The Hetero Ring Shares Ring Members With Each Of Two Benzene Rings In The Tricyclo Ring System (e.g., Morphanthridines, Etc.) Patents (Class 540/587)
  • Patent number: 6878822
    Abstract: A compound represented by formula (IA): in which (A) represents an ethylene group, a vinylene group or an o-arylene group; Ar1 and Ar2 each represent an aryl group; R1 and R2 each represent an alkyl group or an aryl group; R3 represents an alkyl group or an aryl group; R4 and R5 each represent a halogen atom, an alkyl group, an aryl group, an alkoxy group, an aryloxy group, a dialkylamino group, an N-alkyl-N-arylamino group or a diarylamino group; or Ar1 and R1, or Ar2 and R2 are taken together either directly or indirectly to form a ring; Ar1(R1)C?CH—(CH?CH)m— and Ar2(R2)C?CH—(CH?CH)n— are on the 2- or 3-position and the 7- or 8-position of the respective benzene rings; m and n each represent an integer of from 0 to 2; and p and q each represent an integer of from 0 to 3.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: April 12, 2005
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Tadahisa Sato
  • Patent number: 6770668
    Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: August 3, 2004
    Inventors: N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
  • Publication number: 20040002486
    Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Application
    Filed: December 7, 2001
    Publication date: January 1, 2004
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft, Michael H. Zeldin
  • Publication number: 20030191111
    Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Application
    Filed: January 21, 2003
    Publication date: October 9, 2003
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft, Michael H. Zeldin
  • Publication number: 20030065171
    Abstract: Disclosed are a luminescent element material comprising a polymer having a partial structure represented by formula (I) 1
    Type: Application
    Filed: May 9, 2002
    Publication date: April 3, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Tadahisa Sato, Hisashi Okada
  • Patent number: 6534497
    Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds that are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: March 18, 2003
    Assignees: Nuchem Pharmaceuticals, Inc., Children's Medical Center Corporation, Presidents and Fellows of Harvard College
    Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Jr., Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft, Michael H. Zeldin
  • Publication number: 20030004154
    Abstract: The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling the same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art.
    Type: Application
    Filed: February 12, 2002
    Publication date: January 2, 2003
    Inventors: Judith Aronhime, Ben-Zion Dolitzky, Yana Berkovich, Nissim Garti
  • Patent number: 6387544
    Abstract: Organic light emitting devices comprising a heterostructure for producing electroluminescence having a hole transporting layer with a glass structure. The hole transporting layer comprises a compound having a symmetric molecular structure. The end groups of the symmetric molecule are hole transporting diaryl amine moieties.
    Type: Grant
    Filed: December 2, 1998
    Date of Patent: May 14, 2002
    Assignees: The Trustees of Princeton University, The University of Southern California
    Inventors: Mark E. Thompson, Loy Douglas, Stephen R. Forrest, Bryan E. Koene, Diarmuid O'Brien
  • Publication number: 20010011087
    Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula 1,
    Type: Application
    Filed: February 8, 2001
    Publication date: August 2, 2001
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6201120
    Abstract: Disclosed is a three step synthesis of 11-aryl-5,6-dihydro-11H-dibenz[b,e]azepines from a 2-aminobenzophenone represented by the following structural formula: and a starting material represented by the following structural formula: Phenyl Ring A, Phenyl Ring B and Phenyl Ring C are independently unsubstituted or substituted with one, two or three substituents. Each substituent on Phenyl Ring A, Phenyl Ring B and Phenyl Ring C is independently chosen. R is —H, a aliphatic group, a substituted aliphatic group, an aryl group, a substituted aryl group, —C(O)—R′, —C(O)—H, —C(O)—NHR′, —S(O)2R′, —C(O)—C(O)—R′, —C(O)—C(O)—H, —C(S)—R′, —C(S)—H, —C(O)—OR′, —C(S)—OR′, —C(O)—SR′, —C(S)—SR′, —C(O)—NR′2 or —C(O)—C(S)—R′.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: March 13, 2001
    Assignee: Pharm-Eco Laboratories, Inc.
    Inventors: Adel M. Moussa, Richard J. Lombardy, Reem M. Haider, Minghua Sun
  • Patent number: 6172058
    Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: January 9, 2001
    Assignee: Lilly, SA
    Inventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
  • Patent number: 6066632
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds 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 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: August 17, 1999
    Date of Patent: May 23, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
  • Patent number: 6063921
    Abstract: Disclosed is a three step synthesis of 11-aryl-5,6-dihydro-11H-dibenz[b,e]azepines from a 2-aminobenzophenone represented by the following structural formula: ##STR1## and a starting material represented by the following structural formula: ##STR2## Phenyl Ring A, Phenyl Ring B and Phenyl Ring C are independently unsubstituted or substituted with one, two or three substituents. Each substituent on Phenyl Ring A, Phenyl Ring B and Phenyl Ring C is independently chosen.R is --H, a aliphatic group, a substituted aliphatic group, an aryl group, a substituted aryl group, --C(O)--R', --C(O)--H, --C(O)--NHR', --S(O).sub.2 R', --C(O)--C(O)--R', --C(O)--C(O)--H, --C(S)--R', --C(S)--H, --C(O)--OR', --C(S)--OR', --C(O)--SR', --C(S)--SR', --C(O)--NR'.sub.2 or --C(O)--C(S)--R'. R' is an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R.sub.1 is a leaving group.
    Type: Grant
    Filed: November 20, 1997
    Date of Patent: May 16, 2000
    Assignee: Pharm-Eco Laboratories, Inc.
    Inventors: Adel M. Moussa, Richard J. Lombardy, Reem M. Haider, Minghua Sun
  • 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: 6048856
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the formula ##STR1## wherein X, Y, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, R.sup.12, R.sup.13, A, r and s 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. These compounds are also useful for treating 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: December 14, 1998
    Date of Patent: April 11, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Karel Sindelar, Alexandra Silhankova, Otylie Konigova, Zdenek Polivka
  • Patent number: 6008213
    Abstract: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: December 28, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller
  • Patent number: 5952501
    Abstract: This invention encompasses compounds of the formula: where either R.sub.1 or R.sub.2 represents ##STR1## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organinc substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lower alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore 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 26, 1995
    Date of Patent: September 14, 1999
    Assignee: Neurogen Corporation
    Inventors: Alan Hutchison, Jun Yuan, Raymond F. Horvath
  • Patent number: 5929069
    Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: July 27, 1999
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventor: Koichi Shudo
  • Patent number: 5919780
    Abstract: Compounds of formula I ##STR1## wherein X is N or C--R.sup.9, Y is N--R.sup.10, CH.sub.2, O, S, SO, SO.sub.2, C.dbd.O or CH--OH,R is H or alkyl,R.sup.1 is heteroaryl,n is 1-5, andR.sup.2 -R.sup.10 are H or various substituents,are useful as inhibitors of protein farnesyl transferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.
    Type: Grant
    Filed: December 11, 1997
    Date of Patent: July 6, 1999
    Assignee: Warner Lambert Company
    Inventors: Gary L. Bolton, Annette M Doherty, James S. Kaltenbronn, John Quin, III, Jeffrey D. Scholten, Judith Sebolt-Leopold, Harold Zinnes
  • Patent number: 5869483
    Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
    Type: Grant
    Filed: April 24, 1996
    Date of Patent: February 9, 1999
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Fuk-Wah Sum
  • Patent number: 5834459
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: November 10, 1998
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventor: Jian-Min Fu
  • Patent number: 5753643
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent 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.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: May 19, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
  • Patent number: 5686466
    Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: November 11, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
  • Patent number: 5679679
    Abstract: Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl;each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: October 21, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5602124
    Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5602120
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
  • Patent number: 5594152
    Abstract: This invention comprises a process for production of a compound of the formula: ##STR1## in which R.sup.1 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), bromo, chloro, fluoro, iodo, --COlower alkyl(C.sub.1 -C.sub.3), and --CF.sub.3 ;R.sup.2 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), amino, bromo, chloro, fluoro, iodo, and --COlower alkyl(C.sub.1 -C.sub.3);or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy;R.sup.3 is an aldehyde or carboxcylic acid moiety;the moiety ##STR2## wherein Z represents substituted or unsubstituted phenyl ring or an optionally substituted 5 or 6-membered aromatic heterocyclic ring.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: January 14, 1997
    Assignee: American Cyanamid Company
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright
  • Patent number: 5552399
    Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; 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; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11 or R.sup.12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, 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 alkyloxy-carbonyl; R.sup.7 and R.sup.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 3, 1996
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Victor K. Sipido, Francisco J. Fern andez-Gadea, Jos e I. Andr es-Gil, Theo F. Meert, Pilar Gil-Lopetegui
  • Patent number: 5527800
    Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
    Type: Grant
    Filed: January 18, 1994
    Date of Patent: June 18, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
  • Patent number: 5512563
    Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: April 30, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Fuk-Wah Sum, Xuemei Du
  • Patent number: 5488046
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: January 30, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Robert A. Chrusciel, Timothy J. Hagen, E. Ann Hallinan, Jinglin Li, Sofya Tsymbalov, David B. Reitz
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5436333
    Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, amino, bromo, chloro, fluoro, iodo, C.sub.1 -C.sub.3 alkylcarbonyl or trifluoromethyl; R.sup.2 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 --C.sub.3 alkoxy, bromo, chloro, fluoro, iodo, or C.sub.1 -C.sub.3 alkylcarbonyl; or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy; the structure ##STR2## represents, as described in the specification, an ortho-fused phenyl moiety; an aromatic 5-membered heterocycle containing N, O, or S; or an aromatic 6-membered heterocycle containing N; all of which may be optionally substituted, are produced by reaction of ##STR3## where R.sup.3 is a masked aldehyde or carboxyl group, with 2-nitro-benzyl bromide followed by removal of the mask, reduction and cyclization.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: July 25, 1995
    Assignee: American Cyanamid Company
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright
  • Patent number: 5344828
    Abstract: Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.
    Type: Grant
    Filed: March 1, 1991
    Date of Patent: September 6, 1994
    Assignee: Hokuriku Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Sawanishi, Yasuo Ito, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kouji Morikawa
  • Patent number: 5317101
    Abstract: The invention relates to tricyclic heterocycles of the formula I ##STR1## wherein X is oxy, thio, sulphinyl, sulphonyl, amino, (1-4C)alkylamino or methylene;Y is carbonyl or methylene;each R.sup.1 includes hydrogen, halogeno and various other substituents;each of m and n is 1 or 2;A.sup.1, alkylene, alkenylene or alkynylene;Het is a 5 or 6 membered heteroaryl group optionally bearing particular substituents; andG is carboxy, 1H-tetrazol-5-yl or a group of the formula:--CONH--SO.sub.2 R.sup.2wherein R.sup.2 is (1-4C)alkyl, benzyl or phenyl;and pharmaceutically-acceptable salts thereof, which possess anti-hyperalgesic properties. The invention also relates to processes for the manufacture of said tricyclic heterocycles; and to novel pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: May 31, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: John Oldfield, Howard Tucker
  • Patent number: 5244881
    Abstract: The invention provides new inclusion compounds based on imipramine and cyclodextrin and pharmaceutical compositions which can be administered orally and are based on these new inclusion compounds.
    Type: Grant
    Filed: November 22, 1991
    Date of Patent: September 14, 1993
    Assignee: Rhone-Poulenc Sante
    Inventor: Anne Coutel-Egros
  • Patent number: 5216178
    Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: June 1, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 5192760
    Abstract: New 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines of formula I and their pharmaceutically acceptable salts were found to be suitable actives for the treatment of cardiac arrhythmia. Previously unknown 3-carbalkoxyamino-5-(alpha-halogenpropionyl)-5H-dibenz[b,f]azepines are obtained from 3-carbalkoxyamino-5H-dibenz[b,f]azepines by reaction with alpha-halogenpropionyl halides. Through their reaction with ammonia, primary amines or secondary amines, the new 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines are obtained, which can be optionally converted into their pharmaceutically acceptable acid addition salts.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: March 9, 1993
    Assignee: Arzneimittelwerk Dresden GmbH
    Inventors: Helmut Wunderlich, Andreas Stark, Dieter Lohmann, Lothar Zenkar, Reni Bartsch, Hildegard Poppe, Aleksandr P. Skoldinov, Natalja V. Kaverina, Anna N. Grizenko, Valentin V. Lyskovzev, Ekaterina K. Grigoreva
  • Patent number: 5015640
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and X have the significances given herein, their acid addition salts and the preparation of these substances, pest control compositions which contain these substances as active ingredients and the use of the active substances or compositions for the control of pests.
    Type: Grant
    Filed: November 7, 1989
    Date of Patent: May 14, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Rene Zurfluh
  • Patent number: 4962200
    Abstract: A novel nitrogen-containing compound capable of preventing hardening of blood vessels by controlling formation of peroxide lipids in cell membranes, which is valuable as an anti-arteriosclerotic agent, is disclosed.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: October 9, 1990
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Noriaki Kihara, Ikuo Tomino, Hiroaki Tan, Takafumi Ishihara
  • Patent number: 4833245
    Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position of X, and their acid addition salts, processes for their manufacture, pest control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of pests. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: May 23, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Renee Zurfluh
  • Patent number: 4813998
    Abstract: Novel herbicidal 1-heterocyclyl-1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: March 21, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Guy R. E. Van Lommen, William R. Lutz, Jozef F. E. Van Gestel
  • Patent number: 4766115
    Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position to X, and their acid addition salts, processes for their manufacture, insect control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of insects. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: August 23, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Rene Zurfluh
  • Patent number: 4741765
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: May 3, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4678499
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: January 30, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4616011
    Abstract: This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## group and B represents a methylene, carbonyl, or thiocarbonyl group or A represents a --CO--CO-- or ##STR3## group and B represents a methylene group, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.
    Type: Grant
    Filed: November 26, 1984
    Date of Patent: October 7, 1986
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Joachim Heider, Volkhard Austel, Norbert Hauel, Walter Kobinger, Christian Lillie