Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
  • Patent number: 4337340
    Abstract: 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: Grant
    Filed: August 21, 1980
    Date of Patent: June 29, 1982
    Assignee: Sterling Drug Inc.
    Inventors: Paul J. Schmidt, William M. Hung
  • Patent number: 4335241
    Abstract: 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: Grant
    Filed: February 23, 1981
    Date of Patent: June 15, 1982
    Assignee: BASF Aktiengesellschaft
    Inventor: Walter Boell
  • Patent number: 4301287
    Abstract: 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: Grant
    Filed: December 17, 1979
    Date of Patent: November 17, 1981
    Assignee: H. Lundbeck & Co. A/S
    Inventor: Povl Krogsgaard-Larsen
  • Patent number: 4297498
    Abstract: 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: Grant
    Filed: August 23, 1979
    Date of Patent: October 27, 1981
    Assignee: Mead Johnson & Company
    Inventors: John E. Lawson, Ronald D. Dennis
  • Patent number: 4291042
    Abstract: 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: Grant
    Filed: January 21, 1980
    Date of Patent: September 22, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Patent number: 4278676
    Abstract: 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: Grant
    Filed: June 19, 1978
    Date of Patent: July 14, 1981
    Assignee: H. Lundbeck & Co. A/S
    Inventor: Krogsgaard-LarsenPovl
  • Patent number: 4260613
    Abstract: 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: Grant
    Filed: March 17, 1980
    Date of Patent: April 7, 1981
    Assignee: Crinos Industria Farmacobiologica S.p.A.
    Inventor: Alberto Reiner
  • Patent number: 4233304
    Abstract: 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: Grant
    Filed: July 3, 1979
    Date of Patent: November 11, 1980
    Assignee: Crinos Industria Farmacobiologica S.p.A.
    Inventor: Alberto Reiner
  • Patent number: 4232887
    Abstract: 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: Grant
    Filed: March 5, 1979
    Date of Patent: November 11, 1980
    Assignee: Appleton Papers Inc.
    Inventors: William J. Becker, Sheldon Farber, Troy E. Hoover
  • Patent number: 4212976
    Abstract: 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: Grant
    Filed: September 20, 1977
    Date of Patent: July 15, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Tsung-Ying Shen, Howard Jones, Dennis M. Mulvey, Conrad P. Dorn
  • Patent number: 4211872
    Abstract: 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: Grant
    Filed: December 11, 1978
    Date of Patent: July 8, 1980
    Inventors: Paul J. Schmidt, William M. Hung
  • Patent number: 4210652
    Abstract: 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: Grant
    Filed: October 4, 1978
    Date of Patent: July 1, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Patent number: 4206117
    Abstract: 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: Grant
    Filed: March 10, 1978
    Date of Patent: June 3, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerda Von Philipsborn, Walter Boell, Dieter Lenke
  • Patent number: 4200753
    Abstract: 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: Grant
    Filed: November 17, 1978
    Date of Patent: April 29, 1980
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventor: Ronald A. Henry
  • Patent number: 4191827
    Abstract: 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: Grant
    Filed: September 18, 1978
    Date of Patent: March 4, 1980
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson
  • Patent number: 4182888
    Abstract: 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: Grant
    Filed: January 30, 1978
    Date of Patent: January 8, 1980
    Assignee: Mead Johnson & Company
    Inventors: John E. Lawson, Ronald D. Dennis
  • Patent number: 4181661
    Abstract: 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: Grant
    Filed: February 6, 1978
    Date of Patent: January 1, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Joshua Rokach, Edward J. Cragoe, Jr.
  • Patent number: 4179566
    Abstract: 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: Grant
    Filed: July 17, 1978
    Date of Patent: December 18, 1979
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson
  • Patent number: 4170705
    Abstract: 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: Grant
    Filed: July 17, 1978
    Date of Patent: October 9, 1979
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson
  • Patent number: 4168379
    Abstract: 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: Grant
    Filed: March 10, 1978
    Date of Patent: September 18, 1979
    Assignee: BASF Aktiengesellschaft
    Inventors: Walter Boell, Horst Koenig
  • Patent number: 4158735
    Abstract: 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: Grant
    Filed: May 1, 1978
    Date of Patent: June 19, 1979
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson
  • Patent number: 4145432
    Abstract: 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: Grant
    Filed: July 1, 1976
    Date of Patent: March 20, 1979
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventor: Yoshinari Sato
  • Patent number: 4131679
    Abstract: 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: Grant
    Filed: July 26, 1977
    Date of Patent: December 26, 1978
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson