Phthalazines (including Hydrogenated) Patents (Class 544/237)
  • Publication number: 20010036945
    Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
    Type: Application
    Filed: May 10, 2001
    Publication date: November 1, 2001
    Applicant: Neurogen Corporation.
    Inventors: Jun Yuan, Taeyoung Yoon
  • Patent number: 6291481
    Abstract: Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: September 18, 2001
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
  • Patent number: 6288082
    Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: September 11, 2001
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Mark E. Salvati, Philip Frost
  • 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: 6258806
    Abstract: The present invention discloses the compounds of general formula (1) wherein R1, R2, R3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immune deficiency syndrome.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: July 10, 2001
    Assignee: Narhex Limited
    Inventor: Damian Wojciech Grobelny
  • Patent number: 6258812
    Abstract: The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* (I*) or (iii) together form a bridge in subformula I** (I**), wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; c is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, p
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: July 10, 2001
    Assignee: Novartis AG
    Inventors: Guido Bold, Jörg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
  • Patent number: 6255303
    Abstract: The compounds of formula (I) in which R1, R2, R3, R4, R5, X and Y have the meanings as given in the description are novel effective bronchial therapeutica.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: July 3, 2001
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Geert Jan Sterk, Margaretha van der Mey
  • Patent number: 6218392
    Abstract: A fused pyridazine compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof which exhibits an inhibitory activity against cyclic GMP phosphodiesterase (hereinafter referred to as “cGMP-PDE”). The compounds are useful as preventive and therapeutic agents for diseases for which a cGMP-PDE inhibiting action is efficacious, for example, ischemic heart diseases such as angina pectoris, myocardial infarct and chronic and acute cardiac failure, pulmonary hypertension, arteriosclerosis and bronchial asthma.
    Type: Grant
    Filed: September 29, 1998
    Date of Patent: April 17, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Nobuhisa Watanabe, Yasuhiro Kabasawa, Yasutaka Takase, Fumihiro Ozaki, Keiji Ishibashi, Kazuki Miyazaki, Masayuki Matsukura, Shigeru Souda, Kazutoshi Miyake, Hiroki Ishihara, Kohtaro Kodama, Hideyuki Adachi
  • Patent number: 6214857
    Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.
    Type: Grant
    Filed: July 30, 1998
    Date of Patent: April 10, 2001
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • 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: 6194409
    Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: February 27, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
  • Patent number: 6187920
    Abstract: This invention provides pyridazinone derivatives encompassed by the following the formula: wherein, R1, R2, R3, R4, R5 and R7 represent a hydrogen atom and the like, and R6 represents a C1-C3 alkyl and the like. The pyridazinone derivatives have excellent herbicidal activity, therefore, they can be used as an active ingredient for herbicidal compositions and can be utilized in herbicidal method, which are also described.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: February 13, 2001
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventor: Takashi Komori
  • Patent number: 6180629
    Abstract: [4,5]-Fused-1,3-disubstituted-1,2-diazine-6-one derivatives with nitrogen-containing substituents in position one are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia, including precancerous and cancerous lesions.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: January 30, 2001
    Assignee: Cell Pathways, Inc.
    Inventors: Xiaojing Wang, Gerhard Sperl, Paul Gross, Rifat Pamukcu, Gary A. Piazza
  • Patent number: 6140325
    Abstract: Thienopyrimidine derivatives are disclosed. Also disclosed are methods for the production and use of these compounds.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: October 31, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shuichi Furuya, Nobuo Choh, Tetsuya Ohtaki, Toshifumi Watanabe
  • Patent number: 6133259
    Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: October 17, 2000
    Assignee: University of Pittsburgh
    Inventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
  • 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: 6114330
    Abstract: The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Christian Hubschwerlen, Synese Jolidon, Jean-Luc Specklin, Pierre-Charles Wyss
  • Patent number: 6103718
    Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 have the means set forth in the description are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors (specifically of type 4), which are effective bronchial therapeutics.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: August 15, 2000
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Geert Jan Sterk
  • Patent number: 6096761
    Abstract: The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: August 1, 2000
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul Rene Marie Bosmans, John Christopher Love, Michel Anna Jozef Decleyn, Henri Elisabeth Frans D'Haen
  • Patent number: 6077847
    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 and other conditions in both men and women.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
  • Patent number: 6077461
    Abstract: Luminol derived monomers, and luminol derived water-treatment polymers formed from the luminol derived monomers, as well as methods for monitoring of the chemiluminescence of such water-treatment polymers are disclosed. The novel chemiluminescent polymers require only a very low level of incorporation of the chemiluminescent moiety, and are useful for monitoring, even in systems containing impurities which either quench fluorescence or fluoresce themselves.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: June 20, 2000
    Assignee: Nalco Chemical Company
    Inventors: Patrick G. Murray, Amy M. Tseng, Don Sproul
  • Patent number: 6071895
    Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immume deficiency syndrome.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: June 6, 2000
    Assignee: Narhex Limited
    Inventor: Damian Wojciech Grobelny
  • Patent number: 6066638
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## wherein W is O, S(O).sub.n or NR.sup.5 ;n is 0, 1 or 2;Q is O or S;G is a fused phenyl, naphthalene, thiophene, furan, pyrrole, pyridine, thiazole, oxazole, imidazole, pyrazine, pyridazine or pyrimidine ring; andR.sup.1 -R.sup.5 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.
    Type: Grant
    Filed: January 2, 1998
    Date of Patent: May 23, 2000
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: James Francis Bereznak, Zen-Yu Chang, Charlene Gross Sternberg
  • Patent number: 6060492
    Abstract: 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. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: May 9, 2000
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
  • Patent number: 6048853
    Abstract: Substituted 1-arylphthalazine compositions with the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independentlya) H,b) HO,c) R.sup.11 O--,d) halogen,e) C1-C3-alkyl,f) CF.sub.3,g) R.sup.12 CO.sub.2 --, orh) R.sup.12 CONH--;R.sup.1 and R.sup.2, or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 can be taken together to bea) --OCH.sub.2 O--, orb) --OCH.sub.2 CH.sub.2 O--;R.sup.5 isa) H,b) C1-C6-alkyl,c) C3-C6-alkenyl,d) C3-C6-alkynyl,e) C3-C6-cycloalkyl,f) phenyl or substituted phenyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alky, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and CO.sub.2 R.sup.12, org) phenyl-C1-C3-alkyl or substituted phenyl-C1-C3-alkyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alkyl, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and --CO.sub.2 R.sup.12 ;R.sup.6 isa) R.sup.10 R.sup.11 N--,b) R.
    Type: Grant
    Filed: January 18, 1996
    Date of Patent: April 11, 2000
    Assignee: Bearsden Bio, Inc.
    Inventors: Mark A. Collins, Jeffrey C. Pelletier
  • Patent number: 6046227
    Abstract: 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..sub.3 receptor agonists useful in the treatment of Type II diabetes and obesity.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: April 4, 2000
    Assignee: Eli Lilly and Company
    Inventors: Thomas Alan Crowell, Charles David Jones, Anthony John Shuker
  • Patent number: 6011036
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their analogues, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione compounds of the general formula (I), and their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: January 4, 2000
    Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti
  • Patent number: 6005106
    Abstract: Naphthalene derivatives of the formula [I]: wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: December 21, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
  • Patent number: 6004933
    Abstract: The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R.sub.1 is optionally substituted alkyl or aryl.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: December 21, 1999
    Assignee: Cortech Inc.
    Inventors: Lyle W. Spruce, Albert C. Gyorkos, John C. Cheronis, Val S. Goodfellow, Axel H. Leimer, John M. Young, James Ivan Gerrity
  • Patent number: 5985878
    Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Janssen Pharmaceuticals, N.V.
    Inventors: Raymond Antoine Stokbroekx, Marcel Jozef Maria Van der Aa, Marc Willems, Lieven Meerpoel, Marcel Gerebernus Maria Luyckx, Robert Tuman
  • Patent number: 5985869
    Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.
    Type: Grant
    Filed: July 15, 1997
    Date of Patent: November 16, 1999
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5981779
    Abstract: The present invention disclose to non-radioactive vitamin D compounds of formula (1) and methods to assay for the presence of vitamin D, vitamin D analogs and their metabolites which may be present in milk, blood or other biological fluids. The assay methods employed in this invention may be enzyme linked immununoassays (ELISAs) (with biotin containing compounds) and fluorimetric and chemiluminometric assays (with fluorescein or chemiluminiscence containing compounds).
    Type: Grant
    Filed: June 10, 1998
    Date of Patent: November 9, 1999
    Assignee: A and D Assay, Incorporated
    Inventors: Michael F. Holick, Rahul Ray
  • Patent number: 5981528
    Abstract: The invention concerns a compound of formula (I): ##STR1## wherein R.sup.1 -R.sup.6, A, B, and D have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, and methods of treating a bacterial infection by administering such a compound or salt.
    Type: Grant
    Filed: October 21, 1997
    Date of Patent: November 9, 1999
    Assignee: Zeneca Limited
    Inventor: Michael Barry Gravestock
  • Patent number: 5965730
    Abstract: A pyridine derivative of the formula (I): ##STR1## wherein A is group of the following formulae: ##STR2## (R.sup.1 and R.sup.2 are each H, or protected or unprotected OH, R.sup.31, R.sup.41 and R.sup.42 are protected or unprotected hydroxymethyl, R.sup.32 is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.33 is substituted or unsubstituted lower alkyl, and the dotted line means the presence or absence of a double bond), R.sup.5 and R.sup.6 are H, or protected or unprotected amino, or both combine together with the adjacent nitrogen to form substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof, these compounds showing excellent bronchoconstriction inhibitory activity and/or anti-inflammatory activity of airway, and being useful in the prophylaxis or treatment of asthma.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: October 12, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tatsuzo Ukita, Masakatsu Sugahara, Katsuo Ikezawa, Hideo Kikkawa, Kazuaki Naito
  • Patent number: 5942511
    Abstract: The, present invention relates to a novel allylthiopyridazine derivative represented by formula (I) which exhibits a superior effect for prevention and treatment or hepatic diseases induced by toxic substances and for protection of human tissues from radiation: ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sub.1 represents halogen atom, lower alkoxy, dialkylaminoalkoxy, hydroxyalkoxy, phenoxy substituted or unsubstituted with lower alkyl, benzyloxy, or phenyl, andR.sub.2 and R.sub.3 independently of one another represent hydrogen or lower alkyl, or R.sub.2 and R.sub.3 together with carbon atom to which they are attached can form a saturated or unsaturated 6-membered ring,provided that R.sub.2 and R.sub.3 are other than hydrogen when R.sub.1 is chloro; and to a process for preparing thereof and a pharmaceutical composition containing the same as an effective component.
    Type: Grant
    Filed: June 16, 1998
    Date of Patent: August 24, 1999
    Assignees: Soon Kyoung Kwon, Seoul Pharm. Co., Ltd.
    Inventors: Soon Kyoung Kwon, Sang Geon Kim, Young Nam Park, Mi Kyung Kim, Sung Hee Choi, Hea Soon Shin
  • Patent number: 5942504
    Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immune deficiency syndrome.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: August 24, 1999
    Assignee: Narhex Limited
    Inventor: Damian Wojciech Grobelny
  • Patent number: 5939443
    Abstract: 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. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: August 17, 1999
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Donald Paul Matthews, John Hampton McDonald, III, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
  • Patent number: 5925637
    Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: July 20, 1999
    Assignee: Bayer Corporation
    Inventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
  • Patent number: 5889012
    Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: October 16, 1995
    Date of Patent: March 30, 1999
    Assignee: Hoechst-Schering AgrEvo GmbH
    Inventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
  • Patent number: 5863915
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: January 26, 1999
    Assignee: Bayer Corporation
    Inventors: Harold C. E. Kluender, Brian R. Dixon, David R. Brittelli
  • Patent number: 5861380
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 19, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5849741
    Abstract: A fused pyridazine compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof which exhibits an inhibitory activity against cyclic GMP phosphodiesterase (hereinafter referred to as "cGMP-PDE").The compounds are useful as preventive and therapeutic agents for diseases for which a cGMP-PDE inhibiting action is efficacious, for example, ischemic heart diseases such as angina pectoris, myocardial infarct and chronic and acute cardiac failure, pulmonary hypertension, arteriosclerosis and bronchial asthma.
    Type: Grant
    Filed: April 9, 1996
    Date of Patent: December 15, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Nobuhisa Watanabe, Yasuhiro Kabasawa, Yasutaka Takase, Fumihiro Ozaki, Keiji Ishibashi, Kazuki Miyazaki, Masayuki Matsukura, Shigeru Souda, Kazutoshi Miyake, Hiroki Ishihara, Kohtaro Kodama, Hideyuki Adachi
  • Patent number: 5824677
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5817674
    Abstract: Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic properties for angiotensin II receptors and a process and novel intermediates for their properties.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: October 6, 1998
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Michel Fortin, Jean-Luc Haesslein
  • Patent number: 5786356
    Abstract: 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: Grant
    Filed: June 25, 1997
    Date of Patent: July 28, 1998
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5728712
    Abstract: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.
    Type: Grant
    Filed: May 20, 1996
    Date of Patent: March 17, 1998
    Assignee: Chiroscience Limited
    Inventors: John Gary Montana, Hazel Joan Dyke, Robert James Maxey, Christopher Lowe
  • Patent number: 5719155
    Abstract: Chroman derivatives of the formula ?I! ##STR1## wherein R.sup.1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R.sup.2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R.sup.3 is a lower alkoxyalkyl or an aryloxyalkyl; R.sup.4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: February 17, 1998
    Assignee: Japan Tobacco Inc.
    Inventors: Hidetsura Cho, Shinsuke Sayama, Susumu Katoh, Kazuo Aisaka, Itsuo Uchida
  • Patent number: 5719151
    Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: February 17, 1998
    Inventors: Sydney Shall, Manoochehr Tavassoli
  • Patent number: 5716954
    Abstract: Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;R.sup.1 is hydrogen, lower alkyl, aryl, aralkyl, heterocyclo, heterocyclo lower-alkyl, heteroaryl, or heteroaralkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, lower alkyl, halo, carboxy, alkoxycarbonyl, carbamoyl, lower-alkyl carbonyl, halocarbonyl, thiomethyl, trifluoromethyl, cyano or nitro;or a pharmaceutically acceptable ester, ether or salt thereof, have been found to be useful as an anti-inflammatory, antasthmatic, immunosuppressive, anti-allograft rejection, anti-graft-vs-host rejection, autoimmune disease or analgetic agent(s).
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: February 10, 1998
    Assignee: Syntex U.S.A. Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe, Bruce H. Devens, Robert Alvarez, Michael G. Martin