The Five-membered Hetero Ring Shares Ring Carbons With Two Benzene Rings (i.e., Carbazoles) Patents (Class 548/440)
  • Patent number: 6506763
    Abstract: 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: Grant
    Filed: July 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6503998
    Abstract: 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: Grant
    Filed: September 5, 2001
    Date of Patent: January 7, 2003
    Assignee: National Science Council
    Inventors: Ging-Ho Hsiue, Wen-Jang Kuo, Ru-Jong Jeng
  • Publication number: 20020183526
    Abstract: 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: Application
    Filed: July 22, 2002
    Publication date: December 5, 2002
    Inventors: Takashi Kamikawa, Osamu Maruyama
  • Patent number: 6489489
    Abstract: 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: Grant
    Filed: February 8, 2001
    Date of Patent: December 3, 2002
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshio Sakai, Hisahiro Higashi, Hiroaki Nakamura, Hisayuki Kawamura, Chishio Hosokawa
  • Publication number: 20020172885
    Abstract: A carbazole derivative of the following formula (1), 1
    Type: Application
    Filed: March 5, 2002
    Publication date: November 21, 2002
    Inventors: Tomoki Nagai, Jun Numata, Shirou Kusumoto, Eiichi Kobayashi
  • Patent number: 6455704
    Abstract: 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: Grant
    Filed: September 6, 2001
    Date of Patent: September 24, 2002
    Assignee: Equistar Chemicals L.P.
    Inventor: Gregory G. Hlatky
  • Patent number: 6451461
    Abstract: 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: Grant
    Filed: February 8, 2001
    Date of Patent: September 17, 2002
    Assignee: Samsung SDI Co., Ltd.
    Inventors: Ji-Hoon Lee, In-Seo Kee, Sung-Woo Cho, Byung-Hoon Chae
  • Publication number: 20020115707
    Abstract: 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: Application
    Filed: January 11, 2002
    Publication date: August 22, 2002
    Inventors: Rami Lidor-Hadas, Eliezer Bachar
  • Publication number: 20020099223
    Abstract: 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: Application
    Filed: January 22, 2002
    Publication date: July 25, 2002
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6407261
    Abstract: A process for preparing 4-hydroxy carbazoles useful as intermediates for preparing compounds that are useful for inhibiting sPLA2 and novel intermediates.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: June 18, 2002
    Assignee: Eli Lilly and Company
    Inventors: Benjamin Alan Anderson, Nancy Kay Harn
  • Publication number: 20020057050
    Abstract: 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: Application
    Filed: June 28, 2001
    Publication date: May 16, 2002
    Inventor: Xiaobo Shi
  • Publication number: 20020055635
    Abstract: 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: Application
    Filed: March 21, 2001
    Publication date: May 9, 2002
    Inventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Rudi Grutzmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
  • Patent number: 6353102
    Abstract: 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: Grant
    Filed: December 17, 1999
    Date of Patent: March 5, 2002
    Assignee: PPG Industries Ohio, Inc.
    Inventor: Anil Kumar
  • Publication number: 20020026053
    Abstract: 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: Application
    Filed: July 30, 2001
    Publication date: February 28, 2002
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6340548
    Abstract: 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: Grant
    Filed: March 16, 2000
    Date of Patent: January 22, 2002
    Assignee: Imation Corp.
    Inventors: Nusrallah Jubran, Zbigniew Tokarski, Terrance P. Smith
  • Patent number: 6337404
    Abstract: 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: Grant
    Filed: December 16, 1999
    Date of Patent: January 8, 2002
    Assignee: Nessdisplay Co., Ltd.
    Inventors: Ki-jong Han, Youngkyoo Kim, Jae-Gyoung Lee, Dong-Kwon Choi
  • Publication number: 20010049448
    Abstract: 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: Application
    Filed: December 6, 1999
    Publication date: December 6, 2001
    Inventors: TAKASHI KAMIKAWA, OSAMU MARUYAMA
  • Publication number: 20010041731
    Abstract: 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: Application
    Filed: February 23, 2001
    Publication date: November 15, 2001
    Inventors: Robert S. Jacobs, Lisa A. Marshall, William H. Gerwick, Christopher Stevenson
  • Patent number: 6294112
    Abstract: 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: Grant
    Filed: December 16, 1999
    Date of Patent: September 25, 2001
    Assignee: James Robinson Limited
    Inventors: David A. Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
  • Publication number: 20010011134
    Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids
    Type: Application
    Filed: February 12, 2001
    Publication date: August 2, 2001
    Applicant: Hoechst Aktiengesellschaft
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
  • Patent number: 6194439
    Abstract: 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: Grant
    Filed: November 23, 1993
    Date of Patent: February 27, 2001
    Assignee: Pfizer Inc.
    Inventor: Robert L. Dow
  • Patent number: 6177440
    Abstract: 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: Grant
    Filed: April 21, 1998
    Date of Patent: January 23, 2001
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Patent number: 6150532
    Abstract: 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: Grant
    Filed: December 11, 1998
    Date of Patent: November 21, 2000
    Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
  • Patent number: 6100398
    Abstract: 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: Grant
    Filed: June 30, 1999
    Date of Patent: August 8, 2000
    Assignee: Yale University
    Inventors: John F. Hartwig, Motoi Kawatsura, Sheila I. Hauck, Kevin H. Shaughnessy, Luis M. Alcazar-Roman
  • Patent number: 6096246
    Abstract: 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: Grant
    Filed: October 23, 1998
    Date of Patent: August 1, 2000
    Assignee: Corning Incorporated
    Inventors: You-Ping Chan, Nathan Bryson
  • Patent number: 6063800
    Abstract: 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: Grant
    Filed: February 19, 1999
    Date of Patent: May 16, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
  • Patent number: 6037361
    Abstract: 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: Grant
    Filed: March 9, 1998
    Date of Patent: March 14, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
  • Patent number: 6037362
    Abstract: 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: Grant
    Filed: August 5, 1998
    Date of Patent: March 14, 2000
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Patent number: 5977361
    Abstract: 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: Grant
    Filed: October 14, 1998
    Date of Patent: November 2, 1999
    Assignee: Yale University
    Inventors: John F. Hartwig, Grace Mann
  • Patent number: 5955491
    Abstract: 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: Grant
    Filed: June 27, 1995
    Date of Patent: September 21, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
  • Patent number: 5942532
    Abstract: 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: Grant
    Filed: September 5, 1997
    Date of Patent: August 24, 1999
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
  • Patent number: 5902884
    Abstract: 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: Grant
    Filed: February 11, 1998
    Date of Patent: May 11, 1999
    Assignee: Clariant GmbH
    Inventors: Wolfgang Bauer, Klaus Delpy, Gert Nagl, Leonhard Unverdorben
  • Patent number: 5888432
    Abstract: 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: Grant
    Filed: December 3, 1997
    Date of Patent: March 30, 1999
    Assignee: Corning Incorporated
    Inventor: You-Ping Chan
  • Patent number: 5886191
    Abstract: 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: Grant
    Filed: August 18, 1997
    Date of Patent: March 23, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
  • Patent number: 5874588
    Abstract: 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: Grant
    Filed: September 19, 1997
    Date of Patent: February 23, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Bernd Lamatsch, Olof Wallquist
  • Patent number: 5854274
    Abstract: 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: Grant
    Filed: December 5, 1996
    Date of Patent: December 29, 1998
    Assignee: 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
  • Patent number: 5792786
    Abstract: 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: Grant
    Filed: April 12, 1996
    Date of Patent: August 11, 1998
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly
  • Patent number: 5760048
    Abstract: 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: Grant
    Filed: April 19, 1996
    Date of Patent: June 2, 1998
    Assignee: Warner-Lambert Company
    Inventors: Kevin Ka-Wang Wang, Po-Wai Yuen
  • Patent number: 5744070
    Abstract: 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: Grant
    Filed: December 20, 1995
    Date of Patent: April 28, 1998
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 5736284
    Abstract: 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: Grant
    Filed: April 15, 1997
    Date of Patent: April 7, 1998
    Assignee: Takasago International Corporation
    Inventors: Tohru Kobayashi, Yoshimasa Matsushima, Hiroshi Sugiyama, Toshimitsu Hagiwara
  • Patent number: 5714606
    Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: February 3, 1998
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5698740
    Abstract: 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: Grant
    Filed: February 12, 1997
    Date of Patent: December 16, 1997
    Assignee: Toyo Ink Manufacturing Co., Ltd.
    Inventors: Toshio Enokida, Tadashi Ogawa, Yasumasa Suda
  • Patent number: 5684152
    Abstract: 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: Grant
    Filed: September 19, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, William K. Hagmann
  • Patent number: 5658500
    Abstract: 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: Grant
    Filed: June 14, 1995
    Date of Patent: August 19, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5656206
    Abstract: 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: Grant
    Filed: June 14, 1995
    Date of Patent: August 12, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 5651923
    Abstract: 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: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5650098
    Abstract: 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: Grant
    Filed: October 13, 1995
    Date of Patent: July 22, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5648500
    Abstract: 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: Grant
    Filed: February 29, 1996
    Date of Patent: July 15, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Landscheidt, Alexander Klausener, Eberhard Zirngiebl, Jorg-Dietrich Jentsch
  • Patent number: 5574039
    Abstract: 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: Grant
    Filed: September 22, 1994
    Date of Patent: November 12, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
  • Patent number: 5552091
    Abstract: 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: Grant
    Filed: June 30, 1995
    Date of Patent: September 3, 1996
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar