Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
  • Patent number: 6596752
    Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: July 22, 2003
    Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn Company
    Inventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
  • Publication number: 20030109524
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: November 6, 2002
    Publication date: June 12, 2003
    Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
  • Patent number: 6534651
    Abstract: The invention provides a novel class of substituted isoindolinone derivatives, useful for the treatment of inflammation and reperfusion injuries. Pharmaceutical compositions, and methods of making and using the compounds, or pharmaceutically acceptable salts, hydrates, stereoisomers or mixtures thereof are also described. The novel isoindolinone derivatives have the formula: or a pharmaceutically acceptable base or acid addition salt, hydrate, stereoisomer, or mixtures thereof, wherein R14 is described herein.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: March 18, 2003
    Assignee: Inotek Pharmaceuticals Corp.
    Inventors: Prakash Jagtap, Garry Southan, Andrew Salzman, Csaba Szabo, Siya Ram
  • Patent number: 6492363
    Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: December 10, 2002
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
  • Patent number: 6479491
    Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 12, 2002
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Patent number: 6423714
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: July 23, 2002
    Assignee: Ortho McNeil-Pharmaceutical, Inc..
    Inventors: Robert H. Chen, Min A. Xiang
  • Patent number: 6413987
    Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Patent number: 6407120
    Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
    Type: Grant
    Filed: January 28, 2000
    Date of Patent: June 18, 2002
    Assignee: Pfizer Inc.
    Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
  • Patent number: 6399773
    Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: June 4, 2002
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Chunjian Liu, T. G. Murali Dhar, Henry H. Gu, Edwin J. Iwanowicz, Katerina Leftheris, William J. Pitts
  • Patent number: 6395735
    Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: May 28, 2002
    Assignee: Eli Lilly and Company
    Inventors: Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, Bret Eugene Huff, Charles Howard Mitch, Michael Alexander Staszak, John Stanley Ward
  • Patent number: 6392040
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: May 21, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min A. Xiang
  • Patent number: 6384031
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: May 7, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min A. Xiang
  • Publication number: 20020052343
    Abstract: The present invention provides novel compounds of Formula I: 1
    Type: Application
    Filed: December 14, 2000
    Publication date: May 2, 2002
    Inventors: Darin Arthur Allen, Danny Peter Claude McGee, Jeffrey R. Spencer
  • Patent number: 6350884
    Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: February 26, 2002
    Assignee: Eli Lilly and Company
    Inventors: Charles David Jones, Alan David Palkowitz, Kenneth Jeff Thrasher
  • Patent number: 6323229
    Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: November 27, 2001
    Assignee: Pfizer INC
    Inventor: Harry R. Howard
  • Patent number: 6323202
    Abstract: The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or  wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Bruno Simoneau, Michele Liuzzi, Anton Mentrup
  • Patent number: 6313122
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6294531
    Abstract: Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: September 25, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert M. Barmore, Pradip Kumar Bhatnagar, William M. Bryan, Joelle Lorraine Burgess, James Francis Callahan, Raul Rolando Calvo, Eric G. Del Mar, Maria Amparo Lago, Thomas The Nguyen, Derek Sheehan, Robert Lawrence Smith, Linda Sue Southall, Bradford C. Van Wagenen
  • Patent number: 6166013
    Abstract: Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.
    Type: Grant
    Filed: July 30, 1999
    Date of Patent: December 26, 2000
    Assignee: Abbott Laboratories
    Inventors: Michael J. Coghlan, Jay R. Luly, Jeffrey M. Schkeryantz, Alan X. Wang
  • Patent number: 6133266
    Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: October 17, 2000
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
  • Patent number: 6117870
    Abstract: A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: September 12, 2000
    Assignee: Fujirebio Kabushiki Kaisha
    Inventors: Akihiko Hosoda, Nobuo Kobayashi, Naoko Tanabe, Tsuneo Koji, Masahiro Shibata, Akihiro Sekine, Masaharu Dozen
  • Patent number: 6100262
    Abstract: The present invention concerns novel (2-morpholinylmethyl)benzamide derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sup.2 is hydrogen, halo or C.sub.1-6 alkylsulfonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is a radical of formula R.sup.4 --C(.dbd.O)--Alk-- (a); R.sup.5 --C(.dbd.O)--N(R.sup.6)--Alk-- (b); or R.sup.7 --C(.dbd.O)--O--Alk-- (c); wherein each Alk is independently C.sub.1-12 alkanediyl; R.sup.4 is hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.5 and R.sup.7 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.6 is hydrogen or C.sub.
    Type: Grant
    Filed: September 22, 1999
    Date of Patent: August 8, 2000
    Assignee: Janssen Pharmaceutica, NV.
    Inventors: Marie-Louise Hendrickx, Kurt Godfried Cornelius Emile Van Daele, Peter Jules Victor Van Daele, Glenn Kurt Ludo Van Daele, Frans Maria Alfons Van den Keybus, Marc Gustaaf Celine Verdonck
  • Patent number: 6100428
    Abstract: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: August 8, 2000
    Assignee: The University of Kansas
    Inventors: Laxminarayan Bhat, Gunda I. Georg
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6034136
    Abstract: Disclosed are compound of formula I whereinR 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;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl;R.sub.2 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);R.sub.3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C.sub.2 -C.sub.7 -alkyl interrupted by S, SO, SO.sub.2, O or N--R.sub.5 ;R.sub.4 represents hydrogen or acyl;R.sub.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: March 7, 2000
    Assignee: Novartis AG
    Inventor: Cynthia A. Fink
  • Patent number: 6025355
    Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: May 19, 1997
    Date of Patent: February 15, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
  • Patent number: 5972939
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 26, 1999
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
  • Patent number: 5969133
    Abstract: A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: October 19, 1999
    Assignee: Shiongi BioResearch Corp.
    Inventors: Mitsunori Ono, Keizo Koya, Lijun Sun, Yumiko Wada, Wojciech Wrona, Natalie Dales, Xueliang Tao, Sylvia Holden
  • Patent number: 5945413
    Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors 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 HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: August 31, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
  • Patent number: 5929090
    Abstract: The present invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; having activity as a selective estrogen receptor modulator, pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for treating conditions resulting from estrogen deprivation or the inappropriately high presence of estrogen. Also provided are methods and chemical intermediates for the production of a compound of formula I above.
    Type: Grant
    Filed: September 12, 1997
    Date of Patent: July 27, 1999
    Assignee: Eli Lilly and Company
    Inventors: Kenneth Lee Hauser, Alan David Palkowitz
  • Patent number: 5863913
    Abstract: An aromatic compound of the formula (I): ##STR1## specifically, for example, 3-??(4-carboxyphenyl)methyl!valeramido!-4-dimethylaminobenzoic acid 4'-methylpiperazide, or a salt thereof, and a pharmaceutical composition comprising said aromatic compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent which provides sufficiently effective alleviation of renal dysfunction without affecting blood pressure at a low blood concentration.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: January 26, 1999
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Hiroyuki Enari, Toru Yamazaki, Hiroshi Maruoka, Toshikazu Dewa, Fuyuhiko Nishijima, Hiroshi Takahashi, Michihito Ise
  • Patent number: 5776951
    Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: April 11, 1996
    Date of Patent: July 7, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
  • Patent number: 5739131
    Abstract: A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: April 14, 1998
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Toshikazu Dewa, Toru Yamazaki, Michihito Ise
  • Patent number: 5696118
    Abstract: A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: December 9, 1997
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Toshikazu Dewa, Toru Yamazaki, Michihito Ise
  • Patent number: 5693860
    Abstract: There are provided substituted acid amide, arylhydrazone compounds (amaidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: December 2, 1997
    Assignee: American Cyanamid Company
    Inventors: Joseph Augustus Furch, David George Kuhn, David Allen Hunt
  • Patent number: 5677449
    Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G is defined in the claims,to processes for their preparation, and to their use as pesticides.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: October 14, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Christoph Erdelen, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Wilhelm Stendel
  • Patent number: 5659065
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: August 19, 1997
    Assignee: Novartis Corporation
    Inventor: Richard Goschke
  • Patent number: 5643932
    Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), ##STR1## [wherein R.sup.1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R.sup.2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R.sup.3 represents a group of the formula, ##STR2## (R.sup.4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group. m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: July 1, 1997
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5641778
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.
    Type: Grant
    Filed: December 6, 1995
    Date of Patent: June 24, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Jurgen Klaus Maibaum, Pascal Rigollier, Peter Herold, Nissim Claude Cohen, Richard Goschke, Stefan Stutz
  • Patent number: 5607953
    Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5604256
    Abstract: Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: February 18, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
  • Patent number: 5525633
    Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: June 11, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
  • Patent number: 5523303
    Abstract: The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: June 4, 1996
    Assignee: Egis Gyogyszergyar Rt.
    Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Andras Egyed, Marton Fekete, Erika Karaffa, Tibor Mezei, Klara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Eniko Szirt nee Kiszelly
  • Patent number: 5495019
    Abstract: The invention provides a process for the preparation of 3,3-diaryl acrylic acid amides of the general formula ##STR1## in which A, B and Q are as defined in the specification, by condensing a compound of formula ##STR2## with a compound of formulaCH.sub.3 --CO--Q (III)in which Q has the meaning given above, in a solvent in the presence of an alkali metal hydroxide, characterised in that the solvent is selected from alkanes, cycloalkanes or mixtures thereof.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Jurgen Curtze, Bodo Haertel
  • Patent number: 5476860
    Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: December 19, 1995
    Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5453517
    Abstract: The invention relates to fluorescent and/or reactive derivatives of 1,2-bis-(2-aminophenoxyethane)-N,N,N',N'-tetraacetic acid (BAPTA) according to the formula: ##STR1## where at least one of W and X is a functional group, with or without a spacer, that terminates in an alcohol or phenol, a thiol, a haloacetamide, an alkyl halide, an amine or aniline, a carboxylic acid, an anhydride, an isocyanate, an isothiocyanate, a maleimide, or an activated ester. The BAPTA-like molecule may be further substituted, one or more times, by additional functional groups with or without spacers or by CH.sub.3, NO.sub.2, CF.sub.3, F, Cl, Br, I, or carboxylic acid derivatives or pharmaceutically acceptable salts thereof, or by indolyl or benzofuran fluorophores. The functional groups allow for subsequent covalent attachment of one or more oxygen heterocycle fluorophores (e.g. fluorescein, coumarin, rhodamine); or polymolecular assemblies (e.g.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: September 26, 1995
    Assignee: Molecular Probes, Inc.
    Inventors: Michael A. Kuhn, Richard P. Haugland
  • Patent number: 5451394
    Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.4 alkyl, hydrogen and, alternatively, R.sub.1 and R.sub.2, together with the attached cationic nitrogen atom can form a 5 to 6-membered heterocyclic ring selected from the group of ##STR2## and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: September 19, 1995
    Assignee: ISP Van Dyk Inc.
    Inventors: Ratan K. Chaudhuri, Anatoly Alexander, Anna A. Gripp
  • Patent number: 5427774
    Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 together with the attached cationic nitrogen atom forms a 5 to 6-membered heterocyclic ring containing a hetero oxygen atom in addition to the heteronitrogen atom and is selected from the group of ##STR2## and X is an anion. These benzamide heterocyclic derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: June 27, 1995
    Assignee: ISP Van Dyk Inc.
    Inventors: Ratan K. Chaudhuri, Anatoly Alexander, Anna A. Gripp
  • Patent number: 5374724
    Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 20, 1994
    Assignee: Zeneca, Limited
    Inventors: Nigel Hall, Nigel Hughes, Prakash Patel
  • Patent number: RE37556
    Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group, m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.
    Type: Grant
    Filed: February 8, 1999
    Date of Patent: February 19, 2002
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi