: July 23, 1996Date of Patent: June 2, 1998Assignee: L'OrealInventors: Jean-Baptiste Galey, Jacqueline Dumats
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Patent number: 5756739Abstract: The present invention provides a novel process for preparing polyamine derivatives and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents and to novel intermediates thereof.Type: GrantFiled: March 14, 1997Date of Patent: May 26, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Paul T. Angell, John Martin, Peter B. Anzeveno
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Patent number: 5753664Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.Type: GrantFiled: March 13, 1996Date of Patent: May 19, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
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Patent number: 5750469Abstract: Substituted lactic acid derivatives having an N-organic radical in the .beta.-position, of the formula I ##STR1## where substituents R to R.sup.5, X and Y have the meanings mentioned in the description and N is one of the radicals:a) --N.sub.3, --NC, --NCS or --NCOb) ##STR2## where R.sup.14 and R.sup.15 have the meanings described in the descriptionc) ##STR3## in which R.sup.16 is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl or unsubstituted or substituted phenyl; andB is a group ##STR4## OR.sup.19 or --NR.sup.14 R.sup.15, where R.sup.14, R.sup.15, R.sup.17 and R.sup.19 have the meanings described in the description, or ##STR5## where R.sup.14 and R.sup.15.sub.1, have the abovementioned meanings; or ##STR6## where R.sup.20 and R.sup.21, which can be identical or different, are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl, where the organic radicals can in each case be substituted;or R.sup.20 and R.sup.21 together form an unsubstituted or substituted C.sub.4 -C.sub.Type: GrantFiled: March 1, 1996Date of Patent: May 12, 1998Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen
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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: 5739137Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: February 28, 1996Date of Patent: April 14, 1998Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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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: 5723626Abstract: Compounds of formulaA(B).sub.x, (I),whereinx is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m und n, are as defined in claim 1.These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: July 9, 1996Date of Patent: March 3, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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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: 5714488Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.Type: GrantFiled: September 17, 1996Date of Patent: February 3, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
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Patent number: 5714438Abstract: Herbicidal 5-substituted pyrimidine compounds and derivatives thereof of the formula: ##STR1## Herbicidal compositions containing such 5-substituted pyrimidine compounds and derivatives thereof and methods of controlling undesirable vegetation using these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the 5-substituted pyrimidine derivatives of the invention.Type: GrantFiled: December 5, 1996Date of Patent: February 3, 1998Assignee: Zeneca LimitedInventors: David B. Kanne, Michael P. Prisbylla
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Patent number: 5707930Abstract: Herbicidal 4-cycloalkyl-5-substituted pyrimidine compounds of the formula ##STR1## are described. Herbicidal compositions containing such substituted-pyrimidinyl compounds and methods of controlling undesirable vegetation employing these compounds are also disclosed. The compounds in which XR, is hydroxyl are also useful as intermediates for producing the disclosed substituted-pyrimidinyl derivatives.Type: GrantFiled: September 16, 1996Date of Patent: January 13, 1998Assignee: Zeneca LimitedInventors: Raymond A. Felix, Hsiao-Ling M. Chin, Frank X. Woolard, David L. Lee, David B. Kanne
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Patent number: 5705502Abstract: Described are N-phenyl-2-pyrimidineamine derivatives of formula I ##STR1## wherein R.sub.1 is a substituted cyclic radical, the cyclic radical being bonded at a ring carbon atom in each case and being selected from phenyl, pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.3, --C(.dbd.O)--R.sub.4, --SO.sub.2 --N(R.sub.5)--R.sub.6, --N(R.sub.7)--R.sub.8, --OR.sub.9 and fluorine-substituted lower alkyl, whereinR.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino; andR.sub.2 is selected from halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.10, --C(.dbd.O)--R.sub.11, --SO.sub.2 --N(R.sub.12)--R.sub.13, --N(R.sub.14)--R.sub.15, --OR.sub.16 and fluorine-substituted lower alkyl, whereinR.sub.10, R.sub.11, R.Type: GrantFiled: May 31, 1995Date of Patent: January 6, 1998Assignee: Novartis CorporationInventor: Jurg Zimmermann
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Patent number: 5698563Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: January 13, 1995Date of Patent: December 16, 1997Assignee: Alteon Inc.Inventors: Dilip R. Wagle, Michael E. Lankin, David H. Shih
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Patent number: 5698564Abstract: Diphenyl disulfide compounds having an inhibiting activity against the production of Interleukin-1.beta. (IL-1.beta.) or the release of Tumor Necrosis Factor.alpha. (TNF.alpha.), which are useful in the treatment or prophylaxis of the diseases such as chronic rheumatism and sepsis are described.Type: GrantFiled: December 21, 1995Date of Patent: December 16, 1997Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Koichi Katsuyama, Masato Ariga, Yukio Saito, Shigeo Hatanaka, Toshihiro Takahashi
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Patent number: 5686456Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia in a subject in need of such treatment. The methods comprise administering to a subject in need thereof, a pyrimidine of Formula I. ##STR1## wherein the variables are as defined in the specification.Type: GrantFiled: November 28, 1995Date of Patent: November 11, 1997Assignees: The University of North Carolina, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
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Patent number: 5681957Abstract: Unsubstituted or substituted 2-fluoro-pyrimidines can be prepared by reaction of the underlying 2-amino-pyrimidines with diazotization agents, mixtures of HF and H.sub.2 O containing 30-70% by weight of HF, based on the total of HF and H.sub.2 O, serving as reaction medium. The reaction medium can also contain diluents and/or inorganic salts, preferably fluorides.Type: GrantFiled: May 3, 1996Date of Patent: October 28, 1997Assignee: Bayer AktiengesellschaftInventors: Erich Wolters, Guido Steffan, Alexander Klausener
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Patent number: 5679792Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are, for example, an alkyl chain,A is a mesogenic group, andM is a spacer group,are highly suitable as components of liquid-crystal mixtures.Type: GrantFiled: June 1, 1995Date of Patent: October 21, 1997Assignee: Hoechst AktiengesellschaftInventors: Claus Escher, Gerhard Illian, Hubert Schlosser, Rainer Wingen
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5672583Abstract: Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: May 17, 1995Date of Patent: September 30, 1997Assignee: Merck & Co., Inc.Inventors: Kevin Chapman, William Hagmann, Philippe Durette, Craig Esser, Ihor Kopka, Charles Caldwell
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Patent number: 5667721Abstract: Liquid crystalline compounds having two dioxane rings, the dipole moments of which are unidirectional. These are compounds of the general formula ##STR1## wherein A and B each independently is cyclic or acyclic hydrophobic residues; andn is 0, 1 or 2.as well as liquid crystalline mixtures which contain such compounds and the use of such compounds and, respectively, mixtures for electro-optical display devices.Type: GrantFiled: February 21, 1996Date of Patent: September 16, 1997Assignee: Rolic AGInventors: Richard Buchecker, Guy Marck, Alois Villiger
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Patent number: 5668140Abstract: Substituted 4-aminopyrimidines, processes for their preparation, and their use as pesticidesThe invention relates to substituted 4-aminopyrimidines of the formula ##STR1## in which: R.sup.1 is hydrogen, halogen, alkyl or cycloalkyl,R.sup.2 is hydrogen, alkyl, halogen, trifluoromethyl, alkoxy, haloalkoxy, alkoxyalkyl, alkylthio, alkylthioalkyl, alkylamino, dialkylamino or cycloalkylamino,R.sup.3 is hydrogen, alkyl, alkoxy, haloalkoxy, alkylthio, halogen, nitro or dialkylamino,R.sup.4 is hydrogen or optionally substituted carbamoyl;R.sup.5 is hydrogen, (C.sub.1 -C.sub.8)alkyl or (C.sub.3 -C.sub.6)cycloalkyl; andQ has the meaning defined in the description, and their salts. The invention furthermore relates to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 5, 1995Date of Patent: September 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Gerhard Salbeck, Heinz Ehrhardt, Peter Braun, Werner Knauf, Burghard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
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Patent number: 5663336Abstract: A process for the synthesis of compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors.Type: GrantFiled: October 18, 1995Date of Patent: September 2, 1997Assignee: Ciba-Geigy CorporationInventors: Uwe Trinks, Peter Traxler
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Patent number: 5658902Abstract: Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.Type: GrantFiled: December 22, 1994Date of Patent: August 19, 1997Assignee: Warner-Lambert CompanyInventors: Kyunghye Ahn, Xue-Min Cheng, Annette Marian Doherty, Edward Faith Elslager, Brian Kornberg, Chitase Lee, Daniele Leonard, Sham Nikam, Leslie Morton Werbel
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Patent number: 5659065Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: August 19, 1997Assignee: Novartis CorporationInventor: Richard Goschke
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Patent number: 5646269Abstract: The present invention is directed to improved methods to synthesize oligonucleotide analogs having an acetal linkage, such as a 3',5'-formacetal (3' --O--CH.sub.2 --O-- 5'), 3',5'-thioformacetal (3' --S--CH.sub.2 --O-- 5') or an analogous 2',5' linkage between adjacent nucleoside analog residues. Compositions comprising 5', 3' and 2' phosphinate nucleoside analogs useful in the methods are also provided.Type: GrantFiled: April 28, 1994Date of Patent: July 8, 1997Assignee: Gilead Sciences, Inc.Inventors: Mark D. Matteucci, Jiancun Zhang
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Patent number: 5627184Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10, wherein R.sub.8 is loweralkyl, and R.sub.9 and R.sub.10 are each independently selected from the group consisting of H and lower alkyl;R.sub.Type: GrantFiled: May 31, 1995Date of Patent: May 6, 1997Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
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Patent number: 5622955Abstract: The present invention provides methods for treating Cryptosporidium parvum in a subject in need of such treatment.Type: GrantFiled: May 31, 1995Date of Patent: April 22, 1997Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar, Byron L. Blagburn
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Patent number: 5622951Abstract: Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R and R.sup.3 are hydrogen or lower alkyl or R.sup.3 is spirocycloalkyl, R.sup.1 and R.sup.2 are aryl or heteroaryl radicals and n is 1 or 2 and m is 1 to 3 and the total of n+m is 2-4.Type: GrantFiled: May 24, 1995Date of Patent: April 22, 1997Assignee: John Wyeth & Brother Ltd.Inventors: Terence J. Ward, Mark A. Ashwell
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Patent number: 5616537Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.Type: GrantFiled: March 1, 1994Date of Patent: April 1, 1997Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
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Patent number: 5612340Abstract: N-phenyl-2-pyrimidineamine derivatives of formula (I) wherein the substituents are as defined in claim 1 are described. Those compounds can be used for example, in the treatment of tumour diseases.Type: GrantFiled: May 17, 1995Date of Patent: March 18, 1997Assignee: Ciba-Geigy CorporationInventor: J urg Zimmermann
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Patent number: 5610121Abstract: The invention relates to new heterocyclically disubstituted sulphonylamino(thio)carbonyl compounds of the formula (I) ##STR1## in which Q represents oxygen or sulphur,R.sup.1 and R.sup.2 are identical or different and independently of one another represent a radical from the series comprising heterocyclyl, heterocyclylamino and heterocyclylimino, in each case optionally substituted and bonded via N, with the exception of optionally substituted pyrazolylamino in the meaning of R.sup.1,and salts of the compounds of the formula (I), furthermore to processes for their preparation, and to their use as herbicides.Type: GrantFiled: November 15, 1994Date of Patent: March 11, 1997Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Ernst R. F. Gesing, Klaus-Helmut M uller, Peter M uller, Kurt Findeisen, Hans-Joachim Santel, Klaus L urssen, Robert R. Schmidt
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Patent number: 5607932Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R.sub.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is pyridinyl optionally substituted with up to two C.sub.1-4 alkyl groups; di(C.sub.1-4 alkyl) hydroxypyridinyl; di(C.sub.1-4 alkyl)C.sub.1-4 alkyloxypyridinyl; pyridazinyl optionally substituted with C.sub.1-4 alkyloxy; pyrimidinyl optionally substituted with hydroxy or C.sub.1-4 alkyloxy; thiazolyl optionally substituted with C.sub.1-4 alkyl; thiadiazolyl optionally substituted with C.sub.1-4 alkyl; benzoxazolyl or benzothiazolyl; or R.sup.6 is pyrazinyl or pyridazinyl substituted with C.sub.1-4 alkyl; Z is C.dbd.Type: GrantFiled: May 23, 1995Date of Patent: March 4, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Marc Willems, Robert J. M. Hendrickx
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Patent number: 5606058Abstract: The present invention provides compounds useful for treating Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum in a subject in need of such treatment.Type: GrantFiled: May 31, 1995Date of Patent: February 25, 1997Assignee: The University of North Carolina at Chapel HillInventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
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Patent number: 5599771Abstract: 3-Aryluracil derivatives of formula I ##STR1## wherein W is a group of the formula ##STR2## wherein the bond to the ring nitrogen atom is made via the carbon atom; wherein R.sub.1 to R.sub.9 are as defined in claim 1, are suitable as active ingredients in weed control compositions.Type: GrantFiled: December 16, 1994Date of Patent: February 4, 1997Assignee: Ciba-Geigy CorporationInventor: Jean Wenger
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Patent number: 5599522Abstract: A radical compound of formula Ia.C(Ar.sup.12).sub.3 (Ia)wherein:each Ar.sup.12, which may be the same or different, represents a 6-membered carbocyclic, at least one group Ar.sup.12 being a group Ar.sup.1 ;each group Ar.sup.1 represents a 6-membered ring optionally substituted at the or any ortho carbon by a group R.sup.1, R.sup.2, R.sup.3 or R.sup.4, at the or any meta carbon by a group R.sup.2 or R.sup.3, and at any para carbon by a group R.sup.1, R.sup.2, R.sup.3 or R.sup.4,with the proviso that no more than two ring carbons are unsubstituted;each of R.sup.1, R.sup.2, R.sup.3 or R.sup.4, which may be the same or different, independently represents a group of formula --M, --XM, --XAr.sup.2 or --Ar.sup.2 ;M represents a water solubilizing group, each group X, which may be the same or different, represents an oxygen or sulphur atom or a NH or CH.sub.2 group.Type: GrantFiled: September 2, 1992Date of Patent: February 4, 1997Assignee: Nycomed Imaging ASInventors: Mikkel J.o slashed.rgensen, Frode Rise, Sven Andersson, Torsten Almen, Klaes Golman
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Patent number: 5595992Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.Type: GrantFiled: September 12, 1994Date of Patent: January 21, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Preuss, Wolfgang Schaper, Martin M arkl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
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Patent number: 5589477Abstract: The object of the present invention is to obtain new class of compounds which have improving effect on learning and memory disorders with good selectivity in central nervous system and little side effects and then to provide a good medicine for treatment of dementia.The present invention relates to the compounds represented by the following general formula or their pharmacologically acceptable salts and the drugs of improving learning or memory disorders comprising them as active ingredients. ##STR1## (wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, hydroxy, alkoxy, trifluoromethyl or halogen. A represents methyl, trifluoromethyl, or tert-butyl. Y represents O or NH.Type: GrantFiled: February 26, 1993Date of Patent: December 31, 1996Assignee: Nippon Shinyaku Company, LimitedInventors: Shoichi Chokai, Tomiyoshi Aoki, Kiyoshi Kimura
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Patent number: 5589478Abstract: 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 --CH2--, 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: December 16, 1994Date of Patent: December 31, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, K osuke Yasuda, Kohei Kikkawa, Rikako Kohno
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Patent number: 5585328Abstract: This invention relates to certain herbicidal pyrrolesulfonylureas, compositions thereof and a method for their use as herbicides or plant growth regulants.Type: GrantFiled: September 12, 1995Date of Patent: December 17, 1996Assignee: E. I. du Pont de Nemours and CompanyInventors: William T. Zimmerman, Bruce A. Lockett, John Cuomo
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Patent number: 5578631Abstract: Disclosed is a method of combating Pneumocystis carinii Pneumonia in a subject in need of such treatment. The method comprises administering to to the subject an effective Pneumocystis carinii-combating amount of a bis-benzimidazole compound such as bis[5-(2-imidazolyl)-2-benzimidazolyl]methane, 1,4-bis[5-2-imidazolyl)-2-benzimidazolyl]butane, or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations for carrying out the method and novel compounds are also disclosed, along with methods of combating Giardia lamblia.Type: GrantFiled: April 24, 1995Date of Patent: November 26, 1996Assignee: The University of North Carolina at Chapel HillInventors: Richard R. Tidwell, Christine C. Dykstra, James E. Hall
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Patent number: 5576319Abstract: A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.Type: GrantFiled: August 26, 1994Date of Patent: November 19, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Janusz J. Kulagowski, Neil R. Curtis, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
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Patent number: 5571815Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 11, 1993Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, deceased, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
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Patent number: 5561232Abstract: Compounds of formulaA(B).sub.x, (I),whereinx is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores am distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: October 6, 1994Date of Patent: October 1, 1996Assignee: Ciba-Geigy CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5559081Abstract: Herbicidal sulfonamides of the formula: ##STR1## and salts thereof, where: A represents a substituted or unsubstituted benzene ring, or a 5- or 6-membered substituted or unsubstituted heteroaromatic ring; Q is --O--, --S-- or a group --CXX'--; X and X', which may be the same or different, are each hydrogen, halogen, cyano, an optionally-substituted alkyl group, or a group --OR.sup.a, --SR.sup.a, or --COR.sup.b ; or one of X and X' represents hydroxy and the other is as defined above; or X and X' together represent .dbd.O or .dbd.S; R.sup.a is an optionally-substituted alkyl, aryl or acyl group; R.sup.b is an optionally-substituted alkyl or aryl group, or a group --OR.sup.c or --NR.sup.c R.sup.d ; R.sup.c and R.sup.d, which may be the same or different, are each hydrogen, or an optionally-substituted alkyl or aryl group; Y is nitrogen or a group CR.sup.9 ; R.sup.1 is an optionally-substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, benzoheterocyclyl or amino group; R.sup.Type: GrantFiled: May 6, 1994Date of Patent: September 24, 1996Assignee: Agrevo UK LimitedInventors: Peter S. Gates, Graham P. Jones, David E. Saunders