Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
  • Patent number: 5849921
    Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo?1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-?(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo?1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 15, 1998
    Assignee: Astra Aktiebolag
    Inventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
  • Patent number: 5847135
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: December 8, 1998
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Patent number: 5846988
    Abstract: Compounds useful as cytoprotective agents are disclosed. The compounds possess dual activity, containing a phenolic portion selected to have antioxidant or free radical scavenging properties and a thiazolidine-4-carboxylate portion selected for its potential to act as a cysteine prodrug.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: December 8, 1998
    Assignee: Alcon Laboratories, Inc.
    Inventor: Mark R. Hellberg
  • Patent number: 5840739
    Abstract: Thiazoline acids and derivatives useful as chelators of trivalent metals in therapeutic applications have been prepared.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: November 24, 1998
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5837721
    Abstract: The disclosed invention is thifluzamide with an altered crystalline form, prepared by heat-melting and then cooling, and agricultural chemical compositions comprising such a thifluzamide as its effective ingredient.
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: November 17, 1998
    Assignee: Rohm and Haas Company
    Inventors: Norihito Hayakawa, Masatoshi Baba, Norihiro Suwa, Kazuhiro Yamagishi
  • Patent number: 5834468
    Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5827860
    Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5827866
    Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael J. Costanzo, Bruce E. Maryanoff
  • Patent number: 5827859
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, John H. Tatlock
  • Patent number: 5824688
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
  • Patent number: 5821250
    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 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: February 1, 1996
    Date of Patent: October 13, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Laurence Ichih Wu, John Michael Janusz
  • Patent number: 5786515
    Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: July 28, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Patent number: 5780638
    Abstract: 5-Hydroxymethylthiazole is prepared in an improved manner by reducing 5-formylthiazole using a borane compound. Particularly advantageous in this case is the use of 5-formylthiazole which has been obtained by reaction of a 2-halomalonaldehyde compound with thioformamide in the presence of less than 5% by weight of water (based on the reaction mixture).
    Type: Grant
    Filed: December 9, 1996
    Date of Patent: July 14, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Kraus, Helmut Fiege
  • Patent number: 5773455
    Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by one of the two following formulas: ##STR1## Each of the R groups is defined in the disclosure.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: June 30, 1998
    Assignee: Biomeasure, Incorporated
    Inventors: Zheng Xin Dong, Sun H. Kim
  • Patent number: 5756534
    Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds of the formula: ##STR1## such as 3-isoquinolinecarboxamide,N-(,1-dimethylethyl)decahydro-2-?2-hydroxy-3-??2 -methyl-3-(methysulfonyl)-1-oxopropyl!amino!-4-phenylbutyl!-, ?3S-?2?2S*,3R*(R*)!,3.alpha.,4a.beta., 8 a.beta.!!- are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 26, 1998
    Assignee: Monsanto Company
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
  • Patent number: 5750543
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from 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;(e) W is O or S; and(f) 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: February 1, 1996
    Date of Patent: May 12, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Laurence Ichih Wu, John Michael Janusz
  • Patent number: 5750706
    Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: May 12, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
  • Patent number: 5747518
    Abstract: The substituted thiophene derivative of the invention which is represented by the general formula (1) has a broad disease spectrum for a pathogenic fungus of various crops, exhibits an excellent controlling effect on disease such as gray mold, powdery mildew and rust in particular, and is also effective for a resistant fungus of conventional fungicides which has become a serious problem, and consequently is useful for an agricultural and horticultural fungicide.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: May 5, 1998
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Yukihiro Yoshikawa, Kanji Tomiya, Hiroyuki Katsuta, Hideo Kawashima, Osamu Takahashi, Shunichi Inami, Yuji Yanase, Junro Kishi, Hitoshi Shimotori, Naofumi Tomura
  • Patent number: 5733882
    Abstract: The present invention provides compounds, more particularly dipeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are useful for treating diseases related to infection by retroviruses.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: March 31, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Thomas Joseph Carr, Peter Lawrence DeMarsh, Geoffrey Bainbridge Dreyer, Ashley Edward Fenwick
  • Patent number: 5693310
    Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: December 2, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Heinz Gries, Bernd Raduechel, Hans-Joachim Weinmann, Wolfgang Muetzel, Ulrich Speck
  • Patent number: 5691366
    Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
    Type: Grant
    Filed: October 31, 1995
    Date of Patent: November 25, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
  • Patent number: 5691359
    Abstract: Heterocyclylcarbonyl substituted benzofuranyl- and thiophenyl-alkanecarboxylic acid derivatives are prepared by reacting appropriately substituted hydroxybenzene butanoic acid esters with heterocyclic ketones. The inventive compounds can be used for the preparation of medicaments, particularly of medicaments for the treatment and prevention of acute and chronic inflammatory processes.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: November 25, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudiger Fischer, Gabriele Braunlich, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Mary F. Fitzgerald
  • Patent number: 5686622
    Abstract: Thiazolidine derivatives of formula (I), in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification. The invention also concerns the salts of these derivatives, the preparation thereof and drugs containing same.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: November 11, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Marc Capet, Marie-Christine Dubroeucq, Claude Guyon, Franco Manfre
  • Patent number: 5686435
    Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
  • Patent number: 5684198
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 23, 1996
    Date of Patent: November 4, 1997
    Assignee: Imperial Chemical Industries, PLC
    Inventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
  • Patent number: 5684002
    Abstract: A compound having the structure: ##STR1## wherein (a) W is --C(X')--NRR' or --NR--C(X')R';(b) X and X' are independently O or S;(c) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 3 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms;(d) Z is unsubstituted branched or cyclic alkyl, or unsubstituted or alkanyl-substituted phenyl or benzyl, Z having from 3 to about 10 atoms other than hydrogen;(e) R and R' are each independently selected from hydrogen, hydroxy straight, branched or substituted alkyl having from 1 to about 6 carbon atoms, and cyclic alkyl having from 3 to about 7 carbon atoms; unsubstituted or substituted aryl, heteroaryl or heterocyclic groups; or R and R' are bonded together to form a ring having from from 3 to about 8 atoms wherein about 1 to about 4 atoms may be heteroatoms;pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 4, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Michael Wiard Scherz, John Michael Janusz
  • Patent number: 5677320
    Abstract: Compounds of Formula 1 ##STR1## wherein the symbols are as defined in the specification, have retinoid like biological activity.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: October 14, 1997
    Assignee: Allergan
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5675024
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5663200
    Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: September 2, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
  • Patent number: 5661167
    Abstract: The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.
    Type: Grant
    Filed: December 2, 1996
    Date of Patent: August 26, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Shujaath Mehdi, Joseph P. Burkhart
  • Patent number: 5656637
    Abstract: A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: August 12, 1997
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Mitsuaki Ohta, Isao Yanagisawa, Keiji Miyata
  • Patent number: 5656657
    Abstract: 3-amino-5-carbonylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: August 12, 1997
    Assignee: Astra Aktiebolag
    Inventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
  • Patent number: 5639772
    Abstract: 3-amino-5-aryl- and 5-heteroarylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: June 17, 1997
    Assignee: Astra Aktiebolag
    Inventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
  • Patent number: 5637602
    Abstract: This invention relates to a compound of formula (I), their salts, the preparation thereof and drugs containing same. The compounds of formula (I) have interesting pharmacological properties. Said compounds have a high affinity for chloecystokinin (CCK) and gastrin receptors and are therefore useful in the treatment and prevention of CCK and gastrin-related disorders affecting the nervous system and gastrointestinal tract.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 10, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Marc Capet, Marie-Christine Dubroeucq, Franco Manfre, Jean-Paul Martin
  • Patent number: 5633270
    Abstract: Derivatives of formula (I), their salts, the preparation of said derivatives and drugs containing same. The compounds of formula (I) have interesting pharmacological properties.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Marie-Christine Dubroeucq, Franco Manfre
  • Patent number: 5633375
    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: June 7, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
  • Patent number: 5614520
    Abstract: Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): ##STR1## wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group;X is a hydrogen atom, alkyl group or carboxyl group which may be protected, andY is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected.Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: March 25, 1997
    Assignee: Teijin Limited
    Inventors: Shiro Kondo, Hisashi Fukushima, Masaichi Hasegawa, Masahiro Tsuchimoto, Ikuo Nagata, Yoshio Osada, Keiji Komoriya, Hisao Yamaguchi
  • Patent number: 5610144
    Abstract: This invention relates to compositions of formula: ##STR1## and their salts, their preparation and the medicaments containing them.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: March 11, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Marc Capet, Claude Cotrel, Claude Guyon, Michel Joannic, Franco Manfre, G erard Roussel, Marie-Christine Dubroeuco, Michel Cheve, Gilles Dutruc-Rosset
  • Patent number: 5608062
    Abstract: A process is described for preparing trifluoromethyl ketones of the formula I ##STR1## where R has the given meanings, wherein an alcohol of the formula II ##STR2## is reacted with a compound of the formula IVYO.sub.n H (IV)where n has the given meaning.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: March 4, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Uwe D oller, Bernd Scharbert, Laurent Weisse
  • Patent number: 5591758
    Abstract: Organic nitrates, processes for their preparation and their use in the treatment of vascular diseases and in particular in the treatment of angina.The said nitrates correspond to the following formula I:R--CO--(A).sub.n --Y--B (I)in which:R represents, in particular, a sulphur-containing radical and a sulphur-containing amino acid residue; A represents, in particular, a CH.sub.2 group or a substituted amino acid; n is 0 or 1 or greater than 1; Y represents an oxygen atom or an NH group and B represents, in particular, a 1,4:3,6-dianhydro hexitol mononitrate radical, an itol nitrate radical or an inositol radical.The said organic nitrates are prepared by reacting:I. either a thio acid of the type R--COOH, in which R has the same meaning as above, with a derivative of formula II: (A).sub.n --Y--B, in which A, Y, B and n have the same meaning as above,II. or a derivative of formula III: R--CO--(A).sub.
    Type: Grant
    Filed: May 4, 1993
    Date of Patent: January 7, 1997
    Assignee: Laboratoires Hoechst, SA
    Inventors: Jean-Pierre Nallet, Jacques Dreux, Alain Berdeaux, Vincent Richard, Piero Martorana, Helmut Bohn
  • Patent number: 5585486
    Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: December 17, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
  • Patent number: 5580999
    Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, -N(alkoxycarbonyl)-,-N(acyl)- or --S--or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: December 3, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
  • Patent number: 5571920
    Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: November 5, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
  • Patent number: 5567671
    Abstract: The present invention relates to 1-H-3-phenyl-5-cyloalkylpyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents optionally substituted cycloalkyl andB represents hydrogen or optionally substituted alkyl,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## These compounds possess herbicidal and pesticidal activity.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: October 22, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Patent number: 5554581
    Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: September 10, 1996
    Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.
    Inventors: Kenji Hirai, Tomoko Matsukawa, Tomoyuki Yano, Emiko Ejiri, Kiyomi Aizawa, Koichi Shikakura, Tomoko Yoshii, Sadayuki Ugai, Osamu Yamada, Shigeki Kishi
  • Patent number: 5550248
    Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: C.sub.m H.sub.p is an alkylene chain wherein m is 0, 1, 2, or 3 and p=(2.times.m)-1, except that when m is 0, p is also 0;n is 0, 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sup.3, CONHR.sup.4, or --CH.sub.2 --5--tetrazolyl;R' is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0;and the remaining symbols are as defined in the specification.
    Type: Grant
    Filed: November 29, 1990
    Date of Patent: August 27, 1996
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Patent number: 5547978
    Abstract: The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: August 20, 1996
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Burton G. Christensen, Takashi Egawa, Yasuyuki Ichimaru, Shokichi Ohuchi, Tsuneo Okonogi, Arthur A. Patchett, Seiji Shibahara, Seiji Tsutsumni
  • Patent number: 5536723
    Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: July 16, 1996
    Assignee: Brigham & Women's Hospital
    Inventors: Joseph Loscalzo, John Cooke
  • Patent number: 5536737
    Abstract: Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof.The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 16, 1996
    Assignee: Japan Tobacco Inc.
    Inventors: Koji Kobayashi, Minoru Akamatsu, Shinji Yata, Hiroyuki Abe, Katsuo Toide, Motohiro Kogayu, Itsuo Uchida
  • Patent number: 5527829
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: June 18, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventor: Vincent J. Kalish