Tetracyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/457)
  • Patent number: 5422365
    Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1, R'.sub.1 and R.sub.2 are each selected, independently of the others, from hydrogen and an alkyl radical, the two R.sub.2 groups being in the cis position in relation to the rings,and R, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R'a and R'b are as defined in the description,useful therapeutically in the regulation of the secretion of insulin.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: June 6, 1995
    Assignee: Adir et Compagnie
    Inventors: David Billington, Francoise Perron-Sierra, Isabelle Picard, Jacques Duhault, Joseph Espinal
  • Patent number: 5411679
    Abstract: Described are novel reversible photochromic benzopyran compounds, examples of which are compounds substituted at the 2 position of the pyran ring and have fused at the benzo portion of the benzopyran a substituted or unsubstituted heterocyclic ring such as a benzothieno or benzofurano group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel benzopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: September 13, 1994
    Date of Patent: May 2, 1995
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 5338758
    Abstract: Four bicyclic terpenes isolated from a culture broth of Phoma sp SCF0592, ATCC 74077, pharmaceutical compositions containing them and their use as PAF antagonists to treat allergic and inflammatory diseases are disclosed.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: August 16, 1994
    Assignee: Schering Corporation
    Inventors: Min Chu, Mahesh Patel, Ann C. Horan, Vincent P. Gullo
  • Patent number: 5084579
    Abstract: A benzofuran compound of the formula ##STR1## wherein A represents ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, B and D have various meanings. The benzofuran compound is usefully employed in pharmaceutical and cosmetic compositions.
    Type: Grant
    Filed: March 14, 1991
    Date of Patent: January 28, 1992
    Assignee: L'Oreal
    Inventors: Gerard Lang, Serge Forestier, Alain Lagrange, Jean Maignan, Gerard Malle
  • Patent number: 5075331
    Abstract: A benzofuran compound of the formula ##STR1## wherein A represents ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, B and D have various meanings. The benzofuran compound is usefully employed in pharmaceutical and cosmetic compositions.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: December 24, 1991
    Assignee: L'Oreal
    Inventors: Gerard Lang, Serge Forestier, Alain Lagrange, Jean Maignan, Gerard Malle
  • Patent number: 5026759
    Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: June 25, 1991
    Assignee: Du Pont Merck Pharmaceutical
    Inventor: Douglas G. Batt
  • Patent number: 4978679
    Abstract: Positions 7- and/or 6-substituted 1,2,3,4,4a,9b-Hexahydro-8-hydroxydibenzofuran-3-ols and analogs of that general structure are described.These compounds are found to be potent inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful in the treatment of a variety of inflammatory conditions.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: December 18, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Kathleen M. Rupprecht, Joshua S. Boger
  • Patent number: 4935532
    Abstract: All possible isomeric forms of a compound of the formula ##STR1## wherein A has a structure selected from the group consisting of ##STR2## wherein Y.sub.1 and Y.sub.2 are individually selected from the group consisting of hydrogen, fluorine, chlorine, bromine and alkyl of 1 to 6 carbon atoms, or Y.sub.1 and Y.sub.2 together with the carbon to which they are attached form a carbon homocycle of 3 to 7 carbon atoms and Z is selected from the group consisting of hydrogen, chlorine, bromine and iodine, Y is selected from the group consisting of hydrogen, alkyl of 1 to 18 carbon atoms unsubstituted or substituted with at least one halogen, the .beta., .alpha. bond together with Y can be part of A and and R is selected from the group consisting of non-heterocyclic primary, secondary or teritiary alcohol moiety having at least one asymetric carbon or the remainder of a substituted alcohol with a chirality due to the dissymetric spatial configuration of the entire molecule.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: June 19, 1990
    Assignee: Roussel Uclaf
    Inventors: Jean Tessler, Jean-Pierre Demoute
  • Patent number: 4918101
    Abstract: The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is O or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: April 17, 1990
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4857516
    Abstract: A compound of the formula ##STR1## wherein R is a lower alkyl group, R.sup.0 is hydrogen or an acyl group, R.sup.1 and R.sup.2 are lower alkyl groups which may optionally be substituted or wherein R.sup.1 and R.sup.2 are combined to form a butadienylene group which may optionally be substituted, R.sup.3 and R.sup.4 are hydrogen or alkyl groups which may optionally be substituted or wherein R.sup.3 and R.sup.4 are combined to form a polymethylene group, and R.sup.5 is a lower alkyl, aromatic or heterocyclic group which may optionally be substituted or a pharmaceutically acceptable salt thereof, exerts cardiovascular system improving action and antiallergic action and can be used as pharmaceutics, e.g. antithromotics, antiallergic agents etc.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: August 15, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shinji Terao, Yoshitaka Maki
  • Patent number: 4801607
    Abstract: This invention relates to antitumor and antiviral furanoditerpenoid compositions, a process of producing the compositions and a method for inhibiting tumors and viruses utilizing the compositions. More particularly, the new compositions are antitumor and antiviral furanoterpenoids which are derived from marine organisms, i.e., the marine sponge Spongia sp.
    Type: Grant
    Filed: March 25, 1987
    Date of Patent: January 31, 1989
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Shigeo Komoto, Oliver J. McConnell, Sue S. Cross
  • Patent number: 4788305
    Abstract: Compounds of the formula ##STR1## wherein A is a hydrocarbon chain containing 1 to 16 groups, the said chain containing at least one heteroatom, at least one unsaturation, the assembly of the group constituting the chain may be a mono- or polycyclic system including a spiro or endosystem and the assembly of chain A and the carbon atoms attached thereto can contain at least one chiral atom or the hemiacetal moiety thereto which can present a chirality due to the dissymetric spatial configuration of the molecule and Y is selected from the group consisting of hydrogen, alkyl of 1 to 18 carbon atoms optionally substituted, --CY.sub.3 ' and the .beta.,.gamma. bond together with Y can be part of A and Y' is bromine or chlorine.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: November 29, 1988
    Assignee: Roussel Uclaf
    Inventors: Jean Tessier, Jean-Pierre Demoute
  • Patent number: 4775663
    Abstract: A benzofuran derivative which is a compound of formula (I): ##STR1## wherein a to d each are 0 to 1, with a+b+c+d.gtoreq.2; R.sub.1 to R.sub.6 are each H or C.sub.1 -C.sub.6 alkyl; R.sub.7 is --CH.sub.2 OR.sub.8 (R.sub.8 =H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl), --COR.sub.9 (R.sub.9 =H, C.sub.1 -C.sub.6 alkyl, ##STR2## which is an amino acid or amino sugar residue or where R' and R" are H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl, C.sub.3 -C.sub.6 alkenyl or form a heterocycle) or OR.sub.10 (where R.sub.10 is H, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl or --OR.sub.10 is derived from a sugar) has retinoid type action and can be used in cosmetics (body and hair hygiene) and in medicine (treatment of dermatological conditions; atopy; degenerative diseases of connective tissue; or corneopathies).
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: October 4, 1988
    Assignee: L'Oreal
    Inventors: Serge Forestier, Alain Lagrange, Gerard Lang, Braham Shroot
  • Patent number: 4683083
    Abstract: The invention concerns1. Mixtures of tricyclo[5.2.1.0.sup.2,6 ]decane derivatives, having principal isomers corresponding to the general formula A, whereinR.sup.1 and R.sup.2 are hydrogen atoms or are a methyl group or a hydrogen atom, one of the substituents being a methyl group and the other a hydrogen atom,R.sup.3 and R.sup.4 are hydrogen atoms or are a methyl group or a hydrogen atom, one of the substituents being a methyl group and the other a hydrogen atom,Y is a tetrahydrofurane system at C-4/C-5 or a substituted oxymethyl group at C-5 and a hydrogen atom at C-4,R.sup.5 is a hydrogen atom or a C.sub.1 -C.sub.6 -acyl-, C.sub.1 -C.sub.6 -alkyl-, C.sub.1 -C.sub.6 -alkenyl-, C.sub.1 -C.sub.4 -alkoxymethyl-, C.sub.1 -C.sub.2 alkoxycarbonyl-, formylmethyl-, or di-C.sub.1 -C.sub.4 -alkoxyethyl-group, andthe broken lines indicate a C--C-single bond and a C--C-double bond or alternatively two C--C-single bonds. ##STR1## 2.
    Type: Grant
    Filed: January 10, 1985
    Date of Patent: July 28, 1987
    Assignee: Dragoco Gerberding and Co. GmbH
    Inventors: Ernst-Joachim Brunke, Hartmut Struwe
  • Patent number: 4585760
    Abstract: Dimethyfurano analogs of daunomycin are described, including (.+-.)-8.alpha.-acetyl-6,7,8,9-tetrahydro-5,6.beta.,8.beta.,10-tetrahydrox y-1,3-dimethyl-anthra[2,3-c]-furan-4,11-dione-6-(3-amino-2,3-6-trideoxy-.al pha.-L-lyxo-hexopyranoside), which are useful in the treatment of cancer in mammals, such as melanoma, squamous cell, myeloma and pranceatic.
    Type: Grant
    Filed: July 16, 1981
    Date of Patent: April 29, 1986
    Assignee: American Cyanamid Company
    Inventor: Ving J. Lee
  • Patent number: 4470990
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 each is hydrogen or lower alkyl or R.sup.1 and R.sup.2 together form an alkylene of the formula (CH.sub.2).sub.n wherein n is an integer from 4 to 6, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: September 11, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4333877
    Abstract: Dyestuffs having the general formula: ##STR1## wherein Z.sup.1 and Z.sup.2 each independently represent oxygen or ##STR2## in which Y is hydrogen, an optionally substituted hydrocarbon radical or an acyl radical,R.sup.1 and R.sup.2 each independently represent a substituted or unsubstituted aryl radical, preferably phenyl, andX.sup.1 and X.sup.2 each independently represent hydrogen, halogen, cyano, alkyl, alkoxy, nitro, amino, substituted amino, carboxylic acid, carboxylic acid ester, optionally substituted carbamoyl, alkylthio, arylthio, alkylsulphonyl, arylsulphonyl, acyl, acyloxy, hydroxy, sulphonic acid or sulphonic acid ester, orX.sup.1 and X.sup.2 together form a 5- or 6-membered, carbocyclic or heterocyclic, saturated or unsaturated, including aromatic, ring which may carry further substituents; processes for the manufacture of these dyestuffs and their use for coloring aromatic polyester textile materials.
    Type: Grant
    Filed: July 10, 1980
    Date of Patent: June 8, 1982
    Assignee: Imperial Chemical Industries Limited
    Inventors: John L. Carey, Colin W. Greenhalgh