The Hetero Ring Has At Least Seven Members Patents (Class 549/9)
  • Patent number: 6387944
    Abstract: The invention relates to substituted benzo(b)thiepine-1,1-dioxide derivatives and to the acid addition salts thereof. The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5 and Z have the cited descriptions, to the physiologically compatible salts, to physiologically functional derivatives, and to a method for the production thereof. The compounds are suited, for example, as hypolipidemic agents.
    Type: Grant
    Filed: December 7, 2000
    Date of Patent: May 14, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Wendelin Frick, Alfons Enhsen, Heiner Glombik, Hubert Heuer
  • Patent number: 6387924
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: May 14, 2002
    Assignee: G.D. Searle & Co.
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Patent number: 6369220
    Abstract: A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.
    Type: Grant
    Filed: October 2, 2000
    Date of Patent: April 9, 2002
    Inventors: Jinglin (James T.) Li, Ching-Cheng Wang, David B. Reitz, Victor Snieckus, Horng-Chih Huang, Andrew J. Carpenter
  • Patent number: 6355672
    Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: March 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Patent number: 6346527
    Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.
    Type: Grant
    Filed: October 24, 2000
    Date of Patent: February 12, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kohei Takenaka, Yoshikazu Inoue, Masatoshi Minagawa, Atsushi Akahane
  • Patent number: 6346521
    Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.
    Type: Grant
    Filed: December 28, 1995
    Date of Patent: February 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 6346652
    Abstract: A composition and method for the catalytic conversion of a racemic mixture of dienes to a cyclic olefin by a ring-closing metathesis (RCM) reaction are disclosed. The composition, a transition metal complex with an M═C reaction site, contains a bidentate dialkoxide of at least 80% optical purity. Because the M═C reaction site is of a sufficient shape specificity, conferred in part by the dialkoxide of sufficient rigidity and a M═N—R1 site, reacting the composition with a mixture of two enantiomeric dienes results in an olefin metathesis product that has at least a 50% enantiomeric excess of one enantiomer in the mixture. A method is also provided for reacting a composition with a racemic diene mixture to generate a metathesis product that has an enantiomeric excess of at least 50%. Methods are also provided for catalytic enantioselective desymmetrization.
    Type: Grant
    Filed: July 13, 1998
    Date of Patent: February 12, 2002
    Assignee: Massachusetts Institute of Technology
    Inventors: Richard R. Schrock, Amir H. Hoveyda
  • Publication number: 20020010085
    Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1
    Type: Application
    Filed: March 6, 2001
    Publication date: January 24, 2002
    Inventor: Peter Herold
  • Patent number: 6265583
    Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: July 24, 2001
    Assignees: G. D. Searle & Co., Monsanto Company
    Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
  • Patent number: 6262277
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: July 17, 2001
    Assignee: G.D. Searle and Company
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Patent number: 6235771
    Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:  wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5 and R6 are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5 and R6 may bind to each other to form a cy
    Type: Grant
    Filed: March 27, 2000
    Date of Patent: May 22, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Masaki Seto, Naoyuki Kanzaki, Osamu Nishimura
  • Patent number: 6221897
    Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: in which R1, R2, R3, R4, R5 and Z have the meanings indicated, and their physiologically tolerable salts and physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as hypolipidemics.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: April 24, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Wendelin Frick, Alfons Enhsen, Heiner Glombik, Hubert Heuer
  • Patent number: 6201133
    Abstract: Disclosed are compound of formula I wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl; R1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl; R2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl); R3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C2-C7-alkyl interrupted by S, SO, SO2, O or N—R5; R4 represents hydrogen or acyl; R5 represents hydrogen, lower alkyl, aryl-lower alkyl, acyl, or (lower alkyl, aryl or aryl-lower alkyl)-sulfonyl; A together with the carbon to which it is attached forms a ring and repr
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: March 13, 2001
    Assignee: Novartis AG
    Inventor: Cynthia A. Fink
  • Patent number: 6166006
    Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: December 26, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
  • Patent number: 6162915
    Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: December 19, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas L. Pearson, Jimmy J. Tai, Timothy J. Adaway
  • Patent number: 6107494
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: August 22, 2000
    Assignee: G.D. Searle and Company
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Patent number: 6043210
    Abstract: The invention is related to novel thiamacrolides, especially musk odorants, having extremely low threshold values, their use in functional perfumery such as fine perfumery, as well as to the preparation of thiamacrolide compounds.
    Type: Grant
    Filed: January 29, 1998
    Date of Patent: March 28, 2000
    Assignee: Givaudan Roure (International) SA
    Inventors: Jerzy A. Bajgrowicz, Georg Frater, Philip Kraft
  • Patent number: 6043361
    Abstract: The invention relates to compounds of the formulae: processes for their preparation, polymers, co-polymers or block co-polymers containing them or their use as monomers or co-monomers in free radical polymerisation and in the manufacture of adhesives, dental composites or optical lenses.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: March 28, 2000
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Richard Alexander Evans, Ezio Rizzardo, Graeme Moad
  • Patent number: 6034118
    Abstract: Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: March 7, 2000
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Steven H. Krawczyk, Lawrence R. McGee, Michael J. Postich, Wenjin Yang
  • Patent number: 6013809
    Abstract: This invention relates to substituted heterocyclic benzocycloalkenes of general formula I or pharmaceutically acceptable salts thereof, to a method of producing them and to their use as analgesics.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: January 11, 2000
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Wolfgang Strassburger, Claudia Puetz, Werner Englberger, Babette-Yvonne Koegel
  • Patent number: 5998613
    Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.
    Type: Grant
    Filed: August 5, 1997
    Date of Patent: December 7, 1999
    Assignee: H. Lundbeck A/S
    Inventors: Erik Falch, Jens Kristian Perregaard, Arne Schousboe, Povl Krogsgaard-Larsen, Bente Frolund, Sibylle Moltzen Lenz
  • Patent number: 5994391
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: November 30, 1999
    Assignee: G.D. Searle and Company
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Patent number: 5981547
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: November 9, 1999
    Assignee: The Procter & Gamble Company
    Inventors: Laurence Ichih Wu, John Michael Janusz
  • Patent number: 5958969
    Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.
    Type: Grant
    Filed: September 3, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
  • Patent number: 5874549
    Abstract: A bicyclic, non-aromatic hydrocarbon compound, optionally having one or more N, O or S atoms in the bicyclic skeleton, and having as substituents an acid group and an amido group, which are vicinal and in a syn-position, wherein the amido group is not anilido and the acid group is carboxyl or carboxyl in a form metabolizable to a free carboxyl group, and wherein said bicyclic skeleton is optionally unsaturated, except in the bond between said groups, acid-cleavably links an amide-containing active agent to a targeting agent, which is linked by a linker arm to the bicyclic skeleton.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: February 23, 1999
    Assignee: NeoRx Corporation
    Inventor: Stephen Hadley
  • Patent number: 5849784
    Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
    Type: Grant
    Filed: November 2, 1995
    Date of Patent: December 15, 1998
    Assignees: GD Searle & Co., Monsanto Co.
    Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
  • Patent number: 5811450
    Abstract: Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: September 22, 1998
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Choung U. Kim, Steven H. Krawczyk, Lawrence R. McGee, Michael J. Postich, Wenjin Yang
  • Patent number: 5770180
    Abstract: Disclosed are bridge-substituted analogs of tropanes and benztropines as well as methods for: imaging of cocaine receptors; treatment of cocaine abuse; and imaging and treatment of Parkinson's disease.
    Type: Grant
    Filed: April 26, 1996
    Date of Patent: June 23, 1998
    Assignees: Organix, Inc., President and Fellows of Harvard College
    Inventors: Bertha K. Madras, Peter Meltzer
  • Patent number: 5733924
    Abstract: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, ?wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: March 31, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yutaka Kanda, Yutaka Saitoh, Hiromitsu Saito, Tadashi Ashizawa, Kazuyo Sugiyama, Katsushige Gomi, Shingo Kakita, Yuichi Takahashi, Chikara Murakata
  • Patent number: 5705524
    Abstract: Tri- and tetra substituted thiepane and compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: Gilead Sciences, Inc.
    Inventors: Lawrence R. McGee, Choung U. Kim, Norbert W. Bischofberger, Steven Krawczyk
  • Patent number: 5686471
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl or aralkyl having from 1 to about 3 carbon atoms; or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 and R.sub.2 are each independently hydrogen or straight, branched or cyclic alkyl, unsubstituted or substituted, carboxyl, carboxamido, alkoxycarbonyl or alkylcarbonyl; and(f) Het is a heteroaryl group comprising one or more rings containing from about 5 to about 8 atoms in the rings and wherein at least one ring has at least one heteroatom selected from O, N, or S,pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: November 11, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Zhuoliang Chen, John Michael Janusz
  • Patent number: 5663368
    Abstract: This invention relates to novel diastereomeric acid addition salts of homochiral hydroxylamines, to processes for obtaining such, to processes for the conversion thereof to the corresponding homochiral hydroxylamines, to certain novel homochiral hydroxylamines and the processes for using these as intermediates.
    Type: Grant
    Filed: April 11, 1996
    Date of Patent: September 2, 1997
    Assignee: Smithkline Beecham Corporation
    Inventors: Joseph R. Flisak, Stephen Torey Ross
  • Patent number: 5631210
    Abstract: Compounds of Formula I and their agriculturally suitable salts are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q is ##STR2## and R.sup.1 through R.sup.7, m, n, p and q are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: May 20, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 5618943
    Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: April 8, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
  • Patent number: 5618775
    Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: April 8, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
  • Patent number: 5541219
    Abstract: This invention is directed to 1-alkoxy-2-(alkoxy- or cycloalkyloxy-)-4-(cyclothioalkyl- or cyclothioalkenyl-)benzene compounds that inhibit cyclic AMP phosphodiesterase or tumor necrosis factor (TNF) and are useful in treating patients suffering from disease state capable of being modulated by inhibiting production of cyclic AMP phosphodiesterase or TNF by administering the compound to the patient. The invention is also directed to the preparation of these compounds, pharmaceutical compositions containing these compounds and methods for their pharmaceutical use.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: July 30, 1996
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Garry Fenton, Jonathan S. Mason, Malcolm N. Palfreyman, Andrew J. Ratcliffe
  • Patent number: 5527926
    Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 18, 1996
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
  • Patent number: 5525736
    Abstract: A process for the production of a 5-7 membered ring cyclic sulfonium salt compound, including a 5-7 membered ring cyclic sulfonium salt compound having a non-nucleophilic anion, is described. Members of the latter group are potentially useful as initiators for cationic polymerizations. The process comprises reacting a 1.4-, 1.5-, or 1.6-diol compound or a 5-7 membered ring cyclic ether compound with a mercapto compound and a strong protonic acid yielding the cyclic sulfonium salt compound. Some compounds described are also novel compounds per se.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: June 11, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Jan-Erik Nystrom, Per Engelhardt, Katarina Beierlein, Mikael Sellen, Bjorn Elman, Jan Vagberg, Martin Nylof
  • Patent number: 5512683
    Abstract: Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: April 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr
  • Patent number: 5491152
    Abstract: The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: February 13, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Richard G. Wilde, Soo S. Ko, Jeffrey T. Billheimer
  • Patent number: 5484810
    Abstract: This invention relates to alkylated sulfonium alkylene derivatives of certain 2H-1-benzopyrans, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cardioprotective properties and to their end-use application as therapeutic agents.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: January 16, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
  • Patent number: 5484805
    Abstract: The invention concerns a heterocyclene derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted 5-membered heterocyclene moiety;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: July 8, 1994
    Date of Patent: January 16, 1996
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventor: Thomas G. C. Bird
  • Patent number: 5480893
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: January 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, S. Jane deSolms
  • Patent number: 5350860
    Abstract: A compound of the formula [I]. ##STR1## The compounds of this invention has excellent thymulin-line activities and expected to be useful for treatment of various diseases such as immunodeficiency and autoimmune diseases.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: September 27, 1994
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Yoichi Kawashima, Ken-ichi Fujimura, Hiroshi Suhara, Masahiro Okamoto
  • Patent number: 5329016
    Abstract: Thiophene compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, nitro, amino, halogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, nitro, amino, halogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, acyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, aryloxy-C.sub.1-4 alkyl, acyloxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, acyloxy-C.sub.2-5 alkanoyl, C.sub.1-4 alkoxy-C.sub.2-5 alkanoyl, hydroxy-C.sub.2-5 alkanoyl, aryloxy-C.sub.2-5 alkanoyl or C.sub.2-5 haloalkanoyl; R.sup.3 is hydrogen, C.sub.1-8 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.2-5 alkanoyloxy-C.sub.1-4 alkyl, aryl, aryl-C.sub.1-4 alkyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl or aryl, aryl-C.sub.1-4 alkyl, heteroaryl or heteroaryl-C.sub.1-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoylamino, C.sub.1-4 haloalkyl, acyloxy, C.sub.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: July 12, 1994
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tohru Nakao, Yasuto Morimoto, Shuzo Takehara, Hiroshi Tanaka
  • Patent number: 5314891
    Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: May 24, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, Keith Oldham, David Waterson
  • Patent number: 5308863
    Abstract: Thieno[2,3-b]thiopyran-2-sulfonamides and ring homologs with a hydrophilic substituted-alkyl group adjacent to the thiopyran sulfur are carbonic anhydrase inhibitors topically effective in lowering intraocular pressure.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: May 3, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Charles N. Habecker, Harold G. Selnick
  • Patent number: 5298513
    Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: March 29, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 5206387
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond of (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: April 27, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 5175162
    Abstract: Thiophene compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, nitro, amino, halogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, nitro, amino, halogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, acyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, aryloxy-C.sub.1-4 alkyl, acyloxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, acyloxy-C.sub.2-5 alkanoyl, C.sub.1-4 alkoxy-C.sub.2-5 alkanoyl, hydroxy-C.sub.2-5 alkanoyl, aryloxy-C.sub.2-5 alkanoyl or C.sub.2-5 haloalkanoyl; R.sup.3 is hydrogen, C.sub.1-8 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.2-5 alkanoyloxy-C.sub.1-4 alkyl, aryl, aryl-C.sub.1-4 alkyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl or aryl, aryl-C.sub.1-4 alkyl, heteroaryl or heteroaryl-C.sub.1-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoylamino, C.sub.1-4 haloalkyl, acyloxy, C.sub.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: December 29, 1992
    Assignee: Yoshitiomi Pharmaceutical Industries Ltd.
    Inventors: Tohru Nakao, Yasuto Morimoto, Shuzo Takehara, Hiroshi Tanaka