Benzene Ring Containing Patents (Class 514/595)
  • Patent number: 5591775
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein for use in the treatment of a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 6, 1994
    Date of Patent: January 7, 1997
    Assignee: Adir et Compagnie
    Inventors: Patrick Depreux, Hamid A. Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, Gerard Adam, Philippe Delagrange
  • Patent number: 5576334
    Abstract: The invention concerns chemical compounds of formula IR.sup.1 --CON(R.sup.2)--CON(R.sup.3)--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention concerns processes for the preparation of the chemical compounds of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: November 19, 1996
    Assignee: Zeneca Limited
    Inventors: George R. Brown, Richard E. Shute
  • Patent number: 5575993
    Abstract: Ionene polymers having biologically-active organic and/or inorganic anions are described. Methods to prepare the ionene polymers, compositions containing them and their methods of use are also described.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: November 19, 1996
    Assignee: Buckman Laboratories International, Inc.
    Inventors: James A. Ward, Fernando Del Corral
  • Patent number: 5574054
    Abstract: Novel quaternary ammonium salts having utility in the medical field for treating gastrointestinal disorders.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: November 12, 1996
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Osamu Kitagawa, Katsuyuki Ishii, Seiichi Niwa, Sigeru Ueki, Masao Seiki
  • Patent number: 5554641
    Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: September 10, 1996
    Inventors: David C. Horwell, Martyn C. Pritchard, Jennifer Raphy
  • Patent number: 5541228
    Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: July 30, 1996
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
  • Patent number: 5516789
    Abstract: Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: May 14, 1996
    Assignee: Abbott Laboratories
    Inventors: Clint D. W. Brooks, Andrew O. Stewart, Anwer Basha, Randy L. Bell
  • Patent number: 5510349
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 23, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
  • Patent number: 5498635
    Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: March 12, 1996
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
  • Patent number: 5491166
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: February 13, 1996
    Assignee: Eli Lilly and Company
    Inventors: Stephen W. Kaldor, Thomas E. Mabry
  • Patent number: 5484812
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: January 16, 1996
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5484811
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 B is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexyimethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: February 23, 1994
    Date of Patent: January 16, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5476873
    Abstract: Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    Type: Grant
    Filed: April 19, 1994
    Date of Patent: December 19, 1995
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Andrew O. Stewart, Daniel J. Kerkman, Pramila A. Bhatia, Anwer Basha, Jonathan G. Martin
  • Patent number: 5461072
    Abstract: The present invention is concerned with the use of a compound of formula (I): Ar--Y--Q, wherein Ar is either (i) furyl, thienyl, thienyl 1,1-dioxide, pyrryl, pyridyl, benzofuryl, benzothienyl, benzothienyl 1,1-dioxide, indolyl, naphthyl, quinolyl, or tetrahydronaphthyl, any of which is optionally substituted by one or more substituents independently selected from C.sub.1-4 alkyl (which may itself optionally be substituted by one or more halogen atoms), C.sub.1-4 alkoxy, halo, nitro, amino, carboxy, C.sub.1-4 alkoxy-carbonyl and hydroxy, or (ii) phenyl optionally substituted by one or more substituents independently selected from phenyl (which is itself optionally substituted by one or more substituents independently selected from those optional substituents specified in (i) above) and those specified as optional substituents in (i) above, Y is C.sub.1-10 alkylene or C.sub.2-10 alkenylene; Q is formula (II), where R.sup.1 is hydrogen, C.sub.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: October 24, 1995
    Assignee: Burroughs Wellcome Co.
    Inventor: Lawrence G. Garland
  • Patent number: 5449689
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 12, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5449690
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, and medicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 12, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick DePreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5441984
    Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: William F. Heath, Jr., Jill A. Panetta, John K. Shadle
  • Patent number: 5430059
    Abstract: A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: July 4, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Toshiaki Ogawa, Hideyuki Adachi, Takanori Kawamura
  • Patent number: 5401775
    Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: March 28, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
  • Patent number: 5389682
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: February 14, 1995
    Assignee: Warner-Lambert Company
    Inventors: Bradley D. Tait, Michael W. Wilson
  • Patent number: 5389683
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: August 14, 1992
    Date of Patent: February 14, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5387595
    Abstract: Substituted alicyclic compounds of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: February 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Paul E. Finke, Malcolm MacCoss, Daniel J. Miller, Dennis J. Underwood
  • Patent number: 5385944
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: January 31, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5364850
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: November 15, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5288758
    Abstract: New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group;R.sup.2 represents:a C.sub.5 -C.sub.7 cycloalkyl groupa cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atomsa benzyl groupa benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group;A represents an oxygen atom or a methylene radical;n represents 1 or 2;X represents an oxygen or sulfur atom;B represents a direct bond, a methylene radical or a carbonyl radical;as well as the therapeutically acceptable salts of these molecules.The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes.
    Type: Grant
    Filed: July 22, 1992
    Date of Patent: February 22, 1994
    Assignee: Pierre Fabre Medicament
    Inventors: Jean-Louis Vidaluc, Dennis Bigg
  • Patent number: 5272175
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5246965
    Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: September 21, 1993
    Assignee: Ciba-Geigy
    Inventor: Alan J. Main
  • Patent number: 5227401
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: July 13, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5223535
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5190974
    Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: March 2, 1993
    Assignee: Roussel Uclaf
    Inventors: Francoise Clemence, Odile Le Martret, Francis Petit
  • Patent number: 5118709
    Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: June 2, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
  • Patent number: 5099030
    Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: March 24, 1992
    Assignee: The Procter & Gamble Company
    Inventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
  • Patent number: 5091419
    Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.
    Type: Grant
    Filed: October 2, 1990
    Date of Patent: February 25, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5064827
    Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: November 12, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
  • Patent number: 5047420
    Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
  • Patent number: 5045565
    Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: September 3, 1991
    Assignee: The Procter & Gamble Company
    Inventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
  • Patent number: 5037853
    Abstract: Certain carbocyclic aryl- and heterocyclic aryl-substituted cyclopropyl N-hydroxyureas, N-hydoroxycarboxamides, and N-acyl-N-hydroxyamides inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: August 6, 1991
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Karen E. Rodriques
  • Patent number: 5030653
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: July 9, 1991
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5021429
    Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: June 4, 1991
    Assignee: Allen & Hansburys Limited
    Inventor: Michael Martin-Smith
  • Patent number: 5017608
    Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.
    Type: Grant
    Filed: September 6, 1989
    Date of Patent: May 21, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
  • Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5006539
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: April 9, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4983605
    Abstract: A pharmaceutical composition comprising a benzoyl urea compound (A) selected from the group consisting of a benzoyl urea compound (I) having the formula: ##STR1## wherein X is a halogen atom, a nitro group or a trifluoromethyl group, provided that when Y is a nitro group, X is a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, Z.sub.1 is a halogen atom or a trifluoromethyl group, Z.sub.2 is a hydrogen atom or a halogen atom, and A is a .dbd.CH-- group or a nitrogen atom, and a benzoyl urea compound (II) having the formula: ##STR2## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a nitro group, provided that when Y is a nitro group, X.sub.
    Type: Grant
    Filed: October 20, 1987
    Date of Patent: January 8, 1991
    Assignees: Ishihara Sangyo Kaisha Ltd., The Green Cross Corporation
    Inventors: Nobuo Kondo, Masahiro Kikuchi, Tsunetaka Nakajima, Masahiro Watanabe, Kazumasa Yokoyama, Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi
  • Patent number: 4977170
    Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4920135
    Abstract: Certain organic compounds derived from urea or thiourea having insecticidal activity and methods of their preparation are disclosed. The compounds according to the invention have been found to interfere with the mechanism of metamorphoses which occurs in insects. Hence, the substances according to the invention are specifically active against insects. Owing to this specificity and because of the absence of phytotoxicity effects, the compounds of this invention are of prime importance.
    Type: Grant
    Filed: February 7, 1989
    Date of Patent: April 24, 1990
    Assignee: Duphar International Research B.V.
    Inventors: Kobus Wellinga, Rudolf Wulder
  • Patent number: 4908386
    Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: March 13, 1990
    Assignee: Glaxo Group Limited
    Inventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
  • Patent number: 4895840
    Abstract: Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.
    Type: Grant
    Filed: June 10, 1987
    Date of Patent: January 23, 1990
    Assignee: A. H. Robins Company, Incorporated
    Inventor: James R. Shanklin, Jr.
  • Patent number: 4883815
    Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: November 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz