Sulfur In R Patents (Class 514/618)
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Patent number: 5457237Abstract: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).Type: GrantFiled: November 23, 1993Date of Patent: October 10, 1995Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
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Patent number: 5455262Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.Type: GrantFiled: October 6, 1993Date of Patent: October 3, 1995Assignee: Florida State UniversityInventors: Martin A. Schwartz, Harold Van Wart
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Patent number: 5449691Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: June 24, 1993Date of Patent: September 12, 1995Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
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Patent number: 5449692Abstract: The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: September 12, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
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Patent number: 5446066Abstract: The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: August 29, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
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Patent number: 5434188Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.Type: GrantFiled: March 7, 1994Date of Patent: July 18, 1995Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Sony S. Khatana, James B. Kramer, Paul C. Unangst
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Patent number: 5416119Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: October 25, 1993Date of Patent: May 16, 1995Assignee: G. D. Searle & Co.Inventors: Barbara B. Chen, Gunnar J. Hanson, John S. Baran
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Patent number: 5414017Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.Type: GrantFiled: March 26, 1993Date of Patent: May 9, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, George C. Rovnyak, Melanie J. Loots
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5414018Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein q is two or three; wherein r is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl containing moiety; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.12 and R.sup.13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 24, 1993Date of Patent: May 9, 1995Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson
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Patent number: 5405873Abstract: There are provided substituted acetamide derivatives represented by general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, n and Z are defined in the specification. The substituted acetamide derivatives strongly inhibit acylcoenzyme A cholesterol acyltransferase (ACTA) and are expected to be effective for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.Type: GrantFiled: September 7, 1993Date of Patent: April 11, 1995Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Hiromi Hattori, Yasufumi Nagata, Akiko Shimizu, Yoshio Sawasaki
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Patent number: 5401776Abstract: The present invention relates to the use of modafinil for the manufacture of a medicinal product for the treatment of urinary and fecal incontinence and urethrovesical and anal sphincteral disorders.Type: GrantFiled: October 18, 1993Date of Patent: March 28, 1995Assignee: Laboratoire L. LafonInventor: Philippe Laurent
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Patent number: 5395854Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.Type: GrantFiled: September 22, 1993Date of Patent: March 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5393764Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.Type: GrantFiled: August 25, 1993Date of Patent: February 28, 1995Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 5391576Abstract: The invention relates to a method for protecting the cerebral tissue of a human against the repercussions of ischaemia which comprises administering to a patient in need thereof a therapeutically effective amount of modafinil.Type: GrantFiled: December 14, 1992Date of Patent: February 21, 1995Assignee: Laboratoire L. LafonInventor: Louis Lafon, deceased
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Patent number: 5391577Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.Type: GrantFiled: May 25, 1993Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
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Patent number: 5389684Abstract: Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.Type: GrantFiled: August 17, 1993Date of Patent: February 14, 1995Assignee: Lilly Industries LimitedInventors: John Fairhurst, David E. Tupper
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Patent number: 5387607Abstract: O-Benzyloxime ethers of the formula I ##STR1## where X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: December 13, 1993Date of Patent: February 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5382595Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: October 13, 1992Date of Patent: January 17, 1995Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5373024Abstract: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.Type: GrantFiled: February 10, 1993Date of Patent: December 13, 1994Assignee: Hoechst AktiengesellschaftInventors: Florian Lang, Hans-Jochen Lang, Dieter Mania, Andreas Weichert, Wolfgang Scholz, Udo Albus, Heinrich Englert
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Patent number: 5356925Abstract: 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; substituted lower alkyl; aryl; or heteroaryl;R.sup.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 ring;R.sub.5 and R.sub.6 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl or aryl lower alkyl, or R.sub.5 and R.sub.Type: GrantFiled: February 11, 1993Date of Patent: October 18, 1994Assignee: Schering CorporationInventors: Bernard R. Neustadt, Alan Bronnenkant
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Patent number: 5354742Abstract: The invention is directed to a pesticide composition comprising free flowing, essentially spherical, water-dispersible granules wherein said water-dispersible granules are from about 150 to about 850 microns in diameter; wherein said granules contain up to about 8.0% by weight moisture; wherein each individual water-dispersible granule is an aggregation of individual spherical microcapsules which contain at least one water-insoluble pesticide within a polymeric shell wall; and wherein said water-dispersible granule disintegrates upon contact with water to release said individual microcapsules.The invention also relates to dry flowable pesticidal formulations of the above water-dispersible granules, together with formulation adjuvants.The invention is further directed to a process for preparing a water-dispersible granule by spary drying an aqueous suspension comprising discrete microcapsules containing at least one water-insoluble pesticide within a polymeric shell wall suspended in an aqueous liquid.Type: GrantFiled: October 14, 1988Date of Patent: October 11, 1994Assignee: Monsanto CompanyInventors: John M. Deming, John M. Surgant, Sr.
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Patent number: 5352705Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: June 26, 1992Date of Patent: October 4, 1994Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5344841Type: GrantFiled: June 8, 1992Date of Patent: September 6, 1994Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
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Patent number: 5342835Abstract: Compounds of formula ##STR1## in which: CYCLE surrounded by a semicircle represents, with the two carbon atoms to which the semicircle is linked, a carbon-containing, optionally heterocyclic, ring containing at least one ethylenic or aromatic bond between the two carbon atoms which carry the --C(Z).dbd.Y group and the phenyl group, Y is oxygen or sulphur, Z is NR.sub.1 R.sub.2, R.sub.1 and R.sub.2, each represents optionally substituted alkyl, alkoxy or cycloalkyl; alkenyl or alkynyl; or --NR.sub.1 R.sub.2 represents saturated or unsaturated heterocyclyl;R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: January 3, 1992Date of Patent: August 30, 1994Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
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Patent number: 5340827Type: GrantFiled: June 14, 1993Date of Patent: August 23, 1994Assignee: Celltech, LimitedInventors: Nigel R. A. Beeley, Thomas A. Millican
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Patent number: 5321046Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.Type: GrantFiled: October 27, 1992Date of Patent: June 14, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, John J. Wright, Jeff A. Field
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Patent number: 5302595Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.Type: GrantFiled: January 6, 1993Date of Patent: April 12, 1994Assignee: Pfizer Inc.Inventors: Peter E. Cross, Alexander R. MacKenzie
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Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5280044Abstract: Fungicidal compounds of the formula (I): ##STR1## in which A and B are independently H, fluoro, chloro, bromo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halo(C.sub.1-4)alkyl provided that both are not H; D and E are independently H or fluoro; R.sup.1 is H, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is CC.sub.1-4 alkyl, C.sub.1-4 alkoxy or optionally substituted phenyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached join to form a morpholine, piperidine, pyrrolidine or azetidine ring which is optionally substituted with C.sub.1-4 alkyl; R.sup.3 is H; R.sup.4 is trichloromethyl, C.sub.2-8 alkyl (optionally substituted with halogen, C.sub.1-8 alkoxy or R'S(O) in which R' is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl and n is 0, 1 or 2), cyclopropyl (optionally substituted with halogen or C.sub.1-4 alkyl), C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.1-8 alkoxy, mono- or di(C.sub.1-4)alkyl- amino or the group, R"ON.dbd.C(CN) in which R" is C.sub.1-4 alkyl, or R.sup.Type: GrantFiled: December 31, 1990Date of Patent: January 18, 1994Assignee: Imperial Chemical Industries PLCInventors: Patrick J. Crowley, Alasdair T. Glen, Rosamund A. Spence
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Patent number: 5278191Abstract: A class of diphenylmethylaminoacetamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is independently selected from hydrido and halo; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: October 11, 1991Date of Patent: January 11, 1994Assignee: G. D. Searle & Co.Inventors: Alexis A. Cordi, Claude L. Gillet
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Patent number: 5272178Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, phenyl, or hydrogen; R.sup.3 represents hydrogen or alkyl; X represents O, S or (CH.sub.2).sub.m wherein m is 1 or 2; A represents O or S(O).sub.n wherein n is 0, 1, or 2; p is an integer from 0 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl; or NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl, and R.sup.6 is hydrogen, alkyl, heterocyclealkyl, substituted heterocyclealkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, phenylalkyl, or substituted phenylalkyl, or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl; and the pharmaceutically acceptable salts thereof. The compounds are inhibitors or stimulators of superoxide generation.Type: GrantFiled: April 8, 1993Date of Patent: December 21, 1993Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 5264621Abstract: Development of medicament having anti-virus activity, particularly anti-HIV (anti-human immunodeficiency virus) activity. An anti-virus agent comprising bis-naphthalenedisulfonic acids having aliphatic spacer represented by the formula (1) and their physically usable salts.Type: GrantFiled: February 4, 1992Date of Patent: November 23, 1993Assignee: Sanyo-Kokusaku Pulp Co., Ltd.Inventors: Prem Mohan, Masanori Baba
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Patent number: 5262436Abstract: 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: August 6, 1991Date of Patent: November 16, 1993Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
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Patent number: 5260338Abstract: This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations.Type: GrantFiled: January 28, 1992Date of Patent: November 9, 1993Assignee: Eli Lilly and CompanyInventors: Richard W. Harper, Gerald A. Poore, Brent J. Rieder
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Patent number: 5252601Abstract: The present invention relates to novel 2-mercaptomethylene-tetrahydronaphthalene derivatives which are useful as enkephalinase inhibitors.Type: GrantFiled: April 3, 1992Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
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Patent number: 5250570Abstract: The invention concerns novel phenoxy- and phenylthio-acetyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: December 31, 1992Date of Patent: October 5, 1993Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
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Patent number: 5244899Abstract: The compounds of this invention are azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.Type: GrantFiled: July 29, 1992Date of Patent: September 14, 1993Assignee: G. D. Searle and Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5236957Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.Type: GrantFiled: January 25, 1991Date of Patent: August 17, 1993Assignee: Farmitalia Carlo Erba SrlInventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
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Patent number: 5236953Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.ident.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.Type: GrantFiled: October 30, 1991Date of Patent: August 17, 1993Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, Howard Tucker
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Patent number: 5232920Abstract: Novel N-(mercaptoalkyl)amides of the formula ##STR1## wherein R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 is (COR.sub.3)-aryl, heteroaryl, substituted (COR.sub.3)-aryl or substituted heteroaryl, wherein the substituents are 1-3 substituents selected from the group consisting of carboxy, alkoxycarbonyl, lower alkyl, hydroxy, halo, lower alkoxy, cyclolower alkyl, cyano, trifluoromethyl, phenyl, phenoxy and phenylthio;R.sub.3 is --OR.sub.4 or --NR.sub.4 R.sub.5 ;R.sub.4 and R.sub.5 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.4 and R.sub.5 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;Q is hydrogen or R.sub.6 CO--;R.sub.Type: GrantFiled: December 21, 1990Date of Patent: August 3, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5225444Abstract: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.Type: GrantFiled: August 27, 1991Date of Patent: July 6, 1993Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5223539Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).Type: GrantFiled: November 21, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Roger A. Nosal, Michael A. Stealey, Richard M. Weiser
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Patent number: 5204370Abstract: The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.Type: GrantFiled: November 5, 1990Date of Patent: April 20, 1993Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
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Patent number: 5185342Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: May 16, 1990Date of Patent: February 9, 1993Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5180745Abstract: The present invention relates to a method for providing a patient with neuroprotective effect, which consists in administering modafinil to said patient.Type: GrantFiled: June 13, 1991Date of Patent: January 19, 1993Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: RE34440Abstract: 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 radial; 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 16, 1992Date of Patent: November 9, 1993Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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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