Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/241)
-
Patent number: 6417200Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: May 9, 2000Date of Patent: July 9, 2002Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6417178Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 6, 1997Date of Patent: July 9, 2002Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
-
Publication number: 20020061917Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1Type: ApplicationFiled: September 21, 2001Publication date: May 23, 2002Inventors: Hui-Yin Li, Luigi Anzalone, Fuqiang Jin, David J. Meloni, Jung-Hui Sun, Christopher A. Teleha, Jia C. Zhou, Thomas E. Smyser
-
Publication number: 20020055641Abstract: A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described.Type: ApplicationFiled: December 3, 2001Publication date: May 9, 2002Inventors: Jiacheng Zhou, Lynette May Oh, Pasquale N. Confalone, Hui-Yin Li, Philip Ma
-
Publication number: 20020049332Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: ApplicationFiled: October 11, 2001Publication date: April 25, 2002Inventor: John J. Talley
-
Publication number: 20020045581Abstract: We have discovered a method of modifying the tumor cell microenvironment to reduce or prevent the establishment, growth or metastasis of malignant cells comprising administering to a patient having malignant cells a pharmaceutically effective amount of a PAR-1 inhibitor and optionally a PAR-2 inhibitor to prevent or reduce activation of normal cells within the tumor microenviroment. This method also has the effect in some patients of modulating the immune system to facilitate a more efficient immune response to malignant cells and maybe coupled with cytokine therapy and T-cell therapy to enhance the patient's immune response to the malignant cells.Type: ApplicationFiled: May 25, 2001Publication date: April 18, 2002Inventors: Michael D'Andrea, Claudia Derian, Hal Brent Woodrow
-
Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
-
Patent number: 6350754Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: January 12, 2000Date of Patent: February 26, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 6350749Abstract: The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5- to 6-membered aromatic homocyclic ring or an optionally substituted 5- to 6-membered aromatic heterocyclic ring, R1 is a hydrogen atom, a hydroxy group or a lower alkyl group, and n is 0 or 1, or a salt thereof, which is effective for the prevention or treatment of ischemic cardiac disease, etc., and which is useful as an agent for preventing or treating ischemic cardiac disease, etc. such as myocardial infarction, arrhythmia, etc.Type: GrantFiled: August 8, 2000Date of Patent: February 26, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Shoji Fukumoto, Keiji Kusumoto
-
Publication number: 20010053779Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.Type: ApplicationFiled: June 4, 2001Publication date: December 20, 2001Inventors: Timothy J. Church, Neil Scott Cutshall, Anthony R. Gangloff, Thomas E. Jenkins, Martin S. Linsell, Joane Litvak, Kenneth D. Rice, Jeffrey R. Spencer, Vivian R. Wang
-
Patent number: 6331637Abstract: N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)thienylsulfonamides, (phenyl) and (phenoxy)furylsulfonamides, and (phenyl) and (phenoxy)pyrrolylsulfonamides and methods of using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: March 22, 1999Date of Patent: December 18, 2001Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamoori, Vitukudi Narayanaiyengar Balaji
-
Patent number: 6329527Abstract: A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.Type: GrantFiled: October 10, 2000Date of Patent: December 11, 2001Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Lynette May Oh, Pasquale N. Confalone, Hui-yin Li, Philip Ma
-
Patent number: 6313132Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).Type: GrantFiled: September 27, 1999Date of Patent: November 6, 2001Assignee: Pharmacia ABInventors: Rolf Johansson, Martin Haraldsson, Erik Ringberg, Ian Vagberg, Katarina Beierlein, Rikard Emond, Birger Sjoberg
-
Patent number: 6168776Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: April 18, 1997Date of Patent: January 2, 2001Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
-
Patent number: 6165944Abstract: 4-(3-Heterocyclyl-1-benzoyl)pyrazoles of the formula I ##STR1## where: R.sup.1 and R.sup.3 are each hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, N-alkylaminosulfonyl, N,N-dialkyl)aminosulfonyl, N-alkylsulfonylamino, N-haloalkylsulfonylamino, N-alkyl-N-alkylsulfonylamino or N-alkyl-N-haloalkylsulfonylamino;R.sup.2 is a 5- or 6-membered heterocyclyl radical with or without substitution which comprises 1 to 4 identical or different hetero atoms from the following group: oxygen, sulfur or nitrogen;R.sup.4 is hydrogen, halogen or alkyl;R.sup.5 is substituted pyrazole which is attached in position 4;and agriculturally useful salts thereof; processes for preparing the 4-(3-heterocyclyl-1-benzoyl)pyrazoles; compositions comprising them; and the use of these derivatives or these compositions comprising them for controlling undesirable plants.Type: GrantFiled: June 16, 1998Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Ernst Baumann, Stefan Engel, Guido Mayer, Joachim Rheinheimer, Matthias Witschel, Ulf Misslitz, Oliver Wagner, Martina Otten, Helmut Walter, Karl-Otto Westphalen
-
Patent number: 6160000Abstract: The instant invention is concerned with aryl and heteroaryl acetic acid and oxyacetic acid compounds, which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.Type: GrantFiled: June 22, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventors: Alan Adams, Derek Von Langen, Hiroo Koyama, Richard Tolman
-
Patent number: 6150390Abstract: The present invention relates to a novel 3-amino-1,2-benzoisoxazole derivatives, represented by Formula I, LTB-4[leukotriene-B-4; 5(S),12(R)-dihydroxy-6,14-cis-8,10-trans-eicosatetraenoic acid] receptor antagonist, process for preparation thereof, and use thereof for LTB-4 receptor antagonist or therapeutics for osteoporosis. ##STR1## (in which n is integer of 3-5).Type: GrantFiled: July 21, 1999Date of Patent: November 21, 2000Assignee: Dong Wha Pharm. Ind. Co., Ltd.Inventors: Hong-Suk Suh, Jae-Ha Ryu, Yong-Nam Han, Sung-June Yoon, Jong-Woo Kim
-
Patent number: 6107320Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently(a) hydrogen, except that R.sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: January 11, 1996Date of Patent: August 22, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, John T. Hunt
-
Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
-
Patent number: 6090836Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.Type: GrantFiled: January 31, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Joel P. Berger, Gregory D. Berger, Kenneth J. Fitch, Donald W. Graham, Anthony B. Jones, Derek von Langen, Mark D. Leibowitz, David E. Moller, Arthur A. Patchett, Conrad Santini, Soumya P. Sahoo, Richard L. Tolman, Richard B. Toupence, Thomas F. Walsh
-
Patent number: 6080773Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.Type: GrantFiled: October 14, 1997Date of Patent: June 27, 2000Assignee: Akzo Nobel, N.V.Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
-
Patent number: 6080702Abstract: Disclosed are herbicidal heterocyclic benzisoxazoles and benzisoxazolidinones of formula (I): ##STR1## wherein A is (a), (b) or (c); U is N or NR; X is CO or CR.sup.2 ; and R, R.sup.1, R.sup.2, R.sup.3, Y and Z are as disclosed in the disclosure.Type: GrantFiled: September 14, 1998Date of Patent: June 27, 2000Assignee: FMC CorporationInventors: George Theodoridis, Lester L. Maravetz, Scott D. Crawford
-
Patent number: 6051572Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: April 28, 1998Date of Patent: April 18, 2000Assignee: Merck Sharp & Dohme Ltd.Inventor: Jose Luis Castro Pineiro
-
Patent number: 6043240Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 28, 2000Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 6008367Abstract: This invention relates to a chemical intermediate ##STR1## wherein f is 0, 1, 2 or 3, which is useful for the synthesis of a compound of the Formula IX--C(O)--Y--G--R I(wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, which compound of Formula I or salt and pharmaceutical compositions comprising such a compound or salt are useful as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.Type: GrantFiled: January 25, 1999Date of Patent: December 28, 1999Assignee: Eli Lilly and CompanyInventors: Valentine Joseph Klimkowski, Aaron Leigh Schacht, Michael Robert Wiley
-
Patent number: 5998613Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.Type: GrantFiled: August 5, 1997Date of Patent: December 7, 1999Assignee: H. Lundbeck A/SInventors: Erik Falch, Jens Kristian Perregaard, Arne Schousboe, Povl Krogsgaard-Larsen, Bente Frolund, Sibylle Moltzen Lenz
-
Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.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: 5965591Abstract: An isoxazole compound having the following formula: wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 26, 1997Date of Patent: October 12, 1999Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
-
Patent number: 5962490Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: September 27, 1996Date of Patent: October 5, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamorri, Vitukudi Narayanaiyengar Balaji
-
Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
-
Patent number: 5939446Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.Type: GrantFiled: March 21, 1997Date of Patent: August 17, 1999Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, Joel C. Barrish
-
Patent number: 5925766Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful or the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.Type: GrantFiled: March 18, 1997Date of Patent: July 20, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Gerard J. O'Malley, Mark G. Palermo
-
Patent number: 5889035Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 30, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau
-
Patent number: 5880121Abstract: 4,5-Dihydronaphth?1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT.sub.3 antagonists. These compounds art useful for the treatment of anxiety, psychiatric disorders, nausea, vomiting and drug dependency.Type: GrantFiled: December 19, 1996Date of Patent: March 9, 1999Assignee: Hoechst Marion Roussel Inc.Inventor: Nicholas J. Hrib
-
Patent number: 5856503Abstract: Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.Type: GrantFiled: December 6, 1996Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Hans-Peter Marki, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Yu-Hua Ji
-
Patent number: 5856507Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.Type: GrantFiled: January 21, 1997Date of Patent: January 5, 1999Assignee: Bristol-Myers Squibb Co.Inventors: Richard P. Polniaszek, Xuebao Wang, Jeffrey S. DePue, Chennagiri R. Pandit, Kumar G. Gadamasetti, Yadagiri Pendri, Eduardo J. Martinez
-
Patent number: 5854263Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5854243Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 29, 1998Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5854235Abstract: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.Type: GrantFiled: November 3, 1997Date of Patent: December 29, 1998Assignee: Akzo Nobel N.V.Inventors: Johannes Antonius Maria Hamersma, Everardus Otto Maria Orlemans, Johannes Bernardus Maria Rewinkel
-
Patent number: 5843977Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 1, 1998Assignee: Hoechst Marion Rosueel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
-
Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
-
Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
-
Patent number: 5786374Abstract: The present invention relates to benzisoxazole compounds, pesticidal compositions containing them, and their preparations thereof.Type: GrantFiled: May 1, 1997Date of Patent: July 28, 1998Assignee: Novartis CorporationInventors: Saleem Farooq, Stephan Trah, Rene Zurfluh
-
Patent number: 5756532Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.Type: GrantFiled: October 15, 1996Date of Patent: May 26, 1998Assignee: American Home Products CorporationInventors: Gary P. Stack, Richard E. Mewshaw, Byron A. Bravo, Young H. Kang
-
Patent number: 5756754Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.Type: GrantFiled: June 19, 1997Date of Patent: May 26, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Gerard J. O'Malley, Mark G. Palermo
-
Patent number: 5750542Abstract: Described herein are compounds of the formula ##STR1## wherein R.sup.1 R.sup.2, R.sup.7, R.sup.8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: September 28, 1993Date of Patent: May 12, 1998Assignee: PfizerInventors: Anabella Villalobos, Arthur A. Nagel, Yuhpyng L. Chen
-
Patent number: 5716967Abstract: This invention relates to isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The isoxazoline compounds are useful in inhibiting PDE.sub.IV and in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
-
Patent number: 5703070Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen, halogen, alkyl, alkoxy, trihalomethyl or hydroxyl,R.sub.2 represents hydrogen, alkyl or phenyl which is optionally substituted, ##STR2## or alternatively ##STR3## represents --O--N.dbd., 1.ltoreq.n.ltoreq.6, ##STR4## represents any one of the groups defined in the description, its isomers and its addition salts with a pharmaceutically acceptable acid or base, a medicinal products containing the same are useful in the treatment of schizophrenia.Type: GrantFiled: June 6, 1996Date of Patent: December 30, 1997Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Valerie Audinot
-
Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler
-
Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles