Additional Hetero Ring Which Is Unsaturated Patents (Class 544/300)
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Patent number: 6498164Abstract: 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: GrantFiled: October 19, 2000Date of Patent: December 24, 2002Assignee: Aventis Pharma S.A.Inventors: Kunikazu Sakai, Yusuke Satoh
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Patent number: 6472396Abstract: 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: GrantFiled: June 16, 2000Date of Patent: October 29, 2002Assignee: Roche Diagnostics GmbHInventors: Elmar Bosies, Angelika Esswein, Frank Grams, Hans-Willi Krell, Ernesto Menta
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Publication number: 20020132822Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: October 25, 2001Publication date: September 19, 2002Inventors: Mark C. Noe, Lawrence A. Reiter, Martin J. Wythes
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Patent number: 6451738Abstract: 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: GrantFiled: August 9, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Johannes Rudolf Jansen, Klaus-Helmut Müller, Ulrich Philipp, Markus Dollinger
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Patent number: 6420130Abstract: 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: GrantFiled: April 28, 1999Date of Patent: July 16, 2002Assignee: Aurora Biosciences CorporationInventors: Lewis R. Makings, Gregor Zlokarnik
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Patent number: 6406533Abstract: 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: GrantFiled: March 7, 2001Date of Patent: June 18, 2002Assignee: Ciba Specialty Chemicals CorporationInventor: Fridolin Bäbler
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Patent number: 6369002Abstract: 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: GrantFiled: October 30, 2000Date of Patent: April 9, 2002Assignee: Syngenta Crop Properties, Inc.Inventors: Walter Kunz, Kurt Nebel
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Patent number: 6342604Abstract: 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: GrantFiled: January 14, 1997Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
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Publication number: 20020006575Abstract: 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) 1Type: ApplicationFiled: July 29, 1999Publication date: January 17, 2002Applicant: Otfried GaschlerInventors: OTFRIED GASCHLER, ANDREAS ELSAESSER, JOERG JUNG, HANS-JOACHIM SCHLOSSER
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Patent number: 6335332Abstract: 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: GrantFiled: April 3, 2000Date of Patent: January 1, 2002Assignee: Roche Diagnostics GmbHInventors: Ambrogio Oliva, Gianpiero De Cillis, Frank Grams, Valeria Livi, Gerd Zimmermann, Ernesto Menta, Hans-Willi Krell
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Patent number: 6303543Abstract: 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; andType: GrantFiled: May 15, 2000Date of Patent: October 16, 2001Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
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Patent number: 6300337Abstract: 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: GrantFiled: August 8, 2000Date of Patent: October 9, 2001Assignee: Nippon Kayaku Kabushiki KaishaInventors: Koichi Ishida, Yoshikazu Suzuki
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Patent number: 6288082Abstract: 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: GrantFiled: September 24, 1999Date of Patent: September 11, 2001Assignee: American Cyanamid CompanyInventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
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Patent number: 6274728Abstract: 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: GrantFiled: December 16, 1999Date of Patent: August 14, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Véronique Hall-Goulle, Aline Bize
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Patent number: 6268310Abstract: 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: GrantFiled: February 10, 1999Date of Patent: July 31, 2001Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
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Patent number: 6264733Abstract: 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: GrantFiled: February 2, 2000Date of Patent: July 24, 2001Assignee: Ciba Specialty Chemicals CorporationInventor: Fridolin Bäbler
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Patent number: 6254669Abstract: 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: GrantFiled: August 5, 1999Date of Patent: July 3, 2001Assignee: Zeneca LimitedInventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
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Patent number: 6187929Abstract: 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: GrantFiled: June 14, 1999Date of Patent: February 13, 2001Assignee: Konica CorporationInventors: Mitsuhiro Fukuda, Motoaki Sugino, Akira Onishi
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Patent number: 6177437Abstract: 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: GrantFiled: September 1, 1999Date of Patent: January 23, 2001Assignee: University of Massachusetts Medical CenterInventor: George E. Wright
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Patent number: 6174901Abstract: 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: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6100252Type: GrantFiled: December 8, 1998Date of Patent: August 8, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Yoshiyuki Inada
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Patent number: 6063924Abstract: 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: GrantFiled: July 22, 1996Date of Patent: May 16, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Veronique Hall-Goulle
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Patent number: 6057269Abstract: 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: GrantFiled: January 5, 1998Date of Patent: May 2, 2000Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
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Patent number: 6051722Abstract: 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: GrantFiled: July 6, 1998Date of Patent: April 18, 2000Assignee: Hitachi Chemical Company, Ltd.Inventors: Yutaka Honda, Iwao Fukuchi, Kwan-Yue Alex Jen
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Patent number: 6034089Abstract: 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: GrantFiled: September 28, 1998Date of Patent: March 7, 2000Assignee: Merck & Co., Inc.Inventors: Yongxin Han, Andre Giroux, Dwight MacDonald, Robert N. Young, Helene Perrier, Carole Lepine
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Patent number: 6013777Abstract: 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: GrantFiled: June 10, 1998Date of Patent: January 11, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6008350Abstract: 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: GrantFiled: March 13, 1996Date of Patent: December 28, 1999Assignee: Agfa-GevaertInventors: Peter Roschger, Stephan Michaelis, Karin Hassenruck, Horst Berneth, Paul Callant
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Patent number: 6005096Abstract: 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: GrantFiled: May 8, 1995Date of Patent: December 21, 1999Assignee: Gilead Sciences, Inc.Inventors: Mark Matteucci, Robert J. Jones, Kuei-Ying Lin
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Patent number: 5998087Abstract: 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: GrantFiled: January 22, 1999Date of Patent: December 7, 1999Assignee: Agfa-Gevaert, N.V.Inventors: Johan Loccufier, Stefaan Lingier, Sabine Emmers, Jean-Marie Dewanckele, Pierre De Clercq, Noel Hosten, Dirk Van Haver
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Patent number: 5977367Abstract: 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: GrantFiled: January 9, 1998Date of Patent: November 2, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5962685Abstract: 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: GrantFiled: January 28, 1997Date of Patent: October 5, 1999Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
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Patent number: 5962479Abstract: 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: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5952342Abstract: 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: GrantFiled: March 18, 1998Date of Patent: September 14, 1999Assignee: Warner-Lambert CompanyInventors: Clifton John Blankley, Annette Marian Doherty, James Marino Hamby, Robert Lee Panek, Mel Conrad Schroeder, Howard Daniel Hollis Showalter, Cleo Connolly
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Patent number: 5932730Abstract: 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: GrantFiled: March 27, 1997Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 5912261Abstract: 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: GrantFiled: December 19, 1995Date of Patent: June 15, 1999Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Takayuki Kotani, Kaoru Okamoto, Yasuhiro Nagaki
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Patent number: 5892033Abstract: 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: GrantFiled: September 4, 1996Date of Patent: April 6, 1999Assignee: Konica CorporationInventors: Tawara Komamura, Akira Onishi, Tatsuo Tanaka, Yoriko Nakayama, Mari Honda, Norio Miura
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Patent number: 5889013Abstract: 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: GrantFiled: January 4, 1996Date of Patent: March 30, 1999Assignee: 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
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Patent number: 5886160Abstract: 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: GrantFiled: June 12, 1998Date of Patent: March 23, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5885999Abstract: 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: GrantFiled: January 21, 1997Date of Patent: March 23, 1999Assignee: Merck Sharp & Dohme Ltd.Inventors: Jason Matthew Elliott, Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5866586Abstract: 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: GrantFiled: April 17, 1997Date of Patent: February 2, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Ian Thomson Forbes, Graham Elgin Jones
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Patent number: 5861380Abstract: 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: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5859041Abstract: 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: GrantFiled: June 9, 1997Date of Patent: January 12, 1999Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, David A. Claremon, John W. Butcher, Mark T. Bilodeau
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Patent number: 5849751Abstract: 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: GrantFiled: July 3, 1996Date of Patent: December 15, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Stefan Lohmer, Stefan Wohlfeil, Rudi Grutzmann
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Patent number: 5840732Abstract: 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: GrantFiled: December 6, 1996Date of Patent: November 24, 1998Assignee: Takeda Chemical Industries Ltd.Inventors: Muneo Takatani, Hitoshi Ikeda, Kyoko Iida, Hidenori Abe
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Patent number: 5840892Abstract: 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: GrantFiled: April 8, 1997Date of Patent: November 24, 1998Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky
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Patent number: 5807863Abstract: 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: GrantFiled: September 19, 1996Date of Patent: September 15, 1998Assignee: Novartis CorporationInventors: Martin Eberle, Clemens Lamberth, Fritz Schaub
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Patent number: 5783521Abstract: 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: GrantFiled: November 1, 1994Date of Patent: July 21, 1998Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5777118Abstract: 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: GrantFiled: July 12, 1996Date of Patent: July 7, 1998Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5756740Abstract: 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: GrantFiled: April 8, 1992Date of Patent: May 26, 1998Assignee: Eastman Kodak CompanyInventors: Lal Chand Vishwakarma, Chin Hsin Chen
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Patent number: 5750469Abstract: 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: GrantFiled: March 1, 1996Date of Patent: May 12, 1998Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen