Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
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Patent number: 4337340Abstract: Substituted furopyridinones and furopyrazinones which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting diphenylamines with substituted benzoyl (or 3-indolylcarbonyl)pyridinecarboxylic acids and substituted benzoyl (or 3-indolylcarbonyl)pyrazinecarboxylic acids, respectively.Type: GrantFiled: August 21, 1980Date of Patent: June 29, 1982Assignee: Sterling Drug Inc.Inventors: Paul J. Schmidt, William M. Hung
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Patent number: 4335241Abstract: 4-.alpha.-Amino-arylmethyl-6-methyl-1,3-dihydro-furo[3,4-c]pyridin-7-ols of the formula ##STR1## where R.sup.1 and R.sup.2 together are alkylene which may be interrupted by a hetero-atom and may be substituted by C.sub.1-4 -alkyl, andR.sup.3 and R.sup.4 are hydrogen, hydroxyl, C.sub.1-3 -alkyl, C.sub.1-3 -alkoxy or halogen,processes for their preparation, and their use for the preparation of pyridinyl aminoalkyl ethers.Type: GrantFiled: February 23, 1981Date of Patent: June 15, 1982Assignee: BASF AktiengesellschaftInventor: Walter Boell
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Patent number: 4301287Abstract: The compound Ia ##STR1## has been shown to possess GABA-related activity. The invention relates to Ia and derivatives thereof, covered by the formula ##STR2## in which R" is hydrogen, acetyl or a group of the general formula VII ##STR3## in which R.sub.5 is C.sub.1-8 alkyl; phenyl; phenyl substituted in the 4-position with halogen, lower alkoxy, or lower alkyl; or phenylalkyl in which the phenyl group may be substituted in the 4-position with halogen, lower alkoxy, or lower alkyl; and salts thereof.Type: GrantFiled: December 17, 1979Date of Patent: November 17, 1981Assignee: H. Lundbeck & Co. A/SInventor: Povl Krogsgaard-Larsen
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Patent number: 4297498Abstract: A series of 2,6-diamino-4-tertiary-amino-pyridine 1-oxides is disclosed. Substituents in the 4-position include diethylamino, pyrrolidinyl, piperidino, morpholino, thiomorpholino, and N-methylpiperazino. Novel oxadiazolones such as 5-amino-7-(1-piperidinyl)-2H-[1,2,4]oxadiazolo[2,3-a]pyridine-2-one which are useful in the preparation of the pyridine 1-oxides are also disclosed. The compounds of this invention lower blood pressure in normotensive and hypertensive mammals and are particularly useful in the treatment of hypertensive conditions in mammals. 2,6-Diamino-4-(1-piperidinyl)pyridine 1-oxide is a representative embodiment of the invention.Type: GrantFiled: August 23, 1979Date of Patent: October 27, 1981Assignee: Mead Johnson & CompanyInventors: John E. Lawson, Ronald D. Dennis
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Patent number: 4291042Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.Type: GrantFiled: January 21, 1980Date of Patent: September 22, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4278676Abstract: The compound Ia ##STR1## has been shown to possess GABA-related activity. The invention relates to Ia and derivatives thereof, covered by the formula ##STR2## in which R" is hydrogen, acetyl or a group of the general formula ##STR3## in which R.sub.5 is C.sub.1-8 alkyl; phenyl; phenyl substituted in the 4-position with halogen, lower alkoxy, or lower alkyl; or phenylalkyl in which the phenyl group may be substituted in the 4-position with halogen, lower alkoxy, or lower alkyl; and salts thereof.Type: GrantFiled: June 19, 1978Date of Patent: July 14, 1981Assignee: H. Lundbeck & Co. A/SInventor: Krogsgaard-LarsenPovl
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Patent number: 4260613Abstract: The invention concerns novel piridoxine derivatives of the general formula: ##STR1## which show anti-inflammatory activity and moreover may show, although not necessarily, also analgesic and/or anti-pyretic activity.Type: GrantFiled: March 17, 1980Date of Patent: April 7, 1981Assignee: Crinos Industria Farmacobiologica S.p.A.Inventor: Alberto Reiner
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Patent number: 4233304Abstract: The invention concerns novel piridoxine derivatives of the general formula: ##STR1## which show anti-inflammatory activity and moreover may show, although not necessarily, also analgesic and/or anti-pyretic activity.Type: GrantFiled: July 3, 1979Date of Patent: November 11, 1980Assignee: Crinos Industria Farmacobiologica S.p.A.Inventor: Alberto Reiner
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Patent number: 4232887Abstract: Chromogenic compounds of normally colorless form are disclosed having the following structural formula: ##STR1## wherein E represents a six-membered aromatic or heterocyclic ring which may have an aromatic condensed ring and both the E ring and the condensed ring may be substituted, A represents an optionally substituted aminophenyl, indolyl, benzoindolyl, julolidinyl or kairolyl radical or the radical represented by B, and B represents a family of indolizine radicals. The compounds of this invention are eligible for use in pressure-sensitive and heat sensitive record materials and manifold marking systems.Type: GrantFiled: March 5, 1979Date of Patent: November 11, 1980Assignee: Appleton Papers Inc.Inventors: William J. Becker, Sheldon Farber, Troy E. Hoover
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Patent number: 4212976Abstract: Mercaptoalkylpyridines and various derivatives thereof have utility in the treatment of rheumatoid arthritis. The compounds useful in the method of treatment are generally prepared from known pyridine derivatives and, principally, from pyridoxine and related compounds.Type: GrantFiled: September 20, 1977Date of Patent: July 15, 1980Assignee: Merck & Co., Inc.Inventors: Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
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Patent number: 4211872Abstract: Substituted furopyridinones and furopyrazinones which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting diphenylamines with substituted benzoyl (or 3-indolylcarbonyl)pyridinecarboxylic acids and substituted benzoyl (or 3-indolylcarbonyl)pyrazinecarboxylic acids, respectively.Type: GrantFiled: December 11, 1978Date of Patent: July 8, 1980Inventors: Paul J. Schmidt, William M. Hung
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Patent number: 4210652Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(3-methoxy-2-pyridylmethylthio)ethyl)guanidino]propane and 1-[N-(2-(3-methoxy-pyridylmethylthio)ethyl)guanidino]-3-[N'-2-(5-methyl-4- imidazolylmethylthio)ethyl)guanidino]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: October 4, 1978Date of Patent: July 1, 1980Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
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Patent number: 4206117Abstract: New pyridinyl aminoalkyl ethers, their N-oxides and their physiologically acceptable addition salts with acids, processes for their preparation and pharmaceutical formulations which contain these compounds and are useful in the treatment of cardiac arrhythmias.Type: GrantFiled: March 10, 1978Date of Patent: June 3, 1980Assignee: BASF AktiengesellschaftInventors: Gerda Von Philipsborn, Walter Boell, Dieter Lenke
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Patent number: 4200753Abstract: Compounds having the structures: ##STR1## wherein R is CH.sub.3 or CF.sub.3 and wherein R.sup.1 is H or CH.sub.3. compounds are prepared by a four step method involving (1) the formation of a benzylaminophenol or benzylaminohydroxypyridine, (2) the formation of a coumarin or azacoumarin, (3) sulfonation of the coumarin or azacoumarin and (4) neutralization of the sulfonate with sodium bicarbonate. The compounds are useful as water-soluble lasing dyes.Type: GrantFiled: November 17, 1978Date of Patent: April 29, 1980Assignee: The United States of America as represented by the Secretary of the NavyInventor: Ronald A. Henry
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Patent number: 4191827Abstract: This disclosure describes novel compounds of the formula: ##STR1## where R.sub.1 is straight chain lower alkyl or ##STR2## where R.sub.4 is hydrogen or halo having an atomic weight of about 19 to 36, andR.sub.2 is straight chain lower alkyl, andR.sub.3 is hydrogen or halo as defined above,which are useful as minor tranquilizers and muscle relaxants.Type: GrantFiled: September 18, 1978Date of Patent: March 4, 1980Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson
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Patent number: 4182888Abstract: A series of 2,6-diamino-4-tertiary-amino-pyridine 1-oxides is disclosed. Substituents in the 4-position include diethylamino, pyrrolidinyl, piperidino, morpholino, thiomorpholino, and N-methylpiperazino. Novel oxadiazolones such as 5-amino-7-(1-piperidinyl)-2H-[1,2,4]-oxadiazolo[2,3-a]pyridine-2-one which are useful in the preparation of the pyridine 1-oxides are also disclosed. The compounds of this invention lower blood pressure in normotensive and hypertensive mammals and are particularly useful in the treatment of hypertensive conditions in mammals. 2,6-Diamino-4-(1-piperidinyl)pyridine 1-oxides is a prepresentative embodiment of the invention.Type: GrantFiled: January 30, 1978Date of Patent: January 8, 1980Assignee: Mead Johnson & CompanyInventors: John E. Lawson, Ronald D. Dennis
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Patent number: 4181661Abstract: 2-(Substituted imino)thiazolidines and thiazolines are inhibitors of indoleamine-N-methyl transferase in vivo. They are prepared by alkylation or acylation of the free imino group.Type: GrantFiled: February 6, 1978Date of Patent: January 1, 1980Assignee: Merck & Co., Inc.Inventors: Clarence S. Rooney, Joshua Rokach, Edward J. Cragoe, Jr.
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Patent number: 4179566Abstract: Substituted hydroxy pyridones, e.g., 3-(1-iminopropyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone, are prepared by reducing corresponding isoxazolo[4,5-c]pyridin-4(5H)-ones and are useful as minor tranquilizers, sleep inducers and neuroleptics.Type: GrantFiled: July 17, 1978Date of Patent: December 18, 1979Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson
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Patent number: 4170705Abstract: Substituted hydroxy pyridones, e.g., 3-(.alpha.-N-methyliminobenzyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone , are prepared by reacting a corresponding substituted hydroxy pyridone carbonyl with an alkyl amine, and are useful as minor tranquilizers, sleep inducers, muscle relaxants, and neuroleptics.Type: GrantFiled: July 17, 1978Date of Patent: October 9, 1979Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson
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Patent number: 4168379Abstract: New pyridin-3-ols and their N-oxides and acid addition salts, which are useful as intermediates, especially for the preparation of pharmacologically active compounds, and their preparation.Type: GrantFiled: March 10, 1978Date of Patent: September 18, 1979Assignee: BASF AktiengesellschaftInventors: Walter Boell, Horst Koenig
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Patent number: 4158735Abstract: Substituted hydroxy pyridones, e.g., 3-(.alpha.-iminobenzyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone, are prepared by reducing corresponding isoxazolo[4,5-c]pyridin-4(5H)-ones and are useful as minor tranquilizers and sleep inducers.Type: GrantFiled: May 1, 1978Date of Patent: June 19, 1979Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson
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Patent number: 4145432Abstract: This invention relates to 1,4-dihydropyridine derivatives. More particularly, it relates to new 1,4-dihydropyridine derivatives thereof which have vasodilating and anti-hypertensive activity, to processes for the preparation thereof, and to pharmaceutical composition comprising the same for therapeutical treatment in cardiovascular diseases and hypertension in human being.Type: GrantFiled: July 1, 1976Date of Patent: March 20, 1979Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventor: Yoshinari Sato
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Patent number: 4131679Abstract: This disclosure describes novel compounds of the formula: ##STR1## where R.sub.1 is straight chain lower alkyl or ##STR2## where R.sub.4 is hydrogen or halo having an atomic weight of about 19 to 36, andR.sub.2 is straight chain lower alkyl, andR.sub.3 is hydrogen or halo as defined above,Which are useful as minor tranquilizers and muscle relaxants.Type: GrantFiled: July 26, 1977Date of Patent: December 26, 1978Assignee: Sandoz, Inc.Inventor: Jeffrey Nadelson