Additional Hetero Ring Which Is Unsaturated Patents (Class 544/300)
  • Patent number: 6498164
    Abstract: A compound of the formula wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases.
    Type: Grant
    Filed: October 19, 2000
    Date of Patent: December 24, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Kunikazu Sakai, Yusuke Satoh
  • Patent number: 6472396
    Abstract: Compounds of formula I, useful as matrix metalloprotease inhibitors, wherein X, Y and Z are each oxygen; R1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal monocycle for moieties (c)-(d) is unsubstituted or substituted by a substituent selected from the group consisting of —NH2, —NO2, —SO2NH2, —SO2CH3, acetyl, hydroxy, methoxy, ethoxy, cyano and halogen; R2 and R3 are each hydrogen; and R4 and R5, together with the nitrogen atom to which they are bound, form a piperazinyl or piperidyl ring, wherein the piperazinyl ring is substituted in the 4-position with a substituent selected from the group consisting of (a) a 6-membered aromatic monocycle having 0, 1 or 2 nitrogen atoms and the remainder of the atoms in the monocycle being carbon and (b) hydroxy-C1-C6 alkyl, wherein the monocycle is unsubstituted or substituted by a substituent selected from the group consisting of halogen, —
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: October 29, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Elmar Bosies, Angelika Esswein, Frank Grams, Hans-Willi Krell, Ernesto Menta
  • Publication number: 20020132822
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: October 25, 2001
    Publication date: September 19, 2002
    Inventors: Mark C. Noe, Lawrence A. Reiter, Martin J. Wythes
  • Patent number: 6451738
    Abstract: The invention relates to novel substituted thienyl(amino)sulphonyl(thio)ureas of the formula (I) in which A represents nitrogen or a CH grouping, E represents a single bond or an NH grouping, Q represents oxygen or sulphur, R1 and R2 independently of one another represent hydrogen, halogen or in each case optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy, aryloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 and R5 independently of one another each represent cyano, halogen or represent in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and R6 represents hydrogen, cyano, halogen or represents in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and to salts of compounds of the formula (I), to processes for preparing the novel compounds and to their use as herbicides.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: September 17, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ernst Rudolf F. Gesing, Johannes Rudolf Jansen, Klaus-Helmut Müller, Ulrich Philipp, Markus Dollinger
  • Patent number: 6420130
    Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: July 16, 2002
    Assignee: Aurora Biosciences Corporation
    Inventors: Lewis R. Makings, Gregor Zlokarnik
  • Patent number: 6406533
    Abstract: A 6,13-dihydroquinacridone derivative of formula I: (MO3S)m—Q—[CH2—(X)—(Y)n]o  (I) wherein: Q represents a 6,13-dihydroquinacridone moiety of formula II; A and B each independently represent a substituent selected from H, F, Cl, C1-C3alkyl and C1-C3alkoxy M represents a metal cation, quaternary N cation or H; X is an aromatic group, a cyclo-hetero aliphatic group with at least one 5 or 6 atom ring or a hetero aromatic group with at least one 5 or 6 atom ring and which is not a phthalimido group; Y is a sulfonic or carboxylic acid or salt thereof; m and n independently from each other are numbers from zero to 2.5; and o is a number from zero to 4, wherein m and o are not zero simultaneously.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: June 18, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Fridolin Bäbler
  • Patent number: 6369002
    Abstract: Compounds of formula 1 wherein R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1-C4alkyl, C1-C4halogenalkyl, halogen, hydroxy, C1-C4alkoxy, C1-C4halogenalkoxy, nitro, amino or cyano; R3, R15 to R39 and X6 to X19 are as defined in claim 1, and the agrochemically acceptable salts and stereoisomers of these compounds of formula I are suitable for use as herbicides.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: April 9, 2002
    Assignee: Syngenta Crop Properties, Inc.
    Inventors: Walter Kunz, Kurt Nebel
  • Patent number: 6342604
    Abstract: The present invention relates to the use of pyrimidine compounds of the following formula: wherein R1, R2, R3, A, B and Ar have the meanings indicated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
    Type: Grant
    Filed: January 14, 1997
    Date of Patent: January 29, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
  • Publication number: 20020006575
    Abstract: The invention relates to a positive-working, radiation-sensitive mixture which contains an organic polymeric binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solution and at least one IR-absorbing cyanine dye having a betaine structure or having a betaine structure and containing an anion and having the formula (I) 1
    Type: Application
    Filed: July 29, 1999
    Publication date: January 17, 2002
    Applicant: Otfried Gaschler
    Inventors: OTFRIED GASCHLER, ANDREAS ELSAESSER, JOERG JUNG, HANS-JOACHIM SCHLOSSER
  • Patent number: 6335332
    Abstract: The invention is directed to barbituric acid derivatives having inhibitory activity for matrix maetalloproteases comprised of formula (I): pharmaceutical compositions thereof, processes for preparing the derivatives, and methods for treating diseases associated with elevated or uncontrolled levels of matrix metalloprotease activity, e.g., cancer, specifically tumor progression and tumor metastasis, inflammation, or as a method of contraception.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: January 1, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Ambrogio Oliva, Gianpiero De Cillis, Frank Grams, Valeria Livi, Gerd Zimmermann, Ernesto Menta, Hans-Willi Krell
  • Patent number: 6303543
    Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; and
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: October 16, 2001
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
  • Patent number: 6300337
    Abstract: The present Invention relates to a novel acetamide derivative represented by the following Formula 1, which has an inhibition activity for chymotrypsin type proteases and is useful as an inhibitor for the above enzyme, especially as an inhibitor for chymase, and the use thereof as a medicine, for example, an antiasthma drug or a drug for curing vascular injuries complicated with angiogenesis and atheroma. wherein R0 represents a substituted or unsubstituted phenyl group, R1 represents an aryl group, a heteroaryl or an aliphatic lower alkyl group with or without substituents, R2 represents a substituted or unsubstituted alkyl, an aryl alkyl, a heteroaryl alkyl, and a heteroaryloxy alkyl or the like, J represents a carbonyl group, or a methylene group or the like, L represents a methoxy, hydroxyl or acetyloxy group or the like, X and Y independently represents a nitrogen atom or a carbon atom, Z represents a methylene group or a polyethylene group optionally having a substituent.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: October 9, 2001
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Koichi Ishida, Yoshikazu Suzuki
  • Patent number: 6288082
    Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: September 11, 2001
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
  • Patent number: 6274728
    Abstract: Compounds of formula A(B)x  (I), wherein x is an integer from 1 to 8, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, indanthrone, isoindolinone, isoindoline, dioxazine, azo, phthalocyanine or diketopyrrolopyrrole series that is bonded to x groups B via one or more hetero atoms, those hetero atoms being selected from the group consisting of N, O and S and forming part of the radical A, each group B independently of any other(s) is hydrogen or a group of the formula  at least one group B being a group of the formula The compounds according to the invention are used in high-molecular-weight organic materials, thermo-, photo- or chemo-sensitive recording materials, light-sensitive negative or positive resist compositions, ink compositions for ink-jet printing and color tapes for thermal transfer printing.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: August 14, 2001
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Véronique Hall-Goulle, Aline Bize
  • Patent number: 6268310
    Abstract: The present invention is directed to oxazole derivatives represented by the formula [I]; wherein A represents a nitrogen atom or a R3-substituted carbon atom; B represents a nitrogen atom, or an unsubstituted or X-substituted carbon atom; Z represents an oxygen atom, sulfinyl or sulfonyl; R1 and R2 represent each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 haloalkyl or the like; R3 represents hydrogen, C1-C6 alkyl, halogen, nitro, formyl or acyl; X represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C2-C6 alkenyl, C3-C6 alkynyl, C1-C6 haloalkyl or the like; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C2-C6 alkenyl, C3-C6 alkynyl, C1-C6 haloalkyl or the like; m represents an integar of 1 or 2, and n represents an integar of 1, 2, 3 or 4, and the salts thereof. The compounds specified in the present invention have an excellent herbicidal activity and are useful as an active ingredients for herbicides.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: July 31, 2001
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
  • Patent number: 6264733
    Abstract: Pigment particle growth and/or crystal phase directors of the following formula: (MO3S)m—Q—(CH2—(X)—(Y)n)o wherein: Q represents a pigment moiety; M represents a metal cation, quaternary N cation or H; X is an aromatic group, a cyclo-hetero aliphatic group with at least one 5 atom or 6 atom ring or a hetero aromatic group with at least one 6 atom ring and which is not a phthalimido group; Y is a sulfonic or carboxylic acid or salt thereof; m and n independently from each other represent an integer from 0 to 2.5; and o is an integer from 0.05 to 4.
    Type: Grant
    Filed: February 2, 2000
    Date of Patent: July 24, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Fridolin Bäbler
  • Patent number: 6254669
    Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: July 3, 2001
    Assignee: Zeneca Limited
    Inventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
  • Patent number: 6187929
    Abstract: A dye represented by the following formula (1); Formula (1)  wherein A represents an acidic nucleus, L1, L2 and L3 represent a methine group, n represents 0, 1 or 2, Z represents a nonmetalic atom group necessary to form a heterocyclic group by bonding with a nitrogen atom included in the above formula (1), Y represents a substituent represented by the following formula (2) or a heterocyclic group; Formula (2)  wherein R1 and R2 represent an alkyl group, and R1 and R2 may form a ring by bonding with each other, R3 represents a hydrogen atom or an electron withdrawing group: said dye represented by the above formula (1) has at least one carboxy group or one alkylsulfonamide group in an aromatic ring portion of its molecular structure.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: February 13, 2001
    Assignee: Konica Corporation
    Inventors: Mitsuhiro Fukuda, Motoaki Sugino, Akira Onishi
  • Patent number: 6177437
    Abstract: The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: January 23, 2001
    Assignee: University of Massachusetts Medical Center
    Inventor: George E. Wright
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6100252
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: August 8, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 6063924
    Abstract: Compounds of formulaA(B).sub.x (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine, diketopyrrolopyrrole or azo series, which radical A contains x N-atoms linked with B, preferably with at least one immediately adjacent or conjugated carbonyl group.B is a group of formula ##STR1## and, if x=2, 3 or 4, can also be one, two or three hydrogen atom(s), and wherein Q is a group of formula ##STR2## These soluble chromophores can be readily converted to the corresponding pigments by heating, even in the substrate into which they can be incorporated without any difficulty in dissolved form.R.sub.1 -R.sub.9 are as defined herein.
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: May 16, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Veronique Hall-Goulle
  • Patent number: 6057269
    Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: May 2, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
  • Patent number: 6051722
    Abstract: The present invention provides, as heteroaromatic compounds made functional so as to be used for nonlinear optical materials, compounds represented by the following general formula (1), and also provides polymers obtained from these and nonlinear optical parts comprising such polymers. In the formula, Ar.sup.1 and Ar.sup.2 each represents a divalent aromatic group; R.sup.1, R.sup.2 and R.sup.3 each represents an atom or a group independently selected from a hydrogen atom or an alkyl group and an aromatic group; X.sup.1 represents a monovalent organic group; n represents an integer of 2 to 12; and Z.sup.1 and Z.sup.2 each represents a group independently selected from electron attractive functional groups.
    Type: Grant
    Filed: July 6, 1998
    Date of Patent: April 18, 2000
    Assignee: Hitachi Chemical Company, Ltd.
    Inventors: Yutaka Honda, Iwao Fukuchi, Kwan-Yue Alex Jen
  • Patent number: 6034089
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: March 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Yongxin Han, Andre Giroux, Dwight MacDonald, Robert N. Young, Helene Perrier, Carole Lepine
  • Patent number: 6013777
    Abstract: Compounds of formulaA(B).sub.x, (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1.These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.
    Type: Grant
    Filed: June 10, 1998
    Date of Patent: January 11, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 6008350
    Abstract: The present invention relates to a process for the production of cyanine dyes with their methine chain showing group (M) and the charge compensation occuring by linked end groups through transformation of cationic cyanine dyes comprising group (D) with CH-acid compounds of the following formula (I) B.sub.1 --CH.sub.2 --B.sub.2 in an inert solvent, the substituents having the significance given in the description.
    Type: Grant
    Filed: March 13, 1996
    Date of Patent: December 28, 1999
    Assignee: Agfa-Gevaert
    Inventors: Peter Roschger, Stephan Michaelis, Karin Hassenruck, Horst Berneth, Paul Callant
  • Patent number: 6005096
    Abstract: A compound having the structure ##STR1## wherein R.sup.1 is H or a linker group; R.sup.24 is independently halo or C.sub.1 -C.sub.2 haloalkyl;R.sup.25 is independently --SH, --OH, .dbd.S or .dbd.O;A is independently N or C; andM, taken together with the radical --A--C(--R.sup.25), completes an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R.sup.6 ;R.sup.6 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, NO.sub.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: December 21, 1999
    Assignee: Gilead Sciences, Inc.
    Inventors: Mark Matteucci, Robert J. Jones, Kuei-Ying Lin
  • Patent number: 5998087
    Abstract: A silver halide photographic material is disclosed containing a new type of hydrazide compounds represented by following general formula I, the different symbols of which are defined in the description. ##STR1## In a preferred embodiment Q is chosen from pyridinium, quinolinium or isoquinolinium. In a most preferred embodiment Q is a pyridinium substituted on the N.sup.+ with a C.sub.5 to C.sub.8 alkyl group.The photographic material is preferably a graphic arts recording material. High gradation and excellent hard dot quality are obtained.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: December 7, 1999
    Assignee: Agfa-Gevaert, N.V.
    Inventors: Johan Loccufier, Stefaan Lingier, Sabine Emmers, Jean-Marie Dewanckele, Pierre De Clercq, Noel Hosten, Dirk Van Haver
  • Patent number: 5977367
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5962685
    Abstract: The present invention is directed to oxazole derivatives represented by the formula ?I!; ##STR1## wherein A represents a nitrogen atom or a R.sub.3 -substituted carbon atom; B represents a nitrogen atom, or an unsubstituted or X-substituted carbon atom; Z represents an oxygen atom, sulfinyl or sulfonyl; R.sub.1 and R.sub.2 represent each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, C.sub.1 -C.sub.6 haloalkyl or the like; R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, formyl or acyl; X represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like; Y represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like; m represents an integar of 1 or 2, and n represents an integar of 1, 2, 3 or 4, and the salts thereof.
    Type: Grant
    Filed: January 28, 1997
    Date of Patent: October 5, 1999
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5952342
    Abstract: 6-Aryl naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.
    Type: Grant
    Filed: March 18, 1998
    Date of Patent: September 14, 1999
    Assignee: Warner-Lambert Company
    Inventors: Clifton John Blankley, Annette Marian Doherty, James Marino Hamby, Robert Lee Panek, Mel Conrad Schroeder, Howard Daniel Hollis Showalter, Cleo Connolly
  • Patent number: 5932730
    Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: August 3, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
  • Patent number: 5912261
    Abstract: Carboxyalkyl heterocyclic derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (A): ##STR1## The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibiting aldehyde reductase.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: June 15, 1999
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Takayuki Kotani, Kaoru Okamoto, Yasuhiro Nagaki
  • Patent number: 5892033
    Abstract: Disclosed is a metal chelate dye which is composed of a metal ion and a ligand that is a methine dye having 2 or more bonding positions capable of coordinate bond to the metal ion at the bonding position. A thermal transfer recording material, an ink used for an ink jet image recording process and a color toner for electrostatic image recording process are also disclosed.
    Type: Grant
    Filed: September 4, 1996
    Date of Patent: April 6, 1999
    Assignee: Konica Corporation
    Inventors: Tawara Komamura, Akira Onishi, Tatsuo Tanaka, Yoriko Nakayama, Mari Honda, Norio Miura
  • Patent number: 5889013
    Abstract: The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active ingredients and processes of preparation thereof. ##STR1## wherein R.sup.1 is ethyl or isopropyl; R.sup.2 is (3,5 dimethylphenyl)selenenyl; R.sup.3 is phenyl or methyl; X is oxygen; and Y is oxygen.
    Type: Grant
    Filed: January 4, 1996
    Date of Patent: March 30, 1999
    Assignee: Sunkyong Industries Co., Inc.
    Inventors: Dae-Kee Kim, Jongsik Gam, Ganghyeok Kim, Young-Woo Kim, Namkyu Lee, Jinsoo Lim, Hun-Taek Kim, Key Hyup Kim
  • Patent number: 5886160
    Abstract: Compounds of formulaA(B).sub.x, (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1.These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.
    Type: Grant
    Filed: June 12, 1998
    Date of Patent: March 23, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 5885999
    Abstract: The present invention relates to compounds of formula (I): ##STR1## wherein m is zero, 1 or 2; and n is zero or 1, with the proviso that the sum total of m+n is 1 or 2;R.sup.1 represents phenyl; naphthyl; benzhydryl; or benzyl, where the naphthyl group or any phenyl moiety may be substituted;R.sup.2 represents hydrogen; phenyl; heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; naphthyl; benzhydryl; or benzyl; wherein each heteroaryl, the naphthyl group and any phenyl moiety may be substituted;R.sup.3 and R.sup.4 each independently represents hydrogen or C.sub.1-6 alkyl or R.sup.3 and R.sup.4 together are linked so as to form a C.sub.1-3 alkylene chain;Q represents CR.sup.5 R.sup.6 or NR.sup.5 ;X and Y each independently represents hydrogen, or together form a group .dbd.O; andZ represents a bond, O, S, SO, SO.sub.2, NR.sup.c or --(CR.sup.c R.sup.d)--, where R.sup.c and R.sup.d each independently represent hydrogen or C.sub.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: March 23, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jason Matthew Elliott, Angus Murray MacLeod, Graeme Irvine Stevenson
  • Patent number: 5866586
    Abstract: The invention relates to heterocyclic compounds of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein P represents phenyl, a quinoline or isoquinoline residue, or a 5 -membered or 6 -membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur; R.sup.3 is a group of formula (i) or (ii).
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: February 2, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Ian Thomson Forbes, Graham Elgin Jones
  • Patent number: 5861380
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 19, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5859041
    Abstract: Compounds represented by formula I: ##STR1## are disclosed. .sup.AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, David A. Claremon, John W. Butcher, Mark T. Bilodeau
  • Patent number: 5849751
    Abstract: Amides and sulphonamides of benzylamines having heterocyclic substituents are prepared by first converting the corresponding carboxylic acids into the corresponding amines and then substituting these on the amine nitrogen in a corresponding manner. The new amides and sulphonamides of benzylamines having heterocyclic substituents can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: December 15, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Stefan Lohmer, Stefan Wohlfeil, Rudi Grutzmann
  • Patent number: 5840732
    Abstract: This invention provides a new condensed imidazole compound possessing inhibitory activity of adhesion molecule expression.This invention also provides a therapeutic and prophylactic agent for diabetic nephritis and/or autoimmune disease and an immunosuppressor for organ transplantation.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: November 24, 1998
    Assignee: Takeda Chemical Industries Ltd.
    Inventors: Muneo Takatani, Hitoshi Ikeda, Kyoko Iida, Hidenori Abe
  • Patent number: 5840892
    Abstract: A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: November 24, 1998
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky
  • Patent number: 5807863
    Abstract: This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.3-6 cycloalkyl, or di-C.sub.1-4 alkylamino,R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, or di-C.sub.1-4 alkyl-amino,R.sub.3 is hydrogen or methyl,R.sub.4 is aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or heteroaryl-C.sub.1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; andX is CH or nitrogen;the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: September 15, 1998
    Assignee: Novartis Corporation
    Inventors: Martin Eberle, Clemens Lamberth, Fritz Schaub
  • Patent number: 5783521
    Abstract: Substituted pyridylsalicylaldehyde and --salicylic acid derivatives of the formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;Py is a substituted pyridine ring, are described.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: July 21, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5777118
    Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: July 7, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5756740
    Abstract: A process for the preparation of photographic binary sensitizing dyes, which comprise two separate, nonconjugated chromophores, one of which has the capability of adsorbing to a silver halide grain surface, the other of which is substantially non-adsorbing to silver halide. The process comprises reacting two dye compounds in a solvent in the presence of a 2-halo-1-alkylpyridinium salt and a 4-dialkylaminopyridine.
    Type: Grant
    Filed: April 8, 1992
    Date of Patent: May 26, 1998
    Assignee: Eastman Kodak Company
    Inventors: Lal Chand Vishwakarma, Chin Hsin Chen
  • Patent number: 5750469
    Abstract: Substituted lactic acid derivatives having an N-organic radical in the .beta.-position, of the formula I ##STR1## where substituents R to R.sup.5, X and Y have the meanings mentioned in the description and N is one of the radicals:a) --N.sub.3, --NC, --NCS or --NCOb) ##STR2## where R.sup.14 and R.sup.15 have the meanings described in the descriptionc) ##STR3## in which R.sup.16 is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl or unsubstituted or substituted phenyl; andB is a group ##STR4## OR.sup.19 or --NR.sup.14 R.sup.15, where R.sup.14, R.sup.15, R.sup.17 and R.sup.19 have the meanings described in the description, or ##STR5## where R.sup.14 and R.sup.15.sub.1, have the abovementioned meanings; or ##STR6## where R.sup.20 and R.sup.21, which can be identical or different, are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl, where the organic radicals can in each case be substituted;or R.sup.20 and R.sup.21 together form an unsubstituted or substituted C.sub.4 -C.sub.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: May 12, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen