Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 544/400)
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Patent number: 4320067Abstract: A process for preparing modified polyisocyanates in which an organic polyisocyanate is reacted with a polyamine present in less than stoichiometric amount. Polyamines suitable to this process include (a) polyamines having more than three nonaromatically bound, basic nitrogen atoms of which at least two are primary and/or secondary amino nitrogen atoms, and (b) polyamine mixtures having an average of more than three nonaromatically bound, basic nitrogen atoms of which at least two are primary and/or secondary amino nitrogen atoms. These modified polyisocyanates are particularly useful starting materials for production of polyurethane plastics by the isocyanate-polyaddition process.Type: GrantFiled: January 26, 1981Date of Patent: March 16, 1982Assignee: Bayer AktiengesellschaftInventors: Wulf von Bonin, Helmut Kleimann, Hans-Albrecht Freitag
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Patent number: 4303588Abstract: Novel farnesylacetic acid amide compounds represented by general formula ##STR1## wherein A is alkylene of at least 2 carbon atoms, R.sup.1 is H or lower alkyl, and R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, alkenyl, aryl or aralkyl, or either one of R.sup.2 and R.sup.3 is such a group that forms, together with A, a piperidine or pyrrolidine ring which contains as constituent thereof the nitrogen atom lying therebetween, or R.sup.2 and R.sup.3 combinedly represent a group which forms, together with the nitrogen atom to which they are bonded, a piperidine, pyrrolidine or piperazine ring; and salts thereof have antiulcerogenic and antibacterial activities.Type: GrantFiled: March 21, 1980Date of Patent: December 1, 1981Assignee: Kuraray Co., Ltd.Inventors: Susumu Okabe, Yoshiaki Omura, Yoichi Ninagawa, Yoshiji Fujita
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Patent number: 4284776Abstract: Radiation polymerizable acrylyloxy-containing reaction products are provided from Michael addition reaction of an amide acrylate material with a primary or secondary amine. The resulting amine adducts of the amide acrylate compounds possess high cure rates in air.Type: GrantFiled: December 9, 1977Date of Patent: August 18, 1981Assignee: PPG Industries, Inc.Inventors: Gerald W. Gruber, Charles B. Friedlander, William H. McDonald, Rostyslaw Dowbenko
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Patent number: 4278796Abstract: New piperazine derivatives and homologs thereof of formula ##STR1## wherein n is equal to 2 or 3 and m to 1, 2 or 3;X represents hydrogen or a methyl group;R represents hydrogen or a C.sub.1 to C.sub.6 lower alkyl group or a C.sub.1 to C.sub.3 hydroxyalkyl group; andR.sub.1 is a cyclohexyl group of formula ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 to C.sub.6 lower alkyl group. The compounds have antiulcer and antisecretory activity.Type: GrantFiled: November 28, 1979Date of Patent: July 14, 1981Inventor: Camillo Corvi-Mora
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Patent number: 4274837Abstract: Fuel compositions for internal combustion engines are provided containing deposit control additives which maintain cleanliness of intake systems without contributing to combustion chamber deposits. The additives are hydrocarbylpoly(oxyalkylene) aminocarbamates comprising a hydrocarbyl-terminated poly(oxyalkylene) moiety composed of 2-5 carbon oxyalkylene units and one or more 9-30 carbon oxyalkylene groups. Certain additives also find use as dispersants in lubricating oils.Type: GrantFiled: July 2, 1979Date of Patent: June 23, 1981Assignee: Chevron Research CompanyInventor: Jennifer E. Lilburn
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Patent number: 4267354Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R'.sub.3 is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; are intermediates useful in the preparation of substituted amides having antiinflammatory activity.Type: GrantFiled: February 4, 1980Date of Patent: May 12, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4263293Abstract: Mammalian collagenase is inhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; andn is an integer of 1 to 20.Type: GrantFiled: May 30, 1980Date of Patent: April 21, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Joseph E. Sundeen, Tamara Dejneka
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Patent number: 4216335Abstract: Compounds having the formulas ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R.sub.3 ' is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; are intermediates useful in the preparation of substituted amides having antiinflammatory activity.Type: GrantFiled: April 25, 1979Date of Patent: August 5, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4209624Abstract: A process is disclosed for preparing substituted bis-(amidinoureas) by reacting a 1-substituted-4-alkyl-4-isothiobiuret with a compound containing two aliphatic amino groups.Type: GrantFiled: July 19, 1977Date of Patent: June 24, 1980Assignee: Cooper Laboratories, Inc.Inventor: Ronald A. Wohl
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Patent number: 4197308Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4- dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: May 10, 1978Date of Patent: April 8, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4183933Abstract: 2,3,4,7,8,9-Substituted octahydropyrazinopyrimidinones and acid addition salts thereof. A process for the preparation of said compounds. A pharmaceutical composition comprising such a compound and a conventional carrier. A process for the preparation of said composition. Method of medical treatment of human beings and animals using such compounds.Type: GrantFiled: August 30, 1978Date of Patent: January 15, 1980Assignee: AB FerrosanInventors: Anders K. K. Bjork, Aina L. Abramo, Sven E. H. Hernestam, Bengt E. S. Kjellberg
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Patent number: 4179501Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: May 10, 1978Date of Patent: December 18, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4172945Abstract: Compounds are provided having the structure ##STR1## wherein n is 1, 2 or 3, m is 0, 1 or 2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and can be hydrogen, lower alkyl, halo-lower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxyalkylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.Type: GrantFiled: July 27, 1978Date of Patent: October 30, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Joseph E. Sundeen, Joyce Reid
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Patent number: 4169899Abstract: Penicillamine compounds of the formula: ##STR1## and of the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, A and B are as defined hereinafter, and pharmaceutically acceptable acid addition salts thereof are disclosed. II are the products of hydrolysis or alcoholysis of I, and I are in turn the products of dehydration of II or alcohol removal form II. I and II are useful for the treatment of rheumatoid arthritis.Type: GrantFiled: January 6, 1978Date of Patent: October 2, 1979Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masami Shiroki, Yutaka Maruyama, Kazuhiro Goto
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Patent number: 4166072Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.Type: GrantFiled: April 18, 1978Date of Patent: August 28, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4161590Abstract: The invention is directed to fluorinated compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxy-perfluoroalkyl group, R.sup.1 is a branched or straight chain alkylene, alkylenethioalkylene, alkyleneoxy-alkylene or alkyleneiminoalkylene group, X is oxygen or an amino group, Q is an organic group containing at least one amino group and y is zero or 1, and the corresponding succinimides. These compounds are useful as surfactants.Type: GrantFiled: January 12, 1978Date of Patent: July 17, 1979Assignee: Ciba-Geigy CorporationInventor: Karl F. Mueller
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Patent number: 4160648Abstract: Fuel compositions for internal combustion engines are provided which contain deposit control additives which maintain cleanliness of intake systems without contributing to combustion chamber deposits. The additives are polyloxyalkylene carbamates comprising a hydroxy- or hydrocarbyloxy-terminated polyloxyalkylene chain of 2-5 carbon oxyalkylene units bonded through an oxycarbonyl group to a nitrogen atom of a polyamine having from 2 to 10 amine nitrogens and from 2 to 40 carbons with a carbon:nitrogen ratio between about 1:1 and 10:1.Type: GrantFiled: May 27, 1977Date of Patent: July 10, 1979Assignee: Chevron Research CompanyInventors: Robert A. Lewis, Lewis R. Honnen
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Patent number: 4156079Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: June 19, 1978Date of Patent: May 22, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4152459Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4-dichlorobenzamide, and their parmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: May 10, 1978Date of Patent: May 1, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4151354Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: August 2, 1978Date of Patent: April 24, 1979Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4145435Abstract: Cis- and trans-N-(2-aminocycloaliphatic)-2-arylacetamide derivative compounds of the formula ##STR1## e.g., N-?2-(N', N'-dimethylamino)cyclohexyl!-N-methyl-2-(4-bromophenyl)acetamide and trans-N-methyl-N-?2-(1-pyrrolidinyl)cyclohexyl!acetamide, 2-(3,4-dichlorophenyl) and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and the preferred compounds have in addition only low to moderate apparent physical dependence liability, compared to morphine and methadone. As analgesics they would be useful also as antitussives. Processes for preparation of these compounds are also disclosed. This invention also includes compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in humans and animals, as well as methods for alleviating pain in animals and humans with these compositions.Type: GrantFiled: November 12, 1976Date of Patent: March 20, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4123530Abstract: New piperazine derivatives and homologs thereof of formula ##STR1## wherein n is equal to 2 or 3 and m to 1, 2 or 3; X REPRESENTS HYDROGEN OR A METHYL GROUPR represents hydrogen or a C.sub.1 to C.sub.6 lower alkyl group or a C.sub.1 to C.sub.3 hydroxyalkyl group; andR.sub.1 is one of the following groups:A substituted cyclohexyl of formula ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 to C.sub.6 lower alkyl group, A SUBSTITUTED PHENYL OF FORMULA ##STR3## wheein R.sub.3 is hydrogen, methyl or ethyl, OR WHEREIN R.sub.1 is norbornyl, bornyl or cinnamyl, are useful as antiulcerous compounds.Type: GrantFiled: January 12, 1977Date of Patent: October 31, 1978Assignee: Camillo Corvi S.p.A.Inventor: Camillo Corvi-Mora
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Substituted amides and sulfonamides containing a heterocyclic group having antiinflammatory activity
Patent number: 4122255Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.Type: GrantFiled: September 21, 1977Date of Patent: October 24, 1978Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho -
Patent number: 4110328Abstract: Antimicrobial compounds are disclosed having the formula:Z--B--Y--B--Z .rHAwherein B is carbamylguanidino or thiocarbamylguanidino, Y is a nitrogen-containing alkylene group having the structural formula: ##STR1## WHEREIN: N = 2-4m = 2-4p = 1,2q = 2-4x = 0-3y = 0-2x = 0 when y .noteq. 0 and y = 0 when x .noteq. 0,And R is hydrogen or a C.sub.1 -C.sub.8 hydrocarbon radical selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, and aralkyl radicals, R' and R" are each hydrogen or C.sub.1 -C.sub.4 alkyl and may be the same or different and Z is selected from the group consisting of C.sub.1 -C.sub.12 alkyl, di(C.sub.1 -C.sub.10 alkylamino)-C.sub.10 -C.sub.2 having a total carbon content of C.sub.4 -C.sub.12 ; C.sub.3 -C.sub.12 alkenyl; C.sub.3 -C.sub.12 alkynyl; C.sub.3 -C.sub.12 cycloalkyl, C.sub.4 -C.sub.12 cycloalkylalkyl; C.sub.6 -C.sub.12 cycloalkenyl, C.sub.7 -C.sub.14 cycloalkenylalkyl, C.sub.7 -C.sub.12 polycycloalkyl, C.sub.8 -C.sub.14 polycycloalkylalkyl, C.sub.7 -C.sub.Type: GrantFiled: October 26, 1976Date of Patent: August 29, 1978Assignee: Cooper Laboratories, Inc.Inventor: Julius Diamond
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Patent number: 4101671Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##STR2## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy (cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino,Provided, however, that when R.sub.3 is carboxyl or carbalkoxy, R.sub.4 and R.sub.Type: GrantFiled: March 24, 1977Date of Patent: July 18, 1978Assignee: Boehringer Ingelheim GmbHInventors: Johannes Keck, Klaus-Reinhold Noll, Helmut Pieper, Gerd Kruger, Sigfrid Puschmann
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Patent number: 4098789Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alkylene group having 2 to 5 carbon atoms; and n is 1, 2 or 3; have antiinflammatory activity.Type: GrantFiled: March 2, 1977Date of Patent: July 4, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, Chester F. Turk
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Patent number: 4098904Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## E.G., N-methyl-N[2-(N-pyrrolidinyl)cyclohexyl[3,4-dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: November 12, 1976Date of Patent: July 4, 1978Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4098895Abstract: Amino aceto anilides of the formula I shown hereinafter are effective microbicides. They may be used to control fungi on plants or parts of plants or to prevent them from fungi attack.Type: GrantFiled: September 24, 1976Date of Patent: July 4, 1978Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Walter Kunz, Wolfgang Eckhardt
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Patent number: 4093631Abstract: Compounds of the formula (I): ##STR1## and salts thereof wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms or benzyl; R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms or is joined to R.sub.1 so that the NR.sub.1 R.sub.2 moiety is a 5-, 6- or 7-membered saturated heterocyclic ring; R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms or acyl of 1 to 4 carbon atoms; R.sub.4 is an aromatic group; R.sub.5 is hydrogen or alkyl of 1 to 4 carbon atoms R.sub.6 is hydrogen or alkyl of 1 to 4 carbon atoms; X is --CH.sub.2 -- or an oxygen atom and the dotted line represents a single or double bond, are useful for inducing anorexia and for their mood-modifying effects.Type: GrantFiled: June 1, 1976Date of Patent: June 6, 1978Assignee: Beecham Group LimitedInventor: Derek Victor Gardner
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Patent number: 4092318Abstract: Compounds are provided having the structure ##STR1## WHEREIN N IS 1, 2 OR 3, M AND M' ARE 0, 1 OR 2, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## or lower alkoxyalkylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR3## These compounds are useful in the treatment of hypertension.Type: GrantFiled: March 15, 1976Date of Patent: May 30, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic Peter Hauck, Joyce Reid, Venkatachala L. Narayanan, Christopher M. Cimarusti, Rudiger D. Haugwitz, Joseph E. Sundeen
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Patent number: 4091220Abstract: Novel N-benzylpiperazine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are same or different and each stands for a hydrogen atom or an acyl group; R.sup.3 stands for a hydrogen atom; a carbamoyl group, an acyl group which is unsubstituted or substituted by mercapto or morpholino, or an alkyl group which is unsubstituted or substituted by hydroxy, aryl or aminocarbonyl represented by the formula ##STR2## wherein each of R.sup.4 and R.sup.5 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms or a cyclohexyl group, or R.sup.4 and R.sup.5 form a morpholino or piperidino ring together with the nitrogen atom adjacent thereto, and X stands for a halogen atom, and pharmaceutically acceptable acid addition salts thereof. These compounds and salts thereof have respiratory tract fluid secretion stimulatory properties and are useful as medicines such as respiratory track fluid secretion stimulators.Type: GrantFiled: May 3, 1977Date of Patent: May 23, 1978Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshihiro Ishiguro, Yasushi Sanno
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Patent number: RE29628Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##STR2## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.Type: GrantFiled: December 2, 1976Date of Patent: May 9, 1978Assignee: Boehringer Ingelheim GmbHInventors: Johannes Keck, Klaus-Reinhold Noll, Helmut Pieper, Gerd Kruger, Sigfrid Puschmann