Abstract: A method of preparing a thiophene comprises reacting an organic compound containing a chain of at least 4 C atoms linked by single or double bonds with a source of sulphur in the vapour phase, in the presence of a jarosite-type catalyst, having the compositionM(Fe.sub.0.8-1 Cr.sub.0.2-0)(OH).sub.6 X.sub.nwherein M is NH.sub.4 or an alkali metal; and X.sub.n represents one or more suitable anions.
Type:
Grant
Filed:
June 24, 1996
Date of Patent:
March 3, 1998
Assignee:
Shell Research Limited
Inventors:
Graham John Hutchings, Richard William Joyner, Barry William Luke Southward, Russel Andrew Stewart, Lance Svend Fuller
Abstract: There is provided an insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a tetrahydroquinazoline compound of the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as defined herein, and methods of using the same. Certain novel substituted-phenyl tetrahydroquinazoline compounds per se are also identified.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
January 27, 1998
Assignee:
FMC Corporation
Inventors:
Thomas G. Cullen, Robert N. Henrie, II, Clinton J. Peake, Brian D. Bennett
Abstract: This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or bicyclic aryl or heteroaryl quinazoline compounds in inhibiting cell proliferation, including compounds which are useful protein tyrosine kinase (PTK) inhibitors. The method of treating cell proliferation using said quinazoline compounds and their use in pharmaceutical compositions is described.
Type:
Grant
Filed:
April 19, 1994
Date of Patent:
January 20, 1998
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Michael R. Myers, Alfred P. Spada, Martin P. Maguire, Paul E. Persons
Abstract: A pharmaceutical composition, useful for treating animals of the mammalian species, including humans, to treat diseases and conditions which normally respond to treatment with alpha.sub.2 adrenergic agents, contains as its active alpha.sub.2 adrenergic agent ingredient one or more compounds of the formula ##STR1## where X is O, S or NH; n is an integer with the values of 0, 1 or 2; when n is 0 then R.sub.1 is lower alkyl having 1 to 6 carbon atoms and R.sub.2 is H or lower alkyl having 1 to 6 carbon atoms; when n is 1 or 2, then R.sub.1 and R.sub.2 both are methylene (CH.sub.2), or methylene substituted with an R.sub.5 group where R.sub.5 is lower alkyl of 1 to 6 carbons; R.sub.3 and R.sub.4 independently are H or lower alkyl having 1 to 6 carbons; R.sub.6 is H or lower alkyl of 1 to 6 carbons.
Type:
Grant
Filed:
October 29, 1996
Date of Patent:
January 13, 1998
Assignee:
Allergan
Inventors:
Michael E. Garst, James E. Burke, Larry A. Wheeler
Abstract: The invention relates to thiophene compounds of formula: ##STR1## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents hydrogen or halogen, (C.sub.1 -C.sub.5)-alkyl oralkoxy, or trifluoromethyl,R.sub.1 represents hydrogen or (C.sub.1 -C.sub.5)-alkyl,A represents a straight (C.sub.1 -C.sub.5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C.sub.1 -C.sub.5)-alkyl, andR.sub.2 represents hydrogen, (C.sub.1 -C.sub.6)-alkyl, cyclohexyl or benzyl;and their physiologically tolerable salts.The products of the invention may be used as anti-inflammatory agents.
Type:
Grant
Filed:
February 22, 1996
Date of Patent:
January 6, 1998
Assignee:
Adir et Compagnie
Inventors:
Michel Wierzbicki, Frederic Sauveur, Jacqueline Bonnet, Charles Tordjman
Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of benzo?b!thiophenes. Such compounds are characterized by the following structure: ##STR1## In this compound, R.sub.1 is selected from the group consisting of --OR.sub.7, --NR.sub.8 R.sub.9, --NHNR.sub.10 R.sub.11, --NHNHC(X.sub.2)NHR.sub.12, --NHSO.sub.2 NR.sub.8 R.sub.9, --NHNHC(O)R.sub.12, --NHNHSO.sub.2 R.sub.12 and --NHC(O)NR.sub.8 R.sub.9. R.sub.7 -R.sub.12 are selected independently from the group consisting of hydrogen, alkyl, aryl, aralkyl, heteroaryl and heteroaralkyl. X.sub.1 and X.sub.2 are selected independently from the group consisting of oxygen and sulfur. R.sub.2 is hydrogen or halogen. R.sub.3 -R.sub.6 are selected independently from the group consisting of hydrogen, halogen, hydroxyl, --NR.sub.8 R.sub.9, nitro, cyano, alkoxyl, lower alkyl, aryl and aryloxyl.
Type:
Grant
Filed:
April 18, 1995
Date of Patent:
December 30, 1997
Assignee:
Geron Corporation
Inventors:
Federico C. A. Gaeta, Adam Antoni Galan, Elaine C. Stracker
Abstract: Antiviral agents comprising, as an active ingredient, a 1,4-dihydro-2,3-benzodithiin derivative of the formula ##STR1## wherein each symbol is as defined in the Specification, or a pharmacologically acceptable salt thereof. The antiviral agents of the present invention have superior antiviral activity and are effective for the preventive and therapeutic treatment of viral diseases caused typically by RS virus.
Abstract: Compounds of the formula ##STR1## wherein X is O or S, useful for the inhibition of the replication of HIV-1 and reverse transcriptase mutants thereof, in vitro and in vivo.
Type:
Grant
Filed:
November 30, 1995
Date of Patent:
December 9, 1997
Assignees:
Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./Ltee
Inventors:
Walter Gerhard Brouwer, Ewa Maria Osika, Benjamin James Pierce
Abstract: An unsaturated phosphonic ester is produced by reaction of an acetylene compound with a secondary phosphite in the presence of a palladium complex catalyst.
Type:
Grant
Filed:
August 19, 1996
Date of Patent:
December 2, 1997
Assignee:
Director-General Of Agency Of Industrial Science And Technology
Abstract: A composition is described which is useful for treating neurological and mental disorders which are associated with and/or related pathogenetically to deficient serotonin neurotransmission and impaired pineal melatonin functions in humans the composition being administered in combination with a sufficient amount of an AC pulsed magnetic field alone or in combination with a sufficient amount of a DC magnetic field to the brain of a human in need of such treatment which composition comprises an effective amount of a composition which increases serotonin transmission to the human to be treated.
Abstract: A method of retarding the aging process and improving the symptoms of age-related disease conditions in humans which result from diminished pineal melatonin functions and reduced serotonin neurotransmission is described which comprises administering to a human in need thereof an effective amount of a composition which increases serotonin transmission to said human followed by the application to the brain of the human an effective amount of an AC pulsed magnetic field of proper intensity, frequency and waveform. Preferably the composition is supplemented by an effective amount of a dietary composition rich in the amino-acid tryptophan. Optionally an effective amount of an agent which provides growth hormone release is also administered prior to the application of the AC pulsed magnetic field.
Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.
Type:
Grant
Filed:
February 22, 1996
Date of Patent:
November 18, 1997
Assignee:
Allergan
Inventors:
David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
Abstract: A key step in the synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno?2,3-b!thiopyran-2-su lfonamide 7,7-dioxide (dorzolamide) and related compounds is a Ritter reaction with an unexpected tendency to proceed with retention of chirality.
Type:
Grant
Filed:
January 6, 1995
Date of Patent:
November 18, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Thomas J. Blacklock, David J. Mathre, Paul Sohar
Abstract: The invention relates to novel herbicidal and plant growth-regulating compounds of the formula (I) or salts thereof, ##STR1## where Q, W, R, R, R, R, Y and Z are defined as in formula (I) as claimed in claim 1.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 18, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Oswald Ort, Klaus Bauer, Hermann Bieringer
Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 11, 1997
Assignee:
Cambridge NeuroScience, Inc.
Inventors:
Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
Abstract: Compounds of the formula I ##STR1## in which R is a C.sub.1 - to C.sub.22 -alkyl radical,A.sup.1 and A.sup.2 are hydrogen or methyl or,A.sup.1 is hydrogen and A.sup.2 is the nitro group, andB is the cyano group, the nitro group or an electron-attracting organic group having a double bond which is in conjugation with the thieno?3,2-b!thiophene ring system,have a high dipole moment and a high polarizability and are suitable for purposes of nonlinear optics. If R in the formula I is a C.sub.12 - to C.sub.22 -alkyl radical, monomolecular layers can be applied to a substrate by the Langmuir-Blodgett method. The resulting layer elements are suitable, inter alia, as waveguides.
Type:
Grant
Filed:
April 14, 1995
Date of Patent:
November 4, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Ivan Cabrera, Uwe Falk, Werner Hickel, Donald Lupo, Ude Scheunemann, Peter Boldt, Martin Blenkle
Abstract: The invention relates to 7-?5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)!heptanoic or heptenoic acids and derivatives of said adds, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
Abstract: The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-4 alkyl group;R.sup.5 is an aromatic group, a C.sub.1-10 alkyl group or a C.sub.1-4 alkyl groups optionally substituted with an aromatic group; andn is 1 or 2.
Type:
Grant
Filed:
June 6, 1996
Date of Patent:
October 21, 1997
Assignee:
LG Chemical Limited
Inventors:
Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
October 14, 1997
Assignee:
Cambridge NeuroScience, Inc.
Inventors:
Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
Type:
Grant
Filed:
November 22, 1994
Date of Patent:
September 30, 1997
Assignee:
Cambridge NeuroScience, Inc.
Inventors:
Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin