Patents Examined by Diana G. Rivers
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Patent number: 5110818Abstract: The invention relates to novel 9H-purine derivatives, especially to the novel substituted 9-benzyl-9H-purines of the general formula ##STR1## in which Ph is a phenyl radical substituted by halogen, R.sub.1 is hydrogen or a free amino group or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, and R.sub.2 is halogen, lower alkoxy, lower alkyl, a free amino group, or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, with the proviso that R.sub.2 is other than halogen when Ph is 2-fluorophenyl or 2,5- or 2,6-difluorophenyl and R.sub.1 is a radical of the formula --N(R.sub.11)(R.sub.12) (Ia) in which either R.sub.11 is hydrogen, methyl or ethyl and R.sub.12 is hydrogen, methyl, hydroxymethyl, ethyl, n-propyl, isopropyl, cyclopropyl, cyclopenthyl or cyclopropylmethyl, or R.sub.11 is hydrogen and R.sub.12 is methoxymethyl, and with the further proviso that R.sub.Type: GrantFiled: December 19, 1990Date of Patent: May 5, 1992Assignee: Ciba-Geigy CorporationInventor: Hans Allgeier
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Patent number: 5108994Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is a group of formula: ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; orR.sub.3 and R.sub.4 together are: ##STR3## wherein R.sub.6 is as defined above;having antiviral activity, processes for their preparation and their pharmaceutical use.Type: GrantFiled: May 23, 1990Date of Patent: April 28, 1992Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, Leslie J. A. Jennings
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Patent number: 5109003Abstract: Therapeutic agents for the treatment of peptic ulcer disease, containing as active ingredient, at least one compound of the general formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is ##STR2## (wherein m is 1-5, R.sup.4 represents a (C.sub.1 -C.sub.4)alkyl group); the other one of R.sup.1 and R.sup.3 is hydrogen, (C.sub.3 -C.sub.6)alkenyl or (C.sub.1 -C.sub.8)alkyl which can be substituted with up to 2 hydroxyl groups or a (C.sub.1 -C.sub.4)alkoxy group; and R.sup.2 is (C.sub.1 -C.sub.4)alkyl.Type: GrantFiled: August 14, 1990Date of Patent: April 28, 1992Assignee: Hoechst Japan LimitedInventors: Toshizo Tanaka, Shoryo Hayashi, Yuko Morioka, Ulrich Gebert
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Patent number: 5100881Abstract: The invention relates to the compounds of general formula I: ##STR1## in which: R.sub.1 represents a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkenyl radical containing from 2 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and which can bear a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidazolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each represents a linear or branched alkyl radical containing from 1 to 6 carbon atoms,n is equal to 1 or 2,R.sub.4 represents a hydrogen atom, a formyl radical or a methyl radical, with the proviso, however, that R.sub.4 is never the methyl radical when n is equal to 2, andeither R.sub.5 and R.sub.6 together form a double bond, or R.sub.Type: GrantFiled: August 1, 1990Date of Patent: March 31, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Alain Pierre
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Patent number: 5098908Abstract: Novel 17.beta.-hydroxybenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as tetosterone reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethy andR.sup.2 is phenyl substituted with one or more of: --OH, --OFC.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m H, --(CH.sub.2).sub.n COOH, including protected --OH, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above oxygen containing radicals is present, wherein the dotted line represents a double bond which can be present, pharmaceutically acceptable salts and esters thereof, and a pharmaceutical formulation thereof. The above compounds are active as testosterone reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.Type: GrantFiled: June 20, 1990Date of Patent: March 24, 1992Assignee: Merck & Co., Inc.Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann
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Patent number: 5093337Abstract: The invention concerns compounds of formula (I); ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, identical or different, stand for hydrogen, halogen, alkyl or alkoxy (C.sub.1-5), hydroxy, trifluoromethyl, nitro, amino, alkylamino, dialkylamino, acylamino, R.sub.1, R.sub.2 and R.sub.3 being unable to stand for hydrogen simultaneously and in which (a) stands for (b), (c), or (d), all possible isomeric forms of said products of formula (I) being racemic or optically active, as well as their additional salts with acids, their preparation and the new intermediate products obtained, their application as drugs in particular nootropes, antidepressants, neuronal protectors, anti-anoxics, anti-ischemics, and the compositions containing them.Type: GrantFiled: July 18, 1989Date of Patent: March 3, 1992Assignee: Roussel UclafInventors: Nurgun Aktogu, Francois Clemence, Claude Oberlander
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Patent number: 5091431Abstract: Compounds having an optionally-substituted purine derivative portion and a carbobicyclic or heterobicyclic portion, which compounds are useful as phosphodiesterase inhibitors, are disclosed. Also disclosed are intermediates, methods for making the inhibitors, pharmaceutical compositions and methods for treating hypertension using the compounds.Type: GrantFiled: July 18, 1990Date of Patent: February 25, 1992Assignee: Schering CorporationInventors: Deen Tulshian, Ronald J. Doll
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Patent number: 5084574Abstract: A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a .DELTA..sup.1 double bond.Type: GrantFiled: February 7, 1990Date of Patent: January 28, 1992Assignee: Merck & Co., Inc.Inventors: Apurba Bhattacharya, Alan W. Douglas, Edward J. Grabowski, Ulf H. Dolling
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Patent number: 5082845Abstract: Therapeutic agents for the treatment of peptic ulcer disease, containing as active ingredient, at least one compound of the general formula ##STR1## wherein R.sup.1 and R.sup.3 are the same or different and are each (C.sub.1 -C.sub.8)alkyl, ##STR2## R.sup.2 is (C.sub.1 -C.sub.4)alkyl; R.sup.4 and R.sup.5 are the same or different and are each hydrogen or (C.sub.1 -C.sub.2)alkyl; R.sup.6 is (C.sub.1 -C.sub.2)alkyl; and m, n and p are the same or different and are each 1, 2, 3, 4, 5 or 6; with the proviso that one of the groups R.sup.1 and R.sup.3 is ##STR3## or that R.sup.3 represents ##STR4## Some of the compounds of formula I are novel.Type: GrantFiled: February 17, 1989Date of Patent: January 21, 1992Assignee: Hoechst Japan LimitedInventors: Erhard Wolf, Ulrich Gebert, Harald Furrer, Toshizo Tanaka, Masao Sakurai, Masayoshi Goto
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Patent number: 5071985Abstract: The invention relates to a process for the preparation of morphinane derivatives of general formula: ##STR1## by demethylation of 3-methoxylated compound with a sulfonic acid selected from methanesulfonic acid and trifluoromethanesulfonic acid in the presence of a sulfide.Type: GrantFiled: September 12, 1989Date of Patent: December 10, 1991Assignee: SanofiInventors: Jean-Daniel Andre, Jean-Robert Dormoy, Alain Heymes
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Patent number: 5064961Abstract: A process for the preparation of the optically active compound [IR-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-6H-purin-6-one, represented by the formula: ##STR1## and novel intermediates are described.Type: GrantFiled: December 18, 1989Date of Patent: November 12, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Gregory S. Bisacchi, Toomas Mitt
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Patent number: 5064818Abstract: Insecticidal, acaricidal and nematocidal pyrimidinyl(thiono)(thio)-phosphoric(phosphonic) acid (amide) esters of the formula ##STR1## in which R represents hydrogen, or represents an optionally substituted radical selected from the group consisting of alkyl, alkoxy, alkylthio, dialkylamino, cycloalkyl and aryl,R.sup.1 represents hydrogen, aklyl or halogen,R.sup.2 represents alkyl,R.sup.3 represents alkyl, alkoxy, alkylthio, amino, alkylamino, dialkylamino or aryl andX represents oxygen or sulphur.Type: GrantFiled: April 16, 1990Date of Patent: November 12, 1991Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Jurgen Hartwig, Benedikt Becker
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Patent number: 5063233Abstract: The compound of the formula I ##STR1## wherein R, R.sub.3 and R.sub.5 independently represent hydrogen or hydroxy provided that at least one of R, R.sub.3 and R.sub.5 represents hydroxy; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R.sub.Type: GrantFiled: May 31, 1990Date of Patent: November 5, 1991Assignee: Ciba-Geigy CorporationInventors: Jen Chen, Alan J. Hutchison
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Patent number: 5061800Abstract: New campotothecin derivatives and a process for preparing same are disclosed, which are represented by the general formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an amino, hydroxyl, lower acylamino or lower alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, nitro, amino, cyano or di(lower alkyl)amino group, R.sup.4 represents a hydrogen or halogen atom or a lower alkyl, hydroxyl, lower alkoxy, lower alkylthio, amino, cyano or di(lower alkyl)amino group, and R.sup.5 represents a hydrogen or halogen atom or a hydroxyl or lower alkoxy group, with the proviso that all of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 substituents should not be a hydrogen atom and also that if any one of the R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is a hydroxyl or lower alkoxy group, all of the other three substituents should not be a hydrogen atom.Type: GrantFiled: January 19, 1989Date of Patent: October 29, 1991Assignee: Kabushiki Kaisha Yakult HonshaInventors: Takashi Yaegashi, Satoru Okajima, Seigo Sawada, Kenichiro Nokata, Kenichi Tezuka, Hiroshi Nagata, Teruo Yokokura, Tadashi Miyasaka, Tadashi Miyasaka
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Patent number: 5061708Abstract: The present invention relates to certain amino acid esters of the purine nucleoside acyclovir, pharmaceutically acceptable salts thereof and their use in the treatment and prophylaxis of herpes virus infections. The invention also includes pharmaceutical formulations and processes for the preparation of such compounds.Type: GrantFiled: November 21, 1989Date of Patent: October 29, 1991Assignee: Burroughs Wellcome Co.Inventor: Thomas A. Krenitsky
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Patent number: 5059690Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is a purine or pyrimidine base or an analog thereof and R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## wherein X.sub.7 is hydrogen, alkyl, substituted alkyl or aryl.Type: GrantFiled: May 1, 1990Date of Patent: October 22, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Robert Zahler, Joseph A. Tino
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Patent number: 5047407Abstract: Methods and compositions for preventing or treating human immunodeficiency virus (HIV) infections characterized by 2-substituted-5-substituted-1,3-oxathiolanes.Type: GrantFiled: February 8, 1989Date of Patent: September 10, 1991Assignee: IAF BioChem International, Inc.Inventors: Bernard Belleau, Nghe Nguyen-Ba
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Patent number: 5034396Abstract: A compound selected from the group consisting of optically active isomers of a racemic compound of the formula ##STR1## wherein the 3-hydrogen and 16-hydrogen are trans and ##STR2## is selected from the group consisting of ##STR3## with the --OH being .alpha. or .beta. and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant activity and an affinity for alpha.sub.Type: GrantFiled: November 15, 1988Date of Patent: July 23, 1991Assignee: Roussel UclafInventors: Nurgun Aktogu, Francois Clemence, Claude Oberlander
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Patent number: 5030620Abstract: A description is given of conjugates of vinca alkaloid of the indole-dihydroindole type with a protein or a protein fragment, corresponding to the general formula ##STR1## in which R.sub.1 denotes a protein or a protein fragment;R.sub.2 is COO(C.sub.1-3 alkyl) or CO-R.sub.7 where R.sub.7 isNH.sub.2 or an amino acid ester or peptide ester;R.sub.3 is H, CH.sub.3 or CHO;when R.sub.5 and R.sub.6 are taken separately, R.sub.6 is H and one of R.sub.4 and R.sub.5 is ethyl and the other is H or OH;when R.sub.5 and R.sub.6 are taken together with the carbon atoms to which they are attached, they form an oxirane ring and R.sub.4 is ethyl, andA is a residue of a bifunctional organic derivative of the maleoylamino acid or maleoyl peptide or maleoylphenoxy type.Type: GrantFiled: February 13, 1989Date of Patent: July 9, 1991Assignee: OmnichemInventors: Jean A. A. Hannart, Andre B. L. Trouet, Kandukuri S. B. Rao
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Patent number: 4997939Abstract: A process for preparing adenine by reacting an arylazomalononitrile with formic acid or its derivatives in the presence of ammonia and then subjecting the intermediate pyrimidine derivative to a reaction under catalytic reduction condition. Adenine can be prepared in high purity and high yields without isolating the intermediate pyrimidine derivative, when ammonia is removed before conducting the reaction under catalytic reduction condition. Also, the preparation of adenine in high purity and high yields can be more surely attained, when the arylazomalononitrile prepared under a specific condition is employed as a starting material or when Raney nickel is employed as a reduction catalyst in combination with active carbon. The produced adenine is effectively purified by separation of insoluble materials from an aqueous hot solution of adenine adjusted to pH 7.5 to 9.0 and formation of a mineral acid salt of adenine followed by decoloration by heating in the presence of active carbon.Type: GrantFiled: March 15, 1989Date of Patent: March 5, 1991Assignee: Kohjin Co., Ltd.Inventor: Jiro Suzuki