Polycyclo Ring System In Substituent Q Patents (Class 564/180)
  • Patent number: 6121184
    Abstract: Supported bis(phosphorus) ligands are disclosed for use in a variety of catalytic processes, including the hydrocyanation of unsaturated organic compounds. Catalysts are formed when the ligands are combined with a catalytically active metal (e.g., nickel).
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: September 19, 2000
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Joe Douglas Druliner, Kenneth Gene Moloy, Manxue Wang
  • Patent number: 6103762
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R.sub.1 is --CH.sub.3, --CH.sub.2 --O--R.sub.6, --OR.sub.6 or --COR.sub.7 ; R.sub.2 is --OR.sub.8, --SR.sub.8 or a polyether radical if in the latter case R.sub.4 is C.sub.1 -C.sub.20 alkyl and is in ortho or meta position relative to X--Ar; R.sub.3 is alkyl or R.sub.2 and R.sub.3 together form a cycle optionally interrupted by O or S; R.sub.4 is aryl radical; R.sub.5 is H, halogen, C.sub.1 -C.sub.20 alkyl or --OR.sub.8 ; R.sub.6 is H, alkyl or --COR.sub.9 ; R.sub.7 is H, alkyl, --N(r')(r") or --OR.sub.10 ; R.sub.8 is H, alkyl or --COR.sub.9 ; R.sub.9 is alkyl; R.sub.10 is H, C.sub.1 -C.sub.20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r' and r" are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R.sub.11 is H or --OR.sub.6 ; R.sub.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: August 15, 2000
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Patent number: 6096768
    Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
    Type: Grant
    Filed: April 29, 1999
    Date of Patent: August 1, 2000
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
  • Patent number: 6096780
    Abstract: This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: ##STR1## wherein R.sup.1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is --CH.sub.2 --, --S-- or --O--; and R.sup.2, R.sup.3 and R.sup.4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.
    Type: Grant
    Filed: August 19, 1999
    Date of Patent: August 1, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Osamu Nishimura, Naoyuki Kanzaki
  • Patent number: 6069247
    Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: May 30, 2000
    Assignee: Eli Lilly and Company
    Inventors: Lynne Ann Hay, David Mitchell
  • Patent number: 6048877
    Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 6043272
    Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Grant
    Filed: November 20, 1997
    Date of Patent: March 28, 2000
    Assignees: Ion Pharmaceuticals, Inc., President and Fellows of Harvard College, Children's Medical Center Corporation
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
  • Patent number: 6025493
    Abstract: Disclosed arm compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 allyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: February 15, 2000
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5994507
    Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: November 30, 1999
    Assignee: Amersham Pharmacia Biotech AB
    Inventors: .ANG.ke Pilotti, Tor Regberg, Christel Ellstrom, Charlotta Lindqvist, Ann Eckersten, Lars Fagerstam
  • Patent number: 5985910
    Abstract: The present invention relates to new 3-[4-(2-Phenyl-Indole-1-ylmethyl)-Phenyl]-Acrylamide compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, the compounds having the following general structure.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: November 16, 1999
    Assignee: American Home Products Corporation
    Inventors: Chris P. Miller, Bach D. Tran
  • Patent number: 5977368
    Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: November 2, 1999
    Assignee: Rohm and Haas Company
    Inventors: Heather Lynnette Rayle, Renee Caroline Roemmele, Randall Wayne Stephens
  • Patent number: 5968985
    Abstract: A process for preparing a pharmaceutical composition which comprises admixing a compound of claim 1 or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: October 19, 1999
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Atsushi Kuno, Hiroaki Mizuno, Kumi Yamasaki, Yoshikazu Inoue
  • Patent number: 5958971
    Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: September 28, 1999
    Assignees: Zeneca Limited, Cancer Research Campaign Technology Limited
    Inventors: Philip John Burke, Robert Ian Dowell, Anthony Brian Mauger, Caroline Joy Springer
  • Patent number: 5935978
    Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: August 10, 1999
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
  • Patent number: 5925763
    Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid top produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichioroketone can be conveniently formed through adjustment of reaction conditions.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: July 20, 1999
    Assignee: Rohm and Haas Company
    Inventors: Heather Lynnette Rayle, Renee Caroline Roemmele, Randall Wayne Stephens
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5900436
    Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.
    Type: Grant
    Filed: July 28, 1997
    Date of Patent: May 4, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Nirogi Venkata Satya Ramakrishna, Arun Kumar Jain, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Andreas Weichert, Jan-Robert Schwark
  • Patent number: 5883257
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: March 16, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5877218
    Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 2, 1999
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Yaacov Herzig, Jeff Sterling, Alex Veinberg, Benjamin Sklarz, Ramy Lidor, Eliezer Bahar
  • Patent number: 5872118
    Abstract: Novel compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro;R.sup.5 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;R.sup.6 is selected from hydrogen, C.sub.1 -C.sub.4 ally and hydroxy; orR.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;R.sup.7 is selected from hydrogen and hydroxy,R.sup.8 and R.sup.9 are each selected from hydrogen, C.sub.1 -C.sub.4 alkyl and cyclo(C.sub.3 or C.sub.4) alkyl or together with the nitrogen form a morpholino group; andX is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R.sup.5, R.sup.6 and R.sup.7 is other than hydrogen and is always a bond when R.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: February 16, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, Gregory Cooksey Rigdon, Barrett Randolph Cooper, Ed Williams McLean, David Lee Musso, Gloria Faye Orr, Jeffrey Leaman Selph, Virgil Lee Styles
  • Patent number: 5859254
    Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.
    Type: Grant
    Filed: April 13, 1998
    Date of Patent: January 12, 1999
    Assignee: Rohm and Haas Company
    Inventors: Heather Lynnette Rayle, Renee Caroline Roemmele, Randall Wayne Stephens
  • Patent number: 5808135
    Abstract: The present invention relates to novel substituted bicyclic 2-mesityl-cyclopentane-1,3-dione derivatives of the formula (I) ##STR1## in which A and Q together represent alkanediyl or alkenediyl, which is in each case optionally substituted by halogen, hydroxyl, mercapto or in each case optionally substituted alkyl, alkoxy, alkylthio, cycloalkyl, benzyloxy or aryl, and which furthermore optionally contains one of the following groups ##STR2## or is bridged by an alkanediyl group andB, B' and G have the meaning given in the description,process for their preparation and their use as agents for controlling pests, and herbicides.
    Type: Grant
    Filed: January 15, 1997
    Date of Patent: September 15, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5801195
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: September 1, 1998
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 5801253
    Abstract: Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: September 1, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Allen John Lovey, Peter Mohr, Michael Rosenberger
  • Patent number: 5783593
    Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: July 21, 1998
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
  • Patent number: 5780505
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: July 14, 1998
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5766610
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##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: April 26, 1995
    Date of Patent: June 16, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5763635
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: June 9, 1998
    Assignee: ALLERGAN
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 5747542
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: May 5, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
  • Patent number: 5728737
    Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5719186
    Abstract: Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: February 17, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
  • 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: 5714148
    Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: February 3, 1998
    Assignees: Zeneca Limited, Cancer Research Campaign Technology Limited
    Inventors: Philip John Burke, Robert Ian Dowell, Anthony Brian Mauger, Caroline Joy Springer
  • Patent number: 5708033
    Abstract: A compound of formula (I), wherein R.sup.1 and R.sup.2 are independently selected from chloro, fluoro, bromo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 haloalkyl provided that both R.sup.1 and R.sup.2 are not fluoro; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: January 13, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, David Lee Musso
  • Patent number: 5705167
    Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: January 6, 1998
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5686586
    Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: November 11, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5663413
    Abstract: The invention relates to novel contrast media particularly useful for X-ray diagnostic investigations of human and animal body.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: September 2, 1997
    Assignee: Dibra S.p.A.
    Inventors: Fulvio Uggeri, Pier Lucio Anelli, Marino Brocchetta, Massimo Visigalli
  • Patent number: 5637121
    Abstract: Poly(oxyalkylene) aromatic amides having the formula: ##STR1## or a fuel-soluble salt thereof; wherein a is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.3 is hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.4 is hydrogen or an acyl group of the formula: ##STR2## wherein A.sub.1 is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms and each R.sub.5 and R.sub.6 is independently selected in each --O--CHR.sub.5 --CHR.sub.6 -- unit; R.sub.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: June 10, 1997
    Assignee: Chevron Chemical Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5599994
    Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 4, 1997
    Assignee: Pharm-Eco Laboratories, Inc.
    Inventors: Biman Pal, Siya Ram, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard L. Gabriel
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5587161
    Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT).
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: December 24, 1996
    Assignees: Zeneca Limited, Cancer Research Campaign Technology Limited
    Inventors: Philip J. Burke, Robert I. Dowell, Anthony B. Mauger, Caroline J. Springer
  • Patent number: 5532346
    Abstract: A coupling component for use in the synthesis of azo colorants, selected from compounds having the formula: ##STR1## wherein R.sub.1 is Y or arylene-(Y).sub.n, where n is an integer from 1-4; R.sub.2 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, aryl, or Y; provided that if R.sub.1 is arylene-(Y).sub.n, then R.sub.2 is not aryl; R.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, SO.sub.3 H, Br, Cl, OH, or NO.sub.2 and m is an integer from 0-3; and Y is a poly(oxyalkylene) substituent having from 4-200 oxyalkylene units which are the addition products of compounds selected from the group consisting of ethylene oxide and propylene oxide.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: July 2, 1996
    Assignee: Milliken Research Corporation
    Inventors: Patrick D. Moore, Michael A. Valenti, Richard A. VanDahm
  • Patent number: 5523457
    Abstract: This invention relates to a retinoid mpound of formula I ##STR1## in which Y is --CO--NH--, --CR.sup.2 .dbd.CR.sup.3 --, --CO--O--, --O--CO--, --C(.dbd.S)--NH--, --C.tbd.C--, --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --CH.sub.2 --;A is --(CH.sub.2).sub.t -- or a bond;Q is phenyl optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, or --CO.sub.2 R.sup.4 ;R.sup.1 is --CO.sub.2 Z, --CONHR.sup.5, C.sub.1-6 alkyl, --CH.sub.2 OH, or --CHO;R.sup.2, R.sup.3, R.sup.4, R.sup.5, and Z are independently hydrogen or C.sub.1-6 alkyl;t is one to six.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 4, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., Muzammil M. Mansuri, David R. Tortolani
  • Patent number: 5514825
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 10 carbons; R.sub.2 and R.sub.3 are hydrogen, or alkyl of 1 to 6 carbons and the substituted ethynyl group occupies either the 2 or the 3 position of the tetrahydronaphthalene nucleus; m is an integer having the value of 0-3; o is an integer having the value 0-4; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.2 groups; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: May 7, 1996
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 5514683
    Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: May 7, 1996
    Assignee: James Black Foundation Limited
    Inventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
  • Patent number: 5478835
    Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 26, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5470999
    Abstract: Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.
    Type: Grant
    Filed: December 30, 1993
    Date of Patent: November 28, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5466712
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
  • Patent number: 5464867
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: November 7, 1995
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill