Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/380)
  • Patent number: 6818644
    Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc Rf, Rg and m, n and X are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyseride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: November 16, 2004
    Assignee: Boehringer Ingelheim Pharm GmbH & Co, KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Publication number: 20040180884
    Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): 1
    Type: Application
    Filed: December 23, 2003
    Publication date: September 16, 2004
    Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Ichiro Tanaka, Masayuki Tanaka, Masahiko Hagihara
  • Publication number: 20040175314
    Abstract: A method of scavenging oxygen in an atmosphere or liquid comprising the steps of: (i) treating an anthraquinone compound according to the formula: (I) wherein X1-X4 and R1-R4 are as defined in the claims, with predetermined conditions so as to reduce the anthraquinone compound to a reduced form oxidizable by oxygen; and ii) exposing the atmosphere or liquid to said compound; such that at least a portion of teh oxygen in teh atmosphere or liquid is removed through oxidation of the reduced form of the anthraquinone compound, and wherein steps i) and ii) may be carried out in either order.
    Type: Application
    Filed: May 12, 2004
    Publication date: September 9, 2004
    Inventors: Mark Andrew Horsham, Andrew David Scully, James Keith Gerard Murphy
  • Publication number: 20040162430
    Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection.
    Type: Application
    Filed: February 20, 2004
    Publication date: August 19, 2004
    Applicant: Wyeth
    Inventors: Wayne E. Childers, Horace Fletcher, Magid A. Abou-Gharbia, John P. Yardley
  • Publication number: 20040110756
    Abstract: The invention relates to new anthracene derivatives of the general Formula 1 and to their synthesis and use as pharmaceutical preparations, especially for the treatment of a tumor.
    Type: Application
    Filed: July 17, 2003
    Publication date: June 10, 2004
    Inventors: Peter Emig, Eckhard Gunther, Beate Aue, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt
  • Publication number: 20040097734
    Abstract: The invention relates to novel aryl- and heteroarylcarboxamides of the general formula (1), their preparation and use as medicaments, in particular for the treatment of tumors.
    Type: Application
    Filed: June 27, 2003
    Publication date: May 20, 2004
    Inventors: Matthias Gerlach, Peter Emig, Emmanuel Polymeropoulos, Gilbert Muller, Peter Schmidt, Silke Baasner, Eckhard Gunther
  • Patent number: 6730784
    Abstract: Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: May 4, 2004
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
  • Patent number: 6720323
    Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is 0 or an integer from 1 to 4 inclusive, (provided that when b is 0, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazo
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: April 13, 2004
    Assignee: Angiogene Pharmaceuticals Limited
    Inventor: Jean Claude Arnould
  • Patent number: 6713651
    Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 30, 2004
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Patent number: 6703385
    Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is COCONH2 or the like; Q1 is a nitrogen atom or C—R4; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; R21 and R22 are hydrogen atoms or the like; X is —CR23R24— or the like wherein R23 and R24 are hydrogen atoms or the like; Y is —CR25R26— or the like wherein R25 and R26 are hydrogen atoms or the like; Z is CH2 or the like; a broken line ( - - - ) represents the presence or absence of a bond, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: March 9, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Masahiro Fuji, Makoto Adachi, Tomoyuki Ogawa
  • Publication number: 20040029895
    Abstract: Dibenzosuberanyl piperazine derivatives represented by the following formula (I): 1
    Type: Application
    Filed: May 22, 2003
    Publication date: February 12, 2004
    Inventors: Tsutomu Takeuchi, Hiroaki Takayanagi, Seiki Kobayashi, Yumiko Osa, Yumiko Suzuki, Yoko Sato, Masakazu Sakaguchi, Yoshiyuki Miyata
  • Patent number: 6683115
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: January 27, 2004
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Publication number: 20030166637
    Abstract: The present invention relates to substituted piperazine derivatives of general formula 1
    Type: Application
    Filed: October 9, 2002
    Publication date: September 4, 2003
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Patent number: 6593497
    Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: July 15, 2003
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Edmund J. Moran
  • Publication number: 20030114442
    Abstract: The present invention relates to substituted piperazine derivatives of general formula 1
    Type: Application
    Filed: October 8, 2002
    Publication date: June 19, 2003
    Inventors: Armin Heckel, Thorsten Lehmann-Lintz, Leo Thomas, Michael Mark
  • Publication number: 20030078237
    Abstract: Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C═O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof. Compounds of formula (I) are selective NMDA receptor modulating agents and, therefore, may be used to advantage in vitro in neuroassays and in vivo in the treatment of disorders of the CNS.
    Type: Application
    Filed: September 3, 2002
    Publication date: April 24, 2003
    Inventors: Daniel T Monaghan, David E Jane, Heong Wai Tse
  • Patent number: 6541669
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: April 1, 2003
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Publication number: 20030013704
    Abstract: 1
    Type: Application
    Filed: June 12, 2002
    Publication date: January 16, 2003
    Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • Patent number: 6492355
    Abstract: The invention provides compounds of general formula in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: December 10, 2002
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber, Michael P. Mortimore
  • Publication number: 20020173500
    Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (Ia), 1
    Type: Application
    Filed: December 18, 2001
    Publication date: November 21, 2002
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
  • Publication number: 20020169164
    Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Application
    Filed: March 27, 2002
    Publication date: November 14, 2002
    Applicant: Warner-Lambert Company
    Inventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 6451801
    Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferable asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 17, 2002
    Assignee: UCB, S.A.
    Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
  • Publication number: 20020127756
    Abstract: The invention relates to tuned multifunctional linker molecules for charge transport through organic-inorganic composite structures. The problem underlying the present invention is to provide multifunctional linker molecules for tuning the conductivity in nanoparticle-linker assemblies which can be used in the formation of electronic networks and circuits and thin films of nanoparticles.
    Type: Application
    Filed: December 6, 2001
    Publication date: September 12, 2002
    Inventors: Jurina Wessels, William Ford, Akio Yasuda
  • Publication number: 20020107235
    Abstract: The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: August 8, 2002
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20020103191
    Abstract: Dibenzofluorene derivatives having a formula selected from the group consisting of 1
    Type: Application
    Filed: January 14, 2002
    Publication date: August 1, 2002
    Applicant: Board of Regents, The University of Texas System
    Inventors: Frederick F. Becker, Bimal K. Banik
  • Patent number: 6387389
    Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 14, 2002
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
  • Publication number: 20020002169
    Abstract: Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.
    Type: Application
    Filed: December 7, 2000
    Publication date: January 3, 2002
    Inventors: John H. Griffin, Yu-Hua Ji, Mathai Mammen, Daniel Marquess, Edmund J. Moran, Jonathan W. Wray
  • Patent number: 6323206
    Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: November 27, 2001
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
  • Patent number: 6274583
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: August 14, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Patane, Mark G. Bock, Randall C. Newton
  • Patent number: 6184224
    Abstract: Dibenzofluorene derivatives having a formula selected from the group consisting of and salts thereof have antitumor activity. At least one of R1-R13 in formula (I) or R1-R12 in formula (II) is —R14Z. R14 is a substituted or unsubstituted amino or amido group having from 1-12 carbon atoms, and Z is a substituted or unsubstituted heterocyclic group having from 1-12 carbon atoms. The remainder of R1-R13 in formula (I) or R1-R12 in formula (II) are independently selected from the group consisting of hydrogen, hydroxyl, halogen, nitro, substituted or unsubstituted amino or amido groups having from 1-12 carbon atoms, and alkyl groups having 1-12 carbon atoms.
    Type: Grant
    Filed: December 1, 1998
    Date of Patent: February 6, 2001
    Assignee: Board of Regents, The University of Texas System
    Inventors: Frederick F. Becker, Bimal K. Banik
  • Patent number: 6133268
    Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: March 18, 1999
    Date of Patent: October 17, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
  • Patent number: 6130220
    Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: October 10, 2000
    Assignees: Syntex (USA) Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
  • Patent number: 6130221
    Abstract: Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the composition is administered to a test animal that has received an injection of DMS, it reduces the mean volume of tissue occupied by disrupted DMS, reduces the ratio of the number of inflammatory cells per DMS, or increases the ratio of the number of macrophages containing disrupted DMS per DMS, are useful for treating cerebral amyloidosis.
    Type: Grant
    Filed: May 19, 1997
    Date of Patent: October 10, 2000
    Assignee: Nymox Corporation
    Inventors: Paul Averback, Hossein Ghanbari, Iraj Beheshti, David Morse
  • Patent number: 6096888
    Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: August 1, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Antonino Suarato, Jacqueline Lansen, Michele Caruso, Dario Ballinari, Tiziano Bandiera
  • Patent number: 6063924
    Abstract: Compounds of formulaA(B).sub.x (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine, diketopyrrolopyrrole or azo series, which radical A contains x N-atoms linked with B, preferably with at least one immediately adjacent or conjugated carbonyl group.B is a group of formula ##STR1## and, if x=2, 3 or 4, can also be one, two or three hydrogen atom(s), and wherein Q is a group of formula ##STR2## These soluble chromophores can be readily converted to the corresponding pigments by heating, even in the substrate into which they can be incorporated without any difficulty in dissolved form.R.sub.1 -R.sub.9 are as defined herein.
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: May 16, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Veronique Hall-Goulle
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6048877
    Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 6025493
    Abstract: Disclosed arm compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 allyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: February 15, 2000
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 6015900
    Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.
    Type: Grant
    Filed: November 23, 1998
    Date of Patent: January 18, 2000
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5998412
    Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: December 7, 1999
    Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
  • Patent number: 5998615
    Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: December 7, 1999
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Antonino Suarato, Jacqueline Lansen, Michele Caruso, Dario Ballinari, Tiziano Bandiera
  • Patent number: 5994543
    Abstract: A novel class of antibiotics, designated bravomicins, is obtained by fermentation of a strain of Micromonospora polytrota. Six bioactive compounds, designated bravomicins A, B, C, D, E and F, are obtained and found to be useful in the treatment of a wide variety of bacterial diseases.
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: November 30, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yue-Zhong Shu, Jie Chen, Kin Sing Lam, Judith A. Veitch, Daniel Brown
  • Patent number: 5916889
    Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: June 29, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
  • Patent number: 5712280
    Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the Formula 1.0 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: January 27, 1998
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, Randall R. Rossman, F. George Njoroge
  • Patent number: 5703083
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addidon salts thereof wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen, halogen, hydroxy, alkyl, alkoxy, amino, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, cyano, nitro, trifluoromethyl, or trifluoromethoxy;R.sub.8 is hydrogen or lower alkyl;X represents an optionally substituted alkylene group; andY represents a mono-, di- or trisubsituted cyclic amino groupwhich compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parldnsonism 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 15, 1996
    Date of Patent: December 30, 1997
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Jun Yuan
  • Patent number: 5703237
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy; --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.
    Type: Grant
    Filed: April 18, 1996
    Date of Patent: December 30, 1997
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Jan William Francis Wasley
  • Patent number: 5703235
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 21, 1996
    Date of Patent: December 30, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5686586
    Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: November 11, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5659033
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl.Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.
    Type: Grant
    Filed: September 13, 1995
    Date of Patent: August 19, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5612479
    Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.
    Type: Grant
    Filed: August 17, 1994
    Date of Patent: March 18, 1997
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Jimmy D. Earls