The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/153)
  • Patent number: 4191690
    Abstract: Substituted 3,6-diaminophthalides of the formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 independently represents alkyl of not more than 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or represents cycloalkyl, benzyl, or benzyl which is substituted by halogen, lower alkyl or lower alkoxy, and R.sub.1 can also be hydrogen and R.sub.3 can also be phenyl, or R.sub.1 and R.sub.2, together with the nitrogen atom to which they are attached, represent a 5- or 6-membered heterocyclic radical and the ring A is unsubstituted or substituted or contains a fused, unsubstituted or substituted benzene or heterocyclic ring.These compounds are suitable in particular for use as color formers in pressure-sensitive or heat-sensitive recording materials.
    Type: Grant
    Filed: September 15, 1978
    Date of Patent: March 4, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Burri
  • Patent number: 4163843
    Abstract: This invention relates to certain 7a-homo-4-oxo-PGI.sub.1 compounds. These novel prostacyclin-type compounds are useful for pharmacological purposes.
    Type: Grant
    Filed: May 8, 1978
    Date of Patent: August 7, 1979
    Assignee: The Upjohn Company
    Inventor: Donald E. Ayer
  • Patent number: 4160095
    Abstract: The present invention relates to certain 7,8-didehydro-PGI.sub.1 amides, which are pharmacologically active amides of the corresponding 7,8-didehydro-PGI.sub.1 acids. These novel prostacyclin type amides are endoperoxide cyclooxygenase inhibitors which prevent the conversion of unsaturated fatty acids to endoperoxides (e.g., PGG.sub.2 and PGH.sub.2). By virtue of this pharmacological property these analogs represent potent antiinflammatory agents.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: July 3, 1979
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 4154743
    Abstract: Novel halogeno-benzofuranone-carboxylic acids and a novel process for their preparation by reacting substituted or unsubstituted phenols with dihalogenomaleic anhydrides or derivatives thereof are described. The novel halogeno-benzofuranone-carboxylic acids are valuable intermediates for the preparation of pharmaceutical active compounds having an antiallergic action or for the preparation of biocidal active compounds for combating plant and animal pests, in particular phytopathogenic fungi and bacteria.
    Type: Grant
    Filed: February 9, 1978
    Date of Patent: May 15, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Bosshard, Niklaus Buhler
  • Patent number: 4151351
    Abstract: This invention relates to certain structural analogs of 5,6-dihydroprostacyclin (PGI.sub.1) wherein an endocyclic double bond is present at the C-7 to C-8 position. These novel unsaturated prostacyclin type compounds are endoperoxide cyclooxygenase inhibitors which prevent the conversion of unsaturated fatty acids to endoperoxides (e.g., PGG.sub.2 and PGH.sub.2). By virtue of this pharmacological property these analogs represent potent antiinflammatory agents.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: April 24, 1979
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 4133880
    Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.
    Type: Grant
    Filed: July 28, 1977
    Date of Patent: January 9, 1979
    Assignees: Mitsubishi Chemical Industries Ltd., Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
  • Patent number: 4128713
    Abstract: This invention relates to certain structural and pharmacological analogs of 5,6-dihydroprostacyclin (PGI.sub.1) wherein an endocyclic double bond is present at the C-6 to C-7 position. These novel unsaturated prostacyclin-type compounds are useful for the pharmacological purposes for which prostacyclin is used, e.g., as antithrombotic agents, smooth muscle stimulators, gastric antisecretory agents, antihypertensive agents, antiasthma agents, nasal decongestants, or regulators of fertility and procreation.
    Type: Grant
    Filed: December 15, 1977
    Date of Patent: December 5, 1978
    Assignee: The Upjohn Company
    Inventor: William P. Schneider
  • Patent number: 4126744
    Abstract: This invention relates to certain structural and pharmacological analogs of 5,6-dihydro-prostacyclin (PGI.sub.1) wherein the C-4 position is substituted by oxo. These novel 4-oxo-prostacyclin-type compounds are useful for the same pharmacological purposes as prostacyclin, particularly being smooth muscle stimulators and platelet aggregation inhibitors.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: November 21, 1978
    Assignee: The Upjohn Company
    Inventor: Donald E. Ayer
  • Patent number: 4124710
    Abstract: The invention relates to acetamidoxime derivatives represented by the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 represents a branched- or straight-chain alkyl group containing from 1 to 4 carbon atoms or a phenyl group, A represents one of the groups: ##STR2## R.sub.2 represents an amino group such as, for example, a dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino, pyrrolidino, morpholino, piperidino or heptamethyleneimino group or a 1-piperazino group substituted in the 4-position by a straight-chain alkyl group containing from 1 to 4 carbon atoms, X represents a hydrogen or chlorine atom or a methoxy group and n is the integer 2 or 3.The compounds of formula I have been found to be potentially useful in the treatment of disorders of arterial pressure.
    Type: Grant
    Filed: December 9, 1976
    Date of Patent: November 7, 1978
    Assignee: Labaz
    Inventors: Marcel Descamps, Alex Areschka
  • Patent number: 4119776
    Abstract: A chromogenic compound of normally colorless form is disclosed having the following structural formula: ##STR1## wherein A can be ##STR2## T, Q, X, Y and Z can be, among several others, hydrogen, alkyl, alkoxy, aryl, and heterocyclic, substituted and unsubstituted; and E can be a broad family of aromatic and heterocyclic structures. The compound is eligible for use in pressure-sensitive record materials and manifold marking systems. Because of light absorption characteristics, selected compounds of this invention are especially useful where machine readability and machine copiability are important.
    Type: Grant
    Filed: April 25, 1977
    Date of Patent: October 10, 1978
    Assignee: NCR Corporation
    Inventor: Sheldon Farber
  • Patent number: 4107437
    Abstract: 2,3-Dihydrobenzofuran of formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, a lower alkyl or lower phenylalkyl or form, together with the nitrogen atom to which they are attached, a 4 to 8-membered saturated heterocyclic ring having 3 to 7 cyclic carbon atoms, a 4 to 8-membered saturated heterocyclic ring having 2 to 6 cyclic carbon atoms and two heteroatoms one of which is said nitrogen atom and the other is an oxygen atom, a sulphur atom or another nitrogen atom, said other nitrogen atom being optionally substituted by a phenyl, halophenyl, trifluromethylphenyl, lower alkylphenyl or lower alkoxyphenyl; n is 2 or 3, and the salts thereof.
    Type: Grant
    Filed: May 2, 1977
    Date of Patent: August 15, 1978
    Assignee: PARCOR
    Inventors: Jean-Pierre Maffrand, Jean-Marie Pereillo
  • Patent number: 4100294
    Abstract: 5-[Hydroxy(substituted)methyl]-2,3-dihydrobenzo-furan-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: July 11, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., William Hoffman
  • Patent number: 4072705
    Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholesterolaemiant and cholagogic agents or in the preparation of such agents.
    Type: Grant
    Filed: February 9, 1976
    Date of Patent: February 7, 1978
    Assignee: Orchimed S.A.
    Inventor: Andre Mieville