Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 546/197)
  • Patent number: 5559127
    Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## wherein A,B,D,E,Y are as defined in the specification, are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 24, 1996
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Melissa S. Egbertson, Mark E. Duggan, William Hoffman, Wasyl Halezenko, Ben Askew
  • Patent number: 5552553
    Abstract: N-(3-hydroxy-4-pipendinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system are disclosed, wherein the compounds have the formula: ##STR1## A represents a group of the formula: --CH.sub.2 --O--, --CH.sub.2 --CH.sub.2 --O-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --O--wherein one or two hydrogen atoms in the A moiety may be replaced by a C.sub.1-6 alkyl group.
    Type: Grant
    Filed: September 7, 1994
    Date of Patent: September 3, 1996
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Fran M. A. Van den Keybus
  • Patent number: 5543427
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: August 6, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5541183
    Abstract: The present invention is directed to new ginkgolide derivatives, which may be used for the prevention or treatment of various PAF-induced diseases, and the pharmaceutical uses of these derivatives. The present invention is also directed to a process for preparing these ginkgolide derivatives.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: July 30, 1996
    Assignee: Sunkyong Industries Co., Ltd.
    Inventors: Pyeong-Uk Park, Sungsoo Pyo, Suk-Kwan Lee, Jin H. Sung, Wie J. Kwak, Hwa-Kun Park, Yong-Baik Cho, Geun Ho Ryu, Taek S. Kim
  • Patent number: 5536847
    Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 16, 1996
    Assignee: Taiho Pharmaceutical Co. Ltd.
    Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
  • Patent number: 5534511
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the description, the optical isomers thereof, and the addition salts thereof with a pharmaceutically acceptable acid or base and medicinal product containing the same, useful for treating a mammal afflicted with a pathology associated with the sigma receptors.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: July 9, 1996
    Assignee: Adir et Compagnie
    Inventors: Ange Mouithys-Mickalad, Patrick Depreux, Daniel Lesieur, Gerard Adam, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
  • Patent number: 5502027
    Abstract: This invention relates to glutarimide compounds exhibiting herbicidal activity having the structure ##STR1## wherein A is carbonyl, thiocarbonyl or methylene, Al is carbonyl or methylene, Q is O or (CH.sub.2).sub.n where n is 0 or 1, D is CH or N and R, R.sup.1, R.sup.2, T, X, Y and Z are as defined within, compositions containing these compounds and methods of using these compounds as herbicides and algicides.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: March 26, 1996
    Assignee: Rohm and Haas Company
    Inventors: Barry C. Lange, John W. Ashmore, Jane Wissinger-Cornille, Colin M. Tice
  • Patent number: 5500443
    Abstract: A compound of formula (I): ##STR1## in which: X represents oxygen or methylene,n represents 1, 2 or 3,R.sub.1 represents hydrogen, aminocarbonyl or hydroxymethyl,R.sub.2 represents: ##STR2## in which R.sub.3 and R.sub.4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: March 19, 1996
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Olivier Muller, Mark Millan, Mauricette Brocco
  • Patent number: 5496853
    Abstract: Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: March 5, 1996
    Assignee: Teijin Limited
    Inventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
  • Patent number: 5486527
    Abstract: Selective muscarinic receptor antagonists of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are both optionally substituted phenyl, the broken line is an optional bond, X is >COH--, >SiOH-- or CH-- when the double bond is absent or is >C.dbd. when the double bond is present, X being attached to a carbon atom of A, A is selected from certain piperidine and pyrrolidine groups, n is 1 to 3 and R.sup.3 is optionally substituted phenyl or thienyl, pyridyl or pyrazinyl.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: January 23, 1996
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross
  • Patent number: 5478828
    Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols are useful as anxiolytic agents and have other psychotropic properties.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: December 26, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5475109
    Abstract: Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in the prevention or treatment of infection by influenza virus and the treatment of influenza, either as compound, pharmaceutically acceptable salts,. pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating influenza and methods of preventing or treating infection by influenza virus are also described.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, Gerald S. Ponticello, John J. Baldwin, Joanne E. Tomassini
  • Patent number: 5468855
    Abstract: The invention relates to bislactone color formers having improved fastness to sublimation and migration stability, to their preparation, to pressure-sensitive and heat-sensitive recording materials containing said compounds and to their preparation. The novel bislactones have the formula (1) as defined in claim 1.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: November 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Rudolf Zink
  • Patent number: 5457212
    Abstract: A process for the preparation of enantiomerically pure thienopyran derivatives of the formula ##STR1## is described. The thienopyran derivatives are relaxants of smooth muscle tone and as such are useful in vascular tissue for the treatment of hypertension disease, angina and other vascular disorders characterized by poor regional perfusion.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: October 10, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline J. Sanfilippo, Maud Urbanski
  • Patent number: 5428034
    Abstract: Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: June 27, 1995
    Assignees: Sankyo Co., Ltd., Ciba-Geigy Corporation
    Inventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
  • Patent number: 5428043
    Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: June 27, 1995
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 5424455
    Abstract: A heterocyclic compound of the formula, ##STR1## wherein A and B are each hydrogen, halogen, alkyl or alkoxy, R.sup.1 is alkylene having upto 6 carbon atoms, X is direct linkage or divalent group such as --O--, --S--and the like, T and U are each hydrogen or alkyl, l is 0 or 1 to 3, Q is 5-, 6- or 7- membered saturated or unsaturated heterocyclic residue, and Y is hydrogen, halogen, alkyl, alkoxy or ##STR2## and B are taken together with each other to form methylene-dioxy, which is useful for dyeing or printing hydrophobic fiber materials with superior dyeability to give a dyed or printed product of a red color excellent in fastness properties, particularly those such as washing fastness.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: June 13, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
  • Patent number: 5422358
    Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Y is a direct link, --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; R is --CN or --CONH.sub.2 ; and R.sup.1 is ##STR2## where X and X.sup.1 are each independently O or CH.sub.2 ; and m is 1, 2 or 3, are muscarinic receptor antagonists useful in the treatment of diseases and conditions associated with the altered motility and/or tone of smooth muscle, such as irritable bowel syndrome.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: June 6, 1995
    Assignee: Pfizer Inc
    Inventors: Peter E. Cross, Alexander R. Mackenzie
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5410046
    Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.
    Type: Grant
    Filed: May 11, 1993
    Date of Patent: April 25, 1995
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Robert M. Wallis
  • Patent number: 5409937
    Abstract: The invention concerns compounds of the formula I: ##STR1## wherein the variables are described in the specification which are antagonists of platelet activity factor.
    Type: Grant
    Filed: April 18, 1994
    Date of Patent: April 25, 1995
    Assignee: British Biotech Pharmaceuticals Limited
    Inventor: Mark Whittaker
  • Patent number: 5397791
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: March 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
  • Patent number: 5393759
    Abstract: The invention concerns an isochromane derivative having the general formula I ##STR1## in which R.sub.1 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.2 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.3 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.4 is selected from hydrogen or alkyl (1-4 C);A is a bond or an alkylene or alkylidene group with 1-6 carbon atoms;B is an alkylene or alkylidene group with 1-6 carbon atoms when Y is a bond, or B is an alkylene group with 2-6 carbon atoms when Y is a group selected from O, S, or NR.sub.5 ;X is CH or N; andR.sub.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: February 28, 1995
    Assignee: Akzo N.V.
    Inventors: Michel Combourieu, Jean-Claude Laigle, Nadine Simbille
  • Patent number: 5393735
    Abstract: This invention relates to glutarimide compounds exhibiting herbicidal activity having the structure ##STR1## wherein A is carbonyl, thiocarbonyl or methylene, A.sup.1 is carbonyl or methylene, Q is O or (CH.sub.2).sub.n where n is 0 or 1, D is CH or N and R, R.sup.1, R.sup.2, T, X, Y and Z are as defined within, compositions containing these compounds and methods of using these compounds as herbicides and algicides.
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: February 28, 1995
    Assignee: Rohm and Haas Company
    Inventors: Barry C. Lange, John W. Ashmore, Jane Wissinger-Cornille, Colin M. Tice
  • Patent number: 5391740
    Abstract: This disclosure relates to a method and reagents for determining ligands in biological fluids such as serum, plasma, spinal fluid, amnionic fluid and urine. In particular, this disclosure relates to a fluorescence polarization immunoassay procedure and to a novel class of tracer compounds employed as reagents in such procedures. The procedure disclosed combines the specificity of an immunoassay with the speed and convenience of fluorescence polarization techniques to provide a means for determining the amount of the specific ligand present in a sample.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: February 21, 1995
    Assignee: Abbott Laboratories
    Inventors: Chao-Huei J. Wang, Stephen D. Stroupe, Michael E. Jolley
  • Patent number: 5387593
    Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: February 7, 1995
    Assignee: Briston-Myers Squibb
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 5378714
    Abstract: The present invention relates to therapeutically active piperidine derivatives, of formula 1 ##STR1## wherein, R.sup.1, R.sup.2, A, X and Y are as defined in the specification. The compounds are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: January 3, 1995
    Assignee: Novo Nordisk A/S
    Inventors: John B. Hansen, Lone Jeppesen, Frederik C. Gronvald
  • Patent number: 5378713
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: January 3, 1995
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5374637
    Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: March 6, 1990
    Date of Patent: December 20, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
  • Patent number: 5374650
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5356891
    Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: October 18, 1994
    Inventors: Donald T. Witiak, Ineke van Wijngaarden, Raghunathan V. Nair, Josephus H. M. Lange, Jacobus A. J. den Hartog
  • Patent number: 5344835
    Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: September 6, 1994
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross
  • Patent number: 5338745
    Abstract: Therapeutic agents for degressive diseases in the central nervous system, which contain amide derivatives of dihydrocaffeic acid of the general formula (I) ##STR1## wherein, R.sub.1 and R.sub.2 and A are defined in the specification; the compounds exert a nerve growth factor inducing action and thus are effective for the prevention of the progression of degenerative diseases in the central nervous system and the therapeutic treatment thereof.
    Type: Grant
    Filed: April 8, 1992
    Date of Patent: August 16, 1994
    Assignee: Mitsui Toatsu Chemicals, Incorporation
    Inventors: Nobuyuki Fukazawa, Hajime Iizuka, Osamu Yano, Yukio Miyama
  • Patent number: 5332819
    Abstract: This invention relates to photopolymerizable compositions containing initiator systems that absorb in the longer wavelength region of the visible spectrum. Photopolymerizable compositions containing selected photodissociable initiators in combination with photobleachable sensitizers are disclosed.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: July 26, 1994
    Assignee: E.I. Du Pont de Nemours and Company
    Inventor: William K. Smothers
  • Patent number: 5332811
    Abstract: Compounds which are analogs of etoposide and which exhibit anti-tumor activity are disclosed. These compounds having the following structure: ##STR1## wherein R is selected from ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently selected from H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, i--C.sub.3 H.sub.7, C.sub.4 H.sub.9, CF.sub.3, OCH.sub.3, OC.sub.2 H.sub.5 , OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, O--i--C.sub.3 H.sub.7, O--i--C.sub.4 H.sub.9, --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, CH.sub.2 OH, C.sub.2 H.sub.4 OH, CH.sub.2 Cl C.sub.2 H.sub.4 Cl, CH.sub.2 F, C.sub.2 H.sub.4 F, CH.sub.2 OCH.sub.3, COCH.sub.3, COC.sub.2 H.sub.5, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, NO.sub.2, NH.sub.2, NH.sub.2.HCl, NH.sub.2.HAc, NH.sub.2.1/2H.sub.2 SO.sub.4 , NH.sub.2.1/3H.sub.3 PO.sub.4, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, OH, CN, N.sub.3, SO.sub.2 H, SO.sub.2 NH.sub.2 , SO.sub.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: July 26, 1994
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Xiao-Ming Zhou, Zhe-Qing Wang, Jang-Yang Chang, Hong-Xing Chen, Yung-Chi Cheng, Ya-Ching Shen, Fu-Shen Han, Hong Hu, Yi-Lin Zhang
  • Patent number: 5332743
    Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: July 26, 1994
    Assignee: McNeilab, Inc.
    Inventors: Ellen W. Baxter, Allen B. Reitz
  • Patent number: 5328917
    Abstract: The present invention relates to piperidine derivatives of the formula: ##STR1## wherein, R, R.sup.1, R.sup.3, X, and n are defined in the specification, pharmaceutical compositions thereof and methods of treating anoxia, traumatic injury, ischemia, migraine and epilepsy.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: July 12, 1994
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Anders Kanstrup, Jane M. Lundbeck
  • Patent number: 5306720
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: April 26, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5302599
    Abstract: A therapeutically useful compound of formula I ##STR1## or pharmaceutically acceptable salts thereof where A and B are oxygen, sulfur or CH.sub.2, X is an amine moiety as defined herein and R.sub.1 and R.sub.2 are as defined herein having 5HT.sub.1A neuronal activity and/or dopamine receptor activity useful in the treatment of central nervous system and cardiovascular system disorders.
    Type: Grant
    Filed: September 15, 1992
    Date of Patent: April 12, 1994
    Assignee: The Upjohn Company
    Inventors: Michael D. Ennis, Mark E. Baze
  • Patent number: 5300516
    Abstract: Musacarinic receptor antagonists, particularly useful in the treatment of irritable bowel syndrome, of formula (I), or a pharmaceutically acceptable salt thereof, where m is 1 or 2; R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.4 alkyl or together represent --(CH.sub.2).sub.p -- where p is an integer of from 2 to 5; R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; wherein Z is a direct link; --CH.sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; and R.sup.4 is a group of formulae (II), (III), (IV) or Het, where R.sup.5 and R.sup.6 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.7 R.sup.8, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH)(C.sub.1 -C.sub.4 alkyl), --C(OH)(C.sub.1 -C.sub.4 alkyl).sub.2, --SO.sub.2 NH.sub.2 , (CH.sub.2).sub.n CONR.sup.7 R.sup.8 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl); R.sup.7 and R.sup.8 are each independently H or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 11, 1992
    Date of Patent: April 5, 1994
    Assignee: Pfizer Inc.
    Inventors: Alexander R. Mackenzie, Peter E. Cross
  • Patent number: 5300500
    Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed.
    Type: Grant
    Filed: December 8, 1992
    Date of Patent: April 5, 1994
    Assignees: The University of North Carolina at Chapel Hill, Yale University
    Inventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Yi-Lin Zhang
  • Patent number: 5286866
    Abstract: The present invention pertains to a new class of compounds which can be characterized as 1,4-disubstituted piperidinyl compounds useful as antiarrhythmics, analgesics, and serotonin 5HT.sub.2 antagonists.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: February 15, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John E. Koerner, Richard C. Dage, Tung Li
  • Patent number: 5286881
    Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 15, 1994
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
  • Patent number: 5284857
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: February 8, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5281595
    Abstract: The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B ##STR1## wherein R.sub.1 +R.sub.2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 1-3 C-atoms and the remaining R and Z variables are defined as disclosed herein, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: January 25, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Josephus H. M. Lange, Gerrit P. Toorop, Ineke v. Wijngaarden, Jacobus A. J. den Hartog
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5260453
    Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: November 9, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffrey B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
  • Patent number: 5258401
    Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: November 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick
  • Patent number: 5256673
    Abstract: Indole derivatives of the general formula I ##STR1## wherein Ind is an indol-3-yl radical which is substituted by a hydroxymethyl or COW group and can additionally be monosubstituted or disubstituted by alkyl, O-alkyl, OH, F, Cl or Br,W is H, OH, Oalkyl, NH.sub.2, NHalkyl or N(alkyl).sub.2,A is --(CH.sub.2).sub.n --, CH.sub.2 --S--CH.sub.2 CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 CH.sub.2 or --CH.sub.2 --SO.sub.2 --CH.sub.2 CH.sub.
    Type: Grant
    Filed: July 10, 1989
    Date of Patent: October 26, 1993
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Henning Bottcher, Hans-Heinrich Hausberg, Christoph Seyfried, Klaus-Otto Minck
  • Patent number: 5250681
    Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.
    Type: Grant
    Filed: February 15, 1991
    Date of Patent: October 5, 1993
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura