Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 546/146)
  • Patent number: 6323215
    Abstract: This invention provides compounds having the following general structure: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: November 27, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Mark Macielag, Zhihua Sui, Shawn Walsh, Boyo Zhao
  • Patent number: 6316625
    Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: November 13, 2001
    Assignees: Agouron Pharmaceuticals, Inc., Japan Tobacco Inc.
    Inventors: Srinivasan Babu, Bennett C. Borer, Travis P. Remarchuk, Robert J. Szendroi, Kathleen R. Whitten, Juliette K. Busse, Kim F. Albizati
  • Patent number: 6310080
    Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: October 30, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Patent number: 6307049
    Abstract: The present disclosure describes novel compounds and compositions which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair growth. The present compounds and compositions may also be useful against a variety of disorders including, for example, multi-drug resistance, human immunodeficiency virus (HIV), cardiac injury, and neurological disorders, and may be useful for controlling parasites and invoking immunosuppression.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: October 23, 2001
    Assignee: The Procter & Gamble Co.
    Inventors: John McMillan McIver, Charles Raymond Degenhardt, David Joseph Eickhoff
  • Publication number: 20010031870
    Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: 1
    Type: Application
    Filed: February 28, 2001
    Publication date: October 18, 2001
    Inventors: Richard M. Soll, Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
  • Patent number: 6303628
    Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein A is C 1-6 alkylene or —NR1—; Z is C(═L)R2, or SO2R3; U is CH or N; W and Y are independently selected from —CH2—, O, S and —N—R1; m is 1, 2 or 3; q and r are independently 0, 1 or 2; X is independently selected from halogen, C1-4 alkyl, halo-substituted C1-4 alkyl, hydroxy, C1-4 alkoxy, halo-substituted C1-4 alkoxy or the like; n is 1 or 2; L is oxygen or sulfur; R1 is hydrogen or C1-4 alkyl; R2 is hydroxy, C1-6alkyl, halo-substituted C1-6 alkyl, C1-6 alkoxy, halo-substituted C1-6 alkoxy, C3-7 cycloalkoxy, C1-4 alkyl(C3-7 cycloalkoxy), —NR4R5 or the like; R3 is C1-6 alkyl or halo-substituted C1-6 alkyl; and R4 and R5 are independently selected from hydrogen, C1-6 alkyl and halo-substituted C1-6alkyl.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventors: Kazunari Nakao, Shigeo Hayashi, Rodney W. Stevens
  • Patent number: 6303786
    Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive compounds and intermediates.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: October 16, 2001
    Assignees: Agouron Pharmaceuticals, Inc., Japan Tobacco, Inc.
    Inventors: Michael E. Deason, Kathleen R. Whitten
  • Patent number: 6300342
    Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: October 9, 2001
    Assignee: Boehringer Ingelheim Pharm KG
    Inventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
  • Patent number: 6300501
    Abstract: Inhibitors of protein farnesyl transferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating cancer, restenosis, psoriasis, endometriosis, atherosclerosis, or viral infections.
    Type: Grant
    Filed: November 2, 1998
    Date of Patent: October 9, 2001
    Assignee: Warner-Lambert Company
    Inventors: Ellen M. Dobrusin, Annette M. Doherty, James S. Kaltenbronn, Daniele M. Leonard, Dennis J. McNamara, Judith Sebolt-Leopold, Kevon R. Shuler
  • Patent number: 6297257
    Abstract: Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: October 2, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Daniela Botta, Giancarlo Grancini, Gabriele Morazzoni
  • Patent number: 6297283
    Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: October 2, 2001
    Assignee: Kowa Co., Ltd.
    Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
  • Patent number: 6294551
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: September 25, 2001
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
  • Patent number: 6281227
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 28, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
  • Publication number: 20010016657
    Abstract: This invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.
    Type: Application
    Filed: April 24, 2001
    Publication date: August 23, 2001
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Mervyn Thompson, Robert William Ward, Peter David Edwards
  • Patent number: 6277849
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: August 21, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Martin Zeller
  • Patent number: 6274593
    Abstract: The present invention provides compounds of formula (I): which are useful as antipsychotic agents.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: August 14, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Amanda Johns, David John Nash, Geoffrey Stemp
  • Patent number: 6271236
    Abstract: Compounds of the formula wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: August 7, 2001
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6265408
    Abstract: Sulphonamide compounds according to formula (I) or pharmaceutically acceptable salts thereof: wherein: Ar is naphthyl, phenyl or thienyl optionally substituted by one or more substituents selected from the group consisting of C1-6 alkyl optionally substituted by NR7R8, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkylthio, cyano, nitro, halogen, CF3, C2F5, NR7R8, CONR7R8, NR7COR8, S(O)pNR7R8, CHO, OCF3, SCF3, COR9, CH2OR9, CO2R9 or OR9 where p is 1 or 2 and R7, R8 and R9 are independently hydrogen or C1-6 alkyl. R1 and R2 are independently hydrogen or C1-6alkyl or together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring optionally substituted by Cl-6alkyl and optionally containing a further heteroatom selected from nitrogen, sulphur or oxygen, the nitrogen atom being substituted by hydrogen, C1-6 alkyl or cycloC3-7alkyl; R3 is hydrogen or C1-6 alkyl; X is oxygen, sulphur or a bond; n is 2 or 3; and m is 1 or 2; are provided.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: July 24, 2001
    Assignee: SmithKline Beecham plc
    Inventors: Ian Thomson Forbes, Francis David King, Shirley Katherine Rahman
  • Patent number: 6262074
    Abstract: Hetaroyl derivatives of the formula I where: R1 and R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl or C1-C6-alkoxysulfonyl, where the last 6 radicals may be substituted and/or functionalized; phenyl, phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl, where the last 5 radicals may be substituted; Z is an unsubstituted or substituted four-membered unsaturated, partially or fully saturated chain consisting of three carbons and one nitrogen; Q is unsubstituted or substituted hydroxypyrazole linked at position 4; and their agriculturally useful salts. A process for preparing the hetaroyl derivatives, compositions comprising them, and the use of these derivatives or these compositions comprising them for controlling undesirable plants.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: July 17, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Martina Otten, Norbert Götz, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Michael Rack, Regina Luise Hill, Peter Plath, Matthias Witschel, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
  • Patent number: 6239126
    Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders and neurodegenerative diseases.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: May 29, 2001
    Assignee: American Home Products Corporation
    Inventors: Michael G. Kelly, Gan Zhang
  • Patent number: 6231786
    Abstract: In the fluorinated azoles of the formula (I) R1(—A1)a—T—(A2—)b(M—A3—)cR2   (I) the symbols and indices have -the following meanings: T is undirected and is 4-fluorothiazole-2,5-diyl, 5-fluorothiazole-2,4-diyl, 4-fluorooxazole-2,5-diyl, 5-fluorooxazole-2,4-diyl or 4-fluoroisoxazole-2,5-diyl; R1 and R2 are identical or different and are hydrogen or a straight-chain or branched C1-20-alkyl or C2-20-alkenyl radical (with or without asymmetrical carbon atoms); A1, A2 and A3 are identical or different and are, for example, phenylene-1,4-diyl or cyclohexane-1,4-diyl; M is undirected and is —OC(═O)—, —OCH2—, —CH2CH2—, —OC(═O)CH2CH2—, —OCH2CH2CH2—, —C≡C—, —CH2CH2CH2CH2— or a single bond; a, b and c, independently of one another, are 0 or 1, with the proviso that the sum a+b+c is 1 or 2.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: May 15, 2001
    Assignee: Clariant GmbH
    Inventors: Rainer Wingen, Barbara Hornung, Ayako Ogawa, Wolfgang Schmidt
  • Patent number: 6228867
    Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: May 8, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
  • Patent number: 6218393
    Abstract: Anthranilic acids of formula (I): wherein each of R to R9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, —S—(CH2)p or —O—(CHO2)p— wherein p is from 1 to 6 and Ar is an unsaturated carbocyclic or heterocyclic group, and the pharmaceutically acceptable salts thereof, have activity as inhibitors of P-glycoprotein and may thus be used, inter alia, as modulators of multidrug resistance in the treatment of multidrug resistant cancers, for example to potentiate the cytotoxicity of a cancer drug.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: April 17, 2001
    Assignee: Xenova Limited
    Inventors: Hamish Ryder, Philip Anthony Ashworth, Michael Bryan Roe, Julie Elizabeth Brumwell, Sukhjit Hunjan, Adrian John Folkes, Jason Terry Sanderson, Susannah Williams, Levi Michael Maximen
  • Patent number: 6214841
    Abstract: This application relates to a novel compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, processes and Intermediates for its preparation, pharmaceutical formulations comprising the novel compound of formula (I), and the use of the compound of formula (I) as an antithrombotic agent.
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: April 10, 2001
    Assignee: Eli Lilly and Company
    Inventors: Charles Van Jackson, Kenneth Dean Kurz, Robert Theodore Shuman
  • Patent number: 6211196
    Abstract: Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I) in which B, D, R1, and R2 have the meanings indicated herein.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: April 3, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Schölkens
  • Patent number: 6211373
    Abstract: This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: April 3, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 6200957
    Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: July 14, 1998
    Date of Patent: March 13, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Peter Lin, Mitree M. Ponpipom, Matthew J. Wyvratt, Narindar N. Girotra, Jonathan Young
  • Patent number: 6197750
    Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: March 6, 2001
    Assignee: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Robert J. Ternansky
  • Patent number: 6184228
    Abstract: The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands from a first group of chemical compounds, selecting from the first set of HbS ligands a seconds set that exhibit inhibition of HbS polymerization, and selecting from the second set a third set that display anti-sickling activity of red blood cells when in the presence thereof. The method may include the step of performing a methemoglobin S proteolysis assay measuring a percent protease protection for each compound. The method may additionally include the steps of measuring HbS aggregation, inhibition of protease, deoxy-HbS gelation inhibition activity, O2 affinity of HbS, and cytotoxic effect to cell activity. The method may further include assessing red blood cell morphology, and eliminating compounds that contain moieties that bind to heme.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: February 6, 2001
    Assignee: ANADYS Pharmaceuticals, Inc.
    Inventors: Alan F. Corin, Andrew A. Pakula, Julianne Bryan
  • Patent number: 6177443
    Abstract: The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a compound of formula I wherein A together with the double bond of formula I is benzene or thiophene; R1 is optionally substituted C1-6 alkyl or optionally substituted aryl; R2 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or —COR3, wherein R3 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or optionally substituted aryl; R4 and R5 independently are hydrogen, halogen, perhalomethyl, optionally substituted C1-6-alkyl, hydroxy, optionally substituted C1-6-alkoxy, nitro, cyano, amino, optionally substituted mono- or optionally substituted di-C1-6-alkylamino, acylamino, C1-6-alkoxycarbonyl, carboxy or carbamoyl; n is 0, and m is 1, and methods of treating or preventing a disease of the endocrinologic system.
    Type: Grant
    Filed: March 5, 1998
    Date of Patent: January 23, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Peter Madsen, Jane Marie Lundbeck, Niels Westergarrd, Lars Naerum, Annemarie Reinhardt Varming, Helle Demuth, Morten Heide
  • Patent number: 6172081
    Abstract: Tetrahydroisoquinoline 3-carboxamide derivatives of formula and pharmaceutically acceptable salts thereof wherein: X is (a) CH2; (b) S (c) O; or (d) C(CH3)2; R1 and R2 are independently (a) hydrogen; (b) hydroxy; (c) alkyl; (d) alkoxy; (e) aralkoxy; or (f) halogen. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: January 9, 2001
    Assignee: Novartis AG
    Inventor: Robert Damon
  • Patent number: 6166219
    Abstract: Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.
    Type: Grant
    Filed: November 2, 1998
    Date of Patent: December 26, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
  • Patent number: 6162812
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: December 19, 2000
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
  • Patent number: 6150335
    Abstract: Use of a compound of the formula I ##STR1## for the manufacture of a medicament for the treatment of pain. The compounds are .delta. opioid agonists and thus useful in the treatment of pain without the requirement of co-application of a .mu. opioid agonist.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: November 21, 2000
    Assignee: Astra AB
    Inventor: Peter Schiller
  • Patent number: 6150352
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: November 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
  • Patent number: 6143762
    Abstract: Compounds of formula (I), wherein R.sup.1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, arylC.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.3-6 cycloalkylC.sub.1-4 alkoxy, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkylsulphonyl, C.sub.1-4 alkylsulphonyloxy, C.sub.1-4 alkylsulphonylC.sub.1-4 alkyl, arylsulphonyl, arylsulphonyloxy, arylsulphonylC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonamido, C.sub.1-4 alkylamido, C.sub.1-4 alkylsulphonamidoC.sub.1-4 alkyl, C.sub.1-4 alkylamidoC.sub.1-4 alkyl, arylsulphonamido, arylcarboxamido, arylsulphonamidoC.sub.1-4 alkyl, arylcarboxamidoC.sub.1-4 alkyl, aroyl, aroylC.sub.1-4 alkyl, or arylC.sub.1-4 alkanoyl group; a group R.sup.3 OCO(CH.sub.2).sub.p, R.sup.3 CON(R.sup.4)(CH2)p, R.sup.3 R.sup.4 NCO(CH.sub.2).sub.p or R.sup.3 R.sup.4 NSO.sub.2 (CH.sub.2).sub.p where each of R.sup.3 and R.
    Type: Grant
    Filed: February 11, 1999
    Date of Patent: November 7, 2000
    Assignee: SmithKline Beecham, plc
    Inventors: David John Nash, Geoffrey Stemp
  • Patent number: 6140339
    Abstract: The present invention provides new monomeric derivatives of the C-8'-7 linked naphthylisoquinoline alkaloid dioncophylline D. The invention also provides new C-4 substituted monomeric arylisoquinoline alkaloid derivatives. The present invention furthermore provides novel dimeric arylisoquinoline alkaloids comprised of coupled first and second arylisoquinoline monomers, wherein either or both of said monomer(s) is (are) monomeric compound(s) of the present invention. Monomeric and dimeric compounds of the present invention have medically useful properties, such as antimicrobial properties, more specifically such as antimalarial and antiviral properties. Monomeric compounds of the present invention are also useful as building blocks or intermediates for synthesis of novel dimeric arylisoquinoline alkaloids.
    Type: Grant
    Filed: December 31, 1997
    Date of Patent: October 31, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Gerhard Bringmann, Michael R. Boyd, Matthias Wenzel
  • Patent number: 6130231
    Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 10, 2000
    Assignee: DuPont Pharmaceuticals
    Inventors: John Wityak, Aleksandra Ewa Tobin
  • Patent number: 6127372
    Abstract: This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides 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 provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: October 3, 2000
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Mark Andrew Murcko, Perry Michael Novak, Govinda Rao Bhisetti
  • Patent number: 6117999
    Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: September 12, 2000
    Assignees: Agouron Phramaceuticals, Inc., Japan Tobacco, Inc.
    Inventors: Srinivasan Babu, Bennett C. Borer, Travis P. Remarchuk, Robert J. Szendroi, Kathleen R. Whitten, Juliette K. Busse, Kim F. Albizati
  • Patent number: 6110934
    Abstract: This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5,6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: August 29, 2000
    Assignee: SmithKline Beecham p.l.c.
    Inventors: John David Harling, Barry Sidney Orlek, Mervyn Thompson
  • Patent number: 6107316
    Abstract: A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are useful in controlling such protozoan parasites as Giardia lamblia, Leishmania major, Entamoeba histolytica, Cryptosporidium parvum, Toxoplasma gondii and microsporidia.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: August 22, 2000
    Assignee: Rohm and Haas Company
    Inventors: David Hamilton Young, Enrique Luis Michelotti, Thomas David Edlind, Santosh Kumar Katiyar
  • Patent number: 6100276
    Abstract: This application relates to compounds of the formula ##STR1## wherein R, X and Y are defined within, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, and for analgesia, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: August 8, 2000
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Stephen J. Shimshock, Susan M. Chesson, Abdul E. Mutlib
  • Patent number: 6100238
    Abstract: The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 8, 2000
    Assignee: Cortech Inc.
    Inventors: Albert C. Gyorkos, Lyle W. Spruce
  • Patent number: 6093729
    Abstract: Substituted bicyclic heteroaroylguanidines, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them are described, as are the pharmaceutically tolerated salts thereof. A process for their preparation, and their use as medicines and diagnostic aids in cardiovascular diseases, is also described.
    Type: Grant
    Filed: November 18, 1998
    Date of Patent: July 25, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 6077849
    Abstract: Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kun Liu, Harold B. Wood, Anthony B. Jones, Bei Zhang
  • Patent number: 6077864
    Abstract: A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: June 20, 2000
    Assignee: Pfizer Inc.
    Inventors: Laurence Edward Burgess, James Patrick Rizzi
  • Patent number: 6066650
    Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
    Type: Grant
    Filed: July 21, 1997
    Date of Patent: May 23, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino, John E. Lawson, Henry M. Holava, Richard A. Partyka
  • Patent number: RE37029
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: January 23, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler
  • Patent number: RE37094
    Abstract: Compounds of formula in which R1 represents H, an alkyl or a substituted alkyl, R2 represents H or alkyl and R3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R2 and R3 considered together represent the group which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases. Use of these compounds as medicaments. No figure.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: March 13, 2001
    Assignee: Sanofi
    Inventors: Daniel Fréhel, Danielle Gully, Gérard Valette, Jean-Pierre Bras