Polycyclo Ring System In Substituent Q Patents (Class 564/172)
  • Patent number: 6444860
    Abstract: The invention relates to novel naphthopyran- and phenanthropyran-type compounds having a carbobicycle annelated in 5,6- position. These compounds have formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.
    Type: Grant
    Filed: December 29, 2000
    Date of Patent: September 3, 2002
    Assignee: Corning S.A.
    Inventors: You-Ping Chan, Patrick Jean
  • Patent number: 6423870
    Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: July 23, 2002
    Assignee: Les Laboratoires Servier
    Inventors: Michel Langlois, Monique Mathe-Allainmat, Carole Jellimann, Jean Andrieux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6403831
    Abstract: Substituted benzylidene indenyl formamides, acetamides and propionamides are useful in the treatment of precancerous lesions and neoplasms.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: June 11, 2002
    Assignee: Cell Pathways, Inc.
    Inventors: Gerhard Sperl, Paul Gross, Klaus Brendel, Rifat Pamukcu, Gary A. Piazza
  • Patent number: 6369225
    Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: April 9, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
  • Patent number: 6353109
    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: March 5, 2002
    Assignee: Neurogen Corporation
    Inventors: Pamela Albaugh, Gang Liu, Alan Hutchison
  • Patent number: 6340704
    Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: January 22, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
  • Patent number: 6326369
    Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.
    Type: Grant
    Filed: July 6, 1999
    Date of Patent: December 4, 2001
    Assignee: Takeda Chemicals Industries, Ltd.
    Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
  • Patent number: 6288234
    Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 11, 2001
    Assignee: Advanced Medicine, Inc.
    Inventor: John H. Griffin
  • Patent number: 6268520
    Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
    Type: Grant
    Filed: April 5, 1999
    Date of Patent: July 31, 2001
    Assignee: Hoechst Marion Roussel
    Inventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
  • Patent number: 6248781
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: June 19, 2001
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6239179
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and R9 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4, R5, R6, R7, R8 and R9 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R10 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group; 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 dis
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: May 29, 2001
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 6162445
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: December 19, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6160175
    Abstract: A class of novel naphthyl acetamide compounds is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: December 12, 2000
    Assignee: Eli Lilly and Company
    Inventors: Theodore Goodson, Jr., Richard W. Harper, David K. Herron
  • Patent number: 6156750
    Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: January 13, 1999
    Date of Patent: December 5, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6133266
    Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: October 17, 2000
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
  • Patent number: 6124498
    Abstract: In one embodiment, the present invention provides a compound comprising: ##STR1## wherein A=H or OHX=OH, a halogen, OR, NHR, NR'R" where R, R', and R"=H, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, or C.sub.2-8 alkynyl, cycloalkyl, cycloalkenyl, aryl, aralkyl or heterocyclic, substituted or unsubstituted; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 =H, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, or C.sub.2-8 alkynyl, cycloalkyl, cyloalkenyl, aryl or heterocyclic, substituted or unsubstituted, wherein R.sub.1 includes at least one methylene spacer through which R.sub.1 is attached to said compound. The present invention also provides methods for making hydroxynaphthoic acids.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: September 26, 2000
    Assignee: University Of New Mexico
    Inventors: David L. Vander Jagt, Lorraine M. Deck, Robert E. Royer
  • Patent number: 6005003
    Abstract: A subject of the invention is the compounds of general formula (I): ##STR1## in which R1=H, alkyl, acyl, R2 and R3=H, alkyl, R4=aryl, heteroaryl, X=O, CH2, Y=OH, O-alkyl or NRaRb, as well as the salts, their preparation processes, the intermediates of these processes, their use as medicaments and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 5, 1999
    Date of Patent: December 21, 1999
    Assignee: Hoechst Marion Roussel
    Inventor: Francois Nique
  • Patent number: 5935978
    Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: August 10, 1999
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5900436
    Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.
    Type: Grant
    Filed: July 28, 1997
    Date of Patent: May 4, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Nirogi Venkata Satya Ramakrishna, Arun Kumar Jain, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Andreas Weichert, Jan-Robert Schwark
  • Patent number: 5891886
    Abstract: A new treatment schedule for administration of N-?2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: April 6, 1999
    Assignee: Xenova Limited
    Inventors: Bruce Charles Baguley, Graham John Atwell, William Alexander Denny, Graeme John Finlay, Gordon William Rewcastle
  • Patent number: 5877218
    Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 2, 1999
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Yaacov Herzig, Jeff Sterling, Alex Veinberg, Benjamin Sklarz, Ramy Lidor, Eliezer Bahar
  • Patent number: 5827891
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
  • Patent number: 5760246
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 5739374
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5728737
    Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5721276
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, B, X and R.sub.1 are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: February 24, 1998
    Assignee: Adir et Compagnie
    Inventors: Isabelle Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard, Beatrice Guardiola Lemaitre
  • 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: 5674905
    Abstract: Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: October 7, 1997
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Caroline Minli Rachel Low, Michael John Pether, Jonathan Michael Richard Davies, David John Dunstone, Iain Mair McDonald
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5648534
    Abstract: 1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I') wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-ol
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: July 15, 1997
    Assignee: Ichikawa Gosei Chemical Co., Ltd.
    Inventors: Yoshio Igarashi, Fumihiro Asano, Makoto Shimoyamada, Masayuki Harada, Shigeru Nakano, Ryoji Iwai, Keisuke Yagami, Yuzi Konno
  • Patent number: 5607966
    Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Gustav Graff
  • Patent number: 5602181
    Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: February 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5574036
    Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: November 12, 1996
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, Bruno Charpenter
  • Patent number: 5527955
    Abstract: The invention concerns a method for treating depression or senile dementia using a compound which acts selectively as an agonist of gamma aminobutyric acid (GABA) at GABA autoreceptors with the proviso that the compound is not fengabine and progabide.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: June 18, 1996
    Assignee: John Wyeth & Brother, Limited
    Inventors: Michael C. W. Minchin, John F. White
  • Patent number: 5514683
    Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: May 7, 1996
    Assignee: James Black Foundation Limited
    Inventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
  • Patent number: 5498755
    Abstract: Compounds of the formula ##STR1## wherein the R.sub.1 groups independently are hydrogen, lower alkyl, or two geminal R.sub.1 groups jointly represent an oxo (.dbd.O) or a thio (.dbd.S) group; R.sub.2 is hydrogen or lower alkyl, or halogen; M is or --N.dbd.CR.sub.4 -- or --R.sub.4 C.dbd.N-- where R.sub.4 is hydrogen or lower alkyl; X is C(R.sub.1).sub.2 ; Y is phenyl optionally substituted with an R.sub.3 group which is lower alkyl or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: March 12, 1996
    Inventors: Roshantha A. Chandraratna, Min Teng
  • Patent number: 5492917
    Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
  • Patent number: 5478835
    Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 26, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5476860
    Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: December 19, 1995
    Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5434188
    Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.
    Type: Grant
    Filed: March 7, 1994
    Date of Patent: July 18, 1995
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Sony S. Khatana, James B. Kramer, Paul C. Unangst
  • Patent number: 5430060
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: July 4, 1995
    Assignee: Zeneca Limited
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
  • Patent number: 5403953
    Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents halogen, or hydroxy, alkyl, alkoxy, cyano, amino, mercapto, alkylthio or phenoxy,R.sub.2 and R'.sub.2 represent two hydrogen when the ring is unsaturated, or alternatively identical or different, represent hydrogen or halogen, or hydroxy, alkyl, alkoxy, cyano, amino or oxo when the ring is saturated,R.sub.3 represents any one of the following groups: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N-R, R.sub.5 or R.sub.6, which are identical or different, represent hydrogen or alkyl or trifluoromethyl or form (C.sub.3 -C.sub.6) cycloalkyl,n represents 0, 1 or 2,R.sub.7 represents hydroxy, alkoxy, amino, or --O--CH.sub.2 --CO--NRR',R.sub.4 represents hydrogen or halogen or alkyl, alkoxy or trihaloalkyl.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: April 4, 1995
    Assignee: Adir et Compagnie
    Inventors: Guillaume de Nanteuil, Michel Vincent, Christine Lila, Jacqueline Bonnet, Armel Fradin
  • Patent number: 5389684
    Abstract: Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: February 14, 1995
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5340827
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: August 23, 1994
    Assignee: Celltech, Limited
    Inventors: Nigel R. A. Beeley, Thomas A. Millican
  • Patent number: 5300676
    Abstract: Fluorine-substituted .alpha.-(5-aryloxy-naphthalen-1-yl-oxy)-propionic derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, as defined herein, are useful as herbicides. Processes and intermediates for their preparation are also disclosed.
    Type: Grant
    Filed: April 11, 1991
    Date of Patent: April 5, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Michael Haug, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5270342
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: December 14, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Salter
  • Patent number: 5270343
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 .dbd.CR.sup.2 .dbd.CR.sup.3 CR.sup.4 .dbd.CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or is (CH.sub.2).sub.7 ;a=0 or 1; b= 0 or 1;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl;X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from:a) C.sub.1-4 alkyl, C.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: December 14, 1993
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: RE34805
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: December 6, 1994
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon