Plural 1,3-diazine Rings Patents (Class 544/296)
  • Patent number: 6211186
    Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications. In particular, the present invention relates to compounds having the structure: and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L1, L2, L3, L4, Z, X, B1, and B2 are defined herein.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: April 3, 2001
    Assignee: The Procter & Gamble Company
    Inventors: John McMillan McIver, Todd Laurence Underiner, Timothy Bates
  • Patent number: 6211191
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;&ngr;&bgr;3, &agr;&ngr;&bgr;5, and/or &agr;&ngr;&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: April 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, James J. Perkins, Robert S. Meissner
  • Patent number: 6204273
    Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: January 29, 1999
    Date of Patent: March 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
  • Patent number: 6200986
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: March 13, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • Patent number: 6194413
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: February 27, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • 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: 6172227
    Abstract: Novel 4,5-diamino pyrimidine derivatives are described by the following general formula I: in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a direct bond or C1-2 alkyl, R1 is (i) 5-15 membered cyclic or fused heterocompound which includes one or two atoms selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two substituents selected from a group consisting of hydrogen, halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, (ii) C4-10 carbocyclic compound or (iii) hydroxy C1-4 alkoxy, R2 is 5-15 membered cyclic or fused heterocompound which includes one or two nitrogen atoms and, optionally, one oxygen or sulfur atom, and which is substituted with one or two substituents selected from a group consisting of hydrogen, hydroxy, halogen, nitro, hydroxy C1-5 alkyl, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R3 is hydrogen, in which R4 and R5 are
    Type: Grant
    Filed: September 16, 1997
    Date of Patent: January 9, 2001
    Assignee: Cheil Jedang Corporation
    Inventors: Myung Xik Xiang, Byoung Chool Suh, Chung Keun Rhee, Kwang Hyuk Lee, Youn Ha Lee, Young Gi Kim
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6159673
    Abstract: An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W.sup.1 and W.sup.2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
    Type: Grant
    Filed: January 20, 1999
    Date of Patent: December 12, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Junji Nishigaki, Yasuaki Deguchi
  • Patent number: 6143750
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: November 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Patane, Mark G. Bock
  • Patent number: 6124306
    Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: September 26, 2000
    Assignee: Pharmacia & Upjohn Company
    Inventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
  • Patent number: 6114342
    Abstract: 2-(O-[pyrimidin-4-yl]methylenoxy)phenylacetic acid derivatives of the general formula I and the salts and N-oxides thereof where the radicals R.sup.1 to R.sup.4 and Q have the following meanings:R.sup.1 is hydrogen or alkyl;R.sup.2 is halogen, alkyl or haloalkyl;R.sup.3 is hydrogen; amino; hydroxyl; mercapto; halogen; unsubstituted or phenyl-substituted alkyl; haloalkyl; alkoxyalkyl; alkoxy; monoalkylamino; dialkylamino; alkylthio; alkylsulfoxyl; alkylsulfonyl; cycloalkyl; trialkylsilyloxy, or: phenyl, phenoxy, phenoxymethyl, benzyloxy or hetaryl, unsubstituted or substituted in the aromatic ring;R.sup.4 is hydrogen; cyano; halogen; alkyl; haloalkyl or alkoxy;Q is C(=NOCH.sub.3)--CONHCH.sub.3,C(=NOCH.sub.3)--COOCH.sub.3 orN(OCH.sub.3)--COOCH.sub.3,the salts and N-oxides thereof, and their use for controlling harmful fungi and animal pests.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: September 5, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Oberdorf, Wassilios Grammenos, Hubert Sauter, Thomas Grote, Reinhard Kirstgen, Ruth Muller, Bernd Muller, Franz Rohl, Michael Rack, Herbert Bayer, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Patent number: 6107297
    Abstract: The invention relates to new pharmaceutically active compounds which are P2-purinoceptor 7-transmembrane (TM) G-protein coupled receptor antagonists, compositions containing them and processes for their preparation.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: August 22, 2000
    Assignee: Astra Pharmaceuticals Limited
    Inventors: Nicholas Kindon, Premji Meghani, Stephen Thom
  • Patent number: 6103761
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: October 19, 1994
    Date of Patent: August 15, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bradley Dean Tait, Michael William Wilson
  • Patent number: 6096753
    Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as 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, 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 4, 1997
    Date of Patent: August 1, 2000
    Assignee: Amgen Inc.
    Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
  • Patent number: 6093718
    Abstract: This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: February 12, 1999
    Date of Patent: July 25, 2000
    Assignee: Zeneca Limited
    Inventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Nicholas John Newcombe
  • Patent number: 6083955
    Abstract: Novel arylethenesulfonamide derivative having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonist, whereinAr: optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group;X: oxygen atom, sulfur atom or a group represented by a formula --NH--;Y: oxygen atom or sulfur atom;R.sub.1 : hydrogen atom, optionally halogen-substituted lower alkyl group, cycloalkyl group, optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group.R.sub.2 : lower alkyl group, lower alkenyl group or lower alkynyl group where each of which may be substituted with one to three substituent(s) selected from a group consisting of hydroxyl group, lower alkoxy group, cycloalkyl group, halogen atom, carboxyl group and lower alkoxycarbonyl group;R.sub.
    Type: Grant
    Filed: June 19, 1998
    Date of Patent: July 4, 2000
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hironori Harada, Jun-ichi Kazami, Susumu Watanuki, Ryuji Tsuzuki, Katsumi Sudou, Akihiro Tanaka
  • 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: 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: 6008224
    Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: December 28, 1999
    Assignee: Kowa Co., Ltd.
    Inventors: Mitsuteru Hirata, Takeo Deushi, Yoshio Takahashi, Masahiro Tamura, Takeshi Ohshima, Toshiaki Oda, Hiroyuki Sonoki, Masami Shiratsuchi
  • Patent number: 6004965
    Abstract: Compounds of the formula: ##STR1## where A, B, R.sup.1 -R.sup.8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5981537
    Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
    Type: Grant
    Filed: May 9, 1996
    Date of Patent: November 9, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
  • Patent number: 5977363
    Abstract: There is provided a process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds. The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: November 2, 1999
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Salvatore John Cuccia, Robert Brigance
  • Patent number: 5977110
    Abstract: Substituted cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, serotonergic, antipsychotic, and anxiolytic agents.
    Type: Grant
    Filed: March 20, 1998
    Date of Patent: November 2, 1999
    Assignee: Warner-Lambert Company
    Inventors: Thomas R. Belliotti, Suzanne R. Kesten, Thomas A. Pugsley, David J. Wustrow
  • 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: 5948551
    Abstract: The use of conjugated compounds which contain two or more pyrimidine rings as part of the conjugated system as electroluminescence materials. The conjugated compounds containing pyrimidine rings have a high thermal stability and a high photostability. They are partially soluble in acids, which also makes possible processing from solution, as well as by vapor deposition.
    Type: Grant
    Filed: June 29, 1995
    Date of Patent: September 7, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rudolf Gompper, Stefan Brandl, Hans-Jurgen Mair
  • Patent number: 5948781
    Abstract: This invention relates to a method of treating cancer by administering a compound of the formula wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E.sup.1, E.sup.2, p, Het' and Het" are defined as indicated in the specification.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: September 7, 1999
    Assignee: Pfizer Inc
    Inventors: Joseph P. Lyssikatos, Robert A. Volkmann
  • Patent number: 5922645
    Abstract: Compounds of the formula (I) and salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties.They can be prepared by processes analogous to known processes (cf. claim 5), in some cases via novel intermediate products (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: July 13, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5922646
    Abstract: Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators. Compounds of the formula (I) and salts thereof ##STR1## in which W.sup.1, W.sup.2, R, n, R.sup.1, R.sup.2, R.sup.4, X, Y and Z are as defined in claim 1 and R.sup.3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: July 13, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5919945
    Abstract: This disclosure relates to a process for preparing bis(hydroxymethyl)pyrrolopyrrole compounds of the formula wherein A.sub.1 and A.sub.2 are aryl radicals, by reacting a 1,4-diketopyrrolopyrrole with formaldehyde. The compound of formula (II) can be isolated or further reacted in a one pot synthesis to yield a compound of the formula ##STR1## wherein B.sub.1 and B.sub.2 are organic radicals.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: July 6, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Shivakumar Basalingappa Hendi
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5889012
    Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: October 16, 1995
    Date of Patent: March 30, 1999
    Assignee: Hoechst-Schering AgrEvo GmbH
    Inventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
  • 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: 5872255
    Abstract: The invention relates to conjugated compounds of general formula (I) ##STR1## wherein X.sub.1 and X.sub.2 are, independently of one another, electron-withdrawing or electron-donating systems, and to a process for the preparation of these compounds.The invention also relates to any material which includes the compounds of general formula I and to the use of said compounds or of any material which includes them in electronic, optoelectronic, nonlinear optical and electrooptical devices.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: February 16, 1999
    Assignee: Office National D'Etudes et de Recherche Aerospatiales (ONERA)
    Inventors: Andre-Jean Attias, Bertrand Bloch, Chantal Cavalli
  • Patent number: 5866583
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: February 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Henri Stalder, Pierre-Charles Wyss
  • Patent number: 5866036
    Abstract: Chiral nonracemic molecules which are useful as high tilt, high polarization and/or high birefringence FLC materials or are useful as components of such FLC materials and which have the following general structure are provided:RO--(Ph.sub.1).sub.m --(A).sub.a --(Ph.sub.2).sub.n --(B).sub.b --(Ph.sub.3).sub.p --Twhere Ph.sub.1, Ph.sub.2 and Ph.sub.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: February 2, 1999
    Assignee: Displaytech, Inc.
    Inventors: Michael D. Wand, Rohini T. Vohra, David M. Walba, Sean D. Monahan
  • Patent number: 5859009
    Abstract: Substituted spiroalkylamino and -alkoxy heterocycles, processes for their preparation, and their use as pesticides and fungicidesThe invention relates to compounds of the formula ##STR1## in which Het is optionally substituted 4-pyridyl or 4-pyrimidinyl; X is NH, O or S(O).sub.0-2 ; E is a bond or alkanediyl; Y and Z are CH.sub.2, O and/or S(O).sub.0-2 ; W is (CH.sub.2).sub.0-4 ; R.sup.4 and R.sup.5 are halogen, (halo)alkyl, (halo)alkoxy or alkylthio; r and s are 0-2; U is a bond, O, S(O).sub.0-2 or optionally substituted imino; and V is a bond CO, SO.sub.2, --CQ--T-- or --CT'.dbd.N--; or U+V together are a double bond; and R.sup.6 is as defined in the description. The invention furthermore relates to processes for their preparation and to their use as pesticides and fungicides.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: January 12, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Wolfgang Schaper, Rainer Preuss, Peter Braun, Manfred Kern, Werner Knauf, Burkhard Sachse, Ulrich Sanft, Anna Waltersdorfer, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
  • Patent number: 5856484
    Abstract: Compounds of formula I: ##STR1## are disclosed. The compounds inhibit the binding of endothelin to its receptors.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5854179
    Abstract: Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) and salts thereof ##STR1## in which R*, R.sup.1, R.sup.2, R.sup.3, X, Y, Z, W, n and m are defined as in claim 1, and specifically R* is a formyl equivalent of the formula CHO, --CH.dbd.NR or CH(X.sup.1 R')(X.sup.2 R"), are suitable as herbicides and plant growth regulators. They are prepared analogously to known methods, in some cases using novel intermediate products of the formula (XVII) ##STR2## in which U*.dbd.NH.sub.2, Cl or (substituted) amino.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: December 29, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5852019
    Abstract: The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: December 22, 1998
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akio Ejima, Masamichi Sugimori, Ikuo Mitsui
  • Patent number: 5849216
    Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Illian, Anke Kaltbeitzel, Rainer Wingen, Hubert Schlosser
  • Patent number: 5849666
    Abstract: N-substituted hydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulatorsCompounds of the formula (I) or salts thereof ##STR1## in which R.sup.1 to R.sup.6, W, Q, X, Y and Z are defined as in formula (I) as claimed in claim 1, are suitable as herbicides and plant growth regulators.The compounds (I) are prepared by processes analogous to known processes (cf.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 5837708
    Abstract: Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: November 17, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5824624
    Abstract: New herbicidal pyridine and pyrimidine derivatives of general formula (I), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.2 or each R.sup.2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 20, 1998
    Assignee: American Cyanamid Company
    Inventors: Axel Kleeman, Helmut Siegfried Baltruschat, Thelka Hulsen
  • 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: 5808067
    Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: September 15, 1998
    Assignee: Hoechst Celanese Corporation
    Inventors: John Saukaitis, Franklin B. Gupton
  • Patent number: 5804685
    Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 8, 1998
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Alan Hutchison
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel