Plural 1,3-diazine Rings Patents (Class 544/296)
  • Patent number: 5783580
    Abstract: 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: Grant
    Filed: May 23, 1996
    Date of Patent: July 21, 1998
    Assignee: Sandoz, Ltd.
    Inventors: Martin Eberle, Fritz Schaub, Gerald Wayne Craig
  • Patent number: 5779934
    Abstract: 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: Grant
    Filed: February 14, 1995
    Date of Patent: July 14, 1998
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takayuki Higashii, Yukari Fujimoto, Tsutomu Matsumoto, Masayoshi Minai, Chizu Sekine, Kyoko Endo, Koichi Fujisawa
  • Patent number: 5780629
    Abstract: 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: Grant
    Filed: June 6, 1996
    Date of Patent: July 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
  • Patent number: 5773445
    Abstract: 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: Grant
    Filed: May 20, 1996
    Date of Patent: June 30, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Otto Schallner, Stefan Dutzmann, Heinz-Wilhelm Dehne, Gerd Hanssler
  • Patent number: 5763448
    Abstract: 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: Grant
    Filed: March 18, 1996
    Date of Patent: June 9, 1998
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: William Robert Carling, Ian James Collins, Michael Rowley, Paul David Leeson
  • Patent number: 5760037
    Abstract: 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: Grant
    Filed: July 23, 1996
    Date of Patent: June 2, 1998
    Assignee: L'Oreal
    Inventors: Jean-Baptiste Galey, Jacqueline Dumats
  • Patent number: 5756739
    Abstract: 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: Grant
    Filed: March 14, 1997
    Date of Patent: May 26, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Paul T. Angell, John Martin, Peter B. Anzeveno
  • Patent number: 5753664
    Abstract: 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: Grant
    Filed: March 13, 1996
    Date of Patent: May 19, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
  • Patent number: 5750469
    Abstract: 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: Grant
    Filed: March 1, 1996
    Date of Patent: May 12, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5739333
    Abstract: 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: Grant
    Filed: May 9, 1996
    Date of Patent: April 14, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5739137
    Abstract: 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: Grant
    Filed: February 28, 1996
    Date of Patent: April 14, 1998
    Assignee: 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
  • Patent number: 5728706
    Abstract: 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: Grant
    Filed: April 24, 1996
    Date of Patent: March 17, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5723626
    Abstract: 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: Grant
    Filed: July 9, 1996
    Date of Patent: March 3, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 5723409
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: March 3, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5714488
    Abstract: 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: Grant
    Filed: September 17, 1996
    Date of Patent: February 3, 1998
    Assignee: Abbott Laboratories
    Inventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
  • Patent number: 5714438
    Abstract: 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: Grant
    Filed: December 5, 1996
    Date of Patent: February 3, 1998
    Assignee: Zeneca Limited
    Inventors: David B. Kanne, Michael P. Prisbylla
  • Patent number: 5707930
    Abstract: 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: Grant
    Filed: September 16, 1996
    Date of Patent: January 13, 1998
    Assignee: Zeneca Limited
    Inventors: Raymond A. Felix, Hsiao-Ling M. Chin, Frank X. Woolard, David L. Lee, David B. Kanne
  • Patent number: 5705502
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: January 6, 1998
    Assignee: Novartis Corporation
    Inventor: Jurg Zimmermann
  • Patent number: 5698563
    Abstract: 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: Grant
    Filed: January 13, 1995
    Date of Patent: December 16, 1997
    Assignee: Alteon Inc.
    Inventors: Dilip R. Wagle, Michael E. Lankin, David H. Shih
  • Patent number: 5698564
    Abstract: 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: Grant
    Filed: December 21, 1995
    Date of Patent: December 16, 1997
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Koichi Katsuyama, Masato Ariga, Yukio Saito, Shigeo Hatanaka, Toshihiro Takahashi
  • Patent number: 5686456
    Abstract: 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: Grant
    Filed: November 28, 1995
    Date of Patent: November 11, 1997
    Assignees: The University of North Carolina, Georgia State University Research Foundation, Inc., Auburn University
    Inventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
  • Patent number: 5681957
    Abstract: 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: Grant
    Filed: May 3, 1996
    Date of Patent: October 28, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Erich Wolters, Guido Steffan, Alexander Klausener
  • Patent number: 5679792
    Abstract: 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: Grant
    Filed: June 1, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Claus Escher, Gerhard Illian, Hubert Schlosser, Rainer Wingen
  • Patent number: 5674894
    Abstract: 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: Grant
    Filed: May 15, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
  • Patent number: 5672583
    Abstract: 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: Grant
    Filed: May 17, 1995
    Date of Patent: September 30, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Kevin Chapman, William Hagmann, Philippe Durette, Craig Esser, Ihor Kopka, Charles Caldwell
  • Patent number: 5667721
    Abstract: 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: Grant
    Filed: February 21, 1996
    Date of Patent: September 16, 1997
    Assignee: Rolic AG
    Inventors: Richard Buchecker, Guy Marck, Alois Villiger
  • Patent number: 5668140
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: September 16, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Gerhard Salbeck, Heinz Ehrhardt, Peter Braun, Werner Knauf, Burghard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
  • Patent number: 5663336
    Abstract: 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: Grant
    Filed: October 18, 1995
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Uwe Trinks, Peter Traxler
  • Patent number: 5658902
    Abstract: 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: Grant
    Filed: December 22, 1994
    Date of Patent: August 19, 1997
    Assignee: Warner-Lambert Company
    Inventors: Kyunghye Ahn, Xue-Min Cheng, Annette Marian Doherty, Edward Faith Elslager, Brian Kornberg, Chitase Lee, Daniele Leonard, Sham Nikam, Leslie Morton Werbel
  • Patent number: 5659065
    Abstract: 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: Grant
    Filed: April 4, 1995
    Date of Patent: August 19, 1997
    Assignee: Novartis Corporation
    Inventor: Richard Goschke
  • Patent number: 5646269
    Abstract: 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: Grant
    Filed: April 28, 1994
    Date of Patent: July 8, 1997
    Assignee: Gilead Sciences, Inc.
    Inventors: Mark D. Matteucci, Jiancun Zhang
  • Patent number: 5627184
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: May 6, 1997
    Assignees: 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
  • Patent number: 5622955
    Abstract: The present invention provides methods for treating Cryptosporidium parvum in a subject in need of such treatment.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 22, 1997
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn University
    Inventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar, Byron L. Blagburn
  • Patent number: 5622951
    Abstract: 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: Grant
    Filed: May 24, 1995
    Date of Patent: April 22, 1997
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Terence J. Ward, Mark A. Ashwell
  • Patent number: 5616537
    Abstract: 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: Grant
    Filed: March 1, 1994
    Date of Patent: April 1, 1997
    Assignees: 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
  • Patent number: 5612340
    Abstract: 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: Grant
    Filed: May 17, 1995
    Date of Patent: March 18, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: J urg Zimmermann
  • Patent number: 5610121
    Abstract: 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: Grant
    Filed: November 15, 1994
    Date of Patent: March 11, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: 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
  • Patent number: 5607932
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: March 4, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Raymond A. Stokbroekx, Marc Willems, Robert J. M. Hendrickx
  • Patent number: 5606058
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: February 25, 1997
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
  • Patent number: 5599771
    Abstract: 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: Grant
    Filed: December 16, 1994
    Date of Patent: February 4, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean Wenger
  • Patent number: 5599522
    Abstract: 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: Grant
    Filed: September 2, 1992
    Date of Patent: February 4, 1997
    Assignee: Nycomed Imaging AS
    Inventors: Mikkel J.o slashed.rgensen, Frode Rise, Sven Andersson, Torsten Almen, Klaes Golman
  • Patent number: 5595992
    Abstract: 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: Grant
    Filed: September 12, 1994
    Date of Patent: January 21, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Wolfgang Schaper, Martin M arkl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
  • Patent number: 5589477
    Abstract: 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: Grant
    Filed: February 26, 1993
    Date of Patent: December 31, 1996
    Assignee: Nippon Shinyaku Company, Limited
    Inventors: Shoichi Chokai, Tomiyoshi Aoki, Kiyoshi Kimura
  • Patent number: 5589478
    Abstract: 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: Grant
    Filed: December 16, 1994
    Date of Patent: December 31, 1996
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, K osuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5585328
    Abstract: This invention relates to certain herbicidal pyrrolesulfonylureas, compositions thereof and a method for their use as herbicides or plant growth regulants.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: December 17, 1996
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: William T. Zimmerman, Bruce A. Lockett, John Cuomo
  • Patent number: 5578631
    Abstract: 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: Grant
    Filed: April 24, 1995
    Date of Patent: November 26, 1996
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Richard R. Tidwell, Christine C. Dykstra, James E. Hall
  • Patent number: 5576319
    Abstract: 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: Grant
    Filed: August 26, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Janusz J. Kulagowski, Neil R. Curtis, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
  • Patent number: 5571815
    Abstract: 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: Grant
    Filed: March 11, 1993
    Date of Patent: November 5, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, deceased, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
  • Patent number: 5561232
    Abstract: 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: Grant
    Filed: October 6, 1994
    Date of Patent: October 1, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 5559081
    Abstract: 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: Grant
    Filed: May 6, 1994
    Date of Patent: September 24, 1996
    Assignee: Agrevo UK Limited
    Inventors: Peter S. Gates, Graham P. Jones, David E. Saunders