Three Or More Hetero Atoms In The Tetracyclo Ring System Patents (Class 514/287)
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5179100
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which compounds are useful as analgesic agents.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: January 12, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals inc.
    Inventors: Gregory M. Shutske, John D. Tomer, IV
  • Patent number: 5126352
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treatment allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: June 30, 1992
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
  • Patent number: 5095020
    Abstract: The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds.The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms;R.sub.3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group;R.sub.4 is a group of the formula --C(R.sub.11).sub.2 --X--R.sub.12, wherein the groups R.sub.11 are hydrogen, or both groups R.sub.11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR.sub.14, wherein R.sub.14 is hydrogen or alkyl having 1-4 C-atoms, and R.sub.12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group;R.sub.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: March 10, 1992
    Assignee: Duphar International Research B.V.
    Inventors: Antonius Hulkenberg, Ineke Van Wijngaarden
  • Patent number: 5087621
    Abstract: The present invention relates to substituted azetidinylisothiazolopyridone derivatives which correspond to the general formula I: ##STR1## or its tautomeric formula ##STR2## It also relates to a process for preparing them and to their application as a medicinal product.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: February 11, 1992
    Assignee: Laboratorios del Dr. Esteve
    Inventors: Augusto C. Pinol, Jordi F. Constansa, Juan P. Corominas
  • Patent number: 5071848
    Abstract: Isothiazolo-quinoline derivatives are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: December 10, 1991
    Assignee: Abbott Laboratories
    Inventors: Daniel Tim-Wo Chu, Jacob J. Plattner, Linus L. Shen, Larry L. Klein
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5070086
    Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: December 3, 1991
    Assignee: Schering Corporation
    Inventor: Richard Friary
  • Patent number: 5063234
    Abstract: A method of inhibiting bone demineralization comprising administration of an effective amount of a compound having the formula ##STR1## where X is CH or N;Y is O or S;R.sup.1 is 2-propenyl, C.sub.1 -C.sub.3 alkyl, benzyl or substituted benzyl where the substitutents are one or two of the same or different and are selected from methyl, ethyl, methoxy, ethoxy, hydroxy, chloro, bromo, or fluoro;R.sup.2 is C.sub.2 -C.sub.3 alkyl, allyl or cyclopropylmethyl;R.sup.3 and R.sup.4 are both hydrogen or combine to form a carbon-carbon bond; and pharmaceutically acceptable acid addition salts thereof to a mammal requiring bone demineralization inhibition.
    Type: Grant
    Filed: April 11, 1991
    Date of Patent: November 5, 1991
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, James A. Clemens
  • Patent number: 5011845
    Abstract: Compounds of the formula ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group--(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar wherein Z represents O, S or --CH.sub.2 --and Ar is phenyl, optionally substituted by one or two groups selected from the group consisting of hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2, CF.sub.3, CN, R.sup.6 -S(O).sub.x, R.sup.7 --CO--,(R.sup.8 R.sup.9)NCO-and phenyl, wherein x is 0, 1 or 2, and each R.sup.6, R.sup.7, R.sup.8 and R.sup.9 is independently C.sub.1 to C.sub.6 alkyl or two adjacent groups on Ar may form together an additional fused benzenoid ring; n and m independently represent integers of from 1 to 8; and ring Q represents one of the rings Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 below: ##STR2## X is N or C--R.sup.1 ; Y is N or C--R.sup.4 ;W represents O or S;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: April 30, 1991
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Ho-Jane Shue, Ashit K. Ganguly
  • Patent number: 4997831
    Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.
    Type: Grant
    Filed: August 31, 1989
    Date of Patent: March 5, 1991
    Assignee: Glaxo Group Limited
    Inventors: David E. Bays, Ian H. Coates, Alexander W. Oxford, Peter C. North
  • Patent number: 4988705
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: February 7, 1989
    Date of Patent: January 29, 1991
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
  • Patent number: 4985430
    Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: January 15, 1991
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Shuji Morita, Ken-Ichi Saito, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta, Mamoru Sugano
  • Patent number: 4985436
    Abstract: A new antineoplastic substance denominated "pancratistatin". Methods of isolating natural and synthetic pancratistatin and 7-deoxynarciclasine and the pharmaceutically acceptable derivatives thereof to make a pharmaceutical preparation therefrom and methods for treating a host afflicted with a neoplasm with said preparations.
    Type: Grant
    Filed: February 17, 1984
    Date of Patent: January 15, 1991
    Assignee: Arizona Board of Regents
    Inventor: George R. Pettit
  • Patent number: 4960784
    Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.
    Type: Grant
    Filed: October 2, 1989
    Date of Patent: October 2, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: George P. Lahm
  • Patent number: 4920117
    Abstract: There are disclosed compounds having the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andR when present is hydrogen, loweralkyl, allyl, arylloweralkyl, ##STR2## wherein R.sub.1 is loweralkyl, --CH.sub.2 C.tbd.CH, ##STR3## n being 2, 3 or 4 and R.sub.2 and R.sub.3 being independently loweralkyl, or the group ##STR4## taken as a whole constituting ##STR5## which compounds are useful as analgesic agents and also for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: April 24, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4880818
    Abstract: There are disclosed compounds of the formula ##STR1## where X,Y are each independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 ' is hydrogen or loweralkyl and R.sub.4 is hydrogen, loweralkyl or aryl, which are useful as hypotensive agents and as intermediates.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: November 14, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Karl Schonafinger, Helen Hu Ong
  • Patent number: 4868191
    Abstract: Novel alkaloid compounds that are derivatives of methaniminoetheno[d,e]acridine are derived from marine sponges of the genus Dercitus. These compounds and pharmaceutical compositions containing therapeutic effective amounts thereof are useful as antitumor and immunomodulatory medications.
    Type: Grant
    Filed: March 3, 1988
    Date of Patent: September 19, 1989
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Shigeo Komoto, Y. A. Gunawardana
  • Patent number: 4866071
    Abstract: A new antineoplastic substance denominated "pancratistatin". Methods of isolating natural and synthetic pancratistatin and 7-deoxynarciclasine and the pharmaceutically acceptable derivatives thereof to make a pharmaceutical preparation therefrom and methods for treating a host afflicted with a neoplasm with said preparations.
    Type: Grant
    Filed: January 6, 1987
    Date of Patent: September 12, 1989
    Assignee: Arizona Board of Regents
    Inventor: George R. Pettit
  • Patent number: 4863930
    Abstract: 5H-pyrido[2',1':2,3]imidazo[4,5-b]indoles of the formulae ##STR1## their pharmaceutically acceptable acid addition salts and the corresponding compounds bearing one or more halogens and/or lower-alkyl groups on the available ring carbon atoms are administered in cholinomimetic amounts to mammals with low acetylcholine or cholinergic activity to ameliorate the symptoms associated with that condition.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: September 5, 1989
    Inventor: Parimal K. Adhikary
  • Patent number: 4826854
    Abstract: Certain 8 to 12 membered cycloalka-[b]-pyrazolo[3,4,-d]-pyridin-3- one compounds which are useful as benzodiazepine receptor modulators are disclosed.
    Type: Grant
    Filed: November 19, 1987
    Date of Patent: May 2, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Naokata Yokoyama
  • Patent number: 4816461
    Abstract: The invention concerns the provision of 7,8,9,10-tetrahydrothieno[3,2-e]pyrido[4,3-b] indoles, useful, inter alia, as antidepressants, and intermediates for the preparation thereof. Also included in the invention are compositions containing said indoles and methods for the use of said indoles and indole compositions as antidepressants.
    Type: Grant
    Filed: June 10, 1987
    Date of Patent: March 28, 1989
    Assignee: Troponwerke GmbH & Co. KG
    Inventors: Peter-Rudolf Seidel, Gunter Schollnhammer
  • Patent number: 4810708
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: March 7, 1989
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
  • Patent number: 4771052
    Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, loweralkylcarbonyl or arylcarbonyl; and R.sub.3 is hydrogen, loweralkyl, arylloweralkyl, ##STR2## loweralkylcarbonyl or arylcarbonyl, n being an interger of 1 to 6 inclusive and Z being hydrogen, loweralkyl, loweralkoxy, hydroxy or halogen; which are useful as hypotensive agents.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: September 13, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Karl Schonafinger, Helen H. Ong
  • Patent number: 4716168
    Abstract: The present invention involves compounds of the class of imidazo[4,5-f]quinolines and methods for enhancing the immune response system of mammals which comprises systemically administering to mammals having a depressed immune function an effective but nontoxic amount of a composition comprising such a compound.
    Type: Grant
    Filed: April 29, 1986
    Date of Patent: December 29, 1987
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Robert J. Alaimo, Jon A. Andersen
  • Patent number: 4621086
    Abstract: Pyrazolo[3,4,5-kl]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
    Type: Grant
    Filed: January 22, 1986
    Date of Patent: November 4, 1986
    Assignee: Warner-Lambert Company
    Inventor: David B. Capps
  • Patent number: 4588730
    Abstract: Pyrazolo[3,4,5-k1]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
    Type: Grant
    Filed: August 22, 1985
    Date of Patent: May 13, 1986
    Assignee: Warner-Lambert Company
    Inventor: David B. Capps
  • Patent number: 4585775
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen, alkyl, trifluoromethyl, halogen, alkoxycarbonyl, alkoxy or alkanoyl, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, methyl, alkoxy or alkoxyethoxy, and R is hydrogen or a group SR.sup.6, in which R.sup.6 is the lone, unpaired electron of the 12-sulfenyl radical, hydrogen, optionally substituted alkyl, alkenyl, alkynyl, alkanoyl, optionally mono- or poly-substituted benzoyl, fuoryl, phenacyl, phenoxyacetyl, phenylacetyl or another conventional thiol-protective group, and to physiologically acceptable salts thereof, and to processes for their preparation, to their use as a gastric acid secretion inhibitor and to pharmaceutical preparations based on these compounds.
    Type: Grant
    Filed: September 13, 1984
    Date of Patent: April 29, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Hitzel, Gerhard Rackur, Martin Bickel
  • Patent number: 4564613
    Abstract: Pyridoindoles of the formula ##STR1## in which R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, which is optionally substituted by the radical ##STR2## R.sub.2 and R.sub.3 represent H or form a bond, or R.sub.1 and R.sub.2 together represent O, --O--CH.sub.2 --CH.sub.2 --O-- or --S--CH.sub.2 --CH.sub.2 --S--,R.sub.4 represents H or the ##STR3## or R.sub.3 and R.sub.4 represent O, orR.sub.1 and R.sub.4 are members of an N-containing six-membered ring andR.sub.8 and R.sub.9 represent H or C.sub.1 -C.sub.4 -alkyl, or optionally form, with the N atom, a heterocyclic 5-membered or 6-membered ring, which can optionally also contain a further hetero-atom from the series comprising N, O or S,R.sub.5 represents H, C.sub.1 -C.sub.4 -alkyl or the group ##STR4## or R.sub.5 and R.sub.3 form a bond, andR.sub.10 and R.sub.11 represent C.sub.1 -C.sub.4 -alkyl or are members of an N-containing 5-membered or 6-membered ring,R.sub.6 represents H or C.sub.1 -C.sub.4 -alkyl andR.sub.
    Type: Grant
    Filed: September 14, 1984
    Date of Patent: January 14, 1986
    Assignee: Troponwerke GmbH & Co.
    Inventors: Karl-Heinz Boltze, Margaret A. Davies, Bodo Junge, Teunis Schuurman, Jorg Traber