Z Radical Contains Nitrogen Patents (Class 514/551)
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Patent number: 5378692Abstract: A method of lowering lipids is disclosed wherein a patient is administered a lipid metabolism improving composition characterized by comprising a compound of the following formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group; R.sub.2 and R.sub.3 are the same or different and each represents a hydroxyl group, a lower alkoxy group or an amino group, or a pharmacologically acceptable salt thereof as an active ingredient.Since the compound of the present invention lowers blood triglyceride, cholesterol and .beta.-lipoprotein levels, it is of value for ameliorating hyperlipidemia in arteriosclerotic diseases, e.g. myocardinal infarction, angina pectoris, cerebral infarction, cerebral arteriosclerosis, etc., nephrosis, hypertension, diabetes, obesity and other diseases, and prevention of various circulatory diseases.Type: GrantFiled: July 6, 1993Date of Patent: January 3, 1995Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Shinji Ohmori, Kazumi Ogata, Hideki Tsuruoka, Takahiro Sakaue, Yuuichi Isowaki, Yasuko Umegaki
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Patent number: 5364884Abstract: The invention relates to arginine and arginine-like compounds and to methods employing these compounds as ocular hypotensive agents. These compounds are effective when applied topically, may be used in low concentrations and are nontoxic. Additionally, the invention includes several new arginine derivatives with varying lipophilicities particularly suited for topical administration.Type: GrantFiled: January 21, 1993Date of Patent: November 15, 1994Assignee: Baylor College of MedicineInventors: Rajender S. Varma, George C. Y. Chiou
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Patent number: 5350766Abstract: The invention relates to a method for treating the complications of diabetes mellitus which comprises the administration to an individual afflicted with diabetes mellitus of an effective amount of N-alpha acetyl arginine.Type: GrantFiled: December 18, 1992Date of Patent: September 27, 1994Assignee: New York Medical CollegeInventor: Gerardo Suarez
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Patent number: 5318992Abstract: The present invention is a method of treating hypotension and shock using select ornithine or N.sup.G -arginine derivatives.Type: GrantFiled: July 13, 1993Date of Patent: June 7, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jeffrey P. Whitten, Ian A. McDonald, Laurie E. Lambert, Niall S. Doherty
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Patent number: 5278148Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.Type: GrantFiled: March 27, 1990Date of Patent: January 11, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 5232947Abstract: New N,N-di-alkyl- or alkenyl-substituted derivatives of oxamic acid of which the two alkyl or alkenyl groups are different from each other are now produced and found to exhibit the cerebral protective effect against cerebral anoxia in the brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain. Some known N,N-di-alkyl-substituted derivatives of oxamic acid or which the two alkyl groups are identical to each other are now also found to have similar, cerebral protective effect against cerebral anoxia and to be useful as an agent for improving the damaged functions of the brain.Type: GrantFiled: September 4, 1991Date of Patent: August 3, 1993Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Sato, Shinsuke Katoh, Kunio Atsumi, Mitsugu Hachisu, Seiji Shibahara
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Patent number: 5214056Abstract: A 1,3,2-dioxathiolane oxide derivative is represented by the following formula: ##STR1## wherein X represents --S(O)-- or --S(O).sub.2 --;R.sup.1 represents a hydrogen atom, an alkali metal atom, a benzyl group, or a lower alkyl group;R.sup.2 represents a lower alkyl group which may be substituted with a methylthio group, or a benzyl group, andR.sup.3 and R.sup.4 may be the same or different and independently represent a hydrogen atom, an alkyl group having one to ten carbon atoms, a lower alkyl group substituted with a guanidyl group, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group, or a phenethyl group, or together form an alkylene group.Type: GrantFiled: August 20, 1991Date of Patent: May 25, 1993Assignee: Japan Tobacco Inc.Inventors: Jun-ichi Haruta, Masahiro Tanaka, Itsuo Uchida, Akira Ohta, Shin Hara
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Patent number: 5202347Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: January 17, 1992Date of Patent: April 13, 1993Inventor: Nicholas S. Bodor
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Patent number: 5156665Abstract: A synergistic antimicrobial composition comprising 2-alkyl-3-isothiazolones, preferably 4,5-dichloro-2-n-octyl-3-isothiazolone or 2-n-octyl-3-isothiazolone, and certain iodopropargyl compounds, in a ratio to each other which exhibits synergism is disclosed.Type: GrantFiled: January 3, 1991Date of Patent: October 20, 1992Assignee: Rohm and Haas CompanyInventors: Samuel E. Sherba, Raj J. Mehta
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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
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Patent number: 5116992Abstract: The invention relates to glycerol derivatives of general formulae Ia, Ib and Ic ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, A and Y stand for various substituents, to a preparation process of said compounds and to therapeutical compositions containing the same.Type: GrantFiled: December 19, 1990Date of Patent: May 26, 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
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Patent number: 5089492Abstract: Acylamino carboxylic acid derivatives corresponding to the formula I ##STR1## in which the groups R.sup.1, R.sup.2, R.sup.3, Z.sup.1 and Z.sup.2 represent functional groups specified in the claims. The acylamino carboxylic acid derivatives have valuable pharmacological properties which, in particular, favorably influence nitrogen metabolism. The compounds are useful as active ingredients in pharmaceutical and/or dietetic compositions for treatment or prevention of nitrogen metabolism disturbances in large mammals caused, for example, by liver or kidney damage.Type: GrantFiled: May 24, 1990Date of Patent: February 18, 1992Assignees: Kali-Chemie AG, Pfrimmer Kabi GmbH & Co. KGInventors: Klaus Gerling, Henning Heinemanmn, Andreas Meier, Klaus Langer
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Patent number: 5081148Abstract: The invention relates to a therapeutical composition of matter for the treatment by perfusion of shock states comprising as an essential ingredient therein, an effective amount either, of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.4 stant for H or CH.sub.3 or C.sub.2 H.sub.5,R.sub.2 stands for H or NO.sub.2 andR.sub.3 stands for NHR.sub.4 or CH.sub.3 or C.sub.2 H.sub.5alone or of a mixture of said compound with a cyclooxygenase blocker.Type: GrantFiled: December 19, 1990Date of Patent: January 14, 1992Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Pierre-Etienne Chabrier de Lassauniere, Jean-Michel Guillon, Michel Auguet
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Patent number: 5073376Abstract: Tablets, capsules and other preparation forms for oral administration are produced which contain L-carnitine-L-tartrate. In comparison to preparations made with free L-carnitine, the invention preparations exhibit less hygroscopicity, longer stability and better capacity for being stored.Type: GrantFiled: March 27, 1990Date of Patent: December 17, 1991Assignee: Lonza Ltd.Inventors: Willibald E. Kohl, Thomas Scholl
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Patent number: 5051448Abstract: Ester derivatives of gamma-aminobutyric acid (GABA) and GABA analogues which cross the blood-brain barrier are disclosed, as well as methods of synthesizing and using the compounds.The ester derivatives have the formula: ##STR1## where A is a radical compound having at least one esterifiable OH group; n varies from one to the total number of esterifiable OH group contained in A; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or a substituent.Type: GrantFiled: May 7, 1990Date of Patent: September 24, 1991Assignee: The McLean Hospital CorporationInventor: Victor E. Shashoua
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Patent number: 5037851Abstract: The use is described of acetyl L-carnitine and its pharmacologically acceptable salts in the therapeutic treatment of cataract. The medicament may be administered orally or parenterally or be applied as a collyrium containing approximately 10%-15% w/v of acetyl L-carnitine.Type: GrantFiled: November 14, 1989Date of Patent: August 6, 1991Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventor: Claudio Cavazza
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Patent number: 5025029Abstract: A method is provided for inhibiting the .gamma. to .beta.-globin switching in subjects afflicted with .beta.-globin disorders. The method is particularly adapted for ameliorating the clinical symptoms of sickle cell anemia by periodically introducing butyrate, or certain isomers, homologs, analogs or chemical variations thereof, into the bloodstream of the subject prior to natural completion of the switching process.Type: GrantFiled: May 4, 1990Date of Patent: June 18, 1991Assignee: Children's Hospital Medical Center of Northern CaliforniaInventor: Susan Perrine
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Patent number: 5019564Abstract: An agricultural granule capable of carrying and releasing incorporated biocidal or nutritional agricultural chemicals. The granule is formed by the agitative agglomeration of a plant fiber slurry and resembles a clay granule in all respects except for its chemical inertness.Type: GrantFiled: October 19, 1987Date of Patent: May 28, 1991Assignee: Edward Lowe Industries, Inc.Inventors: H. Edward Lowe, Ricky L. Yoder, Clayton C. Nelson
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Patent number: 5017619Abstract: The invention is directed to phenethanolamine derivatives and their pharmaceutically compatible salts, having the formula ##STR1## wherein n is the number 1 or 2; L.sup.1 and L.sup.2 are hydrogen, C.sub.1-3 -(alkyl)carbonyl or C.sub.1-3 (alkoxy) carbonyl; T is hydrogen or methyl; X.sup.1 and X.sup.2 are phenyl or phenyl which is monosubstituted in the m-position by Br, Cl, F, CF.sub.3 and NO.sub.2 ; Y is --(CH.sub.2).sub.1-6 --O--G, --(CH.sub.2).sub.1-6 --CH.dbd.CH--C(O)--Z, --C(O)--Z or --CH(COOR").sub.2 ; G is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or --(CH.sub.2).sub.1-4 --Q; Q is phenoxy, phenyl, p-fluorophenyl or p-phenoxyphenyl; Z is a --OR or --N(R,R'); R and R' are hydrogen or C.sub.1-4 -alkyl or R and R' together with the N-atom to which they are attached form a 5- or 6-membered saturated ring which optionally contains an O-atom or an additional N-atom; and R" is C.sub.1-4 -alkyl.Type: GrantFiled: December 16, 1988Date of Patent: May 21, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 5017611Abstract: The present invention relates to the art of organic chemistry. The novel compounds - ethyl-3-(2-ethyl-2,2-dimethylhydrazinium)-propionate salts have the general formula: ##STR1## wherein X is Cl, Br, I. The compounds of the present invention possess an antiarrhythmic effect.Type: GrantFiled: October 30, 1989Date of Patent: May 21, 1991Inventors: Gunar A. Bremanis, Felix Z. Meerson, Ivars Y. Kalvinsh, Nurlan Abdikaliev, Petr T. Trapentsier, Ma/Ya G. Pshennikova, Irene B. Antsena, Edmund Y. Lukevits, Boris Z. Simkhovich
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Patent number: 5013719Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof, comprising co-administering to said patient an effective amount of an immunosuppressive agent, wherein said immunosuppressive agent is not an ornithine decarboxylase inhibitor, and an effective amount of an ornithine decarboxylase inhibitor.Type: GrantFiled: May 13, 1988Date of Patent: May 7, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Terry L. Bowlin
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Patent number: 4940696Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: November 16, 1987Date of Patent: July 10, 1990Assignee: Centre International de Recherches Dermatologioues (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 4918095Abstract: The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described.Such compounds have antibiotic activity and are useful in human and veterinary therapy.Type: GrantFiled: December 18, 1987Date of Patent: April 17, 1990Assignee: Zambon S.p.A.Inventors: Davide Della Bella, Giancarlo Jommi, Mario Fantucci, Dario Chiarino
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Patent number: 4879314Abstract: Dihaloformaldoximes of the formula: ##STR1## wherein R, X, X.sup.1 and Y are as defined herein having biocidal, fungicidal and pesticidal activity are disclosed.Type: GrantFiled: January 8, 1986Date of Patent: November 7, 1989Inventor: Adam C. Hsu
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Patent number: 4874789Abstract: Quaternary ammonium compounds have the formula R.sup.1 R.sup.2 R.sup.3 N.sup.+ (CH.sub.2).sub.m Y X.sup.- wherein R.sup.1 is an alkyl containing 8-20 carbon atoms, R.sup.2 is an alkyl containing 8-20 carbon atoms or methyl or ethyl, R.sup.3 is methyl or ethyl, m is an integer from 1-6, X is an anion and Y is a group having the structure --Z, --OH, --OR.sup.4, --OC(O)R.sup.5, --CN, --O--S(O) (O)--OQ, --C(O)OR.sup.6, --C.dbd.CH, --SR.sup.7, --S(O) (O)R.sup.8, --S(O)R.sup.9, --NR.sup.10 R.sup.11 and --CH.dbd.CH.sub.2 wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 are alkyls containing 1-12 carbon atoms or are phenyl and Z is halogen and Q is hydrogen or a cation having been found to be very effective bactericides.Type: GrantFiled: February 17, 1989Date of Patent: October 17, 1989Assignee: Ethyl CorporationInventors: Kim R. Smith, James E. Borland, Joe D. Sauer
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Patent number: 4868211Abstract: L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the amino-acid and carnitine protecting groups, thus obtaining the desired compound.Type: GrantFiled: November 8, 1988Date of Patent: September 19, 1989Assignee: 501 Sigma Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Maria O. Tinti, Carlo A. Bagolini, Domenico Misiti, Carlo Scolastico
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Patent number: 4863926Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.Type: GrantFiled: November 10, 1987Date of Patent: September 5, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
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Patent number: 4851441Abstract: This invention relates to antiviral organic guanidine derivatives compositions; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are tubastrines derived from marine coral Tubastrea aurea.Type: GrantFiled: January 28, 1988Date of Patent: July 25, 1989Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Tatsuo Higa, Ryuichi Sakai
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Patent number: 4824867Abstract: Quaternary ammonium compounds have the formula R.sup.1 R.sup.2 R.sup.3 N.sup.+ (CH.sub.2).sub.m Y X.sup.- wherein R.sup.1 is an alkyl containing 8-20 carbon atoms, R.sup.2 is an alkyl containing 8-20 carbon atoms or methyl or ethyl, R.sup.3 is methyl or ethyl, m is an integer from 1-6, X is an anion and Y is a group having the structure --Z, --OH, --OR.sup.4, --OC(O)R.sup.5, --CN, --O--S(O) (O)--OQ, --C(O)OR.sup.6, --C.dbd.CH, --SR.sup.7, --S(O)(O)R.sup.8, --S(O)R.sup.9, --NR.sup.10 R.sup.11 and --CH.dbd.CH.sub.2 wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 are alkyls containing 1-12 carbon atoms or are phenyl and Z is halogen and Q is hydrogen or a cation having been found to be very effective bactericides.Type: GrantFiled: September 22, 1986Date of Patent: April 25, 1989Inventors: Kim R. Smith, James E. Borland, Joe D. Sauer
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Patent number: 4812478Abstract: L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.Type: GrantFiled: June 29, 1987Date of Patent: March 14, 1989Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Maria O. Tinti, Carlo A. Bagolini, Domenico Misiti, Carlo Scolastico
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Patent number: 4803201Abstract: Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.Type: GrantFiled: May 28, 1987Date of Patent: February 7, 1989Assignee: Imperial Chemical Industries PLCInventor: Arnold H. Ratcliffe
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Patent number: 4789681Abstract: Compounds of the general formula I ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 and R.sub.3, which are the same or different, represent hydrogen or methyl, or taken together, form the amidine system to which an imidazole or imidazoline ring is bound;R.sub.4 is a linear or branched C.sub.1 -C.sub.10 alkyl group; cycloalkyl, aryl, aralkyl or hetaryl group;R.sub.5 is hydrogen or methyl;A is a propylene chain optionally substituted by one or two methyl groups in one or more of the positions thereof; a chain of formula --HN--CH.sub.2 --CH.sub.2 -- or of formula --N.dbd.CH--CH.sub.2 --; a 1,4-cyclohexylene group optionally substituted by one or more methyl groups; a 1,4- phenylene group optionally substituted by one or more halogen atoms, alkyl groups or C.sub.1 -C.sub.4 alkoxy group with the proviso that, when R.sub.4 is methyl or ethyl and R.sub.1 =R.sub.2 =R.sub.3 =R.sub.Type: GrantFiled: December 22, 1986Date of Patent: December 6, 1988Assignee: Italfarmaco S.p.A.Inventors: Giancarlo Sportoletti, Pietro Cremonesi, Moniquet Sarret
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Patent number: 4778804Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: October 11, 1985Date of Patent: October 18, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
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Patent number: 4767768Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: December 8, 1983Date of Patent: August 30, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
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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
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Patent number: 4760091Abstract: This invention relates to a method of controlling phytopathogenic rust and smut fungi of the Uredinales order in a plant locus which comprises applying a fungicidally effective amount of an ornithine decarboxylase inhibitor.Type: GrantFiled: February 18, 1987Date of Patent: July 26, 1988Assignee: The Dow Chemical CompanyInventors: Chrislyn M. Carson, Peter P. McCann
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Patent number: 4760061Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: July 26, 1988Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Brian S. Tait
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Patent number: 4749694Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.Type: GrantFiled: April 26, 1984Date of Patent: June 7, 1988Assignee: Merck & Co., Inc.Inventors: Joseph A. Fix, Stefano A. Pogany
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Patent number: 4721728Abstract: Compounds of the following general structure (I) ##STR1## where R.sub.1 stands for an acyl radical of the following structure (II) ##STR2## where p1 X.sup.- is a halogen atom and R.sub.4 is a C.sub.1 -C.sub.4 acyl radical or a hydrogen atomR.sub.2 stands for an R.sub.1 radical as defined above or for a hydrogen atomR.sub.3 stands for a substituted hydroxymethyl CH.sub.2 OR.sub.1 group, where R.sub.1 has the same value as defined above, or for a carboxyl group.Type: GrantFiled: October 7, 1986Date of Patent: January 26, 1988Assignee: SpA Societa' Prodotti Antibiotici S.p.A.Inventors: Tiberio Bruzzese, Franco Ottoni, Holger H. Van Den Heuvel
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Patent number: 4708954Abstract: Pharmaceutical compositions containing an oxaluric acid derivative of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen; an alkyl group or a cycloalkyl group; or R.sub.1 and R.sub.2 are joined to form a heterocyclic ring with the nitrogen atom to which they are both attached; and R.sub.3 is hydrogen or an alkyl group. These compounds have excellent hypoglycemic effects with low toxcicity and safety.Type: GrantFiled: February 7, 1986Date of Patent: November 24, 1987Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kazuharu Ienaga, Ko Nakamura, Akira Ishii
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Patent number: 4703061Abstract: A compound which is 4-(3,5-dihydroxy-3-methylpentylamide)butyric acid or its pharmaceutically acceptable salt or ester; this compound being produced by reacting a salt or an ester of gamma-aminobutyric acid with beta-hydroxy-beta-methyl-delta-valerolactone, and as required, converting the resulting compound in the form of a salt or ester to a free acid, or as required, converting the resulting compound in the form of a free acid to its pharmaceutically acceptable salt or ester; and useful as a medicament for preventing or treating an impediment in cerebral function.Type: GrantFiled: July 9, 1985Date of Patent: October 27, 1987Assignee: Kuraray Co., Ltd.Inventors: Tsutomu Kameyama, Jiro Kitamura, Tetsuo Takigawa, Masao Mizuno
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Patent number: 4695588Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.Type: GrantFiled: March 16, 1978Date of Patent: September 22, 1987Assignee: Merck & Co., Inc.Inventors: Janos Kollonitsch, Arthur A. Patchett
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Patent number: 4683241Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.Type: GrantFiled: May 21, 1984Date of Patent: July 28, 1987Assignee: G. D. Searle & Co.Inventors: Masateru Miyano, James R. Deason
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Patent number: 4675341Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)oxy]ethanol , its derivatives, and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections including that due to AIDS virus, various brain concussions and elevated intracranial pressure.Type: GrantFiled: August 13, 1986Date of Patent: June 23, 1987Assignee: Merck & Co., Inc.Inventor: Edward J. Cragoe, Jr.
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Patent number: 4639468Abstract: A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.Type: GrantFiled: August 23, 1985Date of Patent: January 27, 1987Assignee: Continental Pharma Inc.Inventors: Romeo Roncucci, Claude L. Gillet, Alexis H. Cordi, Mark A. Martens, Joseph L. Roba, Paul J. Niebes, Georges E. Lambelin, William R. Van Dorsser
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Patent number: 4594356Abstract: A method of inducing short-term pupil diameter enlargement and reducing intraocular pressure in animals without significant systemic effects is disclosed. There is provided a site-specific chemical delivery method for topically applying to the eye of an animal, an effective ophthalmologically acceptable amount of an adrenalone diester of the general formula: ##STR1## wherein R prepresents a member selected from the group consisting of hydrogen or a C.sub.1 -C.sub.3 straight alkyl group; and wherein R.sub.1 and R.sub.2 independently represent an acyl group or derivative thereof; or an opthalmologically acceptable acid addition salt thereof. The method allows the pupil diameter to be enlarged for a short period after which the pupil returns to normal and thus restores normal eye sight.Type: GrantFiled: January 8, 1985Date of Patent: June 10, 1986Assignee: Key Pharmaceuticals, Inc.Inventor: Nicholas Bodor
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Patent number: 4584318Abstract: A method is described for the control of nematodes in agricultural crops which comprises applying to the situs of infestation of a nematicidal composition containing as active ingredient a compound of the formula ##STR1## wherein Q is hydroxy, carbamoyloxy, or acyloxy, R is alkyl, alkenyl, alkynyl, X is halogen or methyl, n is 1 or 2. Preparation of active ingredient compounds is described, and nematicidal utility of compositions is exemplified.Type: GrantFiled: June 20, 1983Date of Patent: April 22, 1986Assignee: FMC CorporationInventors: Clinton J. Peake, Carmine P. DiSanzo, John F. Engel
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Patent number: 4563478Abstract: The invention relates to compounds possessing GABA-like sedative and tranquilizing activity, characterized by being of general formula:X.sub.1 OC--(CH.sub.2).sub.2 --NH--(CH.sub.2).sub.3 --CO--X.sub.2whereX.sub.1 and X.sub.2 are hydroxyl, a C.sub.1 -C.sub.6 alkoxy group or a free or substituted amino group, X.sub.1 being the same as or different from X.sub.2.The invention also relates to processes for their preparation, and composition for pharmaceutical and veterinary use which contains them.Type: GrantFiled: May 24, 1985Date of Patent: January 7, 1986Assignee: Hepar Chimie S.A.Inventors: Maria Curti, Fernando Fussi
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Patent number: 4524150Abstract: Pesticidal mixtures of carbamate insecticides and synthetic pyrethroids can be improved by the addition of stabilizers to prevent racemization of the pyrethroid to a less pesticidally-active isomeric form.Type: GrantFiled: March 3, 1983Date of Patent: June 18, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Orn Adalsteinsson
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Patent number: RE34805Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: July 10, 1992Date of Patent: December 6, 1994Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon