Each Of The Three Cyclos Is Six-membered (e.g., Benzoquinolines, Etc.) Patents (Class 546/101)
  • Patent number: 6391887
    Abstract: The invention relates to compounds of formula (I), as defined herein. The invention also relates to the use of the inventive compounds for treatment of a disease caused by the effects of nitrogen monoxide in pathological conditions.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: May 21, 2002
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Holscher, Detlev Sulzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
  • Patent number: 6383666
    Abstract: Disclosed are new organometallic complex molecules having light-emitting and electron-transporting characteristics. Also disclosed is organic EL (electroluminescent) devices using these organometallic complex molecules as electron-transporting materials. The organometallic complex molecules are used to form a light-emitting layer with or without doping of another light-emitting material. The organometallic complex molecules can also be used in an electron-transporting layer of the organic EL device. The organic EL devices incorporating the organometallic complex molecules have high thermal stability.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: May 7, 2002
    Assignee: LG Chem, Ltd.
    Inventors: Kongkyeom Kim, Sehwan Son, Okhee Kim, Seok-Hee Yoon, Hyo-Seok Kim, Jaesoon Bae, Youn-Gu Lee
  • Publication number: 20020045065
    Abstract: An organometallic luminescent material selected from the group consisting of the compounds of formulae (I) to (V) of the present invention can emit blue, green and red lights.
    Type: Application
    Filed: August 31, 2001
    Publication date: April 18, 2002
    Applicant: NESSDISPLAY CO., Ltd.
    Inventors: Youngkyoo Kim, Jae-Gyoung Lee
  • Patent number: 6355650
    Abstract: The present invention relates to non-psychoactive derivatives of tetrahydro-cannabinol, which exhibit anti-inflammatory, analgesic and leukocyte antiadhesion activities. The invention includes novel derivatives of (3R,4R)-&Dgr;8-tetrahydrocannabinol-11-oic acids [hereinafter referred to as (3R,4R)-&Dgr;8-THC-11-oic acid], as well as pharmaceutical compositions containing the (3R,4R)-&Dgr;8-THC-11-oic acid derivatives. The invention further covers methods of administering the novel derivatives and pharmaceutical compositions as therapeutic agents in the treatment of pain and tissue inflammation. Non-psychoactive derivatives of &Dgr;8-THC-11-oic acid are described which have analgesic and anti-inflammatory properties.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: March 12, 2002
    Assignee: Atlantic Technology Ventures, Inc.
    Inventor: Sumner H. Burstein
  • Publication number: 20020002170
    Abstract: The invention provides a compound of formula I 1
    Type: Application
    Filed: July 16, 2001
    Publication date: January 3, 2002
    Inventors: Rainer M. Luond, Markus Banziger, Peter Frey
  • Publication number: 20020002156
    Abstract: An androgenic steroid compound of the formula: 1
    Type: Application
    Filed: June 9, 1999
    Publication date: January 3, 2002
    Inventors: C. EDGAR COOK, JOHN A. KEPLER, YUE-WEI LEE, MANSUKH C. WANI
  • Patent number: 6310208
    Abstract: Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: October 30, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Heinz Stadler, Jürgen Wichmann
  • Publication number: 20010034447
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: February 2, 2001
    Publication date: October 25, 2001
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy P. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Rena Natero, Joel Renick, Robert N. Sibley
  • Patent number: 6300339
    Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, T, X, Y, Z, R5, R6, R7, R8, Ar, k, m, n and p are as defined in the specification. These compounds are useful in treating or preventing conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 9, 2001
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6262064
    Abstract: The present invention relates to a composition, and method of use, of an actahydrobenzo[f]quinoline-based compound represented by the following structural formula: In this formula, R1 is —OH or —OCH3 and R2 is —H, —OH or —OCH3. In addition, R3 is a C1 to C2 saturated or unsaturated, alkyl group. Furthermore, R4 is an aryl group, wherein examples of suitable aryl groups, as defined herein, include phenyl and thienyl groups. The method of this invention relates to the use of the claimed composition to treat psychotic disorders, to treat Parkinson's disease, or to sedate a mammal by administering an effective amount of a claimed composition.
    Type: Grant
    Filed: January 26, 1999
    Date of Patent: July 17, 2001
    Assignees: The Board of Governors for Higher Education, The State of Rhode Island and Providence Plantations.
    Inventors: Mark Froimowitz, James N. Jacob
  • Patent number: 6258851
    Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: July 10, 2001
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
  • Patent number: 6248884
    Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.
    Type: Grant
    Filed: June 3, 1999
    Date of Patent: June 19, 2001
    Assignee: The Perkin-Elmer Corporation
    Inventors: Joe Y. L. Lam, Scott C. Benson, Steven M. Menchen
  • Patent number: 6239143
    Abstract: The present invention relates to compounds having pharmacological activity toward the 5-HT7 receptor. Pharmaceutical compositions and methods for their use in the treatment of CNS disorders are described.
    Type: Grant
    Filed: June 25, 1999
    Date of Patent: May 29, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Gary Avonn Cain, John Francis McElroy
  • Patent number: 6211372
    Abstract: A compound of the formula: wherein X′ is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A′ and A″ are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z′ is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z″ is hydrogen or a substituent other than hydrogen; Y is C═O, C(OH)R′ or C—A, where R′ is hydrogen or lower alkyl is provided.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: April 3, 2001
    Inventors: Peter Anthony Crooks, Niranjan Madhukar Deo
  • Patent number: 6150375
    Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: November 21, 2000
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco, Kevin L. Haehl, Thomas J. Kress, James P. Wepsiec
  • Patent number: 6130217
    Abstract: This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).
    Type: Grant
    Filed: September 20, 1995
    Date of Patent: October 10, 2000
    Assignee: Pfizer Inc
    Inventors: Lee Daniel Arnold, Jotham Wadsworth Coe, Takushi Kaneko, Mikel Paul Moyer
  • Patent number: 6090571
    Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group.Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: July 18, 2000
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
  • Patent number: 6084134
    Abstract: 9-Anthracenecarbaldehydes are obtained in a particularly advantageous manner by reacting the corresponding anthracene derivatives with dimethylformamide in the presence of phosphoryl chloride, hydrolyzing the resulting reaction mixture and precipitating the 9-anthracenecarbaldehyde that is formed by admixing a base.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: July 4, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventor: Wolfram Eichinger
  • Patent number: 6080752
    Abstract: A compound of formula (I): ##STR1## wherein R.sup.1 represents a group of formula (A) or (B): ##STR2## R.sup.2, R.sup.3, Ar, Y Ar.sup.
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: June 27, 2000
    Assignee: SmithKline Beecham PLC
    Inventors: Geoffrey Stemp, Stephen Allan Smith, Christopher Norbert Johnson, Phillip Jeffrey
  • Patent number: 6077850
    Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: June 20, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J. Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
  • Patent number: 6057334
    Abstract: The invention provides a compound of formula (I) wherein A, B, X, Y and R are as defined in the description, and a process for preparing them. The compounds of formula (I) arc useful as pharmaceuticals for the treatment of glaucoma and myopia.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: May 2, 2000
    Assignee: Novartis AG
    Inventors: Peter Gull, Rudolf Markstein, Max Peter Seiler
  • Patent number: 6048869
    Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: April 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Derek Von Langen, Susan D. Aster, Donald W. Graham
  • Patent number: 6034211
    Abstract: N-methylated .beta.-sheet nucleating peptidomimetics containing diarylheterocycle .beta.-turn mimics, and methods of making and using them.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: March 7, 2000
    Inventor: Jeffery W. Kelly
  • Patent number: 6034092
    Abstract: The present invention relates to 2-[2-[(2-hydroxyethyl)amino]ethyl]-5-[[2-methylamino)ethyl]amino]indazolo[ 4,3-gh]isoquinolin-6(2H)-one and the pharmaceutically acceptable acid addition salts thereof, of formula (I). This compound has shown a high a antitumor activity.
    Type: Grant
    Filed: June 22, 1998
    Date of Patent: March 7, 2000
    Assignee: Novuspharma S.p.A.
    Inventors: Ernesto Menta, Ambrogio Oliva, Silvano Spinelli, Paul Krapcho
  • Patent number: 5986100
    Abstract: A compound of the formula: ##STR1## wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C.dbd.O, C(OH)R' or C--A, where R' is hydrogen or lower alkyl is provided.
    Type: Grant
    Filed: April 2, 1998
    Date of Patent: November 16, 1999
    Inventors: Peter Anthony Crooks, Niranjan Madhukar Deo
  • Patent number: 5968944
    Abstract: The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.
    Type: Grant
    Filed: December 3, 1996
    Date of Patent: October 19, 1999
    Assignee: Pfizer Inc.
    Inventors: Gene M Bright, Willard M Welch, Jr.
  • Patent number: 5962469
    Abstract: The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Craig E. Thomas, Thomas L. Fevig, Stephen M. Bowen, Robert A. Farr, Albert A. Carr, David A. Janowick
  • Patent number: 5955468
    Abstract: Compounds of formula I ##STR1## wherein A, B, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, are useful for the treatment of conditions where prevention or delay of progressive atrophy of the optic nerve is desirable.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 21, 1999
    Assignee: Sandoz Ltd.
    Inventor: Rudolf Markstein
  • Patent number: 5952326
    Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: September 14, 1999
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
  • Patent number: 5888422
    Abstract: Fluorinated phenanthrene derivatives of the formula (I) ##STR1## in which the symbols and indices have the following meanings: E.sup.1, E.sup.2, E.sup.3, E.sup.4, E.sup.5 and E.sup.6 are identical or different and are --N--, --CF-- or --CH--;G is --CF.sub.2 CF.sub.2 -- or --CF.dbd.CF--;R.sup.1 and R.sup.2 are, for example, alkyl or alkoxy;M.sup.1, M.sup.2, M.sup.3 and M.sup.4 are, for example, O, --CO--O--, --O--CO-- or a single bond;A.sup.1 and A.sup.2 are, for example, 1,4-phenylene or pyrimidine-2,5-diyl;m and n are zero or one, but in total are not more than one,are suitable as components of liquid-crystalline mixtures.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: March 30, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Javier Manero, Rainer Wingen
  • Patent number: 5863928
    Abstract: The present invention relates to a composition, and method of use, of an octahydrobenzo?f!quinoline-based compound represented by structural formula (I). In this formula, R.sup.1 is --OH or --OCH.sub.3 and R.sup.2 is --H, --OH or --OCH.sub.3. In addition, R.sup.3 is a C1 to C2 saturated or unsaturated, alkyl group. Furthermore, R.sup.4 is an aryl group, wherein examples of suitable aryl groups, as defined herein, include phenyl and thienyl groups. The method of this invention relates to the use of the claimed compositions to treat psychotic disorders, to treat Parkinson's disease, or to sedate a mammal by administering an effective amount of a claimed composition.
    Type: Grant
    Filed: September 26, 1996
    Date of Patent: January 26, 1999
    Assignee: The Board of Governors for Higher Education the State of Rhode Island and Providence Plantation.
    Inventors: Mark Froimowitz, James N. Jacob
  • Patent number: 5854273
    Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: December 29, 1998
    Assignee: ADIR et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
  • Patent number: 5846666
    Abstract: An electroluminescent device comprised of a metal thioxinoid of the formula ##STR1## wherein M represents a metal; each n is a number of from 1 to 3; N is nitrogen, S is sulfur, and Z represents an aromatic moiety.
    Type: Grant
    Filed: February 27, 1997
    Date of Patent: December 8, 1998
    Assignee: Xerox Corporation
    Inventors: Nan-Xing Hu, Shuang Xie, Beng S. Ong, Zoran D. Popovic, Ah-Mee Hor
  • Patent number: 5789402
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 4, 1998
    Assignee: Eli Lilly Company
    Inventors: James E. Audia, David J. Hibschman, Joseph H. Krushinski, Jr., Thomas E. Mabry, Jeffrey S. Nissen, Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
  • Patent number: 5770382
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Beth Ann Badea, Alex M. Nadzan
  • Patent number: 5770378
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Youssef L. Bennani, Stacie S. Canan Koch, Beth Ann Badea, Jonathan J. Hebert, Alex M. Nadzan
  • Patent number: 5770383
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Youssef L. Bennani, Stacie S. Canan Koch, Beth Ann Badea, Jonathan J. Hebert, Luc J. Farmer, Alex M. Nadzan
  • Patent number: 5741789
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 21, 1998
    Assignee: Eli Lilly and Company
    Inventors: David J. Hibschman, Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
  • Patent number: 5723472
    Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: March 3, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Shuhei Miyazawa, Yorihisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
  • Patent number: 5717099
    Abstract: In the search for novel heteroanalogs of anthracendiones, 6,9-bis?(2-aminoethyl)amino!benzo?g!isoquinoline-5,10-dione dimaleate salt (BBR 2778), was selected as the most promising compound. New methods of synthesis produce the compound in purity greater than 99%.
    Type: Grant
    Filed: August 1, 1996
    Date of Patent: February 10, 1998
    Assignee: Boehringer Mannheim Italia S.p.A.
    Inventors: Silvano Spinelli, Roberto DiDomenico
  • Patent number: 5710273
    Abstract: A complex crystal is composed of anion of triiodine and cation of a fused compound consisting essentially of at least one nitrogen atom and at least 3 aromatic fused rings. Since the complex crystal has such a stable structure, it shows excellent heat resistance and excellent moisture resisting property. Furthermore, the complex crystal has light-polarizing performance because of an arrangement of the molecular chain of iodine. Moreover, the complex crystal exhibits excellent polarization because of an interaction between the fused compound and iodine. Therefore, the complex crystal is suitable for use as light-adjusting particles of a light valve or a light-adjusting glass.
    Type: Grant
    Filed: July 25, 1996
    Date of Patent: January 20, 1998
    Assignees: Toyota Jidosha Kabushiki Kaisha, Kabushiki Kaisha Toyota Chuo Kenkyusho
    Inventors: Arimitsu Usuki, Hisato Takeuchi, Narihito Tatsuda, Akane Okada, Toshio Kurauchi, Hiromitsu Tanaka, Shinobu Okayama, Kazuo Tojima, Akio Fukui, Toshiro Okamoto
  • Patent number: 5703231
    Abstract: The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A.sup.1, A.sup.2 and A.sup.3 are independently carbon or nitrogen and R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are known quinolone substituents; and wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety;or a protected form, salt, pharmaceutically-acceptable salt, biohydrolyzable ester, or solvate thereof;the process comprising reacting one or more organosilicon compounds with a compound having a structure according to Formula (II) ##STR2## wherein A.sup.1, A.sup.2 and A.sup.3, R.sup.1, R.sup.3, R.sup.4 and R.sup.6 as described above; wherein one of R.sup.1, R.sup.3 or R.sup.6 may be a lactam-containing moiety; and X is a leaving group;or a protected form, salt, biohydrolyzable ester, or solvate thereof.
    Type: Grant
    Filed: November 14, 1996
    Date of Patent: December 30, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Jared Lynn Randall, Jane Ellen Godlewski
  • Patent number: 5698550
    Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: December 16, 1997
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
  • Patent number: 5688950
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R1-R.sub.4 represent organic or inorganic groups;A represents an alkylene group of 2 to 6 carbon atoms optionally substituted with one or more alkyl groups having from 1 to 4 carbon atoms;Y represents methylene, oxygen, sulfur, or NH; andX is either N, C or CH,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
    Type: Grant
    Filed: April 23, 1996
    Date of Patent: November 18, 1997
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Jun Yuan, Andrew Thurkauf
  • Patent number: 5670511
    Abstract: Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
    Type: Grant
    Filed: January 16, 1996
    Date of Patent: September 23, 1997
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Joachim Marz, Hartmut Greiner, Christoph Seyfried, Gerd Bartoszyk
  • Patent number: 5643917
    Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2##
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: July 1, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel Lee Flynn, Robert L. Shone
  • Patent number: 5624933
    Abstract: Method of preparation of 6-fluoro-2-halogen quinoline of general formula (I) wherein R is a hydrogen atom or an alkyl radical and Hal and Hal' are identical or different halogen atoms. The invention is characterized in that a halogenating agent is made to act on hydroxy-1 quinoline of general formula (II) wherein Hal is defined as above and R.sub.1 is defined as R excepting a hydrogen atom, the acid function being optionally released if a 6-fluoro-2-halogen quinoline is to be obtained for which R is a hydrogen atom.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 29, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Herve Garcia, Roland Jacquot, Patrick Leon
  • Patent number: 5622962
    Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: April 22, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
  • Patent number: 5622961
    Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: April 22, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
  • Patent number: 5616776
    Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: April 1, 1997
    Assignee: Abbott Laboratories
    Inventors: Timothy L. Stuk, Anthony R. Haight, Francis A. J. Kerdesky, M. Robert Leanna, Howard E. Morton, Timothy A. Robbins, David Scarpetti, Jien-Heh J. Tien