Benzo Is The Other Cyclo Patents (Class 544/62)
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Patent number: 5684002Abstract: A compound having the structure: ##STR1## wherein (a) W is --C(X')--NRR' or --NR--C(X')R';(b) X and X' are independently O or S;(c) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 3 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms;(d) Z is unsubstituted branched or cyclic alkyl, or unsubstituted or alkanyl-substituted phenyl or benzyl, Z having from 3 to about 10 atoms other than hydrogen;(e) R and R' are each independently selected from hydrogen, hydroxy straight, branched or substituted alkyl having from 1 to about 6 carbon atoms, and cyclic alkyl having from 3 to about 7 carbon atoms; unsubstituted or substituted aryl, heteroaryl or heterocyclic groups; or R and R' are bonded together to form a ring having from from 3 to about 8 atoms wherein about 1 to about 4 atoms may be heteroatoms;pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: June 7, 1995Date of Patent: November 4, 1997Assignee: The Procter & Gamble CompanyInventors: Michael Wiard Scherz, John Michael Janusz
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Patent number: 5668279Abstract: Novel substituted phthalazinones of the formula (I) ##STR1## are useful as neurotensin antagonists.Type: GrantFiled: April 6, 1995Date of Patent: September 16, 1997Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, Anna Chen
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Patent number: 5658902Abstract: Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.Type: GrantFiled: December 22, 1994Date of Patent: August 19, 1997Assignee: Warner-Lambert CompanyInventors: Kyunghye Ahn, Xue-Min Cheng, Annette Marian Doherty, Edward Faith Elslager, Brian Kornberg, Chitase Lee, Daniele Leonard, Sham Nikam, Leslie Morton Werbel
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Patent number: 5654316Abstract: The invention relates to compounds of the formula ##STR1## wherein X, i, j, n, n', A, A', R.sub.2, R.sub.3, and U are as described herein. The compounds of the invention are NK.sub.1 or NK.sub.2 or NK.sub.3 receptor antagonists and as such are useful in the treatment of diseases such as asthma.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Schering CorporationInventors: Nicholas I. Carruthers, Cheryl A. Alaimo
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Patent number: 5652247Abstract: 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: December 14, 1994Date of Patent: July 29, 1997Assignee: Otsuka Pharmaceutical Co., LtdInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5643922Abstract: The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, rhinitis, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.Type: GrantFiled: July 2, 1996Date of Patent: July 1, 1997Assignee: Abbott LaboratoriesInventors: George S. Sheppard, Steven K. Davidsen, James B. Summers
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Patent number: 5637586Abstract: A benzimidazolesulfonamide derivative of the formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 6 carbon atoms or a haloalkyl group of 1 to 6 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group of 1 to 6 carbon atoms, a haloalkyl group of 1 to 6 carbon atoms, --OR.sup.4, --O(CH.sub.2).sub.m C.sub.6 H.sub.5, --(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.5, --NHC (.dbd.O)R.sup.6, --N(R.sup.7).sub.2, --NHC(.dbd.O) (CH.sub.2).sub.p C.sub.6 H.sub.5, or --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2 ; R.sup.3 is an azole group, --COOH, --COOR.sup.8, or --SO.sub.3 H; A is --O--, --NH--, or --S(O).sub.q --; R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently an alkyl group of to 6 carbon atoms; m, n, and p are independently 0 or an integer of 1 to 6; and q is 0, 1, or 2, or a salt thereof; and a pharmaceutical composition comprising the above compound are disclosed. The compound exhibits a stable and strong antagonism to angiotensin II.Type: GrantFiled: August 4, 1995Date of Patent: June 10, 1997Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Hiroyuki Enari, Toshikazu Dewa, Toru Yamazaki
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Patent number: 5627136Abstract: Pyridine-N-oxide-substituted salicylaldehyde and salicylic acid derivatives of the general formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;R.sup.14 -R.sup.Type: GrantFiled: November 1, 1994Date of Patent: May 6, 1997Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe J. Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5602074Abstract: Substituted isoindolones I ##STR1## where R.sup.1 and R.sup.2 =H, unsubstituted or substituted alkyl, alkenyl, alkynyl, cyano, C.sub.1 -C.sub.6 -alkoxycarbonyl, formyl, C.sub.1 -C.sub.6 -alkylcarbonyl, unsubstituted or substituted phenylcarbonyl, C.sub.3 -C.sub.8 -cycloalkyl, or, if R.sup.1 =H, R.sup.2 additionally=unsubstituted or substituted phenyl, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, are an unsubstituted or substituted 3- to 8-membered carbo- or heterocycle;where R.sup.3 to R.sup.6 have the meanings given in the specification. The compounds are useful as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: November 22, 1994Date of Patent: February 11, 1997Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5589489Abstract: 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 of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: December 12, 1994Date of Patent: December 31, 1996Assignee: Zeneca LimitedInventors: Ashokkumar B. Shenvi, Robert T. Jacobs, Scott C. Miller, Cyrus J. Ohnmacht, Jr., Chris A. Veale
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Patent number: 5585394Abstract: The present invention relates to 1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives of the formula: ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.Type: GrantFiled: July 29, 1994Date of Patent: December 17, 1996Assignee: SanofiInventors: Alain Di Malta, Georges Garcia, Daniel Mettefeu, Dino Nisato, Richard Roux, Claudine Serradeil-Legal
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Patent number: 5563162Abstract: This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof. More particularly, this invention relates to new heterocyclic compounds and salts thereof which display bradykinin antagonist activity, to processes for preparing these compounds, to a pharmaceutical composition comprising these compounds, and to methods of using same in the prevention and/or the treatment of bradykinin- or bradykinin analogue-mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human beings or in animals.Type: GrantFiled: April 26, 1994Date of Patent: October 8, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 5552402Abstract: A class of substituted five-membered heteroaromatic compounds are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: May 18, 1995Date of Patent: September 3, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: V. G. Matassa, L. J. Street, G. A. Showell
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Patent number: 5538950Abstract: A compound of the formula: ##STR1## in which R.sup.3 is hydrogen or lower alkyl, R.sup.4 is pyridyl (lower) alkyl; andR.sup.1, R.sup.2, R.sup.5 and A are defined in the description;or a pharmaceutically acceptable salt thereof, which have endothelin antagonistic activity.Type: GrantFiled: May 12, 1994Date of Patent: July 23, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, Masahiro Neya, Naoki Fukami, Masashi Hashimoto, Hirokazu Tanaka, Natsuko Kayakiri
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Patent number: 5536833Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.Type: GrantFiled: May 26, 1995Date of Patent: July 16, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas C. Sedergran, Nachimuthu Soundararajan
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Patent number: 5519023Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.Type: GrantFiled: July 2, 1993Date of Patent: May 21, 1996Assignee: Adir et CompagnieInventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5504082Abstract: A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobater pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.Type: GrantFiled: December 1, 1994Date of Patent: April 2, 1996Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takeshi Kawakita, Mitsuharu Sano, Yuko Yutoku, Yoshifumi Ikeda, Keiichiro Haga
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Patent number: 5502187Abstract: The pharmaceutically active bicyclic heterocyclic amines (XXX) ##STR1## where W.sub.1 is --N.dbd. or --CH.dbd.; W.sub.3 is --N.dbd. or --CH.dbd.; W.sub.5 is --N.dbd. or --CR.sub.5 -- with the proviso that W.sub.5 is --CR.sub.5 -- when both W.sub.1 and W.sub.3 are --N.dbd. which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.Type: GrantFiled: October 3, 1994Date of Patent: March 26, 1996Assignee: The Upjohn CompanyInventors: Donald E. Ayer, Gordon L. Bundy, Eric J. Jacobsen
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Patent number: 5494908Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.Type: GrantFiled: November 12, 1993Date of Patent: February 27, 1996Assignee: Hoechst-Roussel Pharmaceutical IncorporatedInventors: Gerard J. O'Malley, Mark G. Palermo
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Patent number: 5428033Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. 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: October 10, 1991Date of Patent: June 27, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Michel L. Belley, Serge Leger, Patrick Roy, Yi B. Xiang, Marc Labelle
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Patent number: 5420132Abstract: A compound of formula (I): ##STR1## wherein: X represents O, S or H.sub.2,R and R' each represents hydrogen or together form a bond,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.useful in the treatment or prevention of disorders involving oxidative processes.Type: GrantFiled: May 6, 1994Date of Patent: May 30, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Valerie Thiery, Gerard Adam, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5397801Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: May 10, 1994Date of Patent: March 14, 1995Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5385930Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: January 14, 1994Date of Patent: January 31, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
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Patent number: 5373008Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.Type: GrantFiled: January 27, 1993Date of Patent: December 13, 1994Assignee: The Boots Compant plc.Inventor: Balasubramanian Gopalan
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Patent number: 5358945Abstract: The present invention relates to pyrimidine compounds represented by the formula ##STR1## (wherein X is a substituted or a cyclic amino group and Y is a substituted amino group or a substituted carbonyl group) or their pharmaceutically acceptable salts, and a therapeutic agent for neurological diseases comprising the compounds.These compounds are useful for treatment of various disorders in nervous systems since they are effective on growth of neurons and promotion of the formation and elongation of neutrites.Type: GrantFiled: March 30, 1992Date of Patent: October 25, 1994Assignees: Mitsui Petrochemical Industries, Ltd., Mitsui Pharmaceuticals, Inc.Inventors: Akira Mizuchi, Ken Ikeda, Yuichiro Kokubun, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Noriaki Kihara
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Patent number: 5356891Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.Type: GrantFiled: November 16, 1992Date of Patent: October 18, 1994Inventors: Donald T. Witiak, Ineke van Wijngaarden, Raghunathan V. Nair, Josephus H. M. Lange, Jacobus A. J. den Hartog
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Patent number: 5332741Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, andmedicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: May 17, 1993Date of Patent: July 26, 1994Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5304554Abstract: Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.Type: GrantFiled: March 11, 1992Date of Patent: April 19, 1994Assignees: Emory University, Georgia State University Research FoundationInventors: Lucjan Strekowski, Roman L. Wydra, Steven E. Patterson, Raymond F. Schinazi
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Patent number: 5300522Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen. acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.5 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: August 18, 1992Date of Patent: April 5, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5296499Abstract: An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl group or an acyl group, and A is a hydroxymethyl group or an esterified or amidated carboxyl group; or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, diluent or excipient.Type: GrantFiled: October 19, 1992Date of Patent: March 22, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Iwao Yamazaki, Noriaki Kawamura
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Patent number: 5280032Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: September 8, 1992Date of Patent: January 18, 1994Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5278174Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.Type: GrantFiled: May 17, 1991Date of Patent: January 11, 1994Assignee: Scios Nova, Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
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Patent number: 5270466Abstract: There are provided substituted quinazoline compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by phytopathogenic fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestations and diseases.Type: GrantFiled: June 11, 1992Date of Patent: December 14, 1993Assignee: American Cyanamid CompanyInventor: Gregory J. Haley
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Patent number: 5270331Abstract: Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.Type: GrantFiled: January 26, 1993Date of Patent: December 14, 1993Assignee: Pfizer, Inc.Inventors: Wayne E. Barth, Kelvin Cooper, Edward F. Kleinman, Lawrence A. Reiter, Ralph P. Robinson
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Patent number: 5266568Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. 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: October 10, 1991Date of Patent: November 30, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Michel L. Belley, Yves LeBlanc, Marc Labelle
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Patent number: 5256657Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.Type: GrantFiled: August 19, 1991Date of Patent: October 26, 1993Assignee: Sterling Winthrop, Inc.Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
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Patent number: 5229522Abstract: Novel bis-(indolyl)ethylenes, process for their production and record systems utilizing such bis-(indolyl)ethylene chromogens are described.Bis-(indolyl)ethylenes of the following general formula are prepared: ##STR1## wherein each L.sup.1 and L.sup.2 is the same or different and is each independently selected from indole moieties (J1) through (J4) (L.sup.1 need not be the same as L.sup.2), ##STR2## wherein Z is hydrogen, alkyl (C.sub.1 -C.sub.8), substituted or unsubstituted aryl, aralkyl, aroxyalkyl, alkoxyalkyl or halogen.Type: GrantFiled: September 4, 1990Date of Patent: July 20, 1993Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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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: 5208232Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meanings as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: March 22, 1991Date of Patent: May 4, 1993Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Dreger
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Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
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Patent number: 5192799Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.Type: GrantFiled: June 5, 1992Date of Patent: March 9, 1993Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
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Patent number: 5164387Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R .sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11)=C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: May 28, 1991Date of Patent: November 17, 1992Assignee: Hoffmann-LaRoche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
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Patent number: 5157117Abstract: The invention relates to novel compounds of the formula: ##STR1## useful as an intermediate in the preparation of quinoline carboxylic acid medicaments.Type: GrantFiled: July 1, 1991Date of Patent: October 20, 1992Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Naomi Takagi, Hironobu Fubasami, Hiroshi Matsukubo
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Patent number: 5136034Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.Type: GrantFiled: October 5, 1990Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Michel Therien, Jacques-Yves Gauthier, Robert Zamboni, Michel L. Belley
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Patent number: 5130310Abstract: Benzo[b]pyran derivatives of the formula I ##STR1## with E--D equal to CH--CHOH or C.dbd.CH;X equal to oxygen or sulfur;Y equal to oxygen, sulfur, SO, SO.sub.2 or NR.sup.9 ;R.sup.1 equal to CN, NO.sub.2, Hal, alkoxycarbonyl, SO.sub.1-2 -alkyl or SO.sub.1-2 -aryl;R.sup.2 equal to H, OH, alkoxy, alkyl, Hal, NR.sup.10 R.sup.11 ;R.sup.3 /R.sup.4 equal to alkyl;R.sup.5 /R.sup.6 equal to alkyl, (CH.sub.2).sub.1-6 COO-alkyl, (CH.sub.2).sub.1-6 CONR.sup.10 R.sup.11, (CH.sub.2).sub.0-6 COOH, (CH.sub.2).sub.1-6 CO-alkyl, CO.sub.2 -alkyl, alkylmercaptoalkyl, alkylsulfi(i)(o)nyl, hydroxyalkyl, mercaptoalkyl, aminoalkyl, N-(di)-alkylaminoalkyl or (CH.sub.2).sub.f Ar with f equal to zero-3;R.sup.7 /R.sup.8 equal to hydrogen, alkyl or phenyl, and m equal to zero-2are outstanding antihypertensives and spasmolytics. Preparation processes and use are described.Type: GrantFiled: January 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidman, Heinrich C. Englert, Bernward Scholkens, Martin Bickel
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5116863Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.Type: GrantFiled: March 2, 1987Date of Patent: May 26, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Toshiaki Kumazawa, Shizuo Otaki, Hiroyuki Obase, Kenji Ohmori, Hidee Ishii, Haruhiko Manabe, Tadafumi Tamura, Katsuichi Shuto