C-c(=x)-x-c Containing (x Is Chalcogen And At Least One X Is Other Than Oxygen) Patents (Class 514/513)
-
Patent number: 5231113Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where the R groups are independently hydrogen, or lower alkyl; A is --C(O)O--, --OC(O)--, --C(O)S--, or --SC(O)--; n is 0-5; and Z is H, --COB where B is --OH or a pharmaceutically acceptable salt, or B is --OR.sub.1 where R.sub.1 is an ester-forming group, or B is --N(R).sub.2 where R is hydrogen or lower alkyl, or Z is --OE where E is hydrogen or an ether-forming group or --COR.sub.2 where R.sub.2 is hydrogen, lower alkyl, phenyl or lower alkyl phenyl, or Z is --CHO or an acetal derivative thereof, or Z is --COR.sub.3 where R.sub.3 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4 and the sum of n and m does not exceed 4.Type: GrantFiled: June 4, 1992Date of Patent: July 27, 1993Assignee: Allergan, Inc.Inventors: Roshantha A. S. Chandraratna, Robert J. Weinkam
-
Patent number: 5223529Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.Type: GrantFiled: May 11, 1990Date of Patent: June 29, 1993Assignee: Rhone-Poulenc SanteInventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Gerard Roussel, Franco Manfre
-
Patent number: 5223516Abstract: Compounds of the formula ##STR1## wherein Y can be tetrazolyl are disclosed. These compounds are useful as cardiovascular agents.Type: GrantFiled: April 24, 1991Date of Patent: June 29, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, George C. Rovnyak, Melanie J. Loots
-
Patent number: 5208255Abstract: The (R) or (S) isomer of acetorphan or N-/2-acetylthiomethyl)-1-oxo-3-phenylpropyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-2-benzylpropanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.Type: GrantFiled: November 22, 1988Date of Patent: May 4, 1993Assignee: Societe Civile BioprojetInventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Jean-Christophe Plaquevent, Bruno Giros, Claude Gros, Jean-Charles Schwartz, Jeanne-Marie Lecomte
-
Patent number: 5204338Abstract: The invention relates to oxalylamino acid derivatives of the formula I ##STR1## in which R and R' are identical or different and are C.sub.1 -C.sub.6 -alkyl or hydrogen,R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.3 -alkoxy, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aryl, SH, NH.sub.2 or halogen, where the alkyl radicals are unsubstituted or substituted by aryl, OH, SH or NH.sub.2orR.sup.1 and R.sup.2 together are a C.sub.2 -C.sub.4 -alkylene chain and the compounds in their predominantly pure D- and L-form and the physiologically tolerable salts.The compounds are distinguished as excellent inhibitors of prolyl hydroxylase and lysine hydroxylase.Type: GrantFiled: May 10, 1991Date of Patent: April 20, 1993Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Harald Burghard, Volkmar Gunzler-Pukall
-
Patent number: 5190974Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.Type: GrantFiled: July 5, 1991Date of Patent: March 2, 1993Assignee: Roussel UclafInventors: Francoise Clemence, Odile Le Martret, Francis Petit
-
Patent number: 5179121Abstract: Novel 4-chloro-4,4-difluorothiobutyric acid derivatives of the formula I ##STR1## in which R.sub.1 and R.sub.2 are, independently of one another, hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 halogenoalkyl and R.sub.3 is hydrogen or an organic radical can be employed as pest-control agents. Control of insects and arachnids is possible and preferable.Type: GrantFiled: August 15, 1991Date of Patent: January 12, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Manfred Boger, Eginhard Steiner
-
Patent number: 5177109Abstract: Compounds, compositions and methods are described for treating a CNS disorder such as a cognitive disorder, epilepsy, depression, Parkinson's disease, Alzheimer's disease, a neurodegenerative disease or neurotoxic injury. Compound of interest are 2-amino-4,5-methyleneadipic acid compounds and derivatives defined by the formula I: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, ##STR2## with each of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and ##STR3## with each of R.sup.6 and R.sup.7 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R.sup.1 through R.sup.Type: GrantFiled: July 19, 1991Date of Patent: January 5, 1993Assignee: G. D. Searle & Co.Inventors: Roberto Pellicciari, Benedetto Natalini, Maura Marinozzi, Alexis A. Cordi, Joseph B. Monahan, Thomas H. Lanthorn
-
Patent number: 5173506Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--, --S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sub.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a 5-, 6- or 7-membered carbocyclic ring;R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;R.sub.Type: GrantFiled: August 16, 1990Date of Patent: December 22, 1992Assignee: Schering CorporationInventors: Bernard R. Neustadt, Alan Bronnenkant
-
Patent number: 5173289Abstract: Aromatic esters and thioesters of the formula ##STR1## are useful in human and veterinary medicine and in cosmetic formulations. In the formula, X represents oxygen or sulfur, r' and 4" represent hydrogen, lower alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid or aminated sugar, or taken together form a heterocycle, R.sub.2 represents .alpha., .alpha.'- dissubstituted alkyl having 4-12 carbon atoms or mono- or polycyclic cycloalkyl having 5-12 carbon atoms whose carbon linking carbon is trisubstituted and R.sub.3 and R.sub.4 represent hydrogen or lower alkyl.Type: GrantFiled: February 16, 1990Date of Patent: December 22, 1992Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
-
Patent number: 5166390Abstract: A compound of the formula ##STR1## wherein R.sub.1 is an organic radical having at least 2 carbon atoms;R.sub.2 is an organic radical; andA.dbd.CO,CH.sub.2, or CHR.sub.3 where R.sub.3 is unsubstituted or substituted alkyl; andZ.sub.1 and Z.sub.2 are independently selected from hydrogen, halogen, and (C.sub.1 -C.sub.4)alkyland use as a fungicide and biocide.Type: GrantFiled: January 5, 1990Date of Patent: November 24, 1992Assignee: Rohm and Haas CompanyInventors: Barry Weinstein, Philip Robinson, Katherine E. Flynn, Cherylann Schieber
-
Patent number: 5164413Abstract: Acne can be treated by applying to the skin of a subject a composition containing one of a certain group of acids, acid halides or amides.Type: GrantFiled: May 22, 1991Date of Patent: November 17, 1992Assignee: Bristol-Myers Squibb CompanyInventor: Sandra L. Willis
-
Patent number: 5164412Abstract: A Derivative of 5-hetero-6-oxo-PGE A derivative of 5-hetero-6-oxo-PGE of the formula: ##STR1## wherein R.sup.1 is (1) a group of the formula: COOR11(2) hydroxymethylcarbonyl,(3) hydroxymethyl or(4) a group of the formula:CO--AAwherein AA is an amino acid-residue,Z is oxygen, sulfur or a group of the formula: NR21 wherein R21 is hydrogen or alkyl of C1--4;R2 is a single-bond or alkylene of C1--4;R3 isi) alkyl of C1-7,ii) cycloalkyl of C4-7 or cycloalkyl of C4-7 substituted by alkyl of C1-7,iii) phenyl, phenoxy, phenyl or phenoxy substituted by one group selected from alkyl of C1-4, halogen and trihalomethyl, is single-bond or a double bond.Possess PG-like activity, especially cytoprotection, and therefore are useful for treatment for and/or prevention of cytodamage.Type: GrantFiled: April 8, 1991Date of Patent: November 17, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yoshitaka Konishi, Masanori Kawamura
-
Patent number: 5149695Abstract: Fumaric acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or a metallic cation, andR.sub.2 is a saturated or unsaturated aliphatic C.sub.6 -C.sub.24 alkyl group, psoralen-9-yl, retinyl, .alpha.-tocopheryl (vitamin E), calciferyl, corticosteroid-21-yl or monosaccharid-.omega.-yl; a group of fumaric acid derivatives based on glycerol, alkane diol or polyol molecules; and fumaric acid derivatives of the formula ##STR2## wherein n is an integer from to 30 to 260,R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group,R.sub.4 is one of the R.sub.3 groups and n is the number of molecule repetitions, processes for their production and compositions containing same are described. These compounds are useful as drugs for the treatment of cryptogenically-caused diseases and have antisporiatic as well as antimicrobial action.Type: GrantFiled: March 13, 1989Date of Patent: September 22, 1992Inventors: Peter P. Speiser, Rajendra K. Joshi
-
Patent number: 5147892Abstract: Benzyl ketones of the formula ##STR1## where X is CH or N,Y is O or NR.sup.4,R.sup.1, R.sup.2 are H or alkyl,R.sup.3 is halogen, cyano, nitro, alkyl, cycloalkyl, alkoxy, haloalkyl, arylalkyl, arylalkoxy, aryloxy or aryl, and the aryl groups in turn may be substituted,R.sup.4 is OH, alkoxy or arylalkoxy andR.sup.5 is H, methyl, halogen or methoxy,and fungicides containing these compounds.Type: GrantFiled: June 27, 1991Date of Patent: September 15, 1992Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5140044Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.Type: GrantFiled: March 27, 1990Date of Patent: August 18, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
-
Patent number: 5130336Abstract: Treating a patient for neuro-muscular incontinence by administering a thiol-S-(2-diethyl-aminoethyl)-ester compound selected from the group consisting of trimethylacetyl-thio-S-(2-diethylaminoethyl)-ester, 1-cyclohexyl-1-phenylacetyl-thiol-S-(2-diethylaminoethyl)-ester, palmitoyl-thio-S-(2-diethylaminoethyl)-ester, 4-t-butyl-benzoyl-thiol-S-(2-diethylaminoethyl)-ester, phenylacetyl-thio-S-(2-diethylaminoethyl)-ester, 4-phenyl-butyryl-thio-S-(2-diethylaminoethyl)-ester, and 2-ethyl-butyryl-thio-S-(2-diethylaminoethyl)-ester.Type: GrantFiled: November 15, 1991Date of Patent: July 14, 1992Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
-
Patent number: 5124322Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.Type: GrantFiled: June 19, 1989Date of Patent: June 23, 1992Assignee: Beecham Group p.l.c.Inventor: Ian Hughes
-
Patent number: 5122539Abstract: Compounds of the general structural formula: ##STR1## wherein X, Y and Z may each be CH.sub.2, NH, or O, R.sub.2-6 are either hydrogen, halogen, or a substituted or unsubstituted C.sub.1, C.sub.2, or C.sub.3 alkyl group and these moieties maybe the same or different, or alkyl moieties of aliphatic or aromatic rings incorporating two of the R.sub.2-6 sites, R.sub.7-8 are hydrogen, methyl, or ethyl groups and these moieties may be the same or different, or alkyl moieties as part of an aliphatic ring connecting R.sub.7 and R.sub.8, and R.sub.9 is a hydrogen, loweralkyl such as methyl, ethyl or propyl, or a salt cation such as sodium, potassium, or ammonium are useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: May 20, 1991Date of Patent: June 16, 1992Assignee: Center for Innovative TechnologyInventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad
-
Patent number: 5118674Abstract: The invention relates to 3-(N-methyl-N-alkyl)-amino 2-methoxymethylene propan 1-ol derivatives of the formula ##STR1## wherein R stands for an alkyl chain, A stands for: ##STR2## and Y represents various quaternary ammonia, to a preparation process of said compounds and to therapeutic compositions containing the same.Type: GrantFiled: November 27, 1990Date of Patent: June 2, 1992Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Colette Broquet, Benedicte Vandamme, Paola Principe-Nicolas
-
Patent number: 5112837Abstract: The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.Type: GrantFiled: September 17, 1990Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Kenneth D. Burrows, Leslie R. Hughes, Peter Warner
-
Patent number: 5112860Abstract: Thiocarboxylic esters of the formula I ##STR1## where the substituents have the following meanings: X is oxygen, sulfur, oxymethylene, methyleneoxy, thiomethylene, methylenethio, ethylene, ethenylene or ethynylene,Y, Z are each sulfur or oxygen, but Y and Z are not simultaneously oxygen,R is alkyl, mononuclear, dinuclear or trinuclear aryl or hetaryl, where aryl and hetaryl may be substituted,and fungicidal agents containing these compounds.Type: GrantFiled: November 2, 1990Date of Patent: May 12, 1992Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Siegbert Brand, Bernd Wenderoth, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5098934Abstract: Novel .omega.-mercaptopropanamides and their homologs of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and ##STR2## R.sub.1 ' is selected from the group consisting of alkyl of 1 to 5 carbon atoms and aryl optionally substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and halogen, n is an integer from 1 to 5, R.sub.2 is selected from the group consisting of hydrogen alkyl of 1 to 5 carbon atoms and aryl and aralkyl of 6 to 15 carbon atoms optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, halogen and --CF.sub.3, R.sub.3 is selected from the group consisting of a) hydrogen, b) phenyl optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --NO.sub.2, halogen, --CF.sub.Type: GrantFiled: June 22, 1990Date of Patent: March 24, 1992Assignee: Roussel UclafInventors: Jean-Paul Vevert, Francoise Delevallee, Rogert Deraedt
-
Patent number: 5093361Abstract: The S-[d-2-(6-methoxy-2-naphthyl)-propionyl]d-2-mercaptopropionamidoacetic acid having formula: ##STR1## has improved therapeutic properties not only in comparison with the starting active principle, namely Naproxen, but also with respect to the corresponding racemic derivative, namely the (d,l) compound.Type: GrantFiled: February 26, 1990Date of Patent: March 3, 1992Assignee: Farma Resa S.r.l.Inventors: Valentina Reiner, Caterina Sarda
-
Patent number: 5066672Abstract: The invention relates to compounds of the polyfluoroalkyl acetate, thioacetate or acetamide type, which can be denoted by the general formula: ##STR1## in which Rf denotes a perfluoroalkyl radical, m is an integer ranging from 1 to 4, Q denotes an oxygen or sulphur atom or an NH group, X.sup.- denotes an anion, R.sub.1 denotes an alkyl radical containing from 1 to 3 carbon atoms, R.sub.2 denotes the allyl radical or an alkyl radical containing from 1 to 18 carbon atoms, and R.sub.3 denotes an alkyl radical containing from 7 to 18 carbon atoms or one of the following radicals: ##STR2## wherein n is an integer from 2 to 4, R is hydrogen or methyl, and Y denotes C.sub.2 -C.sub.8 alkylene bridge optionally interrupted by an oxygen atom.These compounds can be used as surface-active agents or an monomers for developing artificial vesicles.Type: GrantFiled: December 27, 1989Date of Patent: November 19, 1991Assignee: Societe AtochemInventors: Alain Sismondi, Parfait Abenin, Aime Cambon
-
Patent number: 5036104Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependent, neutral endopiptidase.Type: GrantFiled: June 14, 1990Date of Patent: July 30, 1991Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James
-
Patent number: 5017604Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: April 11, 1990Date of Patent: May 21, 1991Assignee: Warner-Lambert CompanyInventors: Thomas R. Belliotti, Catherine R. Kostlan
-
Patent number: 5015644Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.Type: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi
-
Patent number: 5010097Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; R.sub.3 is C.sub.3-6 alkyl;R.sub.4 is hydrogen, alkyl, --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl, or a group ##STR3## where R.sub.11 is hydrogen, alkyl, or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.12 is hydrogen or alkyl; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.Type: GrantFiled: December 20, 1988Date of Patent: April 23, 1991Assignee: Beecham PharmaceuticalsInventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes, Laramie M. Gaster
-
Patent number: 4983630Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.Type: GrantFiled: November 28, 1988Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
-
Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
-
Patent number: 4975462Abstract: Disclosed herein are novel .alpha.-arylcarbamoyl cyanoacetic esters, thioesters, and amides which exhibit anti-inflammatory/antiarthritic activities.Type: GrantFiled: July 29, 1988Date of Patent: December 4, 1990Assignee: Bristol-Myers CompanyInventor: William T. Han
-
Patent number: 4938797Abstract: The invention relates to a process for the preparation of microcapsules having a capsule wall of polyurea and encapsulating a water-immiscible pesticide. The process comprises first dispersing a solution of a polyisocyanate in the sparingly water-soluble pesticide, in the presence of an anionic dispersant and at least one nonionic protective colloid and/or a nonionic surfactant, and subsequently reacting the dispersion with a polyamine, to give a stable aqueous suspension of microcapsules which can be used either direct or after dilution with water as pesticidal composition.Type: GrantFiled: June 7, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Hans W. Hasslin, Michael J. Hopkinson
-
Patent number: 4929641Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.Type: GrantFiled: May 11, 1988Date of Patent: May 29, 1990Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
-
Patent number: 4927845Abstract: Anthralin analogues containing a thio-substituent, especially in one or more of the positions 2-, 7- and 10- of the anthralin ring. They may be made by reacting an anthralin derivative (e.g. 10-bromoanthralin) with a thiol or a compound containing a group convertible to a thio-group. Alternatively, a 1,8-dihydroxy anthraquinone containing a thio-substituent may be reduced. Reactive intermediates may be made by introducing one or more nuclear allylic groups into a 1,8-dihydroxy anthraquinone and then converting them into a reactive form, e.g. by epoxidation or halide addition. The intermediate can then reduced to the oxidation state corresponding to anthralin.Additional products having the 10-carbon atom of the anthralin ring as part of a heterocyclic ring, may be made by anthralins containing various substitutes thioalkyl groups as the 10-substituent.The compounds are useful for treatment of psoriasis, and may be formulated in the conventional vehicles for topical application, for example petrolatum.Type: GrantFiled: August 15, 1989Date of Patent: May 22, 1990Assignee: The Victoria University of ManchesterInventor: John M. Bruce
-
Patent number: 4925658Abstract: Aromatic esters and thioesters have the formula ##STR1## wherein X represents oxygen or sulfur,R.sub.1 represents --CH.sub.2 OH, --CH(OH)--CH.sub.3, --COOR.sub.5 or ##STR2## R.sub.5 represents hydrogen, lower alkyl, lower alkenyl, monohydroxyalkyl or polyhydroxyalkyl,r' and r" represent hydrogen, lower alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid or aminated sugar, or taken together form a heterocycle,R.sub.2 represents .alpha.,.alpha.'-disubstituted alkyl having 4-12 carbon atoms or mono- or polycyclic cycloalkyl having 5-12 carbon atoms whose carbon linking carbon is trisubstituted,R.sub.3 represents hydrogen, lower alkyl, or --Si(CH.sub.3).sub.2 R'.sub.3 wherein R'.sub.3 represents lower alkyl, andR.sub.4 represents hydrogen or lower alkyl, andthe salts of these aromatic esters and thioesters of formula (I) when R.sub.5 represents hydrogen.Type: GrantFiled: January 19, 1989Date of Patent: May 15, 1990Assignee: Centre International De Recherches dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
-
Patent number: 4918082Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula ##STR1## where R.sub.2 is a radical selected from the group consisting of ##STR2## where m is an integer from 0 to 3.Type: GrantFiled: September 2, 1988Date of Patent: April 17, 1990Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
-
Patent number: 4910222Abstract: The present invention covers D or L or DL-cysteine derivatives of the general formula (I) ##STR1## wherein R represents H or a fatty saturated or unsaturated acid radical, or a radical of an aromatic acid such as benzoic, cynnamic, salycilic, 2-acetoxybenzoic acid or a heterocyclic acid, as well as their salts, in particular the Ca and Mg salts.The invention refers also to a process for preparing said derivatives and to the pharmaceutical preparations containing them as active principle, having a bronchial liquefying and expectorating activity.Type: GrantFiled: July 29, 1988Date of Patent: March 20, 1990Assignee: Magis Farmaceutici SpAInventor: Laura Puricelli
-
Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
-
Patent number: 4879309Abstract: Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.Type: GrantFiled: January 30, 1989Date of Patent: November 7, 1989Assignee: Schering CorporationInventors: Ronald J. Doll, Bernard R. Neustadt
-
Patent number: 4816482Abstract: A pharmaceutical composition effective in the protection of normal tissues against radiation induced damage comprising administration a compound of the formulaR.sub.1 --CO--NR.sub.3 --/A/--S--R.sub.2in which R.sub.1 is a radical corresponding to an amino acid R.sub.1 --COOH, /A/ is a C.sub.2 or C.sub.3 alkylene radical which can be substituted with a C.sub.1 to C.sub.3 alkyl radical, or with a hydroxy or hydroxycarbonyl radical or a --COR radical where R is an amino or --NH--CH.sub.2 --CO.sub.2 H radical, R.sub.2 is an acyl radical which protects the thiol group and which liberates the thiol group in vivo, R.sub.3 is a hydrogen, and also the salts of this compound with pharmaceutically acceptable acids.Type: GrantFiled: February 22, 1985Date of Patent: March 28, 1989Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Joel Oiry, Jean-Louis Imbach
-
Patent number: 4812477Abstract: A method for the treatment of ischemia and reperfusion syndromes, which consists in administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.6 alkyl group, or of a salt thereof, when R=H, with a pharmaceutically acceptable base.New compounds and pharmaceutical compositions useful in the method of this invention.Type: GrantFiled: August 8, 1988Date of Patent: March 14, 1989Assignee: Zambon S.p.A.Inventors: Vittorio Ferrrari, Angelo Carenzi, Davide Della Bella
-
Patent number: 4808628Abstract: An amide derivative of the formula (I): ##STR1## or a tautomeric form thereof, wherein R is a phenyl group substituted in the 4-position by a group of R.sup.1 XCH.sub.2--, where R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkynyl, C.sub.1 -C.sub.4 alkylcarbonyl, or H, and X is oxygen or sulphur; E is CN, or CSNH.sub.2, or CONH.sub.2 ; and Y is C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.3 -C.sub.4 alkynyloxy, 1-pyrazolyl or 2-furyl. Compositions and processes for using these derivatives to combat plant fungi are also disclosed.Type: GrantFiled: November 12, 1987Date of Patent: February 28, 1989Assignee: Imperial Chemical Industries PLCInventors: Margaret C. Shephard, Patrick J. Crowley
-
Patent number: 4806567Abstract: A method for the treatment of ischemia and reperfusion syndromes, which consists in administering to a patient in need thereof a therapeutically effective amount of a compound of the formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.6 alkyl group, or of a salt thereof, when R.dbd.H, with a pharmaeutically acceptable base.New compounds and pharmaceutical compositions useful in the method of this invention.Type: GrantFiled: July 13, 1987Date of Patent: February 21, 1989Assignee: Zambon S.p.A.Inventors: Vittorio Ferrari, Angelo Carenzi, Davide Della Bella
-
Patent number: 4803225Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 2, 1987Date of Patent: February 7, 1989Assignee: Fisons, plcInventors: John Dixon, Francis Ince
-
Patent number: 4801609Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.Type: GrantFiled: March 27, 1987Date of Patent: January 31, 1989Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
-
Patent number: 4785004Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.Type: GrantFiled: December 15, 1986Date of Patent: November 15, 1988Assignee: Ciba-Geigy CorporationInventors: Andreas Von Sprecher, Werner Breitenstein, Andreas Beck, Robert W. Lang, Konrad Oertle
-
Patent number: 4774256Abstract: Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.Type: GrantFiled: November 13, 1987Date of Patent: September 27, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, Eric M. Gordon, Miguel A. Ondetti
-
Patent number: 4767781Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl or acyl, R.sub.2 is hydroxy, alkoxy or amino, is useful as an antidiabetic agent.Type: GrantFiled: December 8, 1986Date of Patent: August 30, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Shinagawa, Tsuneo Kanamaru, Setsuo Harada
-
Patent number: 4767625Abstract: A lamella type, single phase liquid crystal composition is prepared from a hydrophilic nonionic surfactant, a water-soluble substance having a hydroxyl group in a molecule thereof, an oil substance, and water.Oil-base cosmetic compositions including cleansing compositions, massage creams or drugs for external application are incorporated with the liquid crystal.The compositions are readily washed off simply by water, and exhibit good properties of non-stickiness and long storage stability.Type: GrantFiled: August 14, 1986Date of Patent: August 30, 1988Assignee: Kao CorporationInventors: Yuichiro Mitsuno, Keiko Nomaguchi, Toshiyuki Suzuki