Additional Polycyclo Heterocyclic Ring System Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/454)
  • Patent number: 5651923
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5650098
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: July 22, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5646147
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: July 8, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5645767
    Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: July 8, 1997
    Assignee: Transitions Optical, Inc.
    Inventor: Barry Van Gemert
  • Patent number: 5637262
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: June 10, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5624950
    Abstract: Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught.
    Type: Grant
    Filed: January 29, 1996
    Date of Patent: April 29, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Daniel Achard, Serge Grisoni, Evelyne James-Surcouf, Jean-Luc Malleron, Anne Morgat, Jean-Fran.cedilla.ois Peyronel, Jean-Fran.cedilla.ois Sabuco, Michel Tabart
  • Patent number: 5623005
    Abstract: A naphthopyran compound of general formula (I) ##STR1## wherein R.sub.1 represents a group of the formula --NR.sub.2 R.sub.3 wherein each of R.sub.2 and R.sub.3, which may be the same or different, independently represents an alkyl group, or a carbocyclic or heterocyclic group, or R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are attached represent a heterocyclic ring having one or more hetero atoms and which may optionally carry at least one substituent selected from alkyl, aryl, or heteroaryl groups; each of R.sub.4 and R.sub.5, which may be the same or different, independently represents an alkyl, alkenyl, carbocyclic or heterocyclic group, or R.sub.4 and R.sub.5 taken together with the carbon atom to which they are attached form a carboxylcyclic ring or a heterocyclic ring; and R.sub.6 represents a hydrogen atom or a substituent selected from alkyl, alkoxy, aryl, aryloxy, heteroaryl, halogen, a group of formula R.sub.
    Type: Grant
    Filed: November 2, 1995
    Date of Patent: April 22, 1997
    Assignee: Pilkington PLC
    Inventors: Martin Rickwood, Katharine E. Smith, Christopher D. Gabbutt, John D. Hepworth
  • Patent number: 5616705
    Abstract: Compounds of the formula I ##STR1## where the substituents have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.
    Type: Grant
    Filed: April 19, 1996
    Date of Patent: April 1, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
  • Patent number: 5614633
    Abstract: Novel benzopyran and benzoxazine derivatives represented by the general formula: ##STR1## wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: March 25, 1997
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Haruhiko Sato, Takenori Ishizawa, Hiroyuki Nabata
  • Patent number: 5607939
    Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: March 4, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
  • Patent number: 5607961
    Abstract: Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: March 4, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph A. Cipollina, Ronald J. Mattson, Charles P. Sloan
  • Patent number: 5578252
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, examples of which are substituted with an oxy-bearing substituent at the number 8 carbon atom and with either an alkyl group at the number 7 carbon atom or with a carbonyl bearing substituent at the number 9 carbon atom and certain substituents at the 3-position of the pyran ring, e.g., 3,3-spirofluoren-9-ylidene 8-methoxy-9-carbomethoxy-3H-naphtho[2,1-b]pyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: November 29, 1995
    Date of Patent: November 26, 1996
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5573712
    Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds having certain substituents at the number 5 and 6 carbon atoms of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: November 12, 1996
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, Barry V. Gemert, David B. Knowles
  • Patent number: 5552090
    Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds substituted at the 3 position of the pyran ring with (i) an aryl substituent and (ii) a phenyl substituent having a 5- or 6-member heterocyclic ring fused at the number 3 and 4 carbon atoms of the phenyl substituent, and at the 6 position of the naphthyl portion of the naphthopyran compound with a nitrogen-containing heterocyclic ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 3, 1996
    Assignee: PPG Industries, Inc.
    Inventors: Barry Van Gemert, David B. Knowles
  • Patent number: 5541199
    Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 30, 1996
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5539125
    Abstract: There are disclosed a 1-azabicyclo[3.3.0]octan derivative of the formula ##STR1## wherein n is an integer of 1-5; and Ar is an aromatic residue. a pharmacologically acceptable salt of the compound, a process for the preparation of the compound and salt as well as use thereof as hypermotility agents.
    Type: Grant
    Filed: June 13, 1995
    Date of Patent: July 23, 1996
    Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Yutaka Baba, Toshinao Usui, Takuji Kakigami, Yoshiro Ozeki, Katsura Tsukamoto, Nobuyuki Itoh
  • Patent number: 5539112
    Abstract: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 23, 1996
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tsutomu Akama, Shun-ichi Ikeda, Yasushi Shida, Masaji Kasai, Hiroyuki Ishida, Uichiro Kimura, Katsushige Gomi, Hiromitsu Saito, Kimihisa Ueno
  • Patent number: 5519023
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.
    Type: Grant
    Filed: July 2, 1993
    Date of Patent: May 21, 1996
    Assignee: Adir et Compagnie
    Inventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
  • Patent number: 5516789
    Abstract: Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: May 14, 1996
    Assignee: Abbott Laboratories
    Inventors: Clint D. W. Brooks, Andrew O. Stewart, Anwer Basha, Randy L. Bell
  • Patent number: 5508450
    Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: April 16, 1996
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
  • Patent number: 5506262
    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 synthetase, 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: November 10, 1993
    Date of Patent: April 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
  • Patent number: 5502209
    Abstract: There are disclosed a benzopyrancarboxamide derivative of the formula ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkyl group; R.sup.2 is hydrogen atom, a lower alkyl group, halogen atom, an amino radical or an acylamino group; R.sup.3 is hydrogen atom, a lower alkyl group, a lower alkoxy group or halogen atom; dotted line is a possible double bond; and n is an integer of 1-5,and a pharmacologically acceptable salt of the compound, a process for the preparation of the compound and salt as well as use thereof.
    Type: Grant
    Filed: June 13, 1995
    Date of Patent: March 26, 1996
    Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Yutaka Baba, Toshinao Usui, Takuji Kakigami, Yoshiro Ozeki, Katsura Tsukamoto, Nobuyuki Asaeda, Nobuyuki Itoh
  • Patent number: 5500442
    Abstract: The present invention relates to novel cyclobut-3-ene-1,2-dione-3-yl substituted benzopyrans, indanes and tetrahydronaphthalenones having smooth muscle relaxant activity, pharmaceutical compositions containing them, and to their use in the treatment of diseases and disorders involving excessive smooth muscle contractions in the cardiovascular system, urinary tract, pulmonary system, or gastrointestinal tract.The compounds of this invention are represented by Formula (I): ##STR1## wherein: the substituents are as defined herein.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: March 19, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings, William A. Kinney
  • Patent number: 5500425
    Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: March 19, 1996
    Assignee: Aktiebolaget Astra
    Inventors: Lars-Gunnar Larsson, Lucy A. Renyl, Svante B. Ross, Daniel D. Sohn, Seth-Olov Thorberg
  • Patent number: 5482960
    Abstract: Novel indole and indoline nonpeptide antagonists of endothelin I are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure and subarachnoid hemorrhage.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: January 9, 1996
    Assignee: Warner-Lambert Company
    Inventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
  • Patent number: 5482942
    Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: January 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings
  • Patent number: 5475105
    Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: December 12, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Liiane Unger, Berthold Behl, Hans-Juergen Teschendorf, Rainer Munschauer
  • Patent number: 5468874
    Abstract: A novel benzothiophene/indole-substituted maleimide derivative, a photochromic material and an optical recording material using the same. The benzothiophene/indole-substituted maleimide derivative is represented by the following formula (1): ##STR1## or the following formula (2): ##STR2## wherein R is a substituted or an unsubstituted monovalent hydrocarbon group, R.sup.1 and R.sup.2 are a hydrogen atom, an alkyl group, an alkylthio group or an alkoxy group under the condition where at least either one of them is an alkylthio group or an alkoxy group, R.sup.3 is an alkyl group or an acyl group, and rings A and B may not be substituted or may be substituted with an alkyl group, an alkoxy group or a halogen atom, respectively.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: November 21, 1995
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Fumio Sugai, Masahiro Irie
  • Patent number: 5468767
    Abstract: Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.
    Type: Grant
    Filed: January 6, 1994
    Date of Patent: November 21, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph A. Cipollina, Ronald J. Mattson, Charles P. Sloan
  • Patent number: 5466398
    Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.
    Type: Grant
    Filed: June 21, 1993
    Date of Patent: November 14, 1995
    Assignee: Transitions Optical, Inc.
    Inventors: Barry Van Gemert, Anil Kumar
  • Patent number: 5458815
    Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds substituted at the 3 position of the pyran ring with (i) an aryl substituent and (ii) a phenyl substituent having a 5- or 6-member heterocyclic ring fused at the number 3 and 4 carbon atoms of the phenyl substituent. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: September 8, 1994
    Date of Patent: October 17, 1995
    Assignee: Transitions Optical, Inc.
    Inventor: David B. Knowles
  • Patent number: 5453515
    Abstract: Benzophenone iminodiimides of the formula I ##STR1## which Y denotes hydroxyl or carboxyl, R.sub.1 denotes the optionally substituted radicals alkylene, phenylene or benzylidene, R.sub.2 denotes the radicals OH, substituted or unsubstituted alkyl or NH--CO--NHR.sub.3 and R.sub.3 denotes the radicals H, alkyl, phenyl or benzyl, processes for their preparation and polymers prepared therefrom.
    Type: Grant
    Filed: December 27, 1993
    Date of Patent: September 26, 1995
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Gerd Greber, deceased, Heinrich Gruber, Afschin Hassanein
  • Patent number: 5443940
    Abstract: Disclosed herein is an optical recording material containing a photochromic compound which is expressed in the following general formula (I): ##STR1## where A represents an oxygen atom or a substituted or unsubstituted nitrogen atom, R.sub.1 represents an alkoxy group, R.sub.2 to R.sub.5 represent substituents such as a hydrogen atom, a halogen atom, a hydroxy group, a substituted or unsubstituted alkyl group and the like respectively, and B represents a substituted or unsubstituted thiophene ring, benzothiophene ring, pyrrole ring or indole ring.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: August 22, 1995
    Assignees: Sanyo Electric Co., Ltd., Kobe Natural Products & Chemicals Co., Ltd.
    Inventors: Fumio Tatezono, Toshio Harada, Masahiro Irie, Meguru Ohara
  • Patent number: 5439940
    Abstract: The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: August 8, 1995
    Assignee: EGIS Gyogyszergyar Rt.
    Inventors: Klara Reiter nee Eszes, Zoltan Budai, Tibor Mezei, Gabor Blasko, Gyula Simig, Istvan Gyertyan, Luiza Petocz, Marton Fekete, Katalin Szemeredi, Istvan Gacsalyi, Gabor Gigler, Ludmilla Rohacas nee Zamkovaja, Maria Szecsey nee Hegedus, Eniko Szirt nee Kiszelly
  • Patent number: 5428052
    Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycoalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.
    Type: Grant
    Filed: December 2, 1993
    Date of Patent: June 27, 1995
    Assignee: Centre Internationale de Recherches Dermatologiques (C.I.R.D.)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 5420155
    Abstract: A class of 4-hydroxy-2(1H)-pyrrolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
    Type: Grant
    Filed: May 10, 1993
    Date of Patent: May 30, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
  • Patent number: 5416097
    Abstract: This invention relates to novel potassium channel activators and their acid addition salts. The compounds of the invention as potassium channel activators/openers have therapeutic value in a number of physiological areas such as hypertension, cardiac ischemia, cerebral ischemia, broncho constriction and neurodegenerative diseases. Pharmaceutical compositions are proposed for the compounds which are of the following formulae: ##STR1## wherein: R is H or OH;- - - the dotted line at position 3,4 represents the presence or absence of a double bond. ##STR2## the pharmaceutically acceptable acid addition salts thereof, with the provisos that:a) R is H when 3,4 is a double bond; andb) R is OH when 3,4 is a single bond.
    Type: Grant
    Filed: May 19, 1993
    Date of Patent: May 16, 1995
    Assignee: Berlex Laboratories, Inc.
    Inventors: Paul W. Erhardt, Kenneth J. Shaw
  • Patent number: 5409929
    Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: April 25, 1995
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Engelbert Ciganek
  • Patent number: 5405976
    Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: April 11, 1995
    Assignee: Polaroid Corporation
    Inventors: Stephen J. Telfer, Robert P. Short, Stephen G. Stroud, Anthony J. Puttick, Socorro Ramos, Michael J. Zuraw
  • Patent number: 5405830
    Abstract: This invention relates to certain herbicidal ethers, agriculturally suitable compositions thereof, and a method for their use as broad spectrum preemergent or postemergent herbicides.
    Type: Grant
    Filed: July 29, 1993
    Date of Patent: April 11, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Alan R. Rendina, Wendy S. Taylor
  • Patent number: 5395846
    Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: March 7, 1995
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
  • Patent number: 5391569
    Abstract: A compound selected from those of formula (I): ##STR1## in which the groups R.sub.1 to R.sub.8 are as defined the description. Medicaments.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: February 21, 1995
    Assignee: Adir et Compagnie
    Inventors: Jean-Daniel Brion, Guillaume Le Baut, Guillaume Poissonnet, Lucy De Montarby, Larbi Belachmi, Jacqueline Bonnet, Massimo Sabatini, Charles Tordjman
  • Patent number: 5389668
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: January 12, 1994
    Date of Patent: February 14, 1995
    Assignee: Adir Et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5374643
    Abstract: Novel compounds useful, for example, in the treatment of ischemic conditions and arrhythmia having the formula I ##STR1## wherein X is oxygen, sulfur or --NCN and the R groups are as defined herein.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: December 20, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail S. Atwal, George C. Rovnyak
  • Patent number: 5373019
    Abstract: The present invention provides compounds and pharmaceutical compositions containing indolones of the general formula: ##STR1## These indolones where n.dbd.o and the pharmaceutical compositions containing these compounds are used for the treatment of diseases in which erythrocyte and thrombocyte aggregation play an important part, especially for the inhibition of aggregation of these cells.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: December 13, 1994
    Assignee: Boehringer Mannheim GmbH
    Inventors: Harald Zilch, Alfred Mertens, Wolfgang Von Der Saal, Erwin Boehm, Klaus Strein
  • Patent number: 5371094
    Abstract: Azaheterocyclylmethyl-chromans are prepared by reaction of corresponding methylchromans with corresponding azaheterocyclic compounds, optionally with subsequent variation of the substituents. The azaheterocyclylmethyl-chromans can be used as active compounds in medicaments, in particular for the treatment of diseases of the central nervous system.
    Type: Grant
    Filed: November 30, 1992
    Date of Patent: December 6, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean M. V. De Vry, Wolfgang Dompert, Henning Sommermeyer
  • Patent number: 5354873
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: October 11, 1994
    Assignee: Polaroid Corporation
    Inventors: Richard M. Allen, Peter K. Chu, John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5338735
    Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5326759
    Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5314907
    Abstract: The invention relates to the derivatives of general formula (I): ##STR1## in which: Z represents an oxygen atom or a sulfur atom,R.sub.1 represents a hydrogen atom or an alkyl group,R.sub.2 represents a hydrogen atom or an alkyl group,1.ltoreq.n.ltoreq.6,R.sub.3 represents a nitrile group, an optionally substituted amino group or any one of the groups described in the description andmedicinal products containing the same.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: May 24, 1994
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Beatrice Guardiola