Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/375)
  • Patent number: 4290954
    Abstract: A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.
    Type: Grant
    Filed: October 30, 1979
    Date of Patent: September 22, 1981
    Assignee: Kowa Company Limited
    Inventors: Kazuhiro Onogi, Hisashi Kunieda, Kiyoshi Kawamura, Masami Shiratsuchi, Masahiko Nagakura, Naoki Machida, deceased, by Takayasu Miwa, heir
  • Patent number: 4254116
    Abstract: 5H-[1]Benzopyrano[3,4-d]pyridines represented by the formula ##STR1## wherein each R.sub.1 is loweralkyl, R.sub.2 is alkyl, cycloalkyl or ##STR2## wherein Y is a straight or branched chain alkylene group having from 1 to 10 carbon atoms and each R.sub.4, R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen, halo, trifluoromethyl or loweralkyl; and R.sub.3 is hydroxy, acyloxy, loweralkoxy, loweralkenyloxy, loweralkynyloxy or ##STR3## X is a straight or branched chain alkylene group having from one to eight carbon atoms, and wherein R.sub.7 and R.sub.8 are the same or different members of the group consisting of hydrogen or loweralkyl, or ##STR4## wherein X is a straight or branched chain alkylene group having from one to eight carbon atoms, a is an integer from 1 to 4, b is an integer from 1 to 4, Z is CH.sub.2, O, S or NR.sub.10 with R.sub.10 being hydrogen or loweralkyl, with the limitation that when Z is O or S, the sum of a and b is 3 or 4; and when Z is NR.sub.
    Type: Grant
    Filed: April 8, 1974
    Date of Patent: March 3, 1981
    Assignee: Abbott Laboratories
    Inventor: Cheuk M. Lee
  • Patent number: 4243805
    Abstract: Techniques for the preparation of 3-fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(b,f) thiepins and their addition salts with organic and inorganic acids are disclosed. The described compositions evidence psychotropic activity and low toxicity and are characterized as neuroliptics with a high degree of cataleptic, anti-apomorphine and central depressant action.
    Type: Grant
    Filed: December 22, 1978
    Date of Patent: January 6, 1981
    Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobu
    Inventors: Miroslav Protiva, Miroslav Rajsner, Karel Sindelar, Jiri Jilek, Vaclav Bartl, Jirina Metysova, Antonin Dlabac, Leon Langsadl, Josef Pomykacek, Frantisek Miksik
  • Patent number: 4238611
    Abstract: Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.
    Type: Grant
    Filed: January 6, 1976
    Date of Patent: December 9, 1980
    Assignee: SPOFA, United Pharmaceutical Works
    Inventors: Miroslav Protiva, Karel Sindelar, Irena Cervena, Jirina Metysova
  • Patent number: 4230850
    Abstract: Novel 3-substituted-4-aminoalkoxy-5,6-condensed ring-2-pyranones are disclosed as having utility as pharmacologically active compounds, in particular vasodilatory, hypotensive, anti-ischemic and anti-tussive activity. The compounds may be 3-phenyl-4-morpholinoalkoxy-coumarins. Administration may be by the oral or parenteral route. Intermediates useful in the production of these compounds are also disclosed.
    Type: Grant
    Filed: March 9, 1979
    Date of Patent: October 28, 1980
    Assignee: LIPHA, Lyonnaise Industrielle Pharmaceutique
    Inventors: Philippe Briet, Jean-Jacques Berthelon, Jean-Claude Depin
  • Patent number: 4228284
    Abstract: 9-(.beta.-hydroxyethyl) piperazinyl-carbonyl-2-trifluoromethyl-10, 11-dihydrodibenzo[b,f]thiepin is prepared and disclosed as having antiinflamatory action.
    Type: Grant
    Filed: February 7, 1979
    Date of Patent: October 14, 1980
    Assignee: Nippon Chemiphar Company, Limited
    Inventors: Shigeru Yamabe, Yasuo Fujimoto, Shoji Ryu, Yoshio Suzuki, Yoshihiro Tanaka, Toru Yamanaka, Kiyosato Nyu
  • Patent number: 4206225
    Abstract: A compound of the formula ##STR1## wherein Q is CH.sub.2, C.dbd.O, CHOH or CHCH.sub.2 OH; M is O or NR.sub.6 ; where R.sub.6 is hydrogen, or certain alkyl, aralkyl, acyl or carboalkoxy substituted alkyl groups; R.sub.1 is hydrogen, or certain alkanoyl or amino substituted alkanoyl groups; R.sub.4 and R.sub.5 are each hydrogen or alkyl having from 1 to 4 carbon atoms; Z is alkylene having from 1 to 9 carbon atoms or --(alk.sub.1)--X--(alk.sub.2).sub.n -- where (alk.sub.1) and (alk.sub.2) are certain alkylene groups and X is O, S, SO or SO.sub.2 ; W is a methyl, phenyl, substituted phenyl, pyridyl, piperidyl, cycloalkyl or substituted cycloalkyl group and the pharmaceutically acceptable and addition salts of said compounds having a basic nitrogen atoms. Said compounds are useful as analgesics and as intermediates therefore.
    Type: Grant
    Filed: September 22, 1978
    Date of Patent: June 3, 1980
    Assignee: Pfizer Inc.
    Inventor: Michael R. Johnson
  • Patent number: 4161586
    Abstract: The present invention provides 5-hydroxy-PGI.sub.1, piperazinylamides, which are useful pharmacological agents. These analogs of prostaglandin I.sub.1 are useful for the stimulation of mammalian smooth muscle tissues.
    Type: Grant
    Filed: April 24, 1978
    Date of Patent: July 17, 1979
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, John C. Sih
  • Patent number: 4146624
    Abstract: Antiviral compositions and methods of inhibiting or inactivating viruses by administering to hosts an effective quantity of an active ingredient are disclosed herein. The active ingredients are those compounds having the formula ##STR1## wherein A is a straight or branched alkylene chain of from 1 to 6 carbon atoms and each Y is the group(A) ##STR2## wherein R.sup.1 and R.sup.2 are each individually selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, cycloalkyl of from 3 to 6 carbon atoms, alkenyl of from 3 to 6 carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group; or(B) ##STR3## wherein n is a whole integer of 4, 5 or 6 and R.sup.3 is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl and can be attached to any one of the carbon atoms of the heterocyclic group; or(C) ##STR4## wherein X is oxygen or N--R.sup.4 and R.sup.
    Type: Grant
    Filed: September 14, 1970
    Date of Patent: March 27, 1979
    Assignee: Richardson-Merrell Inc.
    Inventors: William L. Albrecht, Robert W. Fleming
  • Patent number: 4143139
    Abstract: 9-Hydroxydibenzo[b,d]pyrans useful as analgesics, hypotensives, immunosuppressants, tranquilizers; as anti-secretory and anti-anxiety drugs; intermediates therefor and derivatives thereof having the formulae ##STR1## wherein R is hydrogen or alkanoyl having from one to five carbon atoms; R.sub.1 is hydrogen, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.P --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from one to four carbon atoms in the alkyl group;Each of R.sub.4 and R.sub.5 is hydrogen, methyl or ethyl;R.sub.0 is oxo or alkylenedioxy having from two to four carbon atoms;Z is(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.
    Type: Grant
    Filed: July 27, 1977
    Date of Patent: March 6, 1979
    Assignee: Pfizer Inc.
    Inventor: Jasjit S. Bindra
  • Patent number: 4140790
    Abstract: The invention relates to novel piperazine derivatives having the formula (I), ##STR1## wherein R.sub.1 represents a C.sub.1-5 alkyl group having optionally a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl group, a phenyl group having optionally one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituent(s), or a C.sub.2-5 alkoxycarbonyl group,R.sub.2 represents hydrogen or a C.sub.1-4 alkyl group, andR.sub.3 represents furyl group, 9-xanthenyl group or a C.sub.5-6 cycloalkyl group having a C.sub.1-4 alkoxy substituent,Or acid addition salts or quaternary salts thereof.The invention also relates to pharmaceutical compositions containing the above compounds, furthermore to a process for the preparation of the novel compounds and pharmaceutical compositions.The novel compounds according to the invention possess anti-arrhythmic and coronary dilatating effects.
    Type: Grant
    Filed: December 12, 1977
    Date of Patent: February 20, 1979
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Karoly Felfoldi, Jozsef Apjok, Mihaly Bartok, Jozsef Czombos, Arpad Molnar, Ferenc Noteisz, Egon Karpati, Laszlo Szporny
  • 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: 4115568
    Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.
    Type: Grant
    Filed: April 13, 1977
    Date of Patent: September 19, 1978
    Assignee: Lilly Industries Limited
    Inventors: Jiban Kumar Chakrabarti, David Edward Tupper
  • Patent number: 4115574
    Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.
    Type: Grant
    Filed: June 1, 1977
    Date of Patent: September 19, 1978
    Assignee: Lilly Industries Limited
    Inventors: Jiban Kumar Chakrabarti, David Edward Tupper
  • Patent number: 4104280
    Abstract: Novel dibenzo[b.f]thiepin and oxepin compounds of the formula and the pharmaceutically acceptable esters and salts thereof, wherein R is hydrogen or methyl; X is oxygen or S(O).sub.n in which n is the integer 0, 1 or 2 and Z is a single or double bond, provided that when Z is a double bond X is not SO, and when R is methyl the compounds are (dl) mixtures, and methods for the production thereof.
    Type: Grant
    Filed: February 4, 1977
    Date of Patent: August 1, 1978
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Jack Ackrell
  • Patent number: 4101667
    Abstract: Dihydrodibenzo[b,f]thiepin compounds of formula (I) and process for making them. These compounds have antiinflammatory action. ##STR1## wherein R represents a hydrogen, fluorine atom, a trifluoromethyl, 1-5C lower alkoxy, hydroxy, hydroxyethoxy, aminoethoxy group or the group of the formula --OCH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 OH, Y represents a hydroxy group or the group of the formula ##STR2## (R.sub.3 and R.sub.4 represent a 1-4C lower alkyl group or R.sub.3 and R.sub.4 may jointly form a heterocyclic group together with an adjacent nitrogen atom.
    Type: Grant
    Filed: May 25, 1976
    Date of Patent: July 18, 1978
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shigeru Yamabe, Yasuo Fujimoto, Shoji Ryu, Yoshio Suzuki, Yoshihiro Tanaka, Toru Yamanaka, Kiyosato Nyu