The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/142)
  • Patent number: 6867209
    Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 ?, and each of i and j is independently 0 or 1; as Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring
    Type: Grant
    Filed: May 19, 2000
    Date of Patent: March 15, 2005
    Assignee: Scios, Inc.
    Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
  • Patent number: 6849622
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 1, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Publication number: 20040248892
    Abstract: The present invention relates to a method for making an indolopyrrolocarbazole compound of the general formula [I], where the method includes the step of reacting a bisindolylmaleimide compound with an oxidizing agent in the presence of an oxygen containing gas at a temperature and for a time sufficient to yield the indolopyrrolocarbazole compound of the general formula [I]. Methods of making rebeccamycin analogs using the indolopyrrolocarbazole compound are also provided.
    Type: Application
    Filed: July 21, 2004
    Publication date: December 9, 2004
    Inventor: Jianji Wang
  • Patent number: 6730671
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 4, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Patent number: 6719926
    Abstract: A chromene compound which develops yellow to red color, a high color density and a little initial color and which, when used in combination with an existing photochromic compound that exhibits blue color so as to develop a neutral tint, maintains uniformity in the color tone at the time of developing color or fading color, or exhibits a very large color fading rate.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: April 13, 2004
    Assignee: Tokuyama Corporation
    Inventors: Junji Momoda, Shingo Matsuoka, Hironobu Nagou
  • Patent number: 6713473
    Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: March 30, 2004
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Naoyuki Nishikawa, Masaharu Sugai, Kozo Aoki, Makoto Suzuki, Akihiko Ikegawa, Kazunobu Takahashi, Fukuichi Ohsawa, Naomi Masuda, Nobukazu Kakui, Jiro Tanaka, Yuji Tabata, Kenji Asai
  • Publication number: 20040043965
    Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer.
    Type: Application
    Filed: August 20, 2002
    Publication date: March 4, 2004
    Inventors: Ling Jong, Wan-Ru Chao
  • Publication number: 20030166630
    Abstract: The present invention relates to new derivatives of amino acids and their use as medicaments.
    Type: Application
    Filed: October 31, 2002
    Publication date: September 4, 2003
    Inventors: Serge Auvin, Jeremiah Harnett, Pierre-Etienne Chabrier De Lassauniere
  • Patent number: 6608098
    Abstract: This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: August 19, 2003
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 6608057
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Patent number: 6586452
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: July 1, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
  • Publication number: 20030064984
    Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
    Type: Application
    Filed: May 31, 2002
    Publication date: April 3, 2003
    Applicant: MEDAREX, INC.
    Inventors: Howard P. Ng, Danny P. C. McGee, Guoxian Wu, Jimmie Moore, Zhihong Li, Sanjeev Gangwar, Oliver L. Saunders, Irina Astafieva
  • Publication number: 20030050304
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 25, 2002
    Publication date: March 13, 2003
    Inventors: William W. McWhorter, Valentina Badescu
  • Patent number: 6531598
    Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk
  • Patent number: 6525194
    Abstract: A chromene compound which develops yellow to red color, a high color density and a little initial color and which, when used in combination with an existing photochromic compound that exhibits blue color so as to develop a neutral tint, maintains uniformity in the color tone at the time of developing color or fading color, or exhibits a very large color fading rate.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: February 25, 2003
    Assignee: Tokuyama Corporation
    Inventors: Junji Momoda, Shingo Matsuoka, Hironobu Nagou
  • Patent number: 6514968
    Abstract: The present invention provides aminoalkoxy carbazole derivatives, and more specifically, provides compounds of formula (I) wherein R1, R2, R3, R4, R8 and R9 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: February 4, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventor: Ruth Elizabeth TenBrink
  • Publication number: 20020107278
    Abstract: Disclosed are compounds of Formula (I): 1
    Type: Application
    Filed: September 20, 2001
    Publication date: August 8, 2002
    Inventors: Kristine E. Frank, Brad A. Acker, Michael D. Ennis, Jed F. Fisher, Jian-min Fu, William W. McWhorter, Jeanette K. Morris, Donald Joseph Rogier, Eric Jon Jacobsen
  • Publication number: 20020061913
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 22, 2001
    Publication date: May 23, 2002
    Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
  • Patent number: 6294112
    Abstract: Red coloring hyperchromic compounds have the formula: where R1 is H, NR2R3, OR4, SR4 or R7 wherein R2 and R3 are alkyl or carbocyclic groups or together with the nitrogen to which they are attached form a heterocyclic ring; R4 is the same as R1 or is alkyl, perhaloallyl, aryl or heteroaryl; R7 is alkyl, haloalkyl, alkylthio, aryl, arylthio, heteroaryl, halogen, nitrile, carboxylate, ester, nitro, or a carbocyclic or heterocyclic ring fused to faces f, gh, i, j or k; and R5 is a cyclic aminoaryl group, an indolinoaryl group, a tricyclic nitrogen heterocycle, or an unsaturated cyclic aminoaryl group.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: September 25, 2001
    Assignee: James Robinson Limited
    Inventors: David A. Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6080859
    Abstract: Pyrroloindole derivatives having antimicrobial and antitumor activities and having a carbamoyloxy group represented by the following general formula (1), optical isomers thereof, and pharmacologically acceptable salts thereof; and intermediates for production thereof: ##STR1## where R.sup.1 is OH, or a pyrrolidinyl group; n is 1 or 2; R.sup.2 is a lower alkyl group of C.sub.1 -C.sub.4 ; X--Y or Y--X is CH.sub.2, CHOH, CH.sub.2 -CH.sub.2, O--CH.sub.2, or NMe--CH.sub.2 ; Z.sup.1 is Cl or Br; and Ar.sup.1 is ##STR2## wherein Z.sup.2 and Z.sup.3 are O or NH; m is 0 or an integer of 1 to 4; and Ar.sup.2 is any of the above groups a, b, c, and d.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: June 27, 2000
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasumichi Fukuda, Rumiko Shimazawa, Yasuo Oomori, Shiro Terashima
  • Patent number: 6077840
    Abstract: Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. ##STR1## wherein R.sup.1 represents alkyl or aralkyl; R.sup.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: June 20, 2000
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kenichi Kurihara, Rie Shinei, Yasushi Kurata, Yuji Tabata, Kiyoshi Tanabe, Tsuneo Okonogi
  • Patent number: 6040331
    Abstract: The invention provides novel benzindole derivatives, processes for producing them, as well as a neuroprotective agent, an agent to prevent or treat diseases involving the degeneration, retraction or death of neurons, and an analgesic, each containing the benzindole derivatives as an active ingredient.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: March 21, 2000
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Ichiro Yamamoto, Manabu Itoh, Masato Shimojo, Yasunobu Yumiya, Takafumi Mukaihira, Yasushige Akada
  • Patent number: 5972935
    Abstract: The invention relates to novel heterocyclic compounds of formula (I) or a salt or N-oxide thereof, in which R is a group of formulae (i), (ii) or (iii), where R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 akyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyle, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, NR.sup.9 CONR.sup.10 R.sup.11, NR.sup.10 SO.sub.2 R.sup.11, SO.sub.2 NR.sup.11 r.sup.11, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, ##STR1## (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, N.dbd.CNR.sup.9 NR.sup.10 R.sup.11, NR.sup.10 CO(CH.sub.2).sub.a NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, CONHNR.sup.10 R.sup.11, CR.
    Type: Grant
    Filed: April 24, 1998
    Date of Patent: October 26, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventor: Laramie Mary Gaster
  • Patent number: 5744607
    Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: April 28, 1998
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5728709
    Abstract: Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10, or OR.sup.11 ; R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 --; and when R.sup.1 is benzyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen. A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: March 17, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yoji Ikuina, Chikara Murakata, Yutaka Saitoh, Yukimasa Shiotsu, Takako Iida, Tatsuya Tamaoki, Kinya Yamashita, Shiro Akinaga
  • Patent number: 5723072
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: March 3, 1998
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5698141
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 16, 1997
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5691334
    Abstract: New and known 5-?(2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole derivatives, having immunomodulating activity and, represented by the general formula (I) and the pharmaceutically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: November 25, 1997
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Gianfederico Doria, AnnaMaria Isetta, Marcellino Tibolla, MariaChiara Fornasiero, Mario Ferrari, Domenico Trizio
  • Patent number: 5654298
    Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: August 5, 1997
    Assignee: Imperial Chemical Industries
    Inventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
  • Patent number: 5651923
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5641780
    Abstract: DC-89 derivatives represented by the formula ##STR1## wherein X represents CL or Br; R represents substituted or unsubstituted alkyl, substituted or unsubstituted aralkyl, COR.sup.1 or S.sub.2 OR.sup.7 ; and Y represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention exhibit excellent anti-tumor activity and are useful as anti-tumor agents.
    Type: Grant
    Filed: December 15, 1995
    Date of Patent: June 24, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
  • 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: 5639874
    Abstract: To sequence DNA automatically, DNA marked with near infrared fluorescent dyes are electrophoresed in a plurality of channels through a gel electrophoresis slab wherein the DNA samples are resolved in accordance with the size of DNA fragments in the gel electrophoresis slab into fluorescently marked DNA bands. The separated samples are scanned photoelectrically with a laser diode and a sensor, wherein the laser scans with scanning light at a scanning light frequency within the absorbance spectrum of said fluorescently marked DNA samples and light is sensed at the emission frequency of the marked DNA. The light is modulated from said laser at a predetermined modulation frequency and fluorescent light emitted by said DNA bands at said modulation frequency is detected, whereby background noise from the medium through which the light is transmitted is discriminated against.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: June 17, 1997
    Assignee: Li-Cor, Inc.
    Inventors: Lyle Richard Middendorf, Gabor Patonay
  • Patent number: 5541340
    Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 30, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5536721
    Abstract: The present invention relates to therapeutically active heterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: July 16, 1996
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Anders Kanstrup, Peter Faarup, Preben H. Olesen
  • Patent number: 5514700
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 7, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
  • Patent number: 5498727
    Abstract: The invention relates to a process for preparing a substituted 2-amino-benz[cd]indole of the Formula I: ##STR1## The nitro group of a substituted 1-nitro-8-cyano-naphthalene compound is reduced to an amine group to form a substituted 1-amino-8-cyano-naphthalene compound, which is cyclized to form the substituted 2-amino-benz[cd]indole. The reduction and cyclization may be effected in a one-pot procedure using a reducing agent such as stannous chloride, which generates an acid that cyclizes the reduction product. The syntheses of the 1-nitro-8-cyanonaphthalene compound and its precursors are also described.
    Type: Grant
    Filed: July 19, 1994
    Date of Patent: March 12, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, Cindy L. Palmer, Judy G. Deal
  • Patent number: 5470853
    Abstract: The present invention provides 4-amino-6-substituted-hexahydrobenz[cd]indoles which are useful in treating disease states which can be benefited by an alteration of 5-HT.sub.1.sbsb.A receptors.
    Type: Grant
    Filed: March 30, 1994
    Date of Patent: November 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: Michael E. Flaugh, Michael J. Martinelli
  • Patent number: 5462913
    Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## represents a metal ion equivalent or an ammonium ion, L and M represents oxygen and/or sulphur,R.sup.1 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl, which can be interrupted by hetero atoms, optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl or substituted hetaryloxyalkyl,R.sup.2 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or in each case optionally substituted phenyl or benzyl,R.sup.3, R.sup.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: October 31, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Christoph Erdelen, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Wilhelm Stendel
  • Patent number: 5424451
    Abstract: Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.
    Type: Grant
    Filed: January 4, 1994
    Date of Patent: June 13, 1995
    Assignee: Mediolanum Farmaceutici S.p.A.
    Inventors: Maria A. Alisi, Mario Brufani, Maria C. Cesta, Luigi Eieocamo, Gianluca Gostoli, Sperandina Lappa, Pier Giuseppe Pagella, Enrico Ferrari, Stefano Maiorana, Donata Marchesini
  • Patent number: 5380746
    Abstract: The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.
    Type: Grant
    Filed: March 9, 1993
    Date of Patent: January 10, 1995
    Assignee: Goedecke Aktiengesellschaft
    Inventors: Hubert Barth, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hans-Jurgen Betche, Reinhard Reck, Hartmut Osswald
  • Patent number: 5350762
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the various parameters R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, m and n are as defined in the specification, which show activities as a monoamine oxidase inhibitor demonstrating a utility for the treatment of depression, and activities as a cholinesterase inhibitor demonstrating a utility for the treatment of various memory dysfunctions such as Alzheimer's disease.
    Type: Grant
    Filed: March 8, 1993
    Date of Patent: September 27, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Larry Davis
  • Patent number: 5318967
    Abstract: The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl,the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: June 7, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5302593
    Abstract: Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: April 12, 1994
    Assignee: Mediolanum Farmaceutici S.p.A.
    Inventors: Maria A. Alisi, Mario Brufani, Maria C. Cesta, Luigi Filocamo, Gianluca Gostoli, Sperandina Lappa, Pier Giuseppe Pagella, Enrico Ferrari, Stefano Maiorana, Donata Marchesini
  • Patent number: 5302612
    Abstract: The present invention provides 4-amino-6-substituted-hexahydrobenz[cd]indoles which are useful in treating disease states which can be benefited by an alteration of 5-HT.sub.1A receptors.
    Type: Grant
    Filed: May 27, 1993
    Date of Patent: April 12, 1994
    Assignee: Eli Lilly and Company
    Inventors: Michael E. Flaugh, Michael J. Martinelli
  • Patent number: 5258383
    Abstract: DC-89 derivatives represented by the formula: ##STR1## wherein X represents hydrogen or CO.sub.2 CH.sub.3 ; and ##STR2## wherein Z represents Cl or Br; R represents hydrogen, CONR.sup.1 R.sup.2 (in which R.sup.1 and R.sup.2 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl) or ##STR3## (in which n represents an integer of 0 to 4; R.sup.3 represents CH.sub.2, ##STR4## oxygen, N--CH.sub.3, or N--CH.sub.2 CONR.sup.1 R.sup.2 in which R.sup.1 and R.sup.2 have the same significances as defined above); and W represents hydrogen or ##STR5## (in which W.sup.1 and W.sup.2 independently represent hydrogen or OR.sup.2 in which R.sup.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: November 2, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Katsushige Gomi
  • Patent number: 5252560
    Abstract: Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.
    Type: Grant
    Filed: June 29, 1992
    Date of Patent: October 12, 1993
    Assignee: Glaxo Inc.
    Inventors: Peter L. Myers, Andrew B. McElroy, Michael Gregson, Peter J. Brown, Howard G. Davies, David H. Drewry, Michael A. Foley
  • Patent number: 5248692
    Abstract: Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: September 28, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiromitsu Saito, Akira Asai, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi