Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 514/310)
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Patent number: 5514689Abstract: The blue marine sponge Cribrochalina sp., collected in the Republic of the Maldives, was found to contain the new cell growth inhibitory isoquinolinequinones designated cribrostatin 1 (8.8.times.10.sup.-6 % yield) and 2 (3.1.times.10.sup.-6 % yield) which are active against the P388 lymphocytic leukemia cell line (PS ED.sub.50 1.58 .mu.g/mL, PS ED.sub.50 2.73 .mu.g/mL, respectively). Importantly, both cribrostatins 1 and 2 have shown selective activity against all of the nine human melanoma cell lines employed by the U.S. National Cancer Institute. Structural determinations of both substances were accomplished utilizing high field NMR (400 MHz) and mass spectral studies. Confirmation of the cribrostatin 1 structure was achieved by X-ray crystallographic techniques.Type: GrantFiled: August 8, 1991Date of Patent: May 7, 1996Assignee: Arizona Board of RegentsInventors: Jeremiah C. Collins, George R. Pettit
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Patent number: 5514688Abstract: This invention relates to carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: May 12, 1994Date of Patent: May 7, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser
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Patent number: 5508288Abstract: A compound of formula (I) or a salt thereof: ##STR1## Wherein: P represents a quinoline or isoquinoline residue; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2, R.sub.3, R.sub.10, R.sub.11 are independently hydrogenR.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2, R.sub.3, R.sub.10, R.sub.11 are independently hydrogen or C.sub.1-6 alkyl, or R.sub.10 and R.sub.11 together form a bond, or R.sub.2 and R.sub.10 or R.sub.3 and R.sub.11 together form a C.sub.2-6 alkylene chain. R.sub.4 is hydrogen, C.sub.1-6 alkyl, halogen, NR.sub.8 R.sub.9, OR.sub.12 or COOR.sub.12, where R.sub.8 R.sub.9 and R.sub.12 are independently hydrogen or C.sub.1-6 alkyl; R.sub.5 and R.sub.6 are independently hydrogen or C.sub.1-6 alkyl; and R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen; and wherein the urea moiety is attached at the 4-, 5- or 6-position of the indoline ring, which has been found to have 5HT.sub.1c receptor antagonist activity.Type: GrantFiled: August 30, 1994Date of Patent: April 16, 1996Assignee: SmithKline Beecham, p.l.c.Inventors: Ian T. Forbes, Roger T. Martin, Graham E. Jones
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Patent number: 5498779Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.Type: GrantFiled: May 22, 1995Date of Patent: March 12, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Bernhard Neises, Axel Ganzhorn, Celine Tarnus, Robert J. Broersma, Jr.
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Patent number: 5496827Abstract: A composition having therapeutic and cosmetic effects is comprised of an effective concentration of methyl nicotinate in a diluent. When such a composition is topically applied the methyl nicotinate acts to increase circulation in the area of application and also acts as a pain reliever and a muscle relaxant. The composition may also contain various vitamins, minerals and other nutrients. The methyl nicotinate also acts as a facilitator to promote the transdermal penetration of the vitamins, minerals and other nutrients into the skin.Type: GrantFiled: July 15, 1994Date of Patent: March 5, 1996Inventor: Jay Patrick
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Patent number: 5491150Abstract: A supplementary therapeutic agent for the treatment of immunodeficiency syndrome with reduced NK (natural killer) activity and an immunopotentiator preparation containing it are provided.A supplementary therapeutic agent for immunopotentiation which comprises L-cysteine, L-cystine, or L-glutamine, or salts thereof and is used in combination with an immunopotentiator such as lentinan, OK-432, sizofiran or the like, and an immunopotentiator preparation containing the agent. This combination of agents is useful as a supplementary therapeutic agent for the treatment of an immunodeficiency, such as low NK activity syndrome, chronic fatigue syndrome, acquired immunodeficiency syndrome, or congenital immunodeficiency syndromes.Type: GrantFiled: January 27, 1994Date of Patent: February 13, 1996Assignee: Ajinomoto Co., Inc.Inventors: Tadao Aoki, Hideo Miyakoshi
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Patent number: 5480888Abstract: An inhibitor for restenosis after percutaneous coronary arterioplasty, which comprises, as an active ingredient, a compound of the following formula (1), (1') or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C1-C6 alkyl group or a C1-C6 alkoxyl group, and R.sup.1 and R.sup.2 may be linked to form a methylenedioxy group; R.sup.3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R.sup.4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-.alpha.-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; R.sup.5 is a hydrogen atom or a C1-C6 alkyl group, and R.sup.4 and R.sup.Type: GrantFiled: July 11, 1994Date of Patent: January 2, 1996Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kazuhisa Kodama, Atsushi Hirayama, Hiroyuki Masayasu
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Patent number: 5480889Abstract: The present invention provides compositions and methods for promoting hair growth. The methods generally comprise the administration to a patient of a therapeutically effective amount of the compositions of the present invention which employ a vasodilator in combination with estradiol and/or a 5-.alpha.-reductase inhibitor in a pharmaceutically acceptable vehicle. The compositions and methods of the present invention are suitable for the treatment of baldness, in particular, male pattern baldness.Type: GrantFiled: February 17, 1995Date of Patent: January 2, 1996Inventor: Boris E. Goldman
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Patent number: 5475006Abstract: .beta.-Carotene and canthaxanthin, as representative carotenoids, and to a lesser extent, retinoic acid, a representative retinoid, undergo extensive oxidation to yield substances, insofar as oxidized .beta.-carotene is a model, which have properties useful as non-toxic agents active against cell proliferation, tumors, and tumorigenic viruses, and useful as promoters of cell differentiation. It is evident from chemical analysis of the highly oxidized .beta.-carotene product mixture that none of the various forms of vitamin A are present or are present only in minor amounts. Furthermore, the biological activities of oxidized canthaxanthin and retinoic acid, which cannot form, vitamin A, indicate the presence of active substances that are different from vitamin A. Although the anti-proliferative and differentiation promotion activities of oxidized .beta.-carotene resemble those of vitamin A itself, generally the effects are more powerful for oxidized .beta.-carotene in a wide variety of circumstances.Type: GrantFiled: August 10, 1994Date of Patent: December 12, 1995Assignee: National Research Council of CanadaInventors: Graham Burton, Janusz Daroszewski, Jenny Phipps
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Patent number: 5461049Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.Type: GrantFiled: May 27, 1994Date of Patent: October 24, 1995Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic
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Patent number: 5449679Abstract: Methods and pharmaceutical compositions for reducing the biological fluid level of a lipid soluble waste in a subject are provided. The methods involve selecting a subject diagnosed as having a hyperlipidemia-associated condition and subcutaneously introducing into the subject a biodegradable implant containing a pro-inflammatory lipid that promotes formation of an angiogenic tissue capsule containing a plurality of foam cells. The pro-inflammatory lipid is delivered in an amount sufficient to attain a detectable reduction in the biological fluid level of the lipid soluble waste.Type: GrantFiled: July 29, 1994Date of Patent: September 12, 1995Inventor: Robert J. Leonard
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Patent number: 5447940Abstract: Absorbable composite materials are described that comprise a collagen matrix reinforced with a layer of a bioabsorbable polymer. A chemotherapeutic agent is dispersed in the composite material. The layer of bioabsorbable polymer is preferably a woven, nonwoven or knitted mesh layer of a synthetic bioabsorbable polymer such as polylactic/polyglycolic acid copolymer, or oxidised regenerated cellulose. The chemotherapeutic agent may be an antibiotic, an anaesthetic, an antiseptic or an anti-inflammatory. Strips of the composite material are inserted into the periodontal pocket, where they are retained in place and provide effective sustained release of the chemotherapeutic agent over an extended period.Type: GrantFiled: July 27, 1994Date of Patent: September 5, 1995Assignee: Johnson & Johnson Medical, Inc.Inventors: Wilson Harvey, Nicholas D. Light, Carla A. Haynes
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Patent number: 5447939Abstract: Disclosed herein are methods directed generally to the control of neural activity and to the treatment of neural disorders. More particularly, the present invention is directed to methods for the modification of mammalian neural activity through the administration of carbon monoxide dependent guanylyl cyclase modulating purine derivatives. The methods of the present invention may be used to affect a variety of neurological activities and to therapeutically or prophylactically treat a wide variety of neurodegenerative and neurological disorders.Type: GrantFiled: July 25, 1994Date of Patent: September 5, 1995Inventors: Alvin J. Glasky, Michael P. Rathbone
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Patent number: 5446071Abstract: The present invention provides methods for lowering serum cholesterol comprising administering to a mammal in need of treatment a serum cholesterol lowering amount of a compound of formula I or formula II ##STR1## wherein L is --CON< or --N<; andthe dotted line in the B-ring is an optional bond; or a pharmaceutically acceptable salt thereof; and ##STR2## wherein Q is a moiety having the formula ##STR3## L is --CON< or --N<; B is --O--, --S--, --CH.sub.2 -phenyl-O--, -phenyl-O--, or -benzyl-O--;G is a moiety which together with L forms a substituted or unsubstituted heterocyclic ring having at least one nitrogen atom or is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(lower)alkyl, cyano(lower)alkyl, carboxy(lower)alkyl, (lower)alkoxycarbonyl(lower)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.7 -C.sub.11)aryl akyl, di(lower)alkylamino(lower)alkyl, and fluoro-substituted analogs of the foregoing;Z is --O--, --S--, --CH.sub.Type: GrantFiled: November 18, 1994Date of Patent: August 29, 1995Assignee: Eli Lilly and CompanyInventor: Timothy A. Grese
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Patent number: 5434163Abstract: A method of treatment of Cryptococcus neoformans infection by administering to a patient in need thereof an effective amount of a benzimidazile compound.Type: GrantFiled: May 14, 1993Date of Patent: July 18, 1995Assignee: The Medical College of PennsylvaniaInventors: Thomas D. Edlind, Maria C. Cruz
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Patent number: 5428070Abstract: Atherogenesis and restenosis are treated by long term administration of physiologically acceptable compounds which enhance the level of endogenous nitric oxide in the host. Alternatively, or in combination, other compounds may be administered which provide for short term enhancement of nitric oxide, either directly or by physiological processes. In addition, cells may be genetically engineered to provide a component in the synthetic pathway to nitric oxide, so as drive the process to enhance nitric oxide concentration, particularly in conjunction with the administration of a nitric oxide precursor.Type: GrantFiled: June 11, 1993Date of Patent: June 27, 1995Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: John P. Cooke, Victor J. Dzau, Gary H. Gibbons
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Patent number: 5416094Abstract: Described are guanidinocarbonyl isoquinolines of the formula I, ##STR1## wherein R(1) is hydrogen, (amino) (cyclo) (aryl)alk(en)yl (heteroaryl); R(2) is hydrogen, halogen, alkyl, or aryl; G is a radical of the formula VII: ##STR2## X(2), X(3) and X(4) are hydrogen, halogen, nitro, amino, alkyl, sulfonamide, (mono) (di) (lower alkyl) (amino), benzyloxy, hydroxy; X(1) hydrogen, oxygen, sulfur and NR(7)R(8), and their pharmaceutically acceptable salts; described is also a process for their preparation, their use as medicaments, and medicaments containing them for treating congestive heart failure, and arrhythmic conditions as well as cardioprotective agents in mammals.Type: GrantFiled: September 24, 1993Date of Patent: May 16, 1995Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Ramesh Gidwani, Ramanujam Rajagopalan, Radha Panicker, Chinnakulandai Sankar, Hans-Jochen Lang, Heinrich Englert, Wolfgang Scholz
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Patent number: 5407944Abstract: The present invention provides compositions and methods for promoting hair growth. The methods generally comprise the administration to a patient of a therapeutically effective amount of the compositions of the present invention which employ a vasodilator in combination with estradiol and/or a 5-.alpha.-reductase inhibitor in a pharmaceutically acceptable vehicle. The compositions and methods of the present invention are suitable for the treatment of baldness, in particular, male pattern baldness.Type: GrantFiled: February 19, 1993Date of Patent: April 18, 1995Inventor: Boris E. Goldman
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Patent number: 5397790Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; andA is an isoquinoline group which may be substituted by alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: June 13, 1994Date of Patent: March 14, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5397788Abstract: Novel .alpha.-substituted Trp dipeptoid derivatives cyclized at the C-terminal useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds of the invention are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the compounds as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the compounds in diagnostic compositions.Type: GrantFiled: April 20, 1993Date of Patent: March 14, 1995Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson
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Patent number: 5393775Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: September 7, 1993Date of Patent: February 28, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
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Patent number: 5389663Abstract: An azole compound represented by the formula (I): ##STR1## wherein X is a nitrogen atom; Ar is a phenyl group substituted by halogen or a halogenated C.sub.1-4 alkyl group; R.sup.1 and R.sup.2 independently are a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 may combine together to form a lower alkylene group; n denotes an integer of 0 to 2; and R.sup.7 is a hydrogen atom, a hydroxyl group which may be optionally acylated by an acyl group selected from acetyl, propionyl, butyryl, isobutyryl, phenylacetyl and benzoyl, or may form a bond together with R.sup.1 ; or a salt thereof.Type: GrantFiled: November 24, 1993Date of Patent: February 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Kenji Okonogi, Akihiro Tasaka
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Patent number: 5380723Abstract: Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R; R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;R.sub.1 represents H or C.sub.1 -C.sub.6 alkyl;R.sub.2 represents 2-(3-indolyl)ethyl or aralkyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may form an N-containing 5 to 6 membered hetero ring, an N, O-containing hetero ring, which hetero ring may be fused with benzene;n is an integer of 4 to 8;with the proviso that X and Y both do not represent H or piperizinoethyl when n is 4, or pharmaceuticaly acceptable acid addition salts thereof. They are useful as an antiulcer agent.Type: GrantFiled: April 15, 1994Date of Patent: January 10, 1995Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Hitoshi Inoue, Masato Horigome, Kenichi Momose, Masanori Sugita, Kouichi Katsuyama, Chikako Suzuki, Shinji Nagai, Masao Nagase, Koichi Nakamaru
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Patent number: 5352442Abstract: Topical 2,2,6,6-tetramethyl-1-piperdinyloxyl (TEMPO) is disclosed. The compound has utility in a topical pharmaceutical formulation for the cosmetic treatment of hair loss and the cosmetic stimulation of hair growth.Type: GrantFiled: February 24, 1993Date of Patent: October 4, 1994Inventor: Peter H. Proctor
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Patent number: 5350757Abstract: This invention relates to novel substituted 1,2,3,4-tetrahydroisoquinolines which are useful the treatment of vascular restenosis, various disorders of the central nervous system, in the regulation of female reproductive functions, in cognitive enhancement, in atherosclerosis and in treating excessive AVP secretory disorders. Novel intermediates useful in the preparation of the compounds are also disclosed. Methods of using the compounds and pharmaceutical compositions containing them are disclosed.Type: GrantFiled: June 11, 1993Date of Patent: September 27, 1994Assignee: Warner-Lambert CompanyInventors: Clifton J. Blankley, John C. Hodges, Sylvester Klutchko
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Patent number: 5338739Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: March 10, 1994Date of Patent: August 16, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5328914Abstract: Pyrimidine 3-oxide derivatives and their use for the treatment of hair loss. The compositions contain in a physiologically acceptable medium at least one compound corresponding to the formula (I): ##STR1## in which: R.sub.1 denotes a methyl or NHR.sub.4 group in which R.sub.4 denotes a C.sub.1 -C.sub.4 alkyl group or hydrogen;R.sub.2 denotes hydrogen or a group NHR.sub.4 in which R.sub.4 has the same meaning as above; R.sub.2 may also denote methyl when R.sub.1 denotes methyl; when R.sub.1 denotes NH.sub.2, R.sub.2 cannot be hydrogen;R.sub.3 may denote a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group which may optionally carry;a group OR.sub.5 in which R.sub.5 denotes a C.sub.1 -C.sub.4 alkyl group,a benzene nucleus which is optionally substituted by one or more C.sub.1 -C.sub.4 alkoxy groups;R.sub.3 may also denote a halogen atom or a nitro or amino group;and the physiologically acceptable acid addition salts.Type: GrantFiled: January 19, 1993Date of Patent: July 12, 1994Assignee: L'OrealInventors: Michel Hocquaux, Jacqueline Dumats, Jean B. Galey
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Patent number: 5328915Abstract: Arthropodicidal compounds, compositions and arthropodicidal use of compounds having the formula ##STR1## wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m and n are as defined in the text.Type: GrantFiled: September 17, 1992Date of Patent: July 12, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Jeffrey K. Long, Patrick D. Lowder, Thomas M. Stevenson
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Patent number: 5246943Abstract: This invention relates to novel substituted 1,2,3,4-tetrahydroisoquinolines which are useful in the treatment of vascular restenosis, various disorders of the central nervous system, in the regulation of female reproductive functions, in cognitive enhancement, in atherosclerosis and in treating excessive AVP secretory disorders. Novel intermediates useful in the preparation of the compounds are also disclosed. Methods of using the compounds and pharmaceutical compositions containing them are disclosed.Type: GrantFiled: May 19, 1992Date of Patent: September 21, 1993Assignee: Warner-Lambert CompanyInventors: Clifton J. Blankley, John C. Hodges, Sylvester Klutchko
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Patent number: 5242931Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: March 23, 1992Date of Patent: September 7, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5240950Abstract: There are provided carbazate derivatives of the formula:R.sup.1 --N.dbd.CH--NHNH--R.sup.2wherein R.sup.1 is a heterocyclic group; and R.sup.2 is an esterified carboxyl group, and their salts, which are useful as AGE-formation inhibitory agents.The derivatives or the salts can be produced by reacting compounds of the formula: R.sup.1 --N.dbd.CH--OR.sup.3 wherein R.sup.1 is a heterocyclic group; and R.sup.3 is a lower alkyl group, with a carbazic acid ester or its salt.Type: GrantFiled: September 7, 1989Date of Patent: August 31, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5236934Abstract: Provided are 1,2,3,4-tetrahydroisoquinolines, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat disorders of mammals mediated by AT.sub.2 receptors in the central nervous system.Type: GrantFiled: August 26, 1992Date of Patent: August 17, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary K. VanAtten
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Patent number: 5225420Abstract: The invention relates to the use of compounds of the formula ##STR1## in which p is 2 and q is 1 or p is q and q is 2; Ar represents an optionally substituted phenyl, and Z represents NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2, which may be identical or different, represent H or optionally substituted alkyl or, with the nitrogen atom, form a saturated heterocycle, or Z represents OR in which R is H or optionally substituted alkyl, or their addition salts, in the form of pure enantiomer or of mixtures thereof, for administration in a human patient for preventing or treating pathologies involving or dependent upon a neovascularization.Type: GrantFiled: February 11, 1992Date of Patent: July 6, 1993Assignee: Elf-SanofiInventors: Jean-Pierre Cazenave, Jean-Marc Herbert
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Patent number: 5225402Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO-, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO-, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l 'NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.Type: GrantFiled: September 18, 1991Date of Patent: July 6, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5223517Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.Type: GrantFiled: August 23, 1991Date of Patent: June 29, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5221677Abstract: The invention concerns a heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: September 21, 1990Date of Patent: June 22, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards
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Patent number: 5204348Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.Type: GrantFiled: December 3, 1991Date of Patent: April 20, 1993Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
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Patent number: 5200417Abstract: Isoquinoline compounds, compositions containing them and their use in the inhibition of gastric acid secretion in mammals. A compound of the invention is 1-[(2-Methoxyphenylmethyl)amino]isoquinoline hydrochloride.Type: GrantFiled: April 4, 1990Date of Patent: April 6, 1993Assignee: Smithkline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5198462Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.Type: GrantFiled: October 16, 1991Date of Patent: March 30, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Hiroyuki Tawada, Hitoshi Ikeda
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Patent number: 5185335Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: February 4, 1991Date of Patent: February 9, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
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Patent number: 5124337Abstract: N-acyltetrahydroisoquinolines including novel compounds of the formula ##STR1## wherein R.sup.1 is a C10-C25 alkyl chain; a substituted C10-C25 alkyl chain; an interrupted C10-C25 alkyl chain; a substituted interrupted C10-C25 alkyl chain; diphenylamino; di-(R.sup.2 -substituted phenyl)amino; di-(heteroaryl)amino; di-R.sup.2 -substituted heteroary)amino; diphenylmethyl; or di-(R.sup.2 -substituted phenyl)methyl;R.sup.2 is hydroxy, lower alkyl, lower alkoxy, halogeno, amino, lower alkylamino or di-(lower alkyl)amino;R.sup.3, R.sup.4 and R.sup.5 are independently H or --(CH.sub.2 .sub.n --Ar;Ar is phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl;n=0,1 or 2;m=0,1 or 2;or a pharmaceutically acceptable salt thereof, useful in the treatment of atherosclerosis are disclosed.Type: GrantFiled: May 20, 1991Date of Patent: June 23, 1992Assignee: Schering CorporationInventors: Sundeep Dugar, Timothy Kogan
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Patent number: 5120745Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: September 27, 1990Date of Patent: June 9, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
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Patent number: 5100904Abstract: A novel prolinal derivatives of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.Type: GrantFiled: June 5, 1990Date of Patent: March 31, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5086051Abstract: New derivatives of formula (I) in which R.sub.1 =H, halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH, CH, phenyl or phenoxy, Ar=phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, thienyl, thieno[2,3-b]thienyl or thieno[3,2-b]thienyl (these groups optionally substituted with halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH or CN), p=0, 1 or 2, andA--either Z=valency bond and R.sub.2 =HB--or Z=valency bond and R.sub.2 =pyridyl, quinuclidinyl, 3-pyrrolidinyl, 3- or 4-piperidyl (these groups optionally being substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl)C--or Z=alkylene radical (1 to 4C) and R.sub.2 =2-, 3- or 4-pyridyl, 3-quinuclidinyl, 2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl (optionally substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl) or R.sub.2 =CON(R.sub.3)(R.sub.4) wherea) either R.sub.3 and R.sub.4 form a piperazine optionally substituted with alkyl, hydroxyalkyl, pyridyl, phenyl or phenylalkyl,b) or R.sub.Type: GrantFiled: March 14, 1990Date of Patent: February 4, 1992Assignee: Rhone-Poulenc SanteInventors: Claude James, Daniel Lave, Francoise Soler
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Patent number: 5079256Abstract: A compound of the formula (I) or its salt and a process for producing the compounds. The compounds have the effect of dilating neophrovascular tracts; ##STR1## wherein ##STR2## represents the formula ##STR3## wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl;R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt thereof.Type: GrantFiled: September 26, 1989Date of Patent: January 7, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Akihiro Tanaka, Takashi Fujikura, Ryuji Tsuzuki, Masaki Yokota, Takeyuki Yatsu
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Patent number: 5070097Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-20-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.Type: GrantFiled: October 19, 1990Date of Patent: December 3, 1991Assignee: ICI Americas Inc.Inventor: Michael D. Broadhurst
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Patent number: 5064842Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: June 25, 1990Date of Patent: November 12, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5061715Abstract: This invention relates to quinolyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.Type: GrantFiled: October 3, 1990Date of Patent: October 29, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Sai P. Sunkara, Winton D. Jones
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Patent number: 5047412Abstract: The invention describes novel (2-styryl-, 2-naphthyl- and 2-phenethyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)alkenoic acids and related tetrazoles and sulphonamides, of the formula I wherein Q completes a benzene or pyridine ring, Y is vinylene, Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NHSO.sub.2 R.sup.6, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A.sup.1, A.sup.2, n and m have the meanings defined in the specification, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.Type: GrantFiled: February 1, 1989Date of Patent: September 10, 1991Assignee: Imperial Chemical Industries PLCInventors: George R. Brown, Michael J. Smithers
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Patent number: RE34630Abstract: Novel substituted isoquinoline compounds are disclosed together with novel 2-phenylethylamides useful as precursors or intermediates for the production of the isoquinolines. The substituted isoquinolines exhibit activity in antagonizing the effects of platelet activating factor (PAF).Type: GrantFiled: January 27, 1992Date of Patent: June 7, 1994Assignee: Euroceltique, S.A.Inventors: T. Scott Shoupe, Stephen M. Coutts, Lloyd J. Dolby