Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/75)
-
Patent number: 6706895Abstract: Disclosed herein is a compound having the formula: wherein R1 is alkyl and R2 and R3 are independently selected aryl groups. Also disclosed is a method of making bifenazate using the compound as an intermediate.Type: GrantFiled: November 14, 2002Date of Patent: March 16, 2004Assignees: Uniroyal Chemical Company, Inc., Crompton Co./CieInventors: Sheldon B. Park, Gaik-Lean Chee, Mark A. Dekeyser
-
Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Publication number: 20040039033Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: December 10, 2002Publication date: February 26, 2004Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
-
Publication number: 20040013974Abstract: The invention describes the use of oxime alkyl sulfonate compounds of formula 1 1Type: ApplicationFiled: July 2, 2003Publication date: January 22, 2004Inventors: Kurt Dietliker, Martin Kunz, Hitoshi Yamato, Christoph De Leo
-
Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
-
Patent number: 6673932Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is hydrogen, hydroxy, nitro, amino, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy or cyclic alkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group; and y=1 to 3.Type: GrantFiled: January 18, 2002Date of Patent: January 6, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
-
Patent number: 6673934Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is hydrogen, hydroxy, nitro, amino, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy or cyclic alkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group, preferably an aromatic group selected from a furanyl, thienyl, pyridinyl, phenyl, 2,3-dihydro-benzo[1,4]dioxin-5 or -6-yl or benzo[1,3]dioxol-4 or -5-yl group; and y=1 to 3.Type: GrantFiled: January 18, 2002Date of Patent: January 6, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
-
Patent number: 6660728Abstract: The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: November 14, 2002Date of Patent: December 9, 2003Assignees: Aventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
-
Publication number: 20030216392Abstract: The compounds of formula 1, 1Type: ApplicationFiled: June 13, 2003Publication date: November 20, 2003Applicant: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
-
Patent number: 6596863Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Patent number: 6566366Abstract: Compounds of the formula and salts thereof wherein the substituents are defined as in accordance with the specification useful for the treatment of tumor growth, osteoporosis, inflammation and cardiovascular disorders.Type: GrantFiled: March 6, 2001Date of Patent: May 20, 2003Assignees: Aventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
-
Publication number: 20030078434Abstract: A composition for treating or preventing glomerulopathy which contains a compound of the formula (1): 1Type: ApplicationFiled: June 6, 2002Publication date: April 24, 2003Applicant: Shionogi & Co., Ltd.Inventors: Hidetake Kurihara, Fumihiko Watanabe, Yoshinori Tamura, Toshihiro Sinosaki
-
Patent number: 6548534Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: July 27, 2001Date of Patent: April 15, 2003Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
-
Patent number: 6541668Abstract: The present invention provides processes for the preparation of 3-aryloxy-3-arylpropylamines and intermediates thereof using an nucleophilic aromatic displacement in 1,3-dimethyl-2-imidazolidinone or N-methylpyrrolidinone.Type: GrantFiled: September 12, 2001Date of Patent: April 1, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Patton Kjell, Kurt Thomas Lorenz
-
Publication number: 20030045568Abstract: Thiosemicarbazone compounds of formula: 1Type: ApplicationFiled: April 19, 2002Publication date: March 6, 2003Inventors: Sergio Altamura, Uwe Koch
-
Publication number: 20020198388Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: August 9, 2001Publication date: December 26, 2002Applicant: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald G. Sherrill, Andrew Spaltenstein, Eric S. Furfine, Francois Maltais, Clarence W. Andrews, John F. Miller, Vicente Samano
-
Patent number: 6492394Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.Type: GrantFiled: December 22, 1999Date of Patent: December 10, 2002Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
-
Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Patent number: 6420354Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.Type: GrantFiled: December 8, 1999Date of Patent: July 16, 2002Assignee: Advanced Medicine, Inc.Inventors: Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins
-
Patent number: 6417222Abstract: The present invention relates to novel [(2-substituted-5-[3-thienyl])-benzyl]-[2-([2-isopropoxy-5-fluoro]-phenoxy)-ethyl]-amine derivatives having formula (1) and the use thereof as medicaments, especially anti-psychotic medicaments.Type: GrantFiled: September 28, 2001Date of Patent: July 9, 2002Assignee: Pierre Fabre MedicamentInventors: Bernard Vacher, Stéphane Cuisiat, Wouter Koek
-
Patent number: 6410736Abstract: The present invention relates to compounds of formula I, and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.Type: GrantFiled: October 19, 2000Date of Patent: June 25, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Mavis D. Adam
-
Patent number: 6387954Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: May 14, 2002Assignee: Eli Lilly and CompanyInventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Patent number: 6380224Abstract: Amine and amide derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing amines and amides of formula A as the active ingredient are described. The amines and amides of formula A are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.Type: GrantFiled: July 27, 2000Date of Patent: April 30, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott L. Dax, James McNally, Mark Youngman
-
Patent number: 6380392Abstract: The present invention includes array of new chiral ligands that are optically active or racemic. These ligands are bidentate, tridentate, tetradentate or pentadentate ligands which include P-P, P-N, N-N, mixed P-N, Schiff base or carbene sites. The present invention further includes a catalyst prepared by a process, which includes contacting a transition metal salt, or a complex thereof, and a ligand according to the present invention. The present invention still further includes a process for preparation of an asymmetric compound. In this process, a substrate capable of forming an asymmetric product by an asymmetric reaction and a catalyst according to the present invention are contacted to produce an asymmetric product. Transition metal complexes with these ligands are effective catalysts for asymmetric reactions.Type: GrantFiled: June 29, 2000Date of Patent: April 30, 2002Assignee: The Penn State Research FoundationInventor: Xumu Zhang
-
Patent number: 6380429Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.Type: GrantFiled: September 15, 2000Date of Patent: April 30, 2002Assignee: E. I. du Pont Nemours and CompanyInventor: Eric Maurice Smith
-
Patent number: 6372920Abstract: The present invention relates to a process for preparing optically active and racemic nitrogen-substituted 2-aminotetralins of the following Formula (I): wherein R1, R2, R3, R4, and n are set in the specification, wherein the process comprises alkylating the corresponding unsubstituted 2-aminotetralin of Formula (II): with a reactant of the Formula (III): Z—(CH2)n—R3 (III) wherein Z is a leaving group, in the presence of a base, wherein the base is selected from the group consisting of alkali metal carbonate and alkali metal bicarbonate, and wherein the amount of the base is less than about a 1.9-fold molar excess with respect to the amount of the 2-aminotetralin.Type: GrantFiled: November 16, 2000Date of Patent: April 16, 2002Assignee: Aderis Pharmaceuticals, Inc.Inventors: Gevork Minaskanian, Keith Rippel
-
Patent number: 6358981Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: March 19, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Andrew Hendley Fray, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Patent number: 6358883Abstract: The present invention relates to the pesticidal use of 1-aryl-1-(substituted thio, sulfinyl and sulfonyl)-2-nitroethane compounds having the structural formula IType: GrantFiled: November 5, 1999Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: William Wakefield Wood, Annmarie Enos
-
Publication number: 20020013351Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that utilize them can be used, either alone or in conjunction with a neurotrophic factor, such as nerve growth factor, to promote repair of neuronal damage caused by disease or physical trauma.Type: ApplicationFiled: June 27, 2001Publication date: January 31, 2002Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Patricia McCaffrey, Perry M. Novak, Michael Mullican
-
Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
-
Patent number: 6245930Abstract: Proposed is a novel chemical-sensitization resist composition capable of giving a positively or negatively patterned resist layer of excellent pattern resolution and cross sectional profile of the patterned resist layer with high sensitivity. Characteristically, the resist composition is formulated, as combined with a resinous ingredient which is subject to changes in the solubility behavior in an alkaline developer solution by interaction with an acid, with a specific oximesulfonate compound as the radiation-sensitive acid-generating agent represented by the general formula R1—C(CN)═N—O—SO2—R2, in which R1 is an inert organic group and R2 is an unsubstituted or substituted polycyclic monovalent hydrocarbon group selected from the group consisting of polycyclic aromatic hydrocarbon groups such as naphthyl and polycyclic non-aromatic hydrocarbon groups such as a terpene or camphor residue.Type: GrantFiled: May 24, 1999Date of Patent: June 12, 2001Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Katsumi Oomori, Hideo Hada, Fumitake Kaneko, Mitsuru Sato, Kazufumi Sato, Toshimasa Nakayama
-
Patent number: 6232467Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.Type: GrantFiled: June 27, 1997Date of Patent: May 15, 2001Assignee: University of Southern CaliforniaInventors: Nicos A. Petasis, Ilia A. Zavialov
-
Patent number: 6200353Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula at least one coupler comprising a compound of the formula: wherein R is selected from the group consisting of C1 to C2 alkyl and hydroxyethyl, R1 is selected from the group consisting of hydrogen, chlorine, bromine, C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 hydroxyalkyl and C1 to C3 hydroxyalkoxy, and X is O, S or NH.Type: GrantFiled: February 1, 2000Date of Patent: March 13, 2001Assignee: Bristol Myers Squibb CompanyInventors: Mu-Ill Lim, Linas R. Stasaitis, Yuh-Guo Pan
-
Patent number: 6172103Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.Type: GrantFiled: November 24, 1999Date of Patent: January 9, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Wilfried Schwab, Ruth Raiss
-
Patent number: 6166003Abstract: A compound comprising a heterocyclic moiety, such as a thiophene, covalently attached to an alkylene isothiocyanate moiety. The compound is effective to prevent the occurrence or progression of cancer or a precancerous condition, and can be used for therapeutic or prophylactic purposes. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: GrantFiled: February 17, 1999Date of Patent: December 26, 2000Assignee: LKT Laboratories, Inc.Inventor: Luke K. T. Lam
-
Patent number: 6147226Abstract: A water-scavenging solvent, such a polyphosphoric acid, can be used for the synthesis of cyclopentyl 2-thienyl ketone by the direct acylation of cyclopentanecarboxylic acid without first reacting the cyclopentanecarboxylic acid with thionylchloride to form the acid chloride, while achieving new and unexpected yields. A tiletamine-free base can be made from the cyclopentyl 2-thienyl ketone with a halide in the presence of a solvent for the cyclopentyl 2-thienyl ketone to form a halogenated cyclopentane 2-thienyl ketone, aminating the halogenated cyclopentane 2-thienyl ketone by reaction with an amine, and subjecting the reaction product to thermal rearrangement, in a suitable solvent, and at a sufficient temperature to form tiletamine free base. Each step for the formation of tiletamine free base can be accomplished using the same solvent, e.g., dichlorobenzene so that intermediates need not be isolated between reactions.Type: GrantFiled: January 11, 2000Date of Patent: November 14, 2000Assignee: Great Lakes Chemical CorporationInventors: Yuri Aleksandrovich Lapin, Ignacio H. Sanchez
-
Patent number: 6143790Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
-
Patent number: 6140354Abstract: .beta.-Aminotetralin derivatives of the formula: ##STR1## which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a .beta.-aminotetralin derivative as the active ingredient are described. The .beta.-aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.Type: GrantFiled: April 12, 1999Date of Patent: October 31, 2000Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Scott L. Dax, Timothy W. Lovenberg, James McNally, Allen B. Reitz, Mark A. Youngman
-
Patent number: 6080874Abstract: The present invention provides a simple, 1-step process for preparing a N-(aryl or heteroaryl)-hydroxyurea comprising reacting the corresponding alcohol, ester or ether with hydroxyurea and acid. This reaction is particularly useful for preparing a benzo[b]thienyl substituted N-hydroxyurea of formula: ##STR1## from compound 1: ##STR2## by reacting compound 1 with hydroxyurea and acid. R.sup.1 is selected from the group consisting of hydrogen, 1-6 carbon alkyl, 1-6 carbon alkoxy, and halogen; R.sup.2 is an 1-4 carbon alkyl; and R.sup.3 is selected from the group consisting of hydrogen, acyl, methyl, ethyl and mixtures thereof. Additional steps to isolate the pure bulk product follow.Type: GrantFiled: September 25, 1998Date of Patent: June 27, 2000Assignee: Abbott LaboratoriesInventors: John E. Hengeveld, Elise H. Leese, Brian S. Moon, Dennis M. Abad, Kimberly A. Allen, Philip E. Bauer, David B. Murphey, Brian T. Fohey, Richard R. Copp, Jr., Greg S. Lannoye, Rodney M. Mittag
-
Patent number: 6077954Abstract: Novel compounds having the formula: ##STR1## wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: August 1, 1996Date of Patent: June 20, 2000Assignee: ISIS Pharmaceuticals, Inc.Inventors: P. Dan Cook, Haoyun An
-
Patent number: 6075166Abstract: The present invention is to novel photochemically cleavable aryl sulfonamides of the formulaP--A.sub.3 --A.sub.2 --A.sub.1 --S(O).sub.2 NR.sub.1 R.sub.2whereinR.sub.1 and R.sub.2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl;A.sub.1 is an aryl or heteroaryl moiety;A.sub.2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR.sub.3, sulfur or an amide group;R.sub.3 is alkyl;A.sub.3 is an electron rich aryl or heteroaryl moiety having an E.sub.1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex;P is a solid support.Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent.Type: GrantFiled: March 31, 1995Date of Patent: June 13, 2000Assignee: SmithKline Beecham CorporationInventors: Ravi Shunker Garigipati, Jerry Leroy Adams
-
Patent number: 6063928Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.Type: GrantFiled: December 8, 1998Date of Patent: May 16, 2000Assignee: Pfizer IncInventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
-
Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
-
Patent number: 6048890Abstract: A thiophene derivative containing a phenylamidino group represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and are hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxyl group having 1 to 4 carbon atoms; or a pharmacologically acceptable salt thereof. The compound is useful for the treatment of inflammatory diseases.Type: GrantFiled: August 22, 1997Date of Patent: April 11, 2000Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Kiyomi Tanaka, Tokiko Nishida, Jun Nakano, Mamoru Inoue, Tsutomu Nakamura, Hayami Debuchi
-
Patent number: 6043368Abstract: The present invention provides a method of preparing thieno[3,2-c]pyridine derivatives of formula I: ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl; lower alkylene phenyl; substituted lower alkylene phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro and halo; lower alkylene naphthyl, lower alkylene thienyl; lower alkylene diphenyl; lower alkylene-hydroxy-phenyl; substituted lower alkylene-hydroxy-phenyl wherein the phenyl is substituted from 1 to 3 times with lower alkyl, lower alkoxy, lower acyloxy, hydroxy, nitro, and halo; lower alkylene-hydroxy-naphthyl; lower alkylene-hydroxy-thienyl; lower alkylene-hydroxy-diphenyl, and R.sub.2 is H or lower alkylene. The method comprises reacting a compound of a formula II: ##STR2## with a cyclic dioxy or cyclic dithio in the presence of catalyst.Type: GrantFiled: September 4, 1996Date of Patent: March 28, 2000Assignee: Poli Industria Chimica, S.P.A.Inventors: Ambrogio Magni, Giovanni Signorelli
-
Patent number: 6031134Abstract: The invention relates to a novel process for the preparation of 2-amino-2-arylehanols of the formula (I) ##STR1## in which Ar represents aryl or hetaryl each unsubstituted or identically or differently monosubstituted to pentasubstituted, where as substituents there may be mentioned:halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, unsubstituted or substituted cycloalkyloxy or unsubstituted or substituted phenyl,which comprises catalytically hydrogenating .alpha.-hydroxyketoximes of the formula (II) ##STR2## in which Ar has the meaning given above,using Raney nickel or Raney cobalt in the presence of a diluent and in the presence of a base andnovel 2-amino-2-arylethanols and novel .alpha.-hydroxyketoximes.Type: GrantFiled: November 4, 1998Date of Patent: February 29, 2000Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Ernst Kysela, Albrecht Marhold
-
Patent number: 6017947Abstract: R.sup.6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro;R.sup.10 is phenylthio, dialkylamino, alkylthio, alkoxycarbonyl, N-morpholinyl, or N-piperidinyl;R.sup.11 is hydrogen or alkyl;Q is alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkoxycarbonyl, alkoxyiminomethyl, or Y--Ar;Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, or --CH.sub.2 SO.sub.2 --;Ar is a substituted or unsubstituted phenyl or aromatic heterocyclic group,useful for the inhibition of the replication of HIV-1, in vitro and in vivo.Type: GrantFiled: September 17, 1999Date of Patent: January 25, 2000Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
-
Patent number: 6011161Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1999Date of Patent: January 4, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
-
Patent number: 6004724Abstract: New oximsulfonate compounds of the formulae I or II, ##STR1## wherein m is 0 or 1; x is 1 or 2; R.sub.1 is, for example phenyl, which is unsubstituted or substituted or R.sub.1 is a heteroaryl radical that is unsubstituted or substituted, or, if m is 0, R.sub.1 additionally is C.sub.2 -C.sub.6 alkoxycarbonyl, phenoxycarbonyl or CN; R'.sub.1 is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.2 has for example one of the meanings of R.sub.1 ; n is 1 or 2; R.sub.3 is for example C.sub.1 -C.sub.18 alkyl, R'.sub.3 when x is 1, has one of the meanings given for R.sub.3, or R'.sub.3 in the formula IV and when x is 2 in the formula 1, is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.4 and R.sub.5 are independently of each other for example hydrogen, halogen, C.sub.1 -C.sub.6 alkyl; R.sub.6 is for example hydrogen, phenyl; R.sub.7 and R.sub.8 are independently of each other for example hydrogen or C.sub.1 -C.sub.12 -alkyl; R.sub.9 is for example C.sub.1 -C.sub.12 alkyl; A is S, O, NR.sub.Type: GrantFiled: June 25, 1998Date of Patent: December 21, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Hitoshi Yamato, Hartmut Bleier, Jean-Luc Birbaum, Martin Kunz, Kurt Dietliker, Christoph De Leo, Toshikage Asakura
-
Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann