Polycyclo Ring System Patents (Class 544/79)
  • Publication number: 20100210762
    Abstract: 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 e
    Type: Application
    Filed: August 15, 2008
    Publication date: August 19, 2010
    Applicant: FUJIFILM CORPORATION
    Inventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
  • Publication number: 20100155714
    Abstract: 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: Application
    Filed: March 1, 2010
    Publication date: June 24, 2010
    Applicant: LG DISPLAY CO., LTD.
    Inventors: Jeong Dae SEO, Kyung Hoon LEE, Hee Jung KIM, Chun Gun PARK, Hyoung Yun OH
  • Patent number: 7718653
    Abstract: 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: Grant
    Filed: July 16, 2008
    Date of Patent: May 18, 2010
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
  • Patent number: 7645878
    Abstract: 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: Grant
    Filed: September 24, 2002
    Date of Patent: January 12, 2010
    Assignee: Bayer Healthcare LLC
    Inventors: Donald Bankston, Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
  • Publication number: 20090221568
    Abstract: 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: Application
    Filed: November 3, 2006
    Publication date: September 3, 2009
    Inventors: Jared Shaw, Sameer Urgaonkar, Debabrata RayChaudhuri, Henry La Pierre
  • Publication number: 20090062533
    Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.
    Type: Application
    Filed: November 11, 2008
    Publication date: March 5, 2009
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
  • Publication number: 20080312223
    Abstract: 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 hydrocarby
    Type: Application
    Filed: December 30, 2005
    Publication date: December 18, 2008
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio Berdini, Michael Alistair O'Brien, Theresa Rachel Phillips, Paul Graham Wyatt
  • Patent number: 7041669
    Abstract: 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: Grant
    Filed: February 19, 2003
    Date of Patent: May 9, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
  • Patent number: 6319921
    Abstract: 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: Grant
    Filed: January 18, 2000
    Date of Patent: November 20, 2001
    Assignee: Boerhinger Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
  • Patent number: 6130101
    Abstract: 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: Grant
    Filed: September 23, 1997
    Date of Patent: October 10, 2000
    Assignee: Molecular Probes, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
  • Patent number: 5476934
    Abstract: 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: Grant
    Filed: August 23, 1994
    Date of Patent: December 19, 1995
    Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
  • Patent number: 5436243
    Abstract: 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: Grant
    Filed: November 17, 1993
    Date of Patent: July 25, 1995
    Assignees: Research Triangle Institute Duke University, Pharmaceuticals Corporation
    Inventors: Clifford W. Sachs, Robert L. Fine, Lawrence M Ballas, R. Ivy Carroll, Robert Bell
  • Patent number: 5399558
    Abstract: 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: Grant
    Filed: November 24, 1993
    Date of Patent: March 21, 1995
    Assignee: PathoGenesis Corporation
    Inventors: William R. Baker, Lester A. Mitscher
  • Patent number: 5304548
    Abstract: 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: Grant
    Filed: September 29, 1992
    Date of Patent: April 19, 1994
    Assignee: The Upjohn Company
    Inventors: Ronald B. Gammill, Frank P. Bell
  • Patent number: 5208339
    Abstract: 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: Grant
    Filed: September 8, 1992
    Date of Patent: May 4, 1993
    Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
  • Patent number: 5189188
    Abstract: 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: Grant
    Filed: October 31, 1990
    Date of Patent: February 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5093336
    Abstract: 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: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5004813
    Abstract: 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: Grant
    Filed: August 24, 1989
    Date of Patent: April 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Rox Phaff, Davor Bedekovic
  • Patent number: 5001137
    Abstract: 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: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4888433
    Abstract: 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: Grant
    Filed: August 5, 1987
    Date of Patent: December 19, 1989
    Assignee: Zambon, S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4876357
    Abstract: 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: Grant
    Filed: October 26, 1987
    Date of Patent: October 24, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Rox Phaff, Davor Bedekovic
  • Patent number: 4855464
    Abstract: 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: Grant
    Filed: December 17, 1987
    Date of Patent: August 8, 1989
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4833246
    Abstract: 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: Grant
    Filed: December 2, 1987
    Date of Patent: May 23, 1989
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keiichi Adachi, Shigeru Ohno, Yoshio Inagaki, Nobuo Seto, Yoshihiro Jinbo
  • Patent number: 4804394
    Abstract: 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: Grant
    Filed: August 24, 1987
    Date of Patent: February 14, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Naoko Yamaguchi, Akihiko Yanagi, Hidenori Hayakawa, Shigeki Yagi, Hiroshi Miyauchi
  • Patent number: 4797413
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Patent number: 4788187
    Abstract: 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: Grant
    Filed: February 26, 1988
    Date of Patent: November 29, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4766211
    Abstract: 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: Grant
    Filed: August 27, 1986
    Date of Patent: August 23, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Rudolf Zink, Ian J. Fletcher
  • Patent number: 4753934
    Abstract: 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: Grant
    Filed: September 29, 1986
    Date of Patent: June 28, 1988
    Assignee: Celamerck GmbH & Co. KG
    Inventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
  • Patent number: 4741765
    Abstract: 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: Grant
    Filed: April 3, 1987
    Date of Patent: May 3, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4737508
    Abstract: 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: Grant
    Filed: February 1, 1985
    Date of Patent: April 12, 1988
    Assignee: Schering Corporation
    Inventors: Raymond G. Lovey, Arthur J. Elliott
  • Patent number: 4734507
    Abstract: 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: Grant
    Filed: April 5, 1985
    Date of Patent: March 29, 1988
    Assignee: Zambon S.p.A.
    Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
  • Patent number: 4661483
    Abstract: 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: Grant
    Filed: May 5, 1986
    Date of Patent: April 28, 1987
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Clarence S. Rooney, Ta J. Lee
  • Patent number: 4639442
    Abstract: 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: Grant
    Filed: November 1, 1985
    Date of Patent: January 27, 1987
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4639443
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: January 27, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4638001
    Abstract: 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: Grant
    Filed: April 27, 1984
    Date of Patent: January 20, 1987
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4617314
    Abstract: 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: Grant
    Filed: March 20, 1984
    Date of Patent: October 14, 1986
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Tetsuya Tahara, Kiyoharu Hayano, Michihide Setoguchi, Takemi Fukuda
  • Patent number: 4602087
    Abstract: 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: Grant
    Filed: May 18, 1984
    Date of Patent: July 22, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Luthi, Hans R. Meyer, Kurt Weber
  • Patent number: 4540519
    Abstract: 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: Grant
    Filed: April 9, 1984
    Date of Patent: September 10, 1985
    Assignee: American Cyanamid Company
    Inventors: Keith C. Murdock, Frederick E. Durr
  • Patent number: 4419354
    Abstract: 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: Grant
    Filed: June 3, 1982
    Date of Patent: December 6, 1983
    Assignee: American Cyanamid Company
    Inventors: Ralph G. Child, Stanley A. Lang, Jr.
  • Patent number: 4385182
    Abstract: 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: Grant
    Filed: April 28, 1981
    Date of Patent: May 24, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Vratislav Kvita, Hans Zweifel, Louis Felder
  • Patent number: 4375469
    Abstract: 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: Grant
    Filed: February 4, 1982
    Date of Patent: March 1, 1983
    Assignee: American Cyanamid Company
    Inventor: Keith C. Murdock
  • Patent number: 4350812
    Abstract: 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: Grant
    Filed: August 6, 1981
    Date of Patent: September 21, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox
  • Patent number: 4342756
    Abstract: 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: Grant
    Filed: April 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
  • Patent number: 4329357
    Abstract: 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: Grant
    Filed: February 9, 1981
    Date of Patent: May 11, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Melvin H. Rosen
  • Patent number: 4323691
    Abstract: 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: Grant
    Filed: December 1, 1980
    Date of Patent: April 6, 1982
    Assignee: Abbott Laboratories
    Inventors: Carroll W. Ours, Cheuk M. Lee
  • Patent number: 4302453
    Abstract: 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: Grant
    Filed: October 9, 1980
    Date of Patent: November 24, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox
  • Patent number: 4269978
    Abstract: 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: Grant
    Filed: March 27, 1978
    Date of Patent: May 26, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean C. Petitpierre
  • Patent number: 4258181
    Abstract: 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: Grant
    Filed: May 7, 1979
    Date of Patent: March 24, 1981
    Assignee: American Cyanamid Company
    Inventors: Keith C. Murdock, Frederick E. Durr
  • Patent number: 4230850
    Abstract: 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: Grant
    Filed: March 9, 1979
    Date of Patent: October 28, 1980
    Assignee: LIPHA, Lyonnaise Industrielle Pharmaceutique
    Inventors: Philippe Briet, Jean-Jacques Berthelon, Jean-Claude Depin
  • Patent number: 4177270
    Abstract: 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: Grant
    Filed: December 14, 1977
    Date of Patent: December 4, 1979
    Assignee: The Ansul Company
    Inventors: Khalid Rasheed, James D. Warkentin