Benzene Ring Bonded Directly Or Attached Indirectly By An Acyclic Carbon Or An Acyclic Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 548/506)
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Patent number: 6355805Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.Type: GrantFiled: June 8, 1999Date of Patent: March 12, 2002Assignee: Advanced Medicine, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Publication number: 20020006928Abstract: The invention features pharmaceutically-active indoles and indazoles that are substituted with phenyl, methods of making them, and methods of using them.Type: ApplicationFiled: March 29, 2001Publication date: January 17, 2002Inventors: J. Guy Breitenbucher, Wenying Chai
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Patent number: 6300364Abstract: Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;.Type: GrantFiled: January 24, 2000Date of Patent: October 9, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Teruhiko Shimokawa, Satomi Nishijima, Koyo Matsuda, Yuichi Iizumi, Seiichi Hashimoto
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Patent number: 6211224Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: October 26, 1998Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
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Patent number: 6090839Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type 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: December 19, 1997Date of Patent: July 18, 2000Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
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Patent number: 5965745Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.Type: GrantFiled: July 1, 1998Date of Patent: October 12, 1999Assignee: Pfizer IncInventors: Matthew F. Brown, Anthony Marfat
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Patent number: 5932743Abstract: The present invention relates to novel substituted indole compounds of formula (I) ##STR1## having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.Type: GrantFiled: July 29, 1998Date of Patent: August 3, 1999Assignee: American Home Products CorporationInventors: Michael D. Collini, John W. Ellingboe
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Patent number: 5919947Abstract: The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.Type: GrantFiled: September 2, 1998Date of Patent: July 6, 1999Assignee: Merck Sharp & Dohme Ltd.Inventor: Adrian Leonard Smith
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Patent number: 5854277Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: December 29, 1998Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
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Patent number: 5852049Abstract: The present invention relates to new aromatic ethers derived from indole and having general formula (I) as well as to their preparation methods, pharmaceutical compositions containing them and their utilization as a medicament for the treatment of diseases linked to the dysfunction of the 5HT.sub.1 -like receptors.Type: GrantFiled: March 21, 1997Date of Patent: December 22, 1998Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Serge Halazy, Gareth John, Jean-Pierre Valentin, Peter Pauwels
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Patent number: 5817689Abstract: An indole derivative of the formula: ##STR1## wherein R.sub.1 is lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, lower alkoxycarbonyl, phenyl-lower alkoxy, lower alkyl being optionally substituted by hydroxy, di-lower alkylaminosulfonyl, etc., R.sub.2 is hydrogen, halogen, lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, etc., R.sub.3 is hydrogen or lower alkyl, R.sub.4 is halogen or trifluoromethyl, R.sub.5 is lower alkyl, or a salt thereof, these compounds being potent .beta..sub.3 -adrenergic receptor-stimulating agent with excellent adrenoceptor selectivity, and being useful in the prophylaxis or treatment of obesity or diabetes mellitus.Type: GrantFiled: May 29, 1997Date of Patent: October 6, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Hiroshi Harada, Yoshimi Hirokawa, Naoyuki Yoshida, Hitoshi Kawashima
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Patent number: 5804595Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.Type: GrantFiled: December 5, 1995Date of Patent: September 8, 1998Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, An-Chih Chang
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Patent number: 5674889Abstract: The present invention relates to compounds of formula (I) and salts and prodrugs thereof, wherein Q.sup.1 represents a phenyl group substituted by one or more halo optionally substituted naphthyl, optionally substituted indolyl, optionally substituted benzthiophenyl, optionally substituted benzofuranyl, optionally substituted benzyl or optionally substituted fluorenyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; Z.sup.1 represents a group selected from (a) or (b). The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.Type: GrantFiled: August 21, 1995Date of Patent: October 7, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Fintan Kelleher, Richard Thomas Lewis, Angus Murray Macleod
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Patent number: 5607962Abstract: Substituted indole derivatives are prepared by reacting appropriate carboxylic acids, if appropriate in the presence of auxiliaries, with appropriate amines. The substituted indole derivatives are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis and restenosis.Type: GrantFiled: January 25, 1996Date of Patent: March 4, 1997Assignee: Bayer AktiengesellschaftInventors: Matthias M uller-Gliemann, Ulrich M uller, Martin Beuck, Siegfried Zaiss, Christoph Gerdes, Anke Domdey-Bette, Rudi Gr utzmann, Stefan Lohmer, Stefan Wohlfeil, Ozkan Yalkinoglu, James Elting, Dirk Denzer
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Patent number: 5594012Abstract: A novel anti-active oxygen agent which comprises as active ingredient an amino acid derivative represented by the following general formula (I): ##STR1## wherein Ar represents a 2-hydroxyphenyl, 2-hydroxy-1-naphthyl or pyridyl group, and one or more of the hydrogen atoms attached to the aromatic ring of these groups may be substituted with a halogen atom, or an alkyl, hydroxyl, hydroxyalkyl, nitro, alkoxyl or carboxyl group; R represents the side chain of an amino acid; X represents --CH.sub.2 --NH-- or --CH.dbd.N--; Y represents a hydrogen atom, --COOR.sup.1, --SO.sub.3 H, --CON(R.sup.2)R.sup.3, --CONHCH(R.sup.5)COOR.sup.4 or --CH.sub.2 OH (where each of R.sup.1 to R.sup.4 represents a hydrogen atom or an alkyl group, and R.sup.5 represents the side chain of an amino acid); and n represents an integer of 0 or 1;or its salt,and which inhibits generation of active oxygen species, has a high safety and can be prepared at relatively low costs.Type: GrantFiled: October 6, 1994Date of Patent: January 14, 1997Assignee: Ajinomoto Co., Inc.Inventors: Manabu Kitazawa, Keiji Iwasaki
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Patent number: 5532237Abstract: Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid receptor.Type: GrantFiled: February 15, 1995Date of Patent: July 2, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Michel Gallant, Yves Gareau, Daniel Guay, Marc Labelle, Petpiboon Prasit
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Patent number: 5508432Abstract: CCK modulators, e.g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.Type: GrantFiled: June 8, 1994Date of Patent: April 16, 1996Assignee: Glaxo Wellcome Inc.Inventors: Elizabeth E. Sugg, Milana Dezube, Gavin C. Hirst
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Patent number: 5502061Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: September 26, 1994Date of Patent: March 26, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Y. Hui, Charles D. Jones, Louis N. Jungheim, Pamela A. Pennington
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Patent number: 5482960Abstract: Novel indole and indoline nonpeptide antagonists of endothelin I are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure and subarachnoid hemorrhage.Type: GrantFiled: November 14, 1994Date of Patent: January 9, 1996Assignee: Warner-Lambert CompanyInventors: Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
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Patent number: 5403851Abstract: This invention relates to novel substituted tryptamine and phenalkylamine and related compounds, pharmaceutical compositions thereof and methods of using said compounds and compositions for a number of pharmaceutical indications including (but not limited to): 1. central nervous system and psychiatric disorders (e.g., sleep disorders, epilepsy and other convulsive disorders, anxiety, psychiatric diseases, neurodegenerative diseases, fever); 2. chronobiological-based disorders (e.g., jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder); 3. endocrine indications (e.g., contraception and infertility, precocious puberty, premenstrual syndrome, hyperprolactinemia, growth hormone deficiency); 4. cancer and other proliferative diseases; 5. immune system disorders and conditions associated with senescence; 6. ophthalmological diseases; 7. animal breeding (e.g., regulation of fertility, puberty, pelage color).Type: GrantFiled: April 5, 1994Date of Patent: April 4, 1995Assignee: Interneuron Pharmaceuticals, Inc.Inventors: Kay J. D'Orlando, Kenneth W. Locke, Emile M. Bellott, Richard L. Gabriel, Michael D. Nohrden, Yesh P. Sachdeva, Salah A. Zahr, Emile Al-Farhan, Subramaniam Krishnananthan
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Patent number: 5389616Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.Type: GrantFiled: July 29, 1993Date of Patent: February 14, 1995Assignee: Hoffman-LaRoche Inc.Inventors: Quirico Branca, Werner Neidhart, Jenri Ramuz, Henri Ramuz, Heinz Stadler, Wolfgang Wostl
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Patent number: 5348949Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.Type: GrantFiled: February 12, 1993Date of Patent: September 20, 1994Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
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Patent number: 5318994Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.Type: GrantFiled: November 3, 1992Date of Patent: June 7, 1994Assignee: Adir et CompagnieInventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
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Patent number: 5302724Abstract: This invention provides certain sulfonamide compounds, formulations and method of use of certain sulfonamide compounds in treating susceptible neoplasms.Type: GrantFiled: April 29, 1992Date of Patent: April 12, 1994Assignee: Eli Lilly and CompanyInventors: J. Jeffry Howbert, Fariborz Mohamadi, Michael M. Spees
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Patent number: 5206377Abstract: Melatonin compounds are disclosed of the formula ##STR1## where R is hydrogen or C.sub.1 to C.sub.6 linear or branched alkylene substituted with phenyl; R.sub.1 is hydrogen, substituted benzyl, naphthylmethyl or taken together with R.sub.2 and the two carbon atoms of the five-membered hetero ring form the group ##STR2## where R.sub.1 ' is C.sub.1 to C.sub.6 linear or branched alkanoyl and R.sub.1 " is hydrogen, C.sub.1 to C.sub.6 linear or branched alkyl or phenyl optionally substituted with one or more halogen, amino, nitro, hydroxy, alkyl, alkoxy or haloalkyl; R.sub.2 is hydrogen, 1-pyrrolyl, 1-pyrrolyl substituted with one or more alkyl or alkoxy, the group --(CH.sub.2).sub.m --NHR.sub.2 '1, where m is 1 to 3 and R.sub.2 ' is phenyl sulfonyl, the phenyl group optionally substituted with alkyl, or --C(O)--R.sub.2 ", where R.sub.2 " is C.sub.1 to C.sub.Type: GrantFiled: December 5, 1991Date of Patent: April 27, 1993Assignee: Whitby Research, Inc.Inventor: Donald A. McAfee
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Patent number: 5183894Abstract: The present invention relates to 2-substituted-1-hydroxyindoles of the following formula: ##STR1## wherein, R.sup.1 is an electron withdrawing group,R.sup.2 is an alkenyl having 2-10 carbon atoms, and N-substituted .alpha.-iminobenzyl group wherein the substituents are selected from the group consisting of phenyl, anilino and dimethylamino, an unsubstituted aromatic group, and an aromatic group having meta or para substituents which are nitro, trifluoromethyl, fluoro, formyl, hydroxyiminomethyl and carbamoyl,R.sup.3 is a halogen atom, andn is 0, 1, or 2,provided that when R.sup.2 is either phenyl or nitro substituted phenyl and n is 0, then R.sup.1 is not cyano.Type: GrantFiled: July 1, 1991Date of Patent: February 2, 1993Assignee: Eastman Kodak CompanyInventors: William R. Schleigh, Thomas R. Welter
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Patent number: 5124449Abstract: Azaporphyrin derivatives of the formula ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, unsubstituted or substituted C.sub.1 -C.sub.20 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl or unsubstituted or substituted phenyl, or two adjacent R.sup.1 radicals form, together with the carbon atoms to which they are bonded, an unsaturated or aromatic 5- to 7-membered carbocyclic ring,X are each hydrogen or C.sub.1 -C.sub.4 -alkyl andp are each 1 or 2, andbiladienes of the formula ##STR2## where R.sup.1, R.sup.2, X and p each have the abovementioned meanings, m and n are each 0 or 1 and An.sup..crclbar. is an anion, as intermediates therefor, are used for preparing vinylogous porphyrin derivatives.Type: GrantFiled: August 23, 1991Date of Patent: June 23, 1992Assignee: BASF AktiengesellschaftInventors: Burchard Franck, Hartmann Koenig, Christian Eickmeier, Michael Voelker, Thomas Wessel
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Patent number: 5114952Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Said sulfonamide compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO-- or --CH(OH)--; n is two, three or four; and "Het" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is preferably 2H-3,4-dihydroisoquinol-1-on-2-yl or 2H-isoquinol-1-on-2-yl, each optionally substituted with halogen or C.sub.1 -C.sub.4 alkyl.Type: GrantFiled: November 21, 1990Date of Patent: May 19, 1992Assignee: Pfizer Inc.Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
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Patent number: 4987133Abstract: New salicylic acid derivatives of the general formula I ##STR1## in which R.sup.1 is H or CH.sub.3,R.sup.2 is 4-(4-methyl-2-thiazolyl)-piperazino, 4-(tetrahydro-2-furoyl)-piperazino, 4-(4-methyl-2-thiazolyl)-homopiperazino, 4-benzamidopiperidino, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolino, 1-imidazolyl, tribromo-1-imidazolyl or 2-(3-indolyl-1,1-dimethyl-ethylamino andR.sup.3 is alkoxy having 1-C atoms, NH.sub.2 or alkylamino having 1-4 C atoms,as well as the physiologically acceptable acid addition salts thereof, exhibit effects on the circulation, especially effects lowering the blood pressure and relieving the heart, and diuretic effects.Type: GrantFiled: April 17, 1989Date of Patent: January 22, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Adolf Kurmeier, Wolf-Dietrich Weber, Hans-Eckart Radunz, Hans-Jochen Schliep
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Patent number: 4977272Abstract: This invention relates to new compounds of the formula: ##STR1## where each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 has zero to 10 C atoms, and no acetylenic unsaturation; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from H and hydrocarbyl; with the proviso that R.sup.6 is C.sub.1 -C.sub.10 hydrocarbyl; each of R.sup.5 and R.sup.Type: GrantFiled: June 29, 1989Date of Patent: December 11, 1990Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James E. Rinz, Gilles Klopman, Teodora T. Kopp
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Patent number: 4918094Abstract: This invention provides a series of novel heterocyclic amides of formula I in which the group >X-Y-Z< is selected from >C.dbd.CH--N<, >C.dbd.N--N<, >N--(CH.sub.2)--N<, >CH--CH.sub.2 --N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds: pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: October 16, 1986Date of Patent: April 17, 1990Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 4894387Abstract: Compounds are disclosed of the general formula (I) ##STR1## wherein R.sub.1 represents halogen, alkyl, alkoxy or hydroxyl, or a group NR.sub.a R.sub.b or CON.sub.a R.sub.b, where R.sub.a and R.sub.b are hydrogen, alkyl or alkenyl or with the nitrogen atom form a saturated monocyclic 5 to 7-membered ring;R.sub.2 represents hydrogen or alkyl;R.sub.3 and R.sub.4 represent hydrogen, C.sub.1-3 alkyl or propenyl or R.sub.3 and R.sub.4 together form an aralkylidene group; Alk represents a C.sub.2-3 alkylene chain;n and m, are integers of 1 to 4 or n is zero, and their physiologically acceptable salts and solvates.The compounds are described as useful in treating pain originating from dilatation of the cranial vasculature in particular migraine and cluster headache and can be formulated in conventional manner as pharmaceutical compositions with carriers or excipients for administration by any convenient route.Type: GrantFiled: March 26, 1987Date of Patent: January 16, 1990Assignee: Glaxo Group LimitedInventors: Darko Butina, Michael D. Dowle, Ian H. Coates
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Patent number: 4863948Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic moiety is a 5- or 6-membered nitrogen-containing heterocyclic group which is attached to the adjacent carbon atom by a carbon or nitrogen atom and optionally contains a further heteroatom selected from oxygen and nitrogen, said nitrogen-containing heterocyclic group being either (i) substituted by a phenyl or benzyl group or (ii) fused at two adjacent carbon atoms to a benzene ring, with the resulting heterocyclic ring moiety also being optionally substituted. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. The most preferred member compound of the series is 2-hydroxy-2-(4-methanesulphonamidophenyl)-N-methyl-N-[2-(6-chloro-2H-isoin dolin-1-on-2-yl)ethyl]ethylamine.Type: GrantFiled: April 9, 1987Date of Patent: September 5, 1989Assignee: Pfizer, Inc.Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
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Patent number: 4843081Abstract: A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.Type: GrantFiled: June 27, 1988Date of Patent: June 27, 1989Assignee: Rorer Pharmaceutical CorporationInventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
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Patent number: 4837235Abstract: This invention provides a series of novel keto sulfones of formula I ##STR1## in which the group .dbd.A-- is selected from .dbd.C(Ra)-- and .dbd.N-- and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: October 16, 1986Date of Patent: June 6, 1989Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 4772599Abstract: New benzodiazepine derivatives of the general formula ##STR1## wherein X.sup.1 and X.sup.2 independently are ##STR2## wherein R.sup.1 is C.sub.1-3 -alkyl, C.sub.3-5 -cycloalkyl, C.sub.1-3 -alkoxymethyl, C.sub.1-3 -hydroxyalkyl, or aryl,R.sup.4 is hydrogen, andR.sup.5 is C.sub.1-6 -alkyl, or wherein R.sup.4 and R.sup.5 together form a 2-4 membered alkylene chain.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.Type: GrantFiled: March 13, 1987Date of Patent: September 20, 1988Assignee: A/S FerrosanInventor: Frank Watjen
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Patent number: 4740611Abstract: Disclosed are new compounds ##STR1## where each of R and R' have zero to 10 C atoms; R is H or hydrocarbyl; R' is H, hydrocarbyl, or hydrocarbyl substituted with hydrocarbylcarbonylamino, di(hydrocarbylcarbonyl)amino, hydrocarbylcarbonyl(hydrocarbyl)amino, formylamino, diformylamino and formyl(hydrocarbyl)amino, hydrocarbyloxy, hydrocarbylthio, formylthio, hydrocarbylcarbonylthio, hydrocarbyloxycarbonyl, hydrocarbyl carboxyl, hydrocarbylamino, dihydrocarbylamino, formyl, 3-indolyl, 3-(1-hydrocarbyl)indolyl, 3-(1-hydrocarbylcarbonyl)indolyl, 3-(1-formyl)indolyl, carbamoyl, hydrocarbylcarbamoyl, dihydrocarbylcarbamoyl, 5-imidazolyl, 5-(3-hydrocarbyl)imidazolyl, 5-(3-hydrocarbylcarbonyl)imidazolyl, or 5-(3-formyl)imidazolyl, and R" is phenyl or a C.sub.1 to C.sub.6 alkyl group; and methods of making such compounds.Type: GrantFiled: October 30, 1986Date of Patent: April 26, 1988Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James E. Rinz, Gilles Klopman, Teodora T. Kopp
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Patent number: 4672067Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10, whereR.sub.8 represents alkyl, cycloalkyl, aryl or aralkyl,R.sub.9 represents hydrogen or alkyl, andR.sub.10 represents hydrogen or alkyl, cycloalkyl, aryl or aralkyl;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7 each independently represents hydrogen or C.sub.1-3 alkyl;R.sub.5 represents hydrogen, or alkyl, cycloalkyl, alkenyl or aralkyl, orR.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the attached nitrogen atom form a saturated monocyclic 5- to 7-membered ring; andAlk represents C.sub.2-3 alkylene chain optionally substituted by not more than two C.sub.1-3 alkyl groups;and physiologically acceptable salts and solvates thereof.Type: GrantFiled: June 28, 1984Date of Patent: June 9, 1987Assignee: Glaxo Group LimitedInventors: Ian H. Coates, Keith Mills, Colin F. Webb, Michael D. Dowle, David E. Bays
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Patent number: 4663334Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y is alkyl, alkoxy, alkoxyalkyl, chloro, fluoro, bromo or carboxamidoalkyl and R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, chloro, fluoro or dialkylamino, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.Type: GrantFiled: December 11, 1985Date of Patent: May 5, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4579865Abstract: Compounds of the structure; ##STR1## and pharmaceutically acceptable salts thereof, wherein:R.sub.1 is H, alkyl, alkoxy, carboxyl, alkylcarboxy, trifluoromethyl, halogen, nitro or hydroxy;X is O, N, S or C;Y is O, N or S; andR.sub.2 is H, alkyl, cycloalkyl, aryl or heteroaryl useful in the treatment of ischemic heart disease and hypertriglyceridemia.Type: GrantFiled: March 28, 1984Date of Patent: April 1, 1986Assignee: USV Pharmaceutical Corp.Inventors: John H. Musser, Charles A. Sutherland
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Patent number: 4507483Abstract: 3-[(Substituted-amino)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color-formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with amines or precursors thereof in the presence of a base.Type: GrantFiled: March 9, 1983Date of Patent: March 26, 1985Assignee: The Hilton-Davis Chemical Co.Inventors: Paul J. Schmidt, William M. Hung
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Patent number: 4485242Abstract: 3-[(Alkoxy)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with alcohols in the presence of a base.Type: GrantFiled: July 30, 1981Date of Patent: November 27, 1984Assignee: Sterling Drug Inc.Inventors: Paul J. Schmidt, William M. Hung
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Patent number: 4398030Abstract: 3-[(Substituted-amino)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color-formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with amines or precursors thereof in the presence of a base.Type: GrantFiled: January 22, 1982Date of Patent: August 9, 1983Assignee: Sterling Drug Inc.Inventors: Paul J. Schmidt, William M. Hung