Polycyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/257)
  • Patent number: 6046183
    Abstract: Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5.alpha.-reductase inhibitor, e.g. a 17.beta.-substituted 4-azasteroid, a 17.beta.-substituted non-azasteroid, 17.beta.-acyl-3-carboxy-androst-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylaminophenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an .alpha..sub.1 -adrenergic receptor blocker, i.e., terazosin. The combination provides therapy at the molecular level for the underlying cause of the disease as well as providing symptomatic relief. Pharmaceutical compositions useful for treatment are also disclosed.
    Type: Grant
    Filed: February 20, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Glenn J. Gormley, Elizabeth Stoner
  • Patent number: 6030972
    Abstract: Compounds of the formula ##STR1## where A, B, D, R.sup.1 and R.sup.2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases.The novel compounds are prepared via compounds of the formulaH.sub.2 N--CH.sub.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: February 29, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Joachim Bohm, Hans Wolfgang Hoffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
  • Patent number: 6028077
    Abstract: The present invention is directed to the isolation and characterization of six new crambescidin compounds, the structures of which are shown below: ##STR1## .
    Type: Grant
    Filed: April 10, 1998
    Date of Patent: February 22, 2000
    Inventors: Kenneth L. Rinehart, Jiang-Gong Shi, Furong Sun
  • Patent number: 6022895
    Abstract: Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: February 8, 2000
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Wolfgang Werner Alfred Strassburger, Helmut Heinrich Buschmann, Werner Englberger, Elmar Josef Friderichs
  • Patent number: 5998421
    Abstract: The present invention relates to a food and a feed having lipid metabolism improving activity or anti-obesity activity, and a lipid metabolism improving agent or an anti-obesity agent for humans or animals which comprise, as an active ingredient, a compound represented by formula (I): ##STR1## wherein >A--B-- represents >CR.sup.1 --NR.sup.2 -- (wherein R.sup.1 represents hydrogen or hydroxy, and R.sup.2 represents hydrogen or lower alkyl; or R.sup.1 and R.sup.2 are combined together to form a bond) or >C.dbd.N.sup.+ (R.sup.3)-- (wherein R.sup.3 represents lower alkyl); n represents 0 when >A--B-- is >CR.sup.1 --NR.sup.2 --, and represents 1 when >A--B-- is >C.dbd.N.sup.+ (R.sup.3)--; and X.sup.- represents an anion, or a salt thereof.
    Type: Grant
    Filed: February 5, 1998
    Date of Patent: December 7, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yoshiharu Yokoo, Yoshinori Kobayashi, Yumiko Nakano
  • Patent number: 5952331
    Abstract: The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists.
    Type: Grant
    Filed: November 3, 1997
    Date of Patent: September 14, 1999
    Assignee: Syntex (USA) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5945423
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: August 31, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
  • Patent number: 5939442
    Abstract: In accordance with the present invention, there is provided a class of compounds which are capable of modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-.gamma.). The identification of such compounds makes it possible to intervene in PPAR-.gamma. mediated pathways.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 17, 1999
    Assignee: The Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Barry M. Forman
  • Patent number: 5939419
    Abstract: Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein:R.sub.1, R.sub.2, R.sub.3, R.sup.a, R.sup.b and R.sup.c as defined in the disclosure;pharmaceutical compositions containing said compounds;methods of treatment using said compounds; anda process for preparing polycyclic guanines comprisinga) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine;b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine;c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; andd) closing the ring of the substituted aminopurine with a suitable dehydrating agent.
    Type: Grant
    Filed: August 23, 1995
    Date of Patent: August 17, 1999
    Assignee: Schering-Plough Corporation
    Inventors: Deen Tulshian, Brian A. McKittrick, Yan Xia, Samuel Chackalamannil
  • Patent number: 5886008
    Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: March 23, 1999
    Assignee: Pfizer Inc.
    Inventor: John Eugene Macor
  • Patent number: 5880135
    Abstract: A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R.sub.1, and R.sub.21 which are identical or different, are independently selected from a halogen atom; a (C.sub.1 -C.sub.5)hydroxyalkyl radical; a (C.sub.1 -C.sub.5)alkyl; a (C.sub.7 -C.sub.10)aralkyl; a (C.sub.1 -C.sub.5)alkoxy; a trifluoromethyl; a nitro; a nitrile; an --SR group in which R is selected from hydrogen, a (C.sub.1 -C.sub.5)alkyl radical and a (C.sub.7 -C.sub.10)aralkyl radical; an --S--CO--R group in which R is selected from a (C.sub.1 -C.sub.5)alkyl radical and an aralkyl radical in which the aryl part is (C.sub.6 -C.sub.8) and the alkyl part is (C.sub.1 -C.sub.4); a --COOR' group in which R' is selected from hydrogen and a (C.sub.1 -C.sub.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: March 9, 1999
    Assignee: Sanofi
    Inventors: Danielle Gully, Pierre Roger, Camille Georges Wermuth
  • Patent number: 5859016
    Abstract: Dehydroevodiamine-HCl, a constituent of Evodia rutaecarpa Benth. (DHED) exhibits anti-AChE activity and improves the memory impairment of animals produced by scopolamine in the passive avoidance test. Thus, DHED can be a potent, long term memory enhancing and anti-dementia agent if it is used together with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: January 12, 1999
    Assignees: JE IL Pharmaceutical Co., Ltd., Yoo-Hun Suh
    Inventors: Yoo-Hun Suh, Sam-Sik Kang, Seong-Hun Kim, Cheol-Hyoung Park, Woong Choi
  • Patent number: 5856322
    Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: February 8, 1996
    Date of Patent: January 5, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel L. Belley, Serge Leger, Patrick Roy, Marc Labelle, Yi Bin Xiang, Daniel Guay
  • Patent number: 5846969
    Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: December 8, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5824683
    Abstract: Antihypertensive and bronchodilating phosphoclusterose inhibitory compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is fluoro, chloro or bromo.
    Type: Grant
    Filed: November 26, 1996
    Date of Patent: October 20, 1998
    Assignee: Schering Corporation
    Inventors: Brian A. McKittrick, Deen Tulshian
  • Patent number: 5786361
    Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: July 28, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Peter Eckenberg, Rudi Grutzmann, Hilmar Bischoff, Dirk Denzer, Ulrich Nielsch
  • Patent number: 5753663
    Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, in particular use as 5HT.sub.2C - antagonists. The invention is also directed to formulations and methods for treatment.
    Type: Grant
    Filed: September 24, 1996
    Date of Patent: May 19, 1998
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Lee Allen Flippin, Gabriel Stone Weatherhead
  • Patent number: 5728684
    Abstract: A method of ascertaining if a prodrug is useful for treating a disease is disclosed. The prodrug is acceptable if it is metabolized in liver cells by aldehyde oxidase to produce an active drug or metabolite. Prodrugs are shown equally effective in treating diseases as the active drug itself with many benefits and without as many associated side effects. Methods for treating cancers with 5-iodo-2-pyrimidinone-deoxyribose and 5-fluoro-2-pyrimidinone are also described.
    Type: Grant
    Filed: April 19, 1994
    Date of Patent: March 17, 1998
    Assignee: Yale University
    Inventors: Yung-Chi Cheng, Chien-Neng Chang
  • Patent number: 5667792
    Abstract: A cosmetic or dermatological composition with a depigmenting action comprises derivatives of 2,5-dihydroxyphenylcarboxylic acids, their homologs, and their salts, with the derivatives having the following structural formula: ##STR1## wherein: R.sub.1 represents OR.sub.5, OH, or ##STR2## R.sub.5 is a linear or branched C.sub.1 -C.sub.20 alkyl radical, a linear or branched C.sub.2 -C.sub.20 alkenyl radical, or a C.sub.1 -C.sub.20 alkyl radical substituted by one or more hydroxy or alkoxy groups;r' and r", identical or different, represent a hydrogen atom, a C.sub.1 -C.sub.20 alkyl radical, a C.sub.2 -C.sub.6 hydroxyalkyl radical, or a C.sub.3 -C.sub.6 polyhydroxyalkyl, or r' and r" taken together, with the nitrogen atom, form a heterocycle;the number of carbon atoms in the --(CH.sub.2).sub.n --COR.sub.1 chain is less than or equal to 21;R.sub.2 and R.sub.3, identical or different, represent a hydrogen atom, a linear or branched C.sub.1 -C.sub.4 alkyl radical, or a C.sub.1 -C.sub.4 alkoxy; R.sub.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: September 16, 1997
    Assignee: L'Oreal
    Inventors: Alex Junino, Alain Lagrange, Quang Lan N'Guyen, Marie-Alix Bourboulon
  • Patent number: 5654310
    Abstract: Triazolopyrimidines of the formula ##STR1## where A, D and X have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: August 5, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Schlecker, Hans-Joerg Treiber, Berthold Behl, Hans Peter Hofmann
  • Patent number: 5646154
    Abstract: Quinazoline compounds represented by general formula (1) or (2) possess an activity of significantly inhibiting the production or secretion of a tumor necrosis factor and are useful as drugs for the treatment of diseases wherein a tumor necrosis factor is considered to be involved in causing those diseases: ##STR1## wherein R.sup.1 through R.sup.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: July 8, 1997
    Assignee: Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Kenji Irie, Yutaka Ueda, Norio Fujiwara
  • Patent number: 5639756
    Abstract: An antidiabetic compound selected from those of formula (I): ##STR1## wherein A, B, C, D, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y and Z are as defined in the description.Medicaments containing the same.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: June 17, 1997
    Assignee: Adir et Compagnie
    Inventors: Vera Alekseevna Anisimova, Margarita Valentinovna Levchenko, Tatyana Borisovna Korochina, Alexander Alexeyevich Spasov, Sergei Gennadyevich Kovalev, Galina Petrovna Dudchenko
  • Patent number: 5635507
    Abstract: A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 3, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Alistair A. Miller, Malcolm S. Nobbs, Richard M. Hyde, Michael J. Leach
  • Patent number: 5631261
    Abstract: Novel triazoloquinazolines of the formula I ##STR1## where A, X R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: May 20, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Schlecker, Hans-Joerg Treiber, Berthold Behl, Hans P. Hofmann
  • Patent number: 5612344
    Abstract: The use of triazoloquinazolines for the production of drugs for controlling central nervous disorders is described. The triazoloquinazolines have the formula ##STR1## where R.sup.1, R.sup.2 and X have the meanings stated in the description.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: March 18, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Schlecker, Hans-J org Treiber, Berthold Behl, Hans P. Hofmann
  • Patent number: 5604224
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5602137
    Abstract: Compounds for treating cardiovascular or circulatory disorders of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.7, Ar.sup.1, Ar.sup.2, X, Y, and n are defined herein.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: February 11, 1997
    Assignee: Beiersdorf-Lilly GmbH
    Inventors: Gerd R uhter, Theo Schotten, Wolfgang Stenzel, Michael Paal
  • Patent number: 5602136
    Abstract: Compounds having the formula ##STR1## and the other variables are as defined herein, and are indicated for use in the treatment and prophylaxis of, for example, hypertension, congestive heart failure, ocular hypertension, renal failure, and CNS disorders, or are intermediates thereto.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: February 11, 1997
    Assignee: Beiersdorf-Lilly GmbH
    Inventors: Gerd R uhter, Theo Schotten, Wolfgang Stenzel, Michael Paal
  • Patent number: 5574039
    Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.
    Type: Grant
    Filed: September 22, 1994
    Date of Patent: November 12, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
  • Patent number: 5574038
    Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 12, 1996
    Assignee: The Upjohn Company
    Inventor: E. Jon Jacobsen
  • Patent number: 5571813
    Abstract: Pharmaceutical compounds which are azolo-fused pyrimidine compounds having the formula ##STR1## in which .dbd.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: November 5, 1996
    Assignee: Beiersdorf-Lilly GmbH
    Inventors: Gerd R uhter, Theo Schotten, Wolfgang Stenzel, Michael Paal
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5532366
    Abstract: The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: July 2, 1996
    Assignee: Zeneca Limited
    Inventors: Philip D. Edwards, Peter Warner, Donald J. Wolanin
  • Patent number: 5510370
    Abstract: The present invention includes a method for increasing bone mass in a subject by administration of PTH and raloxifene. Another aspect of the invention is a method for treating bone loss in a subject by administration of PTH and raloxifene. The invention further provides for a composition of PTH and raloxifene for increasing bone mass in a subject. Another aspect of the invention is a composition of PTH and raloxifene for treatment of bone loss in a subject.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: April 23, 1996
    Assignee: Eli Lilly and Company
    Inventor: Janet M. Hock
  • Patent number: 5500230
    Abstract: The present invention relates to a method of treating cranial fluid volume dysfunctions such as glaucoma in an individual, comprising administering compounds which effect an increase in cyclic GMP at the site of the dysfunction or at the site of synthesis or removal of the accumulating fluid. In particular, the method of treatment involves the topical use of hydralazine, non-organic nitrites or nitroglycerine, and the systematic use of hydralazine or non-organic nitrites.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: March 19, 1996
    Assignee: The General Hospital Corporation
    Inventor: James A. Nathanson
  • Patent number: 5482936
    Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 9, 1996
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Kyle J. Lindstrom
  • Patent number: 5482967
    Abstract: Novel compound represented by the formula: ##STR1## such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3- acetamide: ##STR2## or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: January 9, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Hitoshi Ikeda, Takenori Ishimaru, Takayuki Doi
  • Patent number: 5478825
    Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: December 26, 1995
    Assignee: Egis Gyogyszergyar
    Inventors: Jozsef Reiter, Gabor Berecz, Gizella Zsila, Lujza Pet cz, Gabor Gigler, Marton Fekete, Maria Szecsey nee Heged s, Enik Szirt nee Kiszelly, Ludmila Rohacs nee Zamkovaja, Frigyes Gorgenyi, Margit Csorg
  • Patent number: 5441955
    Abstract: Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using indolo[2,1-b]quinazoline-6,12-dione compounds of the formula (I): ##STR1## wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofloxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: August 15, 1995
    Assignee: PathoGenesis Corporation
    Inventors: William R. Baker, Lester A. Mitscher
  • Patent number: 5420129
    Abstract: The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: May 30, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5418252
    Abstract: A method of inhibiting cartilage degradation comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino and piperidino, a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: May 23, 1995
    Assignee: Eli Lilly and Company
    Inventor: Daniel C. Williams
  • Patent number: 5393755
    Abstract: Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl;R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino;R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one.The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.
    Type: Grant
    Filed: December 14, 1992
    Date of Patent: February 28, 1995
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
  • Patent number: 5368864
    Abstract: Formulations of oxypurinol and/or its alkali or alkaline earth salts in non-crystalline form, containing the active substance in the form of a solids dispersion with pharmacologically harmless adjuvants. They have more rapid and higher solubility than oxypurinol and/or its alkali or alkaline earth salts. They can be used for the preparation of drugs having high bioavailability of the active substance oxypurinol.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: November 29, 1994
    Assignee: Henning Berlin GmbH Chemie- und Pharmawerk
    Inventors: Wolfgang Lahr, Guido Weickgenannt
  • Patent number: 5360803
    Abstract: A pharmaceutical composition for treatment of cancer comprises:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I) ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, --CH.dbd.CH--, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1 represents a methine group or L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents a alkyl group;R.sub.6 and R.sub.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: November 1, 1994
    Assignees: Dan Farber Cancer Institute, Fuji Photo Film Co., Ltd.
    Inventors: Tadao Shishido, Lan B. Chen
  • Patent number: 5302589
    Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: April 12, 1994
    Assignee: Glaxo, Inc.
    Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
  • Patent number: 5292741
    Abstract: Macrocyclic compounds of general Structure I: ##STR1## Wherein M is C or N are angiotensin II receptor (A-II) antagonists useful in the treatment of certain cardiovascular dysfunctions and ocular hypertension.
    Type: Grant
    Filed: August 18, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. deLaszlo, Tomasz Glinka, Robert B. Nachbar, Eric E. Allen, Kristine Prendergast
  • Patent number: 5284854
    Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: February 8, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo E. J. Kennis, Jan Vandenberk, Jozef M. Boey
  • Patent number: 5268375
    Abstract: This invention relates to compounds of formula ##STR1## in which: R.sub.1 and R.sub.2 are similar or different and are each independently hydrogen or a group selected from CO.sub.2 N.dbd.C(NH.sub.2).sub.2, CONHNHCONH.sub.2, CONHNHCSNH.sub.2, C(OC.sub.2 H.sub.5).dbd.NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 H.sub.5, C(OC.sub.2 H.sub.5).dbd.NH or a nitrogen heterocycle; with the proviso that at least one of the substituents R.sub.1 or R.sub.2 is other than hydrogen;R.sub.3 is a hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl, a phenylalkyl, or a phenylalkenyl;R.sub.4 and R.sub.5 are each independently a C.sub.1 -C.sub.6 alkyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl or a phenylalkyl; orR.sub.4 and R.sub.5, bonded together, are either a group of the formula (CH.sub.2).sub.n or a group of the formula (CH.sub.2).sub.p Y (CH.sub.2).sub.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: December 7, 1993
    Assignee: Elf Sanofi
    Inventors: Claude Bernhart, Bernard Ferrari, Pierre Perreaut
  • Patent number: 5260298
    Abstract: Imidazotriazoloquinazoline compounds having the general formula ##STR1## wherein A together with the .alpha.-marked carbon atom and the .beta.-marked nitrogen atom is one of the groups ##STR2## cyano or CO.sub.2 R.sup.5, wherein R.sup.5 is H, alkyl, cycloalkyl, trifluoromethyl or alkoxymethyl; and R.sup.2, R.sup.3 and R.sup.4 independently are H, hydroxy, halogen, CN, alkyl, alkenyl, alkynyl, trifluoromethyl, alkoxy, dialkylaminoalkoxy, aralkoxy, aryloxy which may be substituted, acyclic amino group, or NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 independently are H or alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, antipsychotics, antiemetics, or in improving the cognitive function of the brain of mammals, or as benzodiazepine antagonsists.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: November 9, 1993
    Assignee: Novo Nordisk A/S
    Inventor: Holger C. Hansen
  • Patent number: 5232915
    Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: August 3, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier