The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/237)
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Patent number: 6342509Abstract: This invention relates to certain piperidine quatemrwy salts of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 18, 1999Date of Patent: January 29, 2002Assignee: Syntex (U.S.A.) LLCInventors: Donald Roy Hirschfeld, Denis John Kertesz, David Berard Smith
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Publication number: 20020007068Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: 1Type: ApplicationFiled: January 11, 2001Publication date: January 17, 2002Inventor: Thomas E. D'Ambra
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Patent number: 6329399Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.Type: GrantFiled: May 18, 2000Date of Patent: December 11, 2001Assignee: Pola Chemical Industries, Inc.Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
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Patent number: 6303637Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.Type: GrantFiled: October 21, 1999Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Publication number: 20010025106Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1Type: ApplicationFiled: March 9, 2001Publication date: September 27, 2001Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Publication number: 20010012896Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas 1 2Type: ApplicationFiled: March 9, 2001Publication date: August 9, 2001Inventors: Daniel R. Henton, Frederick J. McCarty, Susan I. Tripp, Jill E. DeWitt
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Patent number: 6214996Abstract: Naphthalene derivatives of the formula [I]: wherein R1 and R2 are the same or different and are each H, protected or unprotected OH, one of R3 and R4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R5 and R6 are, the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: December 1, 1998Date of Patent: April 10, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
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Patent number: 6191182Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.Type: GrantFiled: June 10, 1999Date of Patent: February 20, 2001Assignee: Ciba Specialty Chemcials CorporationInventors: Rinaldo Hüsler, Rudolf Schwabe, Reto Luisoli
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Patent number: 6147217Abstract: Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R.sup.1 and R.sup.2 are as defined in the specification.Type: GrantFiled: May 24, 1999Date of Patent: November 14, 2000Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Qun Kevin Fang, Scott Harold Wilkinson
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Patent number: 6140321Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
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Patent number: 6124323Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.Type: GrantFiled: September 16, 1998Date of Patent: September 26, 2000Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Po-Wai Yuen, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana, Anthony P. Guzikowski
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Patent number: 6121293Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: June 29, 1998Date of Patent: September 19, 2000Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl
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Patent number: 6107345Abstract: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.Type: GrantFiled: March 3, 1999Date of Patent: August 22, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
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Patent number: 6090824Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists Substance P and NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: November 14, 1996Date of Patent: July 18, 2000Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Bruce T. Dembofsky
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Patent number: 6060488Abstract: This invention is related to novel benzothiophene compounds of formula I: ##STR1## where R, R.sup.1, R.sup.2, X and m are as defined in the specification, which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.Type: GrantFiled: September 22, 1998Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Mark Gregory Stocksdale
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Patent number: 6015899Abstract: Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a compound of the formula II or a mixture of compounds of the formula II and component c) is a compound of the formula III or a mixture of compounds of the formula III, ##STR1## in which the general symbols are as defined in claim 1, the compound of the formula I being, for example, pentaerythritol, thiodiethylene glycol, 1,4-butanediol, 1,4-propanediol, diethylene glycol, triethylene glycol, diethanolamine or glycerol, the compound of the formula II being, for example, sunflower oil or coconut fat, and the compound of the formula III being, for example, methyl 3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate. The abovementioned products can be used as liquid antioxidants in polymers and lubricants.Type: GrantFiled: April 21, 1997Date of Patent: January 18, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Paul Dubs, Roger Martin, Samuel Evans
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Patent number: 6008220Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: June 8, 1998Date of Patent: December 28, 1999Assignee: Warner Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Daniel Fred Ortwine, Claude Forsey Purchase, Jr., Andrew David White, Qi-Zhuang Ye
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Patent number: 5977357Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.Type: GrantFiled: June 1, 1998Date of Patent: November 2, 1999Assignee: Ciba Specialty Chemical CorporationInventors: Rinaldo Husler, Rudolf Schwabe, Reto Luisoli
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Patent number: 5935585Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## 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: GrantFiled: February 23, 1996Date of Patent: August 10, 1999Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Laurence Vigne
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Patent number: 5925653Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O).sub.q where q=0, 1 of 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.Type: GrantFiled: September 6, 1996Date of Patent: July 20, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Preuss, Wolfgang Schaper, Martin Markl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
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Patent number: 5925631Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 3, 1998Date of Patent: July 20, 1999Assignee: Merck & Co., Inc.Inventors: Cameron Black, Greg Hughes, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
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Patent number: 5925761Abstract: Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula II ##STR2## and elaborate the product by reductive amination of an aldehyde of formula IVa ##STR3## with .alpha.,.alpha.-diphenyl-4-piperidinemethanol.Type: GrantFiled: February 4, 1997Date of Patent: July 20, 1999Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Qun Kevin Fang, Scott Harold Wilkinson
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5811552Abstract: A novel cyclobutenedione derivative prepared in accordance with the following reaction formula, a process for the preparation thereof, and a nonlinear optical element comprising such a derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 each represents an alkyl group, an alkenyl group or an alkynyl group; R.sup.3 and R.sup.4 each represents a hydrogen atom, an alkyl group, an alkenyl group or an alkynyl group; and C.sup.* represents an asymmetric carbon atom, with the proviso that R.sup.1, R.sup.2 and the nitrogen atom to which they are connected may form a cyclic structure larger than 3-membered ring, R.sup.1 and R.sup.3, and R.sup.2 and R.sup.4 each may be connected to each other to form a methylene chain --(CH.sub.2).sub.n -, and the hydrogen atoms in R.sup.1 and R.sup.2 may be substituted by halogen atom, alkyloxy group or cyano group.Type: GrantFiled: April 14, 1995Date of Patent: September 22, 1998Assignee: Fuji Xerox Co., Ltd.Inventors: Yasunari Nishikata, Lyong Sun Pu
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Patent number: 5792870Abstract: A group of 2-amino-3-aroyl-benzo?.beta.!thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo?.beta.!thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-?4-(2-peperidinoethoxy)benzoyl!benzo?.beta .!thiophene.Type: GrantFiled: September 10, 1996Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventor: Alexander G. Godfrey
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Patent number: 5750703Abstract: The present invention relates to a process for preparation of substantially pure piperidine derivative compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 has 1 to 6 carbon atoms;A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.Type: GrantFiled: February 2, 1995Date of Patent: May 12, 1998Assignee: Albany Molecular Research, Inc.Inventor: Thomas E. D'Ambra
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Patent number: 5733756Abstract: Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.Type: GrantFiled: January 5, 1996Date of Patent: March 31, 1998Assignee: Celgene CorporationInventors: Andrew L. Zeitlin, David I. Stirling
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Patent number: 5675009Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 1, 1995Date of Patent: October 7, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5663353Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: September 2, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5658929Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: July 21, 1995Date of Patent: August 19, 1997Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell
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Patent number: 5654433Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 3, 1995Date of Patent: August 5, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5652370Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: July 29, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5650516Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 3, 1995Date of Patent: July 22, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5646144Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5644061Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 1, 1995Date of Patent: July 1, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
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Patent number: 5631375Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators, these piperidine derivatives can be described by the following formulas: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen; orR.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;R.sub.3 is --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched;each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts, hydrates and individual optical isomers thereof.Type: GrantFiled: January 6, 1995Date of Patent: May 20, 1997Assignee: Merrell Pharmaceuticals, Inc.Inventors: Chi-Hsin R. King, Michele A. Kaminski, Teng-Man Chen
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Patent number: 5622971Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: April 22, 1997Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5618940Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: April 8, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin R. King, Michele A. Kaminski
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Patent number: 5567820Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.Type: GrantFiled: March 15, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Terry D. Lindstrom, Charles W. Lugar, III, Gilbert S. Staten
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Patent number: 5559111Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: September 24, 1996Assignee: Ciba-Geigy CorporationInventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
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Patent number: 5554755Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6 -hydroxy-2-(4-hydroxyphenyl )-3-[4-(2 -piperidinoethoxy)benzoyl]benzo[.beta.]thiophene.Type: GrantFiled: March 15, 1995Date of Patent: September 10, 1996Assignee: Eli Lilly and CompanyInventor: Alexander G. Godfrey
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Patent number: 5552412Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: January 9, 1995Date of Patent: September 3, 1996Assignee: Pfizer IncInventors: Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati
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Patent number: 5534533Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.Type: GrantFiled: September 28, 1994Date of Patent: July 9, 1996Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Toshiyuki Kato, Yozo Hori
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Patent number: 5512584Abstract: Compounds of the formula ##STR1## where A-B-D, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.Type: GrantFiled: November 1, 1994Date of Patent: April 30, 1996Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liliane Unger, Hans P. Hofmann, Hans-Juergen Teschendorf, Berthold Behl, Rudolf Binder
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5489599Type: GrantFiled: June 28, 1993Date of Patent: February 6, 1996Assignee: Shell Research LimitedInventors: Paul A. Carter, Steven J. Tapp, Nicholas J. Daniels
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Patent number: 5472962Abstract: A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc.This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.Type: GrantFiled: May 13, 1994Date of Patent: December 5, 1995Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Teruaki Matsui, Mamoru Mieda, Hiroo Takahashi, Tomoyuki Saito, Kenyu Shibata
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Patent number: 5466810Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[.beta .]thiophene.Type: GrantFiled: June 10, 1994Date of Patent: November 14, 1995Assignee: Eli Lilly and CompanyInventor: Alexander G. Godfrey
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Patent number: 5464836Abstract: A description follows of benzophenones having an antifungal activity and responding to the general formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, the same or different, represent C.sub.1 -C.sub.6 alkyl groups, C.sub.7 -C.sub.10 arylalkyl groups; or R.sub.1 and R.sub.2, considered jointly with N, represent a C.sub.3 -C.sub.8 heterocyclic group or a C.sub.2 -C.sub.7 heterocyclic group containing a second hetero-atom selected from O and S, said heterocyclic groups being optionally subsituted with one or more C.sub.1 -C.sub.4 alkyl groups;R.sub.3 and R.sub.4, the same or different, represent H atoms, C.sub.1 -C.sub.3 alkyl groups;K represents an oxygen atom or methylene;A represents a benzene group, optionally sustituted with one or more halogen atoms, C.sub.1 -C.sub.4 alkyl or haloalkyl groups, C.sub.1 -C.sub.4 alkoxylics, C.sub.1 -C.sub.4 haloalkoxylics;Y represents a C.sub.6 -C.sub.10 aryl group; said group may be optionally substituted with one or more halogen atomos, C.sub.1 -C.sub.Type: GrantFiled: October 5, 1993Date of Patent: November 7, 1995Assignee: Ministero dell'Universita` e della Ricerca Scientifica e TecnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5462947Abstract: A compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2-- or 4--CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub. 2 -C.sub.8 alkenyl, C.sub.2 -C.sub.Type: GrantFiled: October 12, 1993Date of Patent: October 31, 1995Assignee: The Upjohn CompanyInventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson