The Five-membered Hetero Ring Shares Ring Carbons With Two Benzene Rings (i.e., Carbazoles) Patents (Class 548/440)
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Patent number: 6506763Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: July 30, 2001Date of Patent: January 14, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6503998Abstract: The present invention provides a lambda-shaped carbazole based chromophore, and a main-chain NLO polyurethane containing the same. The lambda-shaped structure reduces the plasticization to the main-chain polymers caused by the chromophore and increases temporal stability of the NLO coefficients of the main-chain NLO polyurethane. The NLO coefficients of the main-chain NLO polyurethane are stable because the efficiency of dipole alignment in electric field is increased due to the dipole thereof being perpendicular to the main chain of the polyurethane.Type: GrantFiled: September 5, 2001Date of Patent: January 7, 2003Assignee: National Science CouncilInventors: Ging-Ho Hsiue, Wen-Jang Kuo, Ru-Jong Jeng
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Publication number: 20020183526Abstract: Disclosed is a method for producing an aminocarbazole by catalytically reducing a nitrocarbazole, wherein as a catalyst is used an active nickel-based catalyst prepared by contacting a nickel-based catalyst with an alkali and an iron compound under a hydrogen gas or inert gas atmosphere in an inert solvent, and according to the method of the present invention, decrease in reaction speed, decrease in yield of a product or the like depending upon the lot of the starting nitrocarbazoles can be prevented, and aminocarbazoles can be produced in a good yield constantly.Type: ApplicationFiled: July 22, 2002Publication date: December 5, 2002Inventors: Takashi Kamikawa, Osamu Maruyama
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Patent number: 6489489Abstract: Disclosed is a practical, organic, blue-emitting EL device having a long life and having high luminous efficiency and good thermal stability. The device comprises organic compound layers, of which at least one is an organic blue-emitting layer, as sandwiched between a pair of electrodes, and is characterized in that the organic blue-emitting layer comprises an organic host compound having a fluorescence quantum efficiency of not smaller than 0.3 in a solid state and a fluorescent substance, and the organic host compound and the fluorescent substance are selected such that the device retains a monomeric blue-emitting ability, and that all the organic compound layers have a glass transition temperature of not lower than 75° C., while the organic compound layers adjacent to the organic blue-emitting layer have a glass transition temperature of not lower than 105° C.Type: GrantFiled: February 8, 2001Date of Patent: December 3, 2002Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshio Sakai, Hisahiro Higashi, Hiroaki Nakamura, Hisayuki Kawamura, Chishio Hosokawa
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Publication number: 20020172885Abstract: A carbazole derivative of the following formula (1), 1Type: ApplicationFiled: March 5, 2002Publication date: November 21, 2002Inventors: Tomoki Nagai, Jun Numata, Shirou Kusumoto, Eiichi Kobayashi
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Patent number: 6455704Abstract: Base-free carbazolides are prepared rapidly and in high yield and purity by reaction of a carbazole reactant with alkyl lithium in the presence of a dibasic ligand to form an intermediate complex, followed by reacting the intermediate complex with alkali metal alkoxide.Type: GrantFiled: September 6, 2001Date of Patent: September 24, 2002Assignee: Equistar Chemicals L.P.Inventor: Gregory G. Hlatky
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Patent number: 6451461Abstract: A hole transporting compound for organic electroluminescent devices with good thermal stability, which includes 6,6′-bis(9H,9-carbazolyl)-N,N′-disubstituted-3,3′-bicarbazyl as a basic molecular structure, is represented by the following formula I: wherein R is a hydrogen atom, a C1-12 aliphatic alkyl group, a C3-12 branched alkyl group, a C5-12 cyclic alkyl group, or a C4-14 aromatic group, wherein the aromatic group can have one or more alkoxy or amine substituents,Type: GrantFiled: February 8, 2001Date of Patent: September 17, 2002Assignee: Samsung SDI Co., Ltd.Inventors: Ji-Hoon Lee, In-Seo Kee, Sung-Woo Cho, Byung-Hoon Chae
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Publication number: 20020115707Abstract: An improved method for preparing dimethylamino-methyl-carbazolone and ondansetron base. A recrystallization process for preparing pure ondansetron hydrochloride dihydrate with a purity of at least 99.0% is also disclosed.Type: ApplicationFiled: January 11, 2002Publication date: August 22, 2002Inventors: Rami Lidor-Hadas, Eliezer Bachar
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Publication number: 20020099223Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.Type: ApplicationFiled: January 22, 2002Publication date: July 25, 2002Inventors: Michelangelo Scalone, Thomas Albert Zeibig
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Patent number: 6407261Abstract: A process for preparing 4-hydroxy carbazoles useful as intermediates for preparing compounds that are useful for inhibiting sPLA2 and novel intermediates.Type: GrantFiled: September 27, 2000Date of Patent: June 18, 2002Assignee: Eli Lilly and CompanyInventors: Benjamin Alan Anderson, Nancy Kay Harn
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Publication number: 20020057050Abstract: The present invention relates to a novel class of thermostable hole-injection and hole-transport compounds having tunable glass transition temperatures and ionization potentials for use in organic light emitting diode (“OLED”) devices. In particular, the compounds of the present invention comprise a trityl aniline core structure with various substituents attached to the nitrogen group, the structures of which allow for the adjustment of the glass transition temperatures and ionization potentials of the compounds. The present invention also relates to microdisplay devices comprising the compounds of the present invention in the hole-injection/hole-transport layers.Type: ApplicationFiled: June 28, 2001Publication date: May 16, 2002Inventor: Xiaobo Shi
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Publication number: 20020055635Abstract: Cycloalcanoindole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with anmines. The cycloahloanindole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.Type: ApplicationFiled: March 21, 2001Publication date: May 9, 2002Inventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Rudi Grutzmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
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Patent number: 6353102Abstract: Described are novel photochromic naphtho[1,2-b]pyran compounds having certain substituents at the 2 position of the pyran ring, certain substituents at the 5 and 6 positions and optionally at the 7, 8, 9 and 10-positions of the naphtho portion of the compound. These compounds may be represented by the following graphic formula: Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or contact lenses that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: December 17, 1999Date of Patent: March 5, 2002Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Publication number: 20020026053Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: ApplicationFiled: July 30, 2001Publication date: February 28, 2002Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6340548Abstract: Organic photoreceptors that include a charge transport compound, a charge generating compound, and an electroconductive support in which the charge transport compound is a novel aryl hydrazone-functional carbazole compound.Type: GrantFiled: March 16, 2000Date of Patent: January 22, 2002Assignee: Imation Corp.Inventors: Nusrallah Jubran, Zbigniew Tokarski, Terrance P. Smith
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Patent number: 6337404Abstract: A novel diamine compound of formula (I) of the present invention having a high glass transition temperature is useful as an improved hole transport agent, and an organic electroluminescent device containing the diamine compound of formula (I) has good thermal and mechanical stabilities, and prolonged lifetime.Type: GrantFiled: December 16, 1999Date of Patent: January 8, 2002Assignee: Nessdisplay Co., Ltd.Inventors: Ki-jong Han, Youngkyoo Kim, Jae-Gyoung Lee, Dong-Kwon Choi
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Publication number: 20010049448Abstract: Disclosed is a method for producing an aminocarbazole by catalytically reducing a nitrocarbazole, wherein as a catalyst is used an active nickel-based catalyst prepared by contacting a nickel-based catalyst with an alkali and an iron compound under a hydrogen gas or inert gas atmosphere in an inert solvent, and according to the method of the present inventions decrease in reaction speed, decrease in yield of a product or the like depending upon the lot of the starting nitrocarbazoles can be prevented, and aminocarbazoles can be produced in a good yield constantly.Type: ApplicationFiled: December 6, 1999Publication date: December 6, 2001Inventors: TAKASHI KAMIKAWA, OSAMU MARUYAMA
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Publication number: 20010041731Abstract: Disclosed are compounds having a scytoneman skeleton, such as scytonemin, and methods of using thereof. Methods of using a compound having a scytoneman skeleton to inhibit, modulate, attenuate, or prevent cell-cycle progression, cell proliferation, kinase activity, or induce apoptosis are disclosed. Also disclosed are methods of treating, preventing, or inhibiting diseases and disorders associated with cell cycle progression, cell proliferation, kinase activity, tissue hyperplasia or angiogenesis, such as cancer or an inflammatory disease.Type: ApplicationFiled: February 23, 2001Publication date: November 15, 2001Inventors: Robert S. Jacobs, Lisa A. Marshall, William H. Gerwick, Christopher Stevenson
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Patent number: 6294112Abstract: Red coloring hyperchromic compounds have the formula: where R1 is H, NR2R3, OR4, SR4 or R7 wherein R2 and R3 are alkyl or carbocyclic groups or together with the nitrogen to which they are attached form a heterocyclic ring; R4 is the same as R1 or is alkyl, perhaloallyl, aryl or heteroaryl; R7 is alkyl, haloalkyl, alkylthio, aryl, arylthio, heteroaryl, halogen, nitrile, carboxylate, ester, nitro, or a carbocyclic or heterocyclic ring fused to faces f, gh, i, j or k; and R5 is a cyclic aminoaryl group, an indolinoaryl group, a tricyclic nitrogen heterocycle, or an unsaturated cyclic aminoaryl group.Type: GrantFiled: December 16, 1999Date of Patent: September 25, 2001Assignee: James Robinson LimitedInventors: David A. Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Publication number: 20010011134Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acidsType: ApplicationFiled: February 12, 2001Publication date: August 2, 2001Applicant: Hoechst AktiengesellschaftInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Patent number: 6194439Abstract: Certain tricyclic polyhydroxylic compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).Type: GrantFiled: November 23, 1993Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 6177440Abstract: A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: April 21, 1998Date of Patent: January 23, 2001Assignee: Eli Lilly and CompanyInventors: Nicholas James Bach, Susan Elizabeth Draheim, Robert Delane Dillard, Edward David Mihelich, Jason Scott Sawyer, Douglas Wade Beight, Michael LeRoy Phillips, Tulio Suarez, Daniel Jon Sall, Jolie Anne Bastian, Michael Lyle Denney, Gary Alan Hite, Michael Dean Kinnick, Robert Theodore Vasileff, John Michael Morin, Jr., Ho-Shen Lin, Michael Enrico Richett, Richard Waltz Harper, John McNeill McGill, III, Benjamin Alan Anderson, Nancy Kay Harn, Richard James Loncharich, Richard Walter Schevitz
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Patent number: 6150532Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: December 11, 1998Date of Patent: November 21, 2000Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Patent number: 6100398Abstract: Disclosed is a process for the preparation of N-aryl amine compounds, comprising reacting an amine compound with an arylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-aryl amine compound, the transition metal catalyst comprising a Group 8 metal and P(t-Bu).sub.3 as a ligand, and wherein the ratio of the ligand to the Group 8 metal is in the range of about 3:1 to about 0.25:1, and wherein the reaction temperature is less than 100.degree. C. The process of the present invention provides a useful general method of N-arylation for the manufacture of pharmaceuticals, polymers, and the like.Type: GrantFiled: June 30, 1999Date of Patent: August 8, 2000Assignee: Yale UniversityInventors: John F. Hartwig, Motoi Kawatsura, Sheila I. Hauck, Kevin H. Shaughnessy, Luis M. Alcazar-Roman
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Patent number: 6096246Abstract: The invention relates to photochromic compounds of general formula (I), in which: R3 and R5 are C1-C6 alkoxy groups and the rest of the R groups represent various substituents.Type: GrantFiled: October 23, 1998Date of Patent: August 1, 2000Assignee: Corning IncorporatedInventors: You-Ping Chan, Nathan Bryson
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Patent number: 6063800Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: February 19, 1999Date of Patent: May 16, 2000Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 6037361Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 9, 1998Date of Patent: March 14, 2000Assignee: Warner-Lambert CompanyInventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 6037362Abstract: Compounds having a .beta.-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R.sup.1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R.sup.2 represents hydrogen, hydroxymethyl, NHR.sup.3, SO.sub.2 NR.sup.4 R.sup.4', or nitro; R.sup.6 represents hydrogen or lower alkyl; and X represents nitrogen, R.sup.9 represents hydrogen, one of R.sup.7 and R.sup.8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.Type: GrantFiled: August 5, 1998Date of Patent: March 14, 2000Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Shiro Miyoshi, Kohei Ogawa
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Patent number: 5977361Abstract: The present invention is directed to a process for the preparation of N-aryl compounds containing at least one unsaturated nitrogen atom, comprising reacting a compound having at least one unsaturated nitrogen atom with an arylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-aryl compound containing at least one unsaturated nitrogen atom, wherein the aryl moiety of the N-aryl compound is bonded to the at least one unsaturated nitrogen atom, the transition metal catalyst comprising a Group 8 metal and at least one chelating ligand selected from the group consisting of Group 15-substituted metallocenes, Group 15-substituted arylenes, unsaturated Group 15 heterocycles, Group 15-substituted alkanes, and combinations thereof. The process of the present invention a useful general method of N-arylation for the manufacture of pharmaceuticals, polymers, and the like.Type: GrantFiled: October 14, 1998Date of Patent: November 2, 1999Assignee: Yale UniversityInventors: John F. Hartwig, Grace Mann
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Patent number: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5942532Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5902884Abstract: Process for preparing N-alkylcarbazolesThe present invention relates to a process for preparing N-alkylcarbazoles of the formula I ##STR1## where R.sup.1 is (C.sub.1 -C.sub.6)-alkyl andY is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, nitro or halogen, by reacting a carbazole of the formula II ##STR2## with an alkyl halide of the formula IIIR.sup.1 -X IIIwhere X is a halogen atom,in an inert solvent in the presence of an inorganic base and a catalyst of the formula IVR.sup.2 R.sup.3 N-(CH.sub.2).sub.n -NR.sup.4 R.sup.5 IVwheren is an integer from 2 to 8,R.sup.2, R.sup.3 and R.sup.4 are, independently of one another, hydrogen or (C.sub.1 -C.sub.4)-alkyl andR.sup.5 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, amino-(C.sub.1 -C.sub.4)-alkyl or N,N-di(C.sub.1 -C.sub.4)-alkylamino-(C.sub.1 -C.sub.4)-alkyl.Type: GrantFiled: February 11, 1998Date of Patent: May 11, 1999Assignee: Clariant GmbHInventors: Wolfgang Bauer, Klaus Delpy, Gert Nagl, Leonhard Unverdorben
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Patent number: 5888432Abstract: The present invention has for subjects, novel benzopyran derivatives, substituted in position 2 with an adamantyl group as well as the compositions and (co)polymer matrices containing such derivatives. Said derivatives possess interesting photochromic properties.Type: GrantFiled: December 3, 1997Date of Patent: March 30, 1999Assignee: Corning IncorporatedInventor: You-Ping Chan
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Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5874588Abstract: Diketopyrrolopyrroles of formula I ##STR1## are prepared by reacting a diketopyrrolopyrrole of formula II ##STR2## with a) formic acid or b) a compound of formula IIIX'--H (III)or with an alkali metal formate or alkaline earth metal formate together with carbon monoxide in the presence of a catalyst, wherein, in formulae I, II and III, A is a direct bond or a group ##STR3## wherein phenylene is bound to the pyrrolopyrrole, R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 alkylmercapto, --CF.sub.3, --CN or --NO.sub.2, X is X' or OH, X' is --OR.sub.4 or --N(R.sub.5)(R.sub.6), wherein R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.6 cycloalkyl; phenyl or naphthyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, --CN or --NO.sub.2, R.sub.5 and R.sub.Type: GrantFiled: September 19, 1997Date of Patent: February 23, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Bernd Lamatsch, Olof Wallquist
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Patent number: 5854274Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.Type: GrantFiled: December 5, 1996Date of Patent: December 29, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
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Patent number: 5792786Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.Type: GrantFiled: April 12, 1996Date of Patent: August 11, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly
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Patent number: 5760048Abstract: The invention covers a novel series of .alpha.-mercaptoacrylic acid derivatives that inhibit both calpain I and calpain II with a high affinity and selectivity. The compounds are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders, brain injury, spinal cord, and peripheral nerve injury, cardiac infarction, cataracts, inflammation, restenosis, muscular dystrophy, and platelet aggregation. Pharmaceutical compositions, methods of using processes for preparing and novel intermediates useful in the processes are also disclosed.Type: GrantFiled: April 19, 1996Date of Patent: June 2, 1998Assignee: Warner-Lambert CompanyInventors: Kevin Ka-Wang Wang, Po-Wai Yuen
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Patent number: 5744070Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are 3H-naphtho?2,1-b!pyrans having an acyl or aroyl oxy-bearing substituent at the number 6 carbon atom and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 7, 8, 9 or 10 carbon atom of the naphthopyran. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: December 20, 1995Date of Patent: April 28, 1998Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 5736284Abstract: A charge transporting material high in solubility in a binder polymer and having high carrier mobility is disclosed, which contains a carbazole derivative represented by the following general formula (1): ##STR1## wherein Ar.sup.1 and Ar.sup.2, which may be the same or different, each represents an aryl group which may have a substituent group; R.sup.1 and R.sup.2, which may be the same or different, each represents a lower alkyl group or an aryl group which may have a substituent group; R.sup.3 represents a lower alkyl group, an alicyclic alkyl group having 5 to 7 carbon atoms, an aryl group which may have a substituent group, or an aralkyl group which may have a substituent group; and m and n each represents an integer of 0 or 1. An electrophotographic photoreceptor containing the charge transporting material is also disclosed.Type: GrantFiled: April 15, 1997Date of Patent: April 7, 1998Assignee: Takasago International CorporationInventors: Tohru Kobayashi, Yoshimasa Matsushima, Hiroshi Sugiyama, Toshimitsu Hagiwara
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Patent number: 5714606Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.Type: GrantFiled: August 15, 1996Date of Patent: February 3, 1998Assignee: ISIS Pharmaceuticals, Inc.Inventors: Oscar L. Acevedo, Normand Hebert
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Patent number: 5698740Abstract: A hole-transport material having excellent hole-transport capability and durability, suitable for use in an organic EL device and as an organic photoconductive material, has the formula (1).Type: GrantFiled: February 12, 1997Date of Patent: December 16, 1997Assignee: Toyo Ink Manufacturing Co., Ltd.Inventors: Toshio Enokida, Tadashi Ogawa, Yasumasa Suda
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Patent number: 5684152Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.Type: GrantFiled: September 19, 1996Date of Patent: November 4, 1997Assignee: Merck & Co., Inc.Inventors: Mitree M. Ponpipom, William K. Hagmann
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Patent number: 5658500Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 14, 1995Date of Patent: August 19, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5656206Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 14, 1995Date of Patent: August 12, 1997Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
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Patent number: 5651923Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 12, 1995Date of Patent: July 29, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5650098Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 22, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5648500Abstract: Substituted 1,2,3,4-tetrahydrocarbazoles of the formula ##STR1## having the meaning for R.sup.1 to R.sup.8 indicated in the description, can be prepared by catalytically hydrogenating a substituted phenol of the formula ##STR2## reacting the hydrogenation solution with a phenylhydrazine of the formula ##STR3## to give the hydrazone and cyclizing the hydrazone under acidic conditions.Type: GrantFiled: February 29, 1996Date of Patent: July 15, 1997Assignee: Bayer AktiengesellschaftInventors: Heinz Landscheidt, Alexander Klausener, Eberhard Zirngiebl, Jorg-Dietrich Jentsch
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Patent number: 5574039Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.Type: GrantFiled: September 22, 1994Date of Patent: November 12, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
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Patent number: 5552091Abstract: Described are novel reversible photochromic benzopyran compounds, examples of which are compounds substituted at the 2-position of the pyran ring with a dibenzo-fused 5 member heterocyclic compound; other enumerated substituents at the other 2-position of the pyran ring; and a substituted or unsubstituted benzo, benzothieno or benzofurano group fused to the benzo portion of the benzopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel benzopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 30, 1995Date of Patent: September 3, 1996Assignee: PPG Industries, Inc.Inventor: Anil Kumar