Sulfur Containing Hetero Ring (e.g., Thioxane, Etc.) Patents (Class 544/145)
  • Patent number: 5843965
    Abstract: The instant invention provides novel benzo?b!thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: December 1, 1998
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5795981
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: August 18, 1998
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5792763
    Abstract: This invention provides novel 5-HT.sub.1F agonists of formula ##STR1## where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: August 11, 1998
    Assignee: Eli Lilly and Company
    Inventors: James E. Fritz, Stephen W. Kaldor, Sidney Xi Liang, Upinder Singh, Yao-Chang Xu
  • Patent number: 5726186
    Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: March 10, 1998
    Assignee: Eli Lilly and Company
    Inventor: Timothy Alan Grese
  • Patent number: 5723072
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: March 3, 1998
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5719147
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5709867
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: January 20, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5698141
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 16, 1997
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5656750
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: Polaroid Corporation
    Inventors: Richard M. Allen, Peter K. Chu
  • Patent number: 5656656
    Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: August 12, 1997
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
  • Patent number: 5651923
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. 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 naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5650098
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. 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 naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: July 22, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5597823
    Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an .alpha.-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 28, 1997
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, Steven W. Elmore, James F. Kerwin, Jr., Suzanne A. Lebold, Edmund L. Lee, Kevin B. Sippy, Karin R. Tietje, Michael D. Wendt
  • Patent number: 5530141
    Abstract: 2,4-Diaryl-1,3-dithiolanes; 2,4-diaryl-1,3-dioxolanes; 2,4-diaryl-1,3-oxathiolanes; and 2,5-diaryl-1,3-oxathiolanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: September 14, 1992
    Date of Patent: June 25, 1996
    Assignee: Center for Innovative Technology
    Inventors: T. Y. Shen, David M. Goldstein
  • Patent number: 5502053
    Abstract: Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: March 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Bruce D. Dorsey, Joel R. Huff, Susan F. Britcher
  • Patent number: 5489603
    Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: February 6, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
  • Patent number: 5420132
    Abstract: A compound of formula (I): ##STR1## wherein: X represents O, S or H.sub.2,R and R' each represents hydrogen or together form a bond,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.useful in the treatment or prevention of disorders involving oxidative processes.
    Type: Grant
    Filed: May 6, 1994
    Date of Patent: May 30, 1995
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Valerie Thiery, Gerard Adam, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard
  • Patent number: 5405976
    Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: April 11, 1995
    Assignee: Polaroid Corporation
    Inventors: Stephen J. Telfer, Robert P. Short, Stephen G. Stroud, Anthony J. Puttick, Socorro Ramos, Michael J. Zuraw
  • Patent number: 5399487
    Abstract: The present invention encompasses compounds of formula I: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof; wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, or phenylalkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, or phenylalkyl; orNR.sub.1 R.sub.2 forms a nitrogen heterocycle; andR.sub.3 is hydrogen, an amino acid or a peptide residue.These compounds may be employed as substrates in assays for determining proteolytic enzyme activity or as enzyme inhibitors. The invention also encompasses methods for determining proteolytic enzyme activity using the compounds of formula I.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: March 21, 1995
    Assignee: Haematologic Technologies, Inc.
    Inventors: Saulius Butenas, Jeffrey H. Lawson, Kenneth G. Mann
  • Patent number: 5397791
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: March 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
  • Patent number: 5385930
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: January 31, 1995
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5376677
    Abstract: The invention relates to novel compounds of the formula ##STR1## in which R is as defined in the description, to their preparation, to fungicidal compositions which contain such compounds as active substances, and to the use of the active substances or compositions for controlling fungi in agriculture and horticulture.
    Type: Grant
    Filed: March 22, 1993
    Date of Patent: December 27, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephan Trah
  • Patent number: 5354873
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: October 11, 1994
    Assignee: Polaroid Corporation
    Inventors: Richard M. Allen, Peter K. Chu, John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5338735
    Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5336676
    Abstract: Compounds of formula (I) ##STR1## wherein R is an alkyl group; R.sub.1 is a cyano, carboxy, alkoxycarbonyl or hydroxylaminocarbonyl group; R.sub.2 is substituted or unsubstituted phenyl (C.sub.3 -C.sub.7)-cycloalkyl, .alpha.-, .beta.- or .gamma.-pyridyl or a benzoheteroxcyclic ring; R.sub.3 is carboxy or carboalkoxy; Y is a group of the formula --COOX; --NHCOA; --NCO; --COA; --CONHOR.sub.e ; --OCOA; A; --COCH.sub.2 COR.sub.f ; --NHCSA; --OCSA; (a); X is hydrogen, alkyl or succinimidyl group; A is a cyclic or acyclic amino group; and n is 1 or 2; having pharmacological characteristics which render them useful in the treatment of inflammatory conditions of the respiratory tract and asthmatic conditions.
    Type: Grant
    Filed: December 4, 1992
    Date of Patent: August 9, 1994
    Assignee: Boehringer Mannheim Italia S.p.A.
    Inventors: Carmelo A. Gandolfi, Giampiero De Cillis, Giorgio Long, Licia Gallico
  • Patent number: 5332741
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, andmedicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: July 26, 1994
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5326759
    Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5310909
    Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: May 10, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer, Walter Fischer, Jurgen Finter, Kurt Meier, Martin Roth
  • Patent number: 5280032
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: September 8, 1992
    Date of Patent: January 18, 1994
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5278174
    Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 11, 1994
    Assignee: Scios Nova, Inc.
    Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
  • Patent number: 5256657
    Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.
    Type: Grant
    Filed: August 19, 1991
    Date of Patent: October 26, 1993
    Assignee: Sterling Winthrop, Inc.
    Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
  • Patent number: 5244893
    Abstract: New compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.6 have the meanings given in the description, their preparation and use in plant protection, the protection of materials and in the field of human and veterinary medicine.Formula (I) gives a definition of the compounds which can be prepared by analogous processes, for example from suitable benzothiophene derivatives by oxidation.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: September 14, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Georg-Wilhelm Ludwig, Manfred Plempel
  • Patent number: 5227499
    Abstract: Squarylium compounds of the formula: ##STR1## in which: Q.sup.1 and Q.sup.2 are each a Chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens;R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group; andR.sup.3, R.sup.4 and R.sup.5 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or an electron-withdrawing group able to lower the electron density at the carbon atom to which it is attached, subject to the provisoes that:two of R.sup.3, R.sup.4 and R.sup.5 may form a divalent group of which a single atom is double bonded to the carbon atom to which the two groups are attached, or all three of R.sup.3, R.sup.4 and R.sup.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: July 13, 1993
    Assignee: Polaroid Corporation
    Inventors: Donald A. McGowan, Mark R. Mischke, Stephen J. Telfer
  • Patent number: 5227498
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a cycloaliphatic or aromatic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: July 13, 1993
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5216002
    Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: June 1, 1993
    Assignee: Eli Lilly and Company
    Inventors: Jaswant S. Gidda, Jill A. Panetta, Michael L. Phillips
  • Patent number: 5216020
    Abstract: Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Kenneth L. Shepard, Ronald J. Hudcosky, Theresa M. Williams
  • Patent number: 5198426
    Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma and diseases caused by retroviruses. Processes for preparing the peptides novel intermediates in the processes, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: March 30, 1993
    Assignee: Warner-Lambert Company
    Inventors: James M. Hamby, John C. Hodges, Sylvester Klutchko
  • Patent number: 5194608
    Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: March 16, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
  • Patent number: 5179092
    Abstract: A compound having the formula (I): ##STR1## wherein A is --CH.sub.2 --, --O--, or --S--; R.sup.1 is CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydroxy or carboxy which may be optionally esterized or amidated; R.sup.3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: January 12, 1993
    Assignee: Suntory Limited
    Inventors: Toshio Tatsuoka, Kenji Suzuki, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
  • Patent number: 5164387
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R .sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11)=C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: November 17, 1992
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5158950
    Abstract: 2-(1,3-Dithiol-2-ylidene)-2-[N-(substituted) carbamoly] acetate esters and salts thereof, having potent therapeutic or prophylactic effect for hepatic disorder, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: October 27, 1992
    Assignee: Yuhan Corporation, Ltd.
    Inventors: Choong S. Kim, Jeong S. Chae, Young R. Choi, Jong W. Lee, Joung K. Yoo
  • Patent number: 5128348
    Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Gregory S. Basarab
  • Patent number: 5104985
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: April 14, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5091526
    Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: February 25, 1992
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, John W. Clader
  • Patent number: 5071841
    Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
  • Patent number: 5047069
    Abstract: An antioxidant for liquid hydrocarbons such as fuels has the structure ##STR1## wherein X is N or S; R is H or a C.sub.1 to C.sub.5 alkyl moiety; R.sup.1 and R.sup.2 are each independently C.sub.5 to C.sub.18 alkyl or cycloalkyl moieties (which may optionally contain a hetero atom such as oxygen), only one of R.sup.1 and R.sup.2 being present if X is S, or may be combined to form a 5 or preferably 6 membered ring; each R.sup.6 is independently the residue of a C.sub.1 to C.sub.5 aldehyde; and R.sup.7 is the residue of a polyamine of the formula ##STR2## wherein R.sup.3 is a C.sub.8 to C.sub.50 alkyl moiety (which may optionally contain one or more ether linkages); R.sup.4 and R.sup.5 are each independently C.sub.2 to C.sub.6 alkylene moieties; a is 0 or 1; and m is at least 3.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: September 10, 1991
    Assignee: Petrolite Corporation
    Inventors: Jerry J. Weers, Thomas V. Bagwell
  • Patent number: 5047406
    Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: September 10, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise