Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/551)
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4882359Abstract: An azacycloalkane derivative useful for promoting the absorption of a medicine, an absorption promoting agent comprising at least one of the azacycloalkane derivatives as the effective ingredient for promoting the absorption and an external preparation containing the absorption promoting agent, the derivative being represented by the following formula ##STR1## wherein A is --CH.sub.2 -- or --S-- for example, B is sulfur or oxygen, R is --SR" in which R" is an alkyl group or alkylthioalkyl group for example, or --OR" in which R" is as defined above, an alkyl group or substituted amino group, R' is a hydrogen atom, alkyl group or alkyloxy group for example, m is an integer of 0-5 and n is an integer of 1-15.Type: GrantFiled: November 18, 1987Date of Patent: November 21, 1989Assignee: Hisamitsu Pharmaceutical Co., Ltd.Inventors: Akira Nakagawa, Michinori Sakai
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Patent number: 4874865Abstract: Preparation of substituted lactams Ia to Ic ##STR1## where n is 0 or 1, X is --O--CO--R.sup.1, --O--SO.sub.2 --R.sup.1, --CO--R.sup.2, --CO--O--R.sup.3 or --CO--NR.sup.4 R.sup.5, R.sup.1 is a C.sub.1 -C.sub.8 -radical of a carboxylic or sulfonic acid, R.sup.2 is C.sub.1 -C.sub.8 -alkyl, R.sup.3 is H or alkyl, aryl or aralkyl of not more than 8 carbon atoms, R.sup.4 and R.sup.5 are each H or C.sub.1 -C.sub.4 -alkyl or together form a 5-membered or 6-membered ring, by reacting a lactam II ##STR2## with a vinyl compound IIICH.sub.2 .dbd.CH-Xand a compound IV which forms free radicals to give Ia, and preparation of Ib by hydrolysis of a compound Ia in which X is (--O--CO--R.sup.1) or (--O--SO.sub.2 --R.sup.1), and preparation of Ic by thermolysis of Ib or of a compound Ia in which X is (--O--CO--R.sup.1) or (--O--SO.sub.2 --R.sup.1), and the novel substituted lactams Ia and Ib where X is (--O--CO--R.sup.1) and (--O--SO.sub.2 --R.sup.1).Type: GrantFiled: June 2, 1988Date of Patent: October 17, 1989Assignee: BASF AktiengesellschaftInventors: Ludwig Wambach, Martin Fischer
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Patent number: 4864055Abstract: A compound represented by the following formula: ##STR1## wherein R is a C.sub.3 -C.sub.24 olefinically unsaturated organic radical having functionality which renders the nitrogen atom electron deficient, the olefinic unsaturation functionality being polymerizable,R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl radical, orR and R.sup.1 together with the nitrogen atom can form an olefinically unsaturated 5 to 7-member ring which has functionality that renders the nitrogen atom electron deficient and the olefinic unsaturation functionality is polymerizable,R.sup.2 and R.sup.3 are hydrogen, a C.sub.1 -C.sub.4 alkyl or acyl radical, orR.sup.2 and R.sup.3 together are a C.sub.1 -C.sub.4 alkylene group,R.sup.4 is hydrogen or a C.sub.1 -C.sub.4 alkyl, acyl, ester, amide or acid group, andn is an integer from 1 to 10, provided n is not 1 when R is (meth)acryloyl, R.sup.2 and R.sup.3 are methyl and R.sup.1 and R.sup.4 are hydrogen.Type: GrantFiled: September 3, 1987Date of Patent: September 5, 1989Assignee: Air Products and Chemicals, Inc.Inventors: Robert K. Pinschmidt, Jr., Dale D. Dixon, William F. Burgoyne, Jr.
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Patent number: 4841078Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.Type: GrantFiled: August 9, 1984Date of Patent: June 20, 1989Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence Sherman
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Patent number: 4837337Abstract: Disclosed herein is a process for producing a pyrrolidone derivative represent by the general formula (I): ##STR1## wherein R is an organic residue obtained by removing hydroxy radical from a C.sub.1-10 primary alcohol, C.sub.1-10 secondary alcohol or derivative thereof, comprising (1) reacting 2-pyrrolidone with acetaldehyde in the presence of a catalyst, thereby obtaining N-(.alpha.-hydroxyethyl)pyrrolidone, and (2) reacting the thus obtained N-(.alpha.-hydroxyethyl)pyrrolidone with a primary alcohol, a secondary alcohol or a derivative thereof in the presence of an acidic catalyst to obtain the pyrrolidone derivative.Type: GrantFiled: February 3, 1988Date of Patent: June 6, 1989Assignee: Mitsubishi Chemical Industries LimitedInventors: Yoshikazu Murao, Masao Miyake
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Patent number: 4835277Abstract: In one embodiment this invention provides a nonlinear optical medium whcih is a transparent film of a thermoplastic polymer composed of recurring monomeric units corresponding to the formula: ##STR1##Type: GrantFiled: October 5, 1987Date of Patent: May 30, 1989Assignee: Hoechst Celanese CorporationInventor: Eui W. Choe
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Patent number: 4833139Abstract: There are disclosed compounds of the formula ##STR1## where R.sub.1 is loweralkoxycarbonyl, --CH.sub.2 OH or --CONR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is --CH.sub.2 CH.dbd.CH.sub.2, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group -NR.sub.5 R.sub.6 as a whole being ##STR3## R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; which are useful for enhancing cholinergic activity in mammals and hence for the treatment of various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: July 5, 1988Date of Patent: May 23, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Lawrence L. Martin
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Patent number: 4833164Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 19, 1986Date of Patent: May 23, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4831159Abstract: A process is disclosed for preparing isomeric aldehydes by contacting N-vinyl-2-pyrrolidinone and synthesis gas in the presence of a rhodium-containing compound with or without additional phosphine ligand and a solvent. The alpha and beta isomeric aldehydes such as 2-N-(2-pyrrolionyl)propanaldehyde and 3-N-(2-pyrrolidonyl)propanaldehyde can be converted to 1,2- or 1,3-diaminopropanes via reductive amination or to alcohol amines via reduction.Type: GrantFiled: June 20, 1986Date of Patent: May 16, 1989Assignee: Texaco Inc.Inventor: Jiang-Jen Lin
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Patent number: 4803285Abstract: A process for the preparation of a C(3)-C(4)-transconfigurated.gamma.-butyrolactam of the formula (I) ##STR1## in which R.sup.1 represents hydrogen or alkyl, aryl or aralkyl with in each case up to 10 carbon atoms andR.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, alkoxy, aryloxy or aralkoxy with in each case up to 10 carbon atoms, acyl with up to 18 carbon atoms, trifluoromethyl, trifluoromethoxy, nitro, hydroxyl, halogen, amino, carboxyl, sulpho, dialkylamino with up to 4 carbon atoms in the alkyl groups or acylamino with up to 18 carbon atoms, in the form of their isomers, isomer mixtures, racemates or optical antipodes, comprising oxidizing a compound of the formula (II) ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the above-mentioned meanings, in an inert organic solvent in the presence of a base. Such .gamma.-butyrolactams have an antiamnesic action.Type: GrantFiled: August 27, 1987Date of Patent: February 7, 1989Assignees: Bayer Aktiengesellschaft & Chinese, Chinese Academy of Medical SciencesInventor: Wolfgang Hartwig
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Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
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Patent number: 4792603Abstract: A method for producing a polyether-polyamide block copolymer is disclosed, comprising copolymerizing, in the presence of an anionic polymerization catalyst, a lactam and a polyether prepolymer presented by the formula: ##STR1## wherein R.sup.1 is an aliphatic hydrocarbon residual group having 2 to 6 carbon atoms, R.sup.2 is an aliphatic hydrocarbon residual group having 3 to 12 carbon atoms, and n is an integer of 4 to 450. The polyester prepolymer is prepared by reacting a polyoxyalkylene having two terminal hydroxy groups with an N-chlorocarbonyl lactam. The polyether-polyamide block according to the invention has high impact strength and is substantially colorless.Type: GrantFiled: October 2, 1986Date of Patent: December 20, 1988Assignee: Sumitomo Chemical Co., Ltd.Inventors: Takeo Saegusa, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
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Patent number: 4786649Abstract: Novel 1-thienyl-4-oxoquinoline-3-carboxylic acid compounds of the formula ##STR1## wherein R.sup.1 is an amino (lower) alkyl, R.sup.2 is thienyl, and X is a halogen atom, and a pharmaceutically acceptable salt thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition comprising as an active ingredient said 1-thienyl-4-oxoquinoline-3-carboxylic acid compounds or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable diluent or carrier.Type: GrantFiled: November 13, 1986Date of Patent: November 22, 1988Assignee: Otsuka Pharmaceutical Company LimitedInventors: Hiraki Ueda, Hisashi Miyamoto
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Patent number: 4766110Abstract: Novel inhibitors of angiotensin converting enzyme are disclosed which have the general formula ##STR1## wherein R.sub.1 and/or R.sub.3 form complex amides and imides thereof, R.sub.4 and R.sub.5 form with --N--C-- a 4-6 membered ring structure as described and the other R substituents are selected from a variety of disclosed groups.Type: GrantFiled: October 31, 1986Date of Patent: August 23, 1988Inventors: James W. Ryan, Alfred Chung
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Patent number: 4760152Abstract: (1) Pyrrolidonyl acrylate block polymers having the formula ##STR1## wherein n has a value of 1 to 3; X and X' are dissimilar and each is hydrogen or methyl; y and z each have a value of from 1 to 40, except that at least one of y and z is greater than 1 and R is hydrogen or methyl;(2) preparation of said polymers and(3) uses of said polymers.Type: GrantFiled: March 2, 1987Date of Patent: July 26, 1988Assignee: GAF CorporationInventors: David J. Tracy, Mohamed M. Hashem, Fulvio J. Vara
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Patent number: 4751315Abstract: A new synthetic route to clausenamide having the formula ##STR1## has been found. It has been found that a compound of the formula ##STR2## can be oxidized to provide the stereochemically correctly configured product, clausenamide. A number of new compounds useful in the total synthesis of clausenamide have also been found. These compounds have the general formula ##STR3## wherein R is ##STR4## and CH.sub.2 OH.Type: GrantFiled: September 1, 1987Date of Patent: June 14, 1988Assignees: Bayer Aktiengesellschaft, Chinese Academy of Medical SciencesInventor: Wolfgang Hartwig
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Patent number: 4731456Abstract: A new synthetic route to clausenamide having the formula ##STR1## has been found. It has been found that a compound of the formula ##STR2## can be oxidized to provide the stereochemically correctly configured product, clasuenamide. A number of new compounds useful in the total synthesis of clausenamide have also been found. These compounds have the general formula ##STR3## wherein R is ##STR4## and CH.sub.2 OH.Type: GrantFiled: October 3, 1986Date of Patent: March 15, 1988Assignees: Bayer Aktiengesellschaft, Chinese Academy of Medical SciencesInventor: Wolfgang Hartwig
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Patent number: 4731455Abstract: A process for the preparation of a C(3)-C(4)-transconfigurated .gamma.-butyrolactam of the formula (I) ##STR1## in which R.sup.1 represents hydrogen or alkyl, aryl or aralkyl with in each case up to 10 carbon atoms andR.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, alkoxy, aryloxy or aralkoxy with in each case up to 10 carbon atoms, acyl with up to 18 carbon atoms, trifluoromethyl, trifluoromethoxy, nitro, hydroxyl, halogen, amino, carboxyl, sulpho, dialkylamino with up to 4 carbon atoms in the alkyl groups or acylamino with up to 18 carbon atoms,in the form of their isomers, isomer mixtures, racemates or optical antipodes, comprising oxidizing a compound of the formula (II) ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the above-mentioned meanings, in an inert organic solvent in the presence of a base. Such .gamma.-butyrolactams have an antiamnesic action.Type: GrantFiled: October 1, 1986Date of Patent: March 15, 1988Assignees: Bayer Aktiengesellschaft, Chinese Academy of Medical SciencesInventor: Wolfgang Hartwig
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Patent number: 4730050Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.Type: GrantFiled: April 3, 1987Date of Patent: March 8, 1988Assignee: Beecham Group p.l.c.Inventor: Richard A. G. Smith
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Patent number: 4692532Abstract: Substituted (4-hydroxyphenylthioalkyl) derivatives of the formula ##STR1## are prepared by the reaction of the appropriate ring and hydroxybenzene thiol compounds and are useful stabilizers of organic materials.Type: GrantFiled: November 23, 1984Date of Patent: September 8, 1987Assignee: Ciba-Geigy CorporationInventors: John D. Spivack, Ramanathan Ravichandran, Stephen D. Pastor
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Patent number: 4691026Abstract: A compound represented by the following formula: ##STR1## wherein R is a C.sub.3 -C.sub.24 olefinically unsaturated organic radical having functionality which renders the nitrogen atom electron deficient, the olefinic unsaturation functionality being polymerizable,R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl radical, orR and R.sup.1 together with the nitrogen atom can form an olefinically unsaturated 5 to 7-member ring which has functionality that renders the nitrogen atom electron deficient and the olefinic unsaturation functionality is polymerizable,R.sup.2 and R.sup.3 are hydrogen, a C.sub.1 -C.sub.4 alkyl or acyl radical, orR.sup.2 and R.sup.3 together are a C.sub.2 -C.sub.4 alkylene group,R.sup.4 is hydrogen or a C.sub.1 -C.sub.4 alkyl, acyl, ester, amide or acid group, andn is an integer from 1 to 10, provided n is not 1 when R is (meth)acryloyl, R.sup.2 and R.sup.3 are methyl and R.sup.1 and R.sup.4 are hydrogen.Under acidic conditions the above compounds having R.sup.Type: GrantFiled: July 30, 1985Date of Patent: September 1, 1987Assignee: Air Products and Chemicals, Inc.Inventors: Robert K. Pinschmidt, Jr., Dale D. Dixon, William F. Burgoyne, Jr.
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Patent number: 4680307Abstract: A compound of the formula: ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group, Y.sup.1 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or C.sub.1 -C.sub.4 alkyl group), ##STR4## (R.sup.6 is as defined above), ##STR5## R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a shingle linkage to from a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.Type: GrantFiled: January 26, 1984Date of Patent: July 14, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Masami Muraoka, Toshio Nakamura, Akihiko Sugie, Keiichi Ono, Michihiro Yamamoto
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Patent number: 4680338Abstract: A selective bifunctional sequential linker has the formulaY.dbd.C.dbd.N--Q--A--C(O)--Zwherein Q is a homoaromatic or heteroaromatic ring system; A is a single bond or an unsubstituted or substituted divalent C.sub.1-30 bridging group; Y is O or S; and Z is Cl, Br, I, N.sub.3, N-succinimidyloxy, imidazolyl, 1-benzotriazolyloxy, OAr where Ar is an electron-deficient activating aryl group, or OC(O)R where R is --A--Q--N.dbd.C.dbd.Y or C.sub.4-20 tertiary-alkyl. A method for activating an amine function towards reaction with a second amine involves reacting the amine with the foregoing linker. The resultant isocyanate or isothiocyanate derivative can then be reacted with a second amine to form a urea or thiourea conjugate.The linker is useful for producing conjugates of ligands with amine-containing polymers and/or proteins, especially for forming antibody conjugates with chelators, drugs, enzymes, detectable labels and the like.Type: GrantFiled: October 17, 1985Date of Patent: July 14, 1987Assignee: Immunomedics, Inc.Inventor: Boby M. Sundoro
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Patent number: 4677114Abstract: Novel derivatives of substituted pyrrolizine diones and the pharmaceutically acceptable salts and esters thereof, have therapeutic utility for reducing amnesia induced by electroconvulsive shock and for treating senility.Type: GrantFiled: November 22, 1985Date of Patent: June 30, 1987Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Anthony J. Thomas
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Patent number: 4668703Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
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Patent number: 4663464Abstract: Dihydro-1H-pyrrolizine-3,5-(2H,6H)-dione is produced in higher overall yield in a process which comprises catalytically hydrogenating a lower alkyl ester of 4-(hydroxyimino)heptanedioic acid in the presence of a tri-(lower alkyl)amine, followed by cyclization of the product thus produced in the presence of a cyclizing agent such as acetic anhydride.Type: GrantFiled: March 21, 1986Date of Patent: May 5, 1987Assignee: Warner-Lambert CompanyInventor: Marvin S. Hoekstra
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Patent number: 4650608Abstract: A novel star block copolymer represented by the general formula as shown below and a process for the production thereof are described. The copolymer has superior physical properties, particularly impact strength and, furthermore, is reduced in coloration. Thus the copolymer can find numerous uses; for example, it can be used in preparation of fibers, foams, automotive parts, and electrical components. The copolymer is produced by copolymerizing a star-shaped polyether prepolymer and a lactam, said prepolymer being prepared by reacting a star-shaped polyoxyalkylene having at least 3 terminal hydroxy groups and an N-chlorocarbonyl lactam, in the presence of an anionic polymerization catalyst. ##STR1## In this formula, all the symbols are as defined hereinbefore.Type: GrantFiled: August 6, 1985Date of Patent: March 17, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Saegusa Takeo, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
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Patent number: 4620949Abstract: Amino acid derivatives are synthesized by reacting paraformaldehyde, cyclic amides and synthesis gas with a bimetallic catalyst comprising a rhodium-containing compound and a cobalt-containing compound, optionally in the presence of a solvent at a pressure of at least 500 psi and a temperature of at least 50.degree. C. The novel amino acid products may be hydrolyzed to amino dicarboxylic acids or used as monomers to polyamides.Type: GrantFiled: April 5, 1985Date of Patent: November 4, 1986Assignee: Texaco Inc.Inventor: Jiang-Jen Lin
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Patent number: 4612132Abstract: Disclosed are additives which are useful as dispersants in lubricating oils, gasolines, marine crankcase oils and hydraulic oils. In particular, disclosed are polyamino alkenyl or alkyl succinimides which contain carbamate functionalities.Type: GrantFiled: April 12, 1985Date of Patent: September 16, 1986Assignee: Chevron Research CompanyInventors: Robert H. Wollenberg, Frank Plavac, Timothy R. Erdman
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Patent number: 4590204Abstract: 5-oxo-2,2-pyrrolidinedipropanoic acid, base addition salts and esters are useful as agents for the reversal of amnesia. Intermediates for preparing said compounds, pharmaceutical compositions containing said compounds and methods for using said pharmaceutical compositions for treating senility and reversal of amnesia are also taught.Type: GrantFiled: April 5, 1984Date of Patent: May 20, 1986Assignee: Warner-Lambert CompanyInventor: Donald E. Butler
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Patent number: 4582838Abstract: Certain derivatives of dihydro-1H-pyrrolo-[1,2-c]imidazol-3,5[2H,6H]-dione are cognition-activating compounds, possessing pharmacological activity for treating senility or for reversing the effects of electroconvulsive shock-induced amnesia. Pharmaceutical compositions including these compounds, a method of preparing the compounds, and of treating senility or of reversing the effects of induced amnesia are also disclosed.Type: GrantFiled: August 24, 1984Date of Patent: April 15, 1986Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, James D. Leonard
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Patent number: 4581364Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.2 is pyridyl, phenyl or mono-, di- or tri-substituted phenyl, where the substituents are alkyl of 1 to 2 carbon atoms, alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, nitro, benzyloxy or hydroxyl.The compounds are useful as nootropics.Type: GrantFiled: July 9, 1984Date of Patent: April 8, 1986Assignee: Boehringer Ingelheim KGInventors: Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
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Patent number: 4560767Abstract: Amino-cycloalkenyl-amide compounds, e.g., (1.alpha.,6.beta.)-(.+-.)-3,4-dichloro-N-methyl-N-(6-(1-pyrrolidinyl)-3-cy clohexen-1-yl)benzeneacetamide, and tritiated derivatives thereof, are useful as analgesics and as radio labeled compounds for pharmacological and metabolism studies in animals.Type: GrantFiled: June 17, 1983Date of Patent: December 24, 1985Assignee: The Upjohn CompanyInventors: John M. McCall, Robert A. Lahti
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Patent number: 4559358Abstract: 5-Oxo-2-pyrrolidinepropanoic acids, base addition salts, esters and amides are useful as agents for the reversal of amnesia. Pharmaceutical compositions containing said compounds and methods for using said compositions for treating senility and reversal of amnesia are also taught.Type: GrantFiled: March 24, 1983Date of Patent: December 17, 1985Assignee: Warner-Lambert CompanyInventor: Donald E. Butler
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Patent number: 4552889Abstract: This invention provides for certain lactam derivatives, their pharmaceutical formulations, and a method of treating hypertension.Type: GrantFiled: June 9, 1983Date of Patent: November 12, 1985Assignee: Eli Lilly and CompanyInventor: William L. Scott
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Patent number: 4548936Abstract: The present invention relates to .DELTA..sup.1 -pyrroline thiolactim ethers of the general formula I ##STR1## which have a more specific action and/or a longer-lasting action than PGI.sub.2, and to a process for their preparation.The compounds are distinguished by a platelet aggregation-inhibiting action and a blood vessel-relaxing and hypotensive action, and can therefore be used as medicaments.Type: GrantFiled: May 5, 1982Date of Patent: October 22, 1985Assignee: Hoechst AktiengesellschaftInventors: Gerhard Beck, Wilhelm Bartmann, Jochen Knolle, Richard H. Rupp
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Patent number: 4539408Abstract: Quaternary sulfoalkyl or sulfoalkenyl salts of tertiary amine bases are prepared by reacting the tertiary amine bases at elevated temperatures with a hydroxy alkane sulfonic acid or a hydroxyalkene sulphonic acid.Type: GrantFiled: April 28, 1978Date of Patent: September 3, 1985Assignee: Agfa-Gevaert AktiengesellschaftInventors: Helmut Kampfer, Marie Hase, Max Glass
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Patent number: 4528299Abstract: 1-(2,3-Dimethyl-4-methoxyphenyl)-2-methyl-3-(1-pyrrolidinyl)-1-propanone and its pharmaceutically acceptable acid addition salts, which are useful as centrally acting muscle relaxants in the treatment of spasticity in mammals including humans, process for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: September 7, 1983Date of Patent: July 9, 1985Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Hitoshi Uno, Tadahiko Karasawa, Tatsuya Kon, Tsugutaka Ito
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Patent number: 4500343Abstract: 1-Heterocyclic-2-pyrrolidinone analogs, and intermediates thereof, as aquatic and terrestrial herbicides and aquatic algicides. The compounds and intermediates can also be used together with one or more herbicides to provide useful terrestrial herbicidal combinations.Type: GrantFiled: September 30, 1982Date of Patent: February 19, 1985Assignee: Eli Lilly and CompanyInventor: Kenneth W. Burow, Jr.
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Patent number: 4476311Abstract: Analgesic and anti-inflammatory compounds are provided. These compounds possess the following general formula: ##STR1## wherein R=--COOR.sub.5, --CH.sub.2 CO.sub.2 H, ##STR2## wherein A and B=hydrogen, lower alkyl, hydroxy alkyl, lower alkyl amine, substituted lower alkyl amine, aminoalkyl, substituted aminoalkyl;R.sub.5 =lower alkyl;R.sub.1 =aryl, substituted aryl, aralkyl, alkyl, hydrogen, substituted aralkyl and heterocycle;R.sub.2 =aryl, substituted aryl, aralkyl, alkyl, substituted aralkyl, heterocycle, substituted heterocycle, biphenyl, substituted biphenyl, naphthyl, and substituted naphthyl;R.sub.3 =aryl, substituted aryl, hydrogen, aralkyl, substituted aralkyl, alkyl, heterocycle and substituted heterocycle;R.sub.2 and R.sub.3 together form a ring;R.sub.4 =hydrogen, phenyl, substituted phenyl, heterocycle; alkyl, substituted alkyl; or, R.sub.1 and R.sub.4 may form a ring;X=>C.dbd.O, --CH.sub.2 --;Y=--S--CHR.sub.4 --, --O--OHR.sub.4 --, --CHR.sub.4 --, --CR.sub.6 R.sub.7 --CHR.sub.Type: GrantFiled: February 19, 1982Date of Patent: October 9, 1984Assignee: The Purdue Frederick CompanyInventors: Bola V. Shetty, Arthur McFadden, Peter Hofer
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Patent number: 4466981Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy or lower alkylthio;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.Type: GrantFiled: October 27, 1982Date of Patent: August 21, 1984Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, Young, John M.
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Patent number: 4463177Abstract: m-Hydroxyphenyl substituted compounds of formula ##STR1## where R is an organic radical and R.sup.1 is hydroen or an organic radical are prepared by dehydrohalogenating a compound of formula ##STR2## (where X is chlorine or bromine, and R and R.sup.1 have the above meanings). Preferred novel starting materials of formula (II) are of the formula ##STR3## (where R.sup.1 and X are as above, n is 2,3 or 4, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl(lower)alkyl or aryl(lower)alkyl).Type: GrantFiled: November 26, 1982Date of Patent: July 31, 1984Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shepherd
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Patent number: 4463014Abstract: Esters in their stereoisomeric form or mixtures thereof of the formula ##STR1## wherein R.sub.1 and R are different and individually selected from the group consisting of hydrogen, fluorine and bromine, R.sub.2 is selected from the group consisting of --CN and --C.tbd.CH and R.sub.3 is a hydrocarbyl group having pesticidal properties and their preparations.Type: GrantFiled: April 5, 1982Date of Patent: July 31, 1984Assignee: Roussel UclafInventors: Jacques Martel, Jean Tessier, Jean-Pierre Demoute
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Patent number: 4460480Abstract: The present invention relates to novel oligomers of the formula R.sub.f --E--S--M.sub.1 ].sub.x [M.sub.2 ].sub.y H, and mixutes thereof, wherein R.sub.f is a perfluoroalkyl group, E is a linkage group, --M.sub.1 -- represents a hydrophilic monomer unit, --M.sub.2 -- represents a hydrophobic monomer unit, x and y represent the number of monomer units present in the novel oligomers. The sum of x and y is between 4 and 500 and x/(x+y) is between 1 and 0.5. The novel oligomers are useful as additives in protein foam type fire fighting compositions improving foam expansion, foam drainage and extinguishing times and reducing flammability of hydrocarbon contaminated protein foams. The novel oligomers are further useful as surface tension depressants providing improved wetting, spreading and leveling properties in aqueous systems.Type: GrantFiled: March 13, 1980Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventors: Eduard K. Kleiner, Thomas W. Cooke, Robert A. Falk
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Patent number: 4458090Abstract: Novel .gamma.-lactone derivatives are provided. These lactone derivatives, when reacted with hydrogen halide in alcohol, yield .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters. This ring-opening process is useful for the purpose of increasing the yield of pyrethrin analogs which are of value as insecticides and agricultural chemicals. Thus, the .gamma.-lactone derivatives by-produced in the production process for dihalogenovinyl chrysanthemumates are caused to undergo ring-opening reaction to yield the corresponding .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters which are important intermediates for said pyrethrin analogs.Type: GrantFiled: October 15, 1981Date of Patent: July 3, 1984Assignee: Kuraray Co., Ltd.Inventors: Mori Fumio, Omura Yoshiaki, Nishida Takashi, Itoi Kazuo
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Patent number: 4456613Abstract: Biologically active 6-keto- and 6-hydroxy-8-azaprostanoids having the formula: ##STR1## wherein A is O or ##STR2## R is CO.sub.2 R.sup.4 or CH.sub.2 OH; R.sup.1 is H, CH.sub.3, or C.sub.2 H.sub.5 ;R.sup.2 is H, CH.sub.3, or F;R.sup.3 is CH.sub.3 or CF.sub.3 ;R.sup.4 is H, C.sub.1 to C.sub.12 n-alkyl, branched chain alkyl, or cycloalkyl, or a physiologically acceptable metal or amine salt cation; andn is an integer from 3 to 8.Type: GrantFiled: December 27, 1982Date of Patent: June 26, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chia-Lin J. Wang
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Patent number: 4454327Abstract: 5-oxo-2,2-pyrrolidinedipropanoic acid, base addition salts and esters are useful as agents for the reversal of amnesia. Intermediates for preparing said compounds, pharmaceutical compositions containing said compounds and methods for using said pharmaceutical compositions for treating senility and reversal of amnesia are also taught.Type: GrantFiled: May 24, 1982Date of Patent: June 12, 1984Assignee: Warner-Lambert CompanyInventor: Donald E. Butler
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Patent number: 4452990Abstract: 1-Aroyl-5-oxo-2-pyrrolidinepropanoic acids, salts, and esters which are useful as pharmacological agents, especially as agents for the reversal of amnesia, enhancing performance in poorly motivated subjects and treatment of senility and methods for their preparations are disclosed. Pharmaceutical compositions containing said compounds, salts, and esters and methods for using said compositions in treating senility, improving motivation and reversal of amnesia are also taught.Type: GrantFiled: November 15, 1982Date of Patent: June 5, 1984Assignee: Warner-Lambert CompanyInventor: Donald E. Butler
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Patent number: 4450102Abstract: Novel compositions are provided for the cleaning and inhibiting corrosion of metallic surfaces. The cleaning composition has an active ingredient consisting of at least one sulfur containing compound selected from the group consisting of a bis(N-2 pyrrolidonyl), an (N-2 pyrrolidonyl), or a bis(N-succinimidyl) sulfur-containing compound.Type: GrantFiled: November 2, 1982Date of Patent: May 22, 1984Assignee: Phillips Petroleum CompanyInventors: Merlin R. Lindstrom, Gary D. Macdonell, Rector P. Louthan, Donald H. Kubicek