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
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
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.
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.
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
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
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
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.
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
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
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.
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
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
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
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.
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.
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
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
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
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
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
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.
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
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.
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.
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.
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.
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.
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
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
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
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
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
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
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!.
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%.
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
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
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.
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.
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
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##
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
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
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
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