Chalcogen Bonded Directly To The Bicyclo Ring System Patents (Class 544/144)
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Patent number: 6503907Abstract: The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: November 20, 2001Date of Patent: January 7, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Olivier Morand, Narendra Panday, Thomas Weller
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Publication number: 20020187978Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.Type: ApplicationFiled: June 29, 2001Publication date: December 12, 2002Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
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Publication number: 20020143177Abstract: The present invention is disubstituted amines of formula (I) 1Type: ApplicationFiled: June 29, 2001Publication date: October 3, 2002Inventors: James P. Beck, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard
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Patent number: 6403792Abstract: The present invention is to novel sulfonyl isatin compounds of Formula (I), their pharmaceutical compositions, and the novel inhibition of caspases for use in the treatment of apoptosis, and disease states caused by excessive or inappropriate cell death.Type: GrantFiled: December 9, 1999Date of Patent: June 11, 2002Assignee: SmithKline Beecham CorporationInventors: Dennis Lee, Scott Allen Long
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Patent number: 6395734Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: May 28, 1999Date of Patent: May 28, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Publication number: 20020052369Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: June 4, 2001Publication date: May 2, 2002Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
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Patent number: 6380185Abstract: The present invention provides compounds of the formula: wherein R1, R2, R3, R4, X, n Y and Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical formulations and methods of treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.Type: GrantFiled: February 25, 2000Date of Patent: April 30, 2002Assignee: American Home Products CorporationInventors: Marci C. Koko, John W. Ullrich, Arthur A. Santilli
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Patent number: 6362334Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN (VIIIA) and processes for production of pharmacologically useful oxazolidinones.Type: GrantFiled: April 10, 2000Date of Patent: March 26, 2002Assignee: Pharmacia & Upjohn CompanyInventor: Bruce Allen Pearlman
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Patent number: 6358943Abstract: This invention provides compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, X, n and Y, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods utilizing the compounds for treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.Type: GrantFiled: February 25, 2000Date of Patent: March 19, 2002Assignee: American Home Products CorporationInventor: John W. Ullrich
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Patent number: 6350747Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.Type: GrantFiled: February 28, 2000Date of Patent: February 26, 2002Assignee: Glaxo Wellcome Inc.Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
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Publication number: 20020022623Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) 1Type: ApplicationFiled: March 23, 2001Publication date: February 21, 2002Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Publication number: 20020022626Abstract: The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1′ position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety.Type: ApplicationFiled: July 13, 2000Publication date: February 21, 2002Inventors: Peng Cho Tang, LI Sun, Gerald McMahon, Klaus Peter Hirth, Laura Kay Shawver
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Publication number: 20020019395Abstract: Novel compounds of general formula I: 1Type: ApplicationFiled: February 1, 2001Publication date: February 14, 2002Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020015938Abstract: The invention relates to a method of simultaneous high-throughput preformulation quantification of potential drug candidates, where an aliquot of a mixture of solutions containing different compounds is injected into a high pressure liquid chromatograph. The concentration of each compound can be determined by high pressure liquid chromatographic analysis, and correlated to a physico-chemical property of the compound.Type: ApplicationFiled: October 29, 1998Publication date: February 7, 2002Inventor: NARMADA SHENOY
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Patent number: 6277878Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group; R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula: Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloType: GrantFiled: August 26, 1999Date of Patent: August 21, 2001Assignee: Pfizer IncInventors: Kazunari Nakao, Rodney W. Stevens, Kiyoshi Kawamura, Chikara Uchida
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Patent number: 6274578Abstract: The compound, ((3(2-amino-1,2-dioxoethyl)-2-methyl-1-(phenylmethyl)-1H-indol-4-yl)oxy)acetic acid N-morpholino ester, is disclosed together with its use as a highly bioavailable indole sPLA2 inhibitor compound.Type: GrantFiled: October 17, 2000Date of Patent: August 14, 2001Assignee: Eli Lilly and CompanyInventors: Michael Lyle Denney, John Michael Morin, Daniel Jon Sall, Jason Scott Sawyer
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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: VĂ©ronique Hall-Goulle, Aline Bize
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Publication number: 20010007033Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to e useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: ApplicationFiled: March 1, 2000Publication date: July 5, 2001Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6211365Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R3-R6 are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: August 31, 1999Date of Patent: April 3, 2001Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Kenneth Shaw, Alan Hutchison
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Patent number: 6180637Abstract: The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) wherein X is —SO2—, —SO—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Y is —(C═O)—, —(C═O)—NH—, —(C═O)—NH—(CH2)p—, —C═O)—(CH2)p—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—(C═O)—NH—(CH2)p—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Z is —O—, —O—(CH2)p—, —NH—, —NH—(Type: GrantFiled: May 5, 1999Date of Patent: January 30, 2001Assignee: Arzneimittelwerk Dresden GmbHInventors: Rudolf Schindler, Norbert Höfgen, Hildegard Poppe, Kay Brune
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Patent number: 6177426Abstract: The compound, ((3(2-amino-1,2-dioxoethyl)-1-((1,1′-biphenyl)-3-ylmethyl)-2-methyl-1H-indol-4-yl)oxy)acetic acid morpholino-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: March 29, 2000Date of Patent: January 23, 2001Assignee: Eli Lilly and CompanyInventors: Michael L Denney, John M Morin, Daniel J Sall, Jason S Sawyer
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Patent number: 6177425Abstract: According to the invention there are provided Hexahydro-Pyrrolo[3,4-b]pyrrol-2-one compounds of formula (1), (relative stereochemistry indicated), wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (1) are useful inter alia in the treatment or chronic bronchitis.Type: GrantFiled: May 5, 2000Date of Patent: January 23, 2001Assignee: Glaxo Wellcome Inc.Inventors: Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Adam Inglis, Martin Redpath Johnson, Simon John Fawcett MacDonald, Pritom Shah
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Patent number: 6162803Abstract: Compounds effective in treating disorders of the serotonin-affected neurological symptoms are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 and R.sub.5 are each, independently, hydrogen, halogen, lower alkoxy, lower alkyl, cyano, or trifluoromethyl;R.sub.2 and R.sub.4 are each, independently, hydrogen, lower alkyl, phenyl, or substituted phenyl;R.sub.3 is hydrogen or lower alkyl; andX and Y are each, independently, O, NR.sub.6, or CH.sub.2, whereinR.sub.6 is hydrogen, lower alkyl, phenyl, or substituted phenyl; or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 7, 1999Date of Patent: December 19, 2000Assignee: American Home Products Corp.Inventors: Richard E. Mewshaw, Ping Zhou
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Patent number: 6159995Abstract: 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: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6147073Abstract: A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.Type: GrantFiled: January 12, 1998Date of Patent: November 14, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Antonella Ermoli, Sergio Vioglio, Franco Buzzetti, Dario Ballinari
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Patent number: 6147106Abstract: The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1' position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety.Type: GrantFiled: August 20, 1997Date of Patent: November 14, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Klaus Peter Hirth, Laura Kay Shawver
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Patent number: 6140327Abstract: The compound, ((3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl)oxy)ac etic acid morpholino-N-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: May 12, 1999Date of Patent: October 31, 2000Assignee: Eli Lilly and CompanyInventors: Jason Scott Sawyer, John Michael Morin, Jr., Douglas Wade Beight, Daniel Jon Sall, John Andrew Buben
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Patent number: 6133305Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: September 25, 1998Date of Patent: October 17, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6130238Abstract: The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: October 10, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6127549Abstract: Compounds of formula:A(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 und 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 2, 1998Date of Patent: October 3, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6114371Abstract: The present invention relates to novel 3-(cyclohexano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: November 12, 1998Date of Patent: September 5, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Robert A. Blake
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Patent number: 6087359Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: September 10, 1999Date of Patent: July 11, 2000Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo
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Patent number: 6013648Abstract: The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.Type: GrantFiled: December 22, 1997Date of Patent: January 11, 2000Assignee: SanofiInventors: Murielle Rinaldi, Francis Barth, Pierre Casellas, Christian Congy, Didier Oustric, Malcolm R. Bell, Thomas E. D'Ambra, Richard E. Philion
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Patent number: 5994344Abstract: There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.Type: GrantFiled: September 25, 1998Date of Patent: November 30, 1999Assignee: Glaxo Wellcome Inc.Inventors: Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Inglis, Martin Redpath Johnson, Simon John Fawcett Macdonald, Pritom Shah, Robin Andrew Smith
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Patent number: 5977154Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: June 26, 1997Date of Patent: November 2, 1999Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Christine Ann Droste, Cynthia Darshini Jesudason, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
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Patent number: 5972937Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: September 16, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
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Patent number: 5973146Abstract: A process for the preparation of compounds of formula I ##STR1## by reacting a pyrrolopyrrole of formula ##STR2## wherein X.sub.1 is a group selected from ##STR3## X.sub.2 is a group selected from ##STR4## or has the same meaning as X.sub.1, with a secondary amine of formula ##STR5## in the molar ratio 1:2, in the presence of an anhydrous dipolar aprotic solvent and of an amount 0.1 to 15 times in excess of stoichiometric proportion, based on the amine of formula III, of an anhydrous organic base, in the temperature range from 50.degree. to 230.degree. C. and under a pressure from 0 to 10 bar.The substituents R.sub.1 to R.sub.8, Y and Hal are as defined in claim 1.The compounds of formula I are especially suitable for use as photoconductive substances.Type: GrantFiled: September 29, 1993Date of Patent: October 26, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Alain Claude Rochat, Olof Wallquist, Abul Iqbal, Jin Mizuguchi
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Patent number: 5891902Abstract: The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, --O--(CH.sub.2).sub.n --OR.sup.5, or ##STR2## R.sup.3 represents hydrogen, lower alkyl, or ##STR3## R.sup.4 represents hydroxy, lower alkoxy, substituted or unsubstituted aryloxy, or --NR.sup.10 R.sup.11, and X represents CO or SO.sub.2, with the proviso that when R.sup.3 is hydrogen or lower alkyl, and X is CO, R.sup.4 is --NR.sup.10 R.sup.11, or pharmaceutically acceptable salts thereof.Type: GrantFiled: July 15, 1996Date of Patent: April 6, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Daisuke Machii, Haruki Takai, Nobuo Kosaka, Hisakatsu Seo, Tomomi Sugiyama, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi, Soichiro Sato, Masako Uchii, Koji Suzuki
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Patent number: 5849780Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.Type: GrantFiled: October 17, 1994Date of Patent: December 15, 1998Assignee: SanofiInventors: Alain Di Malta, Loic Foulon, Georges Garcia, Dino Nisato, Richard Roux, Claudine Serradeil-Legal, Gerard Valette, Jean Wagnon
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Patent number: 5847156Abstract: 1,4-Diketopyrrolopyrroles of the formula ##STR1## in which A and B independently of one another are a group of the formula ##STR2## R.sub.1 is a long-chain radical containing a reactive group capable of polymerization, and R.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR3## or R.sub.1. The novel diketopyrrolopyrroles are suitable for preparing coloured polymers with unexpectedly advantageous colour effects.Type: GrantFiled: January 29, 1997Date of Patent: December 8, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Sameer Hosam Eldin, Abul Iqbal
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Patent number: 5840745Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.Type: GrantFiled: September 25, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S. p. A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
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Patent number: 5840738Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: June 25, 1997Date of Patent: November 24, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Cynthia Darshini Jesudason, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
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Patent number: 5817832Abstract: Diketopyrrolo?3,4-c!pyrroles of the formula ##STR1## in which X and Y independently of one another are a divalent aromatic radical and R is a radical CN, COR.sub.5, CO.sub.2 R.sub.5, CON(R.sub.5).sub.2, NO.sub.2, SO.sub.2 R.sub.5, SOR.sub.5, SO.sub.2 N(R.sub.5).sub.2 or PO(OR.sub.6).sub.2.For the definition of the substituents R.sub.1, R.sub.2 and R.sub.5, refer to claim 1.These compounds are blue to violet, tinctorially strong pigments with good stability properties, in particular good light stability and weather stability.Type: GrantFiled: June 11, 1996Date of Patent: October 6, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Olof Wallquist, Bernd Lamatsch, Thomas Ruch
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Patent number: 5808061Abstract: The present invention provides a novel process for preparing a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 combine to form C.sub.4 -C.sub.6 polymethylene, --CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.2 --, --CH.sub.2 C(CH.sub.3).sub.2 CH.sub.2 CH.sub.2 --, or --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 --; or a pharmaceutically acceptable salt or solvate thereof.Also provided intermediates of formulae II and IV ##STR2## wherein Z is a leaving group.Type: GrantFiled: July 17, 1995Date of Patent: September 15, 1998Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Mark G. Stocksdale
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Patent number: 5807883Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 24, 1996Date of Patent: September 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Masataka Hikota, Toshiro Shikano, Masaaki Nagasaki
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Patent number: 5786487Abstract: The present invention relates to pyrrolopyrrole derivatives of the formula (I) ##STR1## wherein A and B are identical or different aryl radicals, and DPP is a diaryldiketopyrrolopyrrole radical; which diketopyrrolopyrrole derivative is substituted by from 0 to 6 moles of --SO.sub.3 M per mole of the pyrrolopyrrole derivative; wherein M is hydrogen or a metal or ammonium cation. The pyrrolopyrrole derivatives of formula I are useful as rheology-improving agents for pigment dispersions.Type: GrantFiled: September 26, 1997Date of Patent: July 28, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Shivakumar B. Hendi
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Patent number: 5773612Abstract: A compound of formula II' ##STR1## in whichR.sub.I is an ethoxy group or a chlorine atom;R.sub.II is hydrogen, a chlorine atom or a methyl group;R.sub.III is a chlorophenyl group or a methoxyphenyl group;R.sub.IV is an amino group, a group NR.sub.9 R.sub.10 or NR.sub.9 R.sub.XI, or a piperazin-1-yl radical substituted in the 4-position by a (C.sub.2 -C.sub.10)alkylene group substituted by an amino group which is free or carries a protective group;R.sub.10 is (CH.sub.2).sub.p R.sub.35 or a (C.sub.2 -C.sub.10)alkylene group substituted by R.sub.21 ;R.sub.XI is a (C.sub.1 -C.sub.12)alkyl group or a group .omega.-R.sub.32 R.sub.33 N(C.sub.1 -C.sub.4)-alkylcarbonyl; andR.sub.21 is R.sub.36 ; a group OR.sub.37 ; a group NR.sub.32 R.sub.33 ; a cyano group; a group S(C.sub.1 -C.sub.7)alkyl; a group SO(C.sub.1 -C.sub.7)alkyl; or a group SO.sub.2 (C.sub.1 -C.sub.7)alkyl;R.sub.35 is a piperid-4-yl group which is unsubstituted or substituted in the 1-position by a (C.sub.1 -C.sub.7)alkoxycarbonyl group or by a (C.sub.Type: GrantFiled: April 30, 1996Date of Patent: June 30, 1998Assignee: SanofiInventors: Jean Wagnon, Bernard Tonnerre, Alain Di Malta, Richard Roux, Marie-Sophie Amiel, Claudine Serradeil-Legal
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Patent number: 5723462Abstract: Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents;W represents optionally substituted thiazolyl or quinoxalinyl;X is hydrogen, hydroxy or lower alkyl; andT is hydrogen, halogen, hydroxy, nitro, amino or alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: April 26, 1996Date of Patent: March 3, 1998Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Patent number: 5708188Abstract: The invention relates to mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formulae ##STR1## as well as single-phase solid solutions of two different compounds of formulae I and II, wherein the diketopyrrolopyrrole having the smaller geometrical constitution is present in an amount of 53 to 70 mol %. A and B are as defined in claim 1. The novel mixed crystals as well as the novel solid solutions are admirably suited for pigmenting organic material of high molecular weight.Type: GrantFiled: September 28, 1995Date of Patent: January 13, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, Abul Iqbal, Bernhard Medinger, Olof Wallquist
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Patent number: 5679670Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: December 15, 1994Date of Patent: October 21, 1997Assignee: Alcon Laboratories, Inc.Inventors: Thomas Robert Dean, Hwang-Hsing Chen, Jesse Albert May