Polycyclo Ring System Patents (Class 544/79)
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Publication number: 20100210762Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: ApplicationFiled: August 15, 2008Publication date: August 19, 2010Applicant: FUJIFILM CORPORATIONInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
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Publication number: 20100155714Abstract: Disclosed is an organic electroluminescent device including a substrate, a first and a second electrode, and an emitting layer formed between the first electrode and the second electrode. The emitting layer includes a plurality of materials which is a blue emitting material using a following chemical formula as dopant. In this case, at least one of A1 and A2 is selected from a substituted or non-substituted aromatic group, a heterocyclic group, an aliphatic group, and hydrogen.Type: ApplicationFiled: March 1, 2010Publication date: June 24, 2010Applicant: LG DISPLAY CO., LTD.Inventors: Jeong Dae SEO, Kyung Hoon LEE, Hee Jung KIM, Chun Gun PARK, Hyoung Yun OH
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Patent number: 7718653Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic ring which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: GrantFiled: July 16, 2008Date of Patent: May 18, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Patent number: 7645878Abstract: A process for the preparation of various quinazoline compounds which are useful as Rho-Kinase inhibitors, and thus having utility in the treatment of hypertension and other indications.Type: GrantFiled: September 24, 2002Date of Patent: January 12, 2010Assignee: Bayer Healthcare LLCInventors: Donald Bankston, Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
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Publication number: 20090221568Abstract: FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2??-hydroxy-5?-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.Type: ApplicationFiled: November 3, 2006Publication date: September 3, 2009Inventors: Jared Shaw, Sameer Urgaonkar, Debabrata RayChaudhuri, Henry La Pierre
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Publication number: 20090062533Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.Type: ApplicationFiled: November 11, 2008Publication date: March 5, 2009Applicant: TRANSITIONS OPTICAL, INC.Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
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Publication number: 20080312223Abstract: The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or —(CH2)m—(B)n—; B is C?O, NR8(C?O) or O(C?O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyType: ApplicationFiled: December 30, 2005Publication date: December 18, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Michael Alistair O'Brien, Theresa Rachel Phillips, Paul Graham Wyatt
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Patent number: 7041669Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: February 19, 2003Date of Patent: May 9, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
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Patent number: 6319921Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: January 18, 2000Date of Patent: November 20, 2001Assignee: Boerhinger Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
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Patent number: 6130101Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.Type: GrantFiled: September 23, 1997Date of Patent: October 10, 2000Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
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Patent number: 5476934Abstract: A nitrogen-containing perfluoroalkanoyl peroxide is provided which is represented by the formula: ##STR1## wherein Rf.sub.1 and Rf.sub.2 independently stand for an alkyl group of 1 to 5 carbon atoms, provided that Rf.sub.1 and Rf.sub.2 are joined to each other in one of the three patterns of union, 1) direct union, 2) union through the medium of an oxygen atom or 3) union through the medium of a nitrogen atom to form one of the three rings, i.e. five-membered ring, six-membered ring or seven-membered ring.Type: GrantFiled: August 23, 1994Date of Patent: December 19, 1995Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
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Patent number: 5436243Abstract: Potentiating agents inhibit the development of multidrug resistance, reduce drug-resistance in drug-resistant tumors, or sensitize tumors to antineoplastic drugs, thereby potentiating the effect of antineoplastic agents. The potentiating agents are aminoanthraquinones, preferably 1,4-bis(N-substituted) amino anthraquinones, and pharmaceutically acceptable salts thereof.Type: GrantFiled: November 17, 1993Date of Patent: July 25, 1995Assignees: Research Triangle Institute Duke University, Pharmaceuticals CorporationInventors: Clifford W. Sachs, Robert L. Fine, Lawrence M Ballas, R. Ivy Carroll, Robert Bell
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Patent number: 5399558Abstract: Methods, compounds and compositions are provided for inhibiting the growth of mycobacteria and gram-positive organisms in vitro and of treatment of mycobacterial and gram-positive infections in vivo using compounds of the formula (I) or (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, amino or loweralkyl; and R.sub.2 is selected from the group consisting of --CONR.sub.4 R.sub.5, --(CH.sub.2).sub.n- NR.sub.4 R.sub.5, --NHCO--NR.sub.4 R.sub.5 and --NHCO.sub.2 R.sub.4, wherein R.sub.4 and R.sub.5 are selected from hydrogen, loweralkyl, alkoxy, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, arylalkylaryl, arylaryl, aryoxy, aryloxyaryl, aryloxyarylalkyl, arylalkoxy, arylalkoxyaryl, arylalkoxyarylalkyl, arylalkoxyaryl, alkenyl, alkynyl and heterocycle, or R.sub.4 and R.sub.Type: GrantFiled: November 24, 1993Date of Patent: March 21, 1995Assignee: PathoGenesis CorporationInventors: William R. Baker, Lester A. Mitscher
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Patent number: 5304548Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.Type: GrantFiled: September 29, 1992Date of Patent: April 19, 1994Assignee: The Upjohn CompanyInventors: Ronald B. Gammill, Frank P. Bell
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Patent number: 5208339Abstract: A nitrogen-containing perfluoroalkanoyl peroxide is provided which is represented by the formula: ##STR1## wherein Rf.sub.1 and Rf.sub.2 independently stand for an alkyl group of 1 to 5 carbon atoms, provided that Rf.sub.1 and Rf.sub.2 are joined to each other in one of the three patterns of union, 1) direct union, 2) union through the medium of an oxygen atom or 3) union through the medium of a nitrogen atom to form one of the three rings, i.e. five-membered ring, six-membered ring or seven-membered ring.Type: GrantFiled: September 8, 1992Date of Patent: May 4, 1993Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
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Patent number: 5189188Abstract: Compounds of the general formula ##STR1## in which the symbols have the meaning given in the description, are highly suitable as color formers in recording materials based on acid developers. They give deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness.Type: GrantFiled: October 31, 1990Date of Patent: February 23, 1993Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5004813Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: August 24, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4888433Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.Type: GrantFiled: August 5, 1987Date of Patent: December 19, 1989Assignee: Zambon, S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4876357Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: October 26, 1987Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4855464Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.Type: GrantFiled: December 17, 1987Date of Patent: August 8, 1989Assignee: Zambon S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4833246Abstract: A novel pyrazolone dye represented by the following formula (I), which can be effectively used as a filter dye, an irradiation inhibiting dye, an antihalation dye or the like in a photographic light-sensitive material: ##STR1## wherein R.sub.1 and R.sub.2 each represents --COOR or ##STR2## R and R' each represents a hydrogen atom, an alkyl group, or an aryl group or may combine with each other to form a 5- or 6-membered ring; Q.sub.1 and Q.sub.2 each represents an aryl group; X.sub.1 and X.sub.2 each represents a linkage group; Y.sub.1 and Y.sub.2 each represents a sulfo group or a carboxyl group; L.sub.1, L.sub.2 and L.sub.3 each represents a methine group; L.sub.4 and L.sub.5 each represents an alkylene group; m.sub.1 and m.sub.2 each represents 1 or 2; n represents 0, 1 or 2; p.sub.1 and p.sub.2 each represents 0 or 1; q.sub.1 and q.sub.2 each represent 0, 1, 2, 3 or 4; and s.sub.1 and s.sub.2 each represents 1 or 2.Type: GrantFiled: December 2, 1987Date of Patent: May 23, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Keiichi Adachi, Shigeru Ohno, Yoshio Inagaki, Nobuo Seto, Yoshihiro Jinbo
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Patent number: 4804394Abstract: Novel benzoxazines of the formula (I) ##STR1## wherein X is hydrogen or halogen,R.sup.1 is hydrogen or C.sub.1 -C.sub.2 -alkyl,R.sup.2 is cyano, trimethylsilyl, trimethylsilylmethoxycarbonyl, C.sub.1 -C.sub.4 -alkylthio or cyclopropyl andQ is ##STR2## and the use of the novel compounds as herbicides, and intermediates for the preparation of the novel benzoxazines.Type: GrantFiled: August 24, 1987Date of Patent: February 14, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Naoko Yamaguchi, Akihiko Yanagi, Hidenori Hayakawa, Shigeki Yagi, Hiroshi Miyauchi
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Patent number: 4797413Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: June 26, 1987Date of Patent: January 10, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
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Patent number: 4788187Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: February 26, 1988Date of Patent: November 29, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4766211Abstract: Chromogenic quinazolines of formula ##STR1## wherein R is an aryl radical or a heterocyclic radical,Z.sub.1 is oxygen or sulfur,Z.sub.2 is oxygen, sulfur or ##STR2## R' is hydrogen, alkyl which is unsubstituted or substituted by halogen, cyano or lower alkoxy, or is cycloalkyl, phenyl, benzyl, phenethyl or acyl, or --NRR' is a 5- or 6-membered heterocyclic radical,Q is an aliphatic radical which may be interrupted by a further member Z.sub.2,Y is the radical of a couplable compound, and the ringA is unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy or lower alkoxycarbonyl.These quinazolines are exceedingly fast to sublimation and are particularly suitable color formers in pressure-sensitive or heat-sensitive recording materials and give strong and lightfast yellow and orange colorations.Type: GrantFiled: August 27, 1986Date of Patent: August 23, 1988Assignee: Ciba-Geigy CorporationInventors: Rudolf Zink, Ian J. Fletcher
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Patent number: 4753934Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.Type: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4741765Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: April 3, 1987Date of Patent: May 3, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4737508Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.Type: GrantFiled: February 1, 1985Date of Patent: April 12, 1988Assignee: Schering CorporationInventors: Raymond G. Lovey, Arthur J. Elliott
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Patent number: 4734507Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.Type: GrantFiled: April 5, 1985Date of Patent: March 29, 1988Assignee: Zambon S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4661483Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 5, 1986Date of Patent: April 28, 1987Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Clarence S. Rooney, Ta J. Lee
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Patent number: 4639442Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: November 1, 1985Date of Patent: January 27, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4639443Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 4, 1986Date of Patent: January 27, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4638001Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: April 27, 1984Date of Patent: January 20, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4617314Abstract: Benzofuran- and benzopyran-carboxamide derivatives of the formula: ##STR1## wherein l is 1 or 2; X is hydrogen atom, amino group or halogen atom; Y is --S(O).sub.m --R.sup.3 wherein R.sup.3 is lower alkyl group and m is 0, 1 or 2, or ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or lower alkyl group; R.sup.1 is hydrogen atom, lower alkyl group, arylthiomethyl group, halogenomethyl group or ##STR3## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen atom or lower alkyl group or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom form a hetrocycle; R.sup.2 is hydrogen atom or lower alkyl group; and Z is ##STR4## wherein p is 2 or 3, R.sup.8 and R.sup.9 are the same or different and are each lower alkyl group or R.sup.8 and R.sup.9 together with the adjacent nitrogen atom form a heterocycle, or ##STR5## wherein q is 0 or 1, n is 1 or 2, R.sup.Type: GrantFiled: March 20, 1984Date of Patent: October 14, 1986Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Tetsuya Tahara, Kiyoharu Hayano, Michihide Setoguchi, Takemi Fukuda
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Patent number: 4602087Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1-3 -alkylene-CON(R.sub.4)--CON(R.sub.4)--, --O--C.sub.1-3 alkylene-COO--, OCO or --COO--, with the proviso that if n+n'=O, X and X' may not be --CON(R.sub.4)-- or O--C.sub.1-3 -alkylene-CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)-- or --COO--, A.sup..crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1-20 -alkyene, R.sub.1 and R.sub.1 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, R.sub.1 together with R.sub.2, or R.sub.1 ' together with R.sub.2 ', is a heterocyclic ring, R.sub.2 and R.sub.2 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2 ' together with R.sub.1 ', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1 ' and R.sub.Type: GrantFiled: May 18, 1984Date of Patent: July 22, 1986Assignee: Ciba-Geigy CorporationInventors: Christian Luthi, Hans R. Meyer, Kurt Weber
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Patent number: 4540519Abstract: This disclosure describes symmetrical 1,4-bis-(substituted-amino)-5,8-hydroxyanthraquinones useful as chelating agents and for inducing regression and/or palliation of cancer diseases in mammals.Type: GrantFiled: April 9, 1984Date of Patent: September 10, 1985Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Frederick E. Durr
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Patent number: 4419354Abstract: This disclosure describes certain substituted 9,10-bis(2-aminoethoxy)anthracenes which are useful as modulators of the immune response system in warm-blooded animals and for inducing the regression of tumors in such animals.Type: GrantFiled: June 3, 1982Date of Patent: December 6, 1983Assignee: American Cyanamid CompanyInventors: Ralph G. Child, Stanley A. Lang, Jr.
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Patent number: 4385182Abstract: Novel thioxanthonecarboxylic acids and thioxanthonecarboxylic acid derivatives of the formula I ##STR1## in which Y is --COOH, --CO-halogen, --CN or a carboxylic acid ester, thioester or amide group and X, Z and W are as defined in the patent claim, are described. The compounds of the formula I in which Y is other than --CO--halogen are suitable as sensitizers for photo-crosslinkable polymers or as initiators for photo-polymerization of ethylenically unsaturated compounds or for photo-chemical crosslinking of polyolefins. The acid halides of the formula I are starting materials for the preparation of the corresponding nitriles and carboxylic acid esters, thioesters and amides.Type: GrantFiled: April 28, 1981Date of Patent: May 24, 1983Assignee: Ciba-Geigy CorporationInventors: Walter Fischer, Vratislav Kvita, Hans Zweifel, Louis Felder
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Patent number: 4375469Abstract: Novel 1,4-di(substituted amino)-5,8-dihydroxyanthraquinones wherein the substituents are alkylamino alcohol and/or alkyl cyclicamide and their pharmacologically acceptable acid-addition salts useful as antitumor and chelating agents are described.Type: GrantFiled: February 4, 1982Date of Patent: March 1, 1983Assignee: American Cyanamid CompanyInventor: Keith C. Murdock
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Patent number: 4350812Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, lower alkenyl, or hydroxylower alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached also form a heterocyclic radical which may contain another heteroatom, namely nitrogen, oxygen or sulfur; R.sup.3 and R.sup.4 may be the same or different and are hydrogen or lower alkyl. These compounds are useful in the treatment of arrhythmia.In addition, novel intermediates are provided having the structure ##STR2## wherein R is hydrogen, benzyl or ##STR3## These intermediates are also useful in treating acute myocardial infarction.Type: GrantFiled: August 6, 1981Date of Patent: September 21, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox
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Patent number: 4342756Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: April 29, 1981Date of Patent: August 3, 1982Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
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Patent number: 4329357Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g. those of the formula ##STR1## Am=arylamino or N-alkyl-N-arylamino substituted by R X=HO, alkoxy, alkanoyloxy or alkyleneiminoR=alkyl, alkoxy, alkylmercapto, halo, CF.sub.3, CN, or NO.sub.2n=0-2or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.Type: GrantFiled: February 9, 1981Date of Patent: May 11, 1982Assignee: Ciba-Geigy CorporationInventor: Melvin H. Rosen
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Patent number: 4323691Abstract: Described are compounds of the formula ##STR1## wherein ##STR2## wherein Z is hydrogen or loweralkyl, R.sub.5 and R.sub.6 may be the same or different and are hydrogen, loweralkyl or together are alkylene of 4 or 5 carbon atoms,R.sub.2 is hydrogen, halo, haloloweralkyl, loweralkyl, loweralkoxy, loweralkylthio or ##STR3## wherein R.sub.5 and R.sub.6 are previously defined, R.sub.3 is hydroxy, alkoxy, branched alkoxy, adamantyloxy, morpholino, amino or amino substituted by loweralkyl or alkylene of 4 or 5 carbon atoms,R.sub.4 is hydrogen or loweralkyl, andX.sub.1 and X.sub.2 are hydrogen, loweralkyl, halo or when substituted on adjacent carbon atoms of the benzene ring form a 1,3-butadienylene linkage, Y is oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds are effective as diuretic agents in increasing urinary excretion.Type: GrantFiled: December 1, 1980Date of Patent: April 6, 1982Assignee: Abbott LaboratoriesInventors: Carroll W. Ours, Cheuk M. Lee
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Patent number: 4302453Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, lower alkenyl, or hydroxy-lower alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached also form a heterocyclic radical which may contain another heteroatom, namely nitrogen, oxygen or sulfur; R.sup.3 and R.sup.4 may be the same or different and are hydrogen or lower alkyl. These compounds are useful in the treatment or arrhythmia.In addition, novel intermediates are provided having the structure ##STR2## wherein R is hydrogen, benzyl or ##STR3## These intermediates are also useful in treating acute myocardial infarction.Type: GrantFiled: October 9, 1980Date of Patent: November 24, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox
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Patent number: 4269978Abstract: Thiazolylphthalide compounds of the general formula ##STR1## wherein A represents a p-aminophenyl readical of formula ##STR2## or a 3-indolyl radical of formula ##STR3## or a 2-thiazolyl radical of formula ##STR4## each of R.sub.1, R.sub.2, X.sub.1, X.sub.2, R.sub.1 ' and R.sub.2 ' independently represents hydrogen, alkyl of 1 to 12 carbon atoms, alkoxyalkyl of 2 to 8 carbon atoms, cycloalkyl of 5 or 6 carbon atoms, or unsubstituted or substituted benzyl or phenyl, oreach pair of substituents R.sub.1 and R.sub.2, X.sub.1 and X.sub.2 or R.sub.1 ' and R.sub.2 ' together with the nitrogen atom to which they are attached, independently represents a heterocyclic ring,each of Y.sub.1 and Y.sub.1 ' represents hydrogen, alkyl of 1 to 12 carbon atoms, cycloalkyl or 5 or 6 carbon atoms or unsubstituted or substituted benzyl or phenyl,V.sub.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, alkoxy of 1 to 12 carbon atoms or acyloxy of 2 to 12 carbon atoms,Z.sub.Type: GrantFiled: March 27, 1978Date of Patent: May 26, 1981Assignee: Ciba-Geigy CorporationInventor: Jean C. Petitpierre
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Patent number: 4258181Abstract: This disclosure describes anthracene-9,10-bis-carbonyl-hydrazones and derivatives thereof useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the regression and/or palliation of leukemia and related cancers.Type: GrantFiled: May 7, 1979Date of Patent: March 24, 1981Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Frederick E. Durr
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Patent number: 4230850Abstract: Novel 3-substituted-4-aminoalkoxy-5,6-condensed ring-2-pyranones are disclosed as having utility as pharmacologically active compounds, in particular vasodilatory, hypotensive, anti-ischemic and anti-tussive activity. The compounds may be 3-phenyl-4-morpholinoalkoxy-coumarins. Administration may be by the oral or parenteral route. Intermediates useful in the production of these compounds are also disclosed.Type: GrantFiled: March 9, 1979Date of Patent: October 28, 1980Assignee: LIPHA, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Jean-Claude Depin
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Patent number: 4177270Abstract: 1,3-Benzodithiole-2-one and 1,3-benzodithiole-2-thione compounds are disclosed including the novel method of preparing said compounds and their biocidal activity.Type: GrantFiled: December 14, 1977Date of Patent: December 4, 1979Assignee: The Ansul CompanyInventors: Khalid Rasheed, James D. Warkentin