The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/142)
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Patent number: 6867209Abstract: 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 ringType: GrantFiled: May 19, 2000Date of Patent: March 15, 2005Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 6849622Abstract: 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: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Publication number: 20040248892Abstract: 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: ApplicationFiled: July 21, 2004Publication date: December 9, 2004Inventor: Jianji Wang
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Patent number: 6730671Abstract: 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: GrantFiled: February 13, 2003Date of Patent: May 4, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6719926Abstract: 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: GrantFiled: February 19, 2002Date of Patent: April 13, 2004Assignee: Tokuyama CorporationInventors: Junji Momoda, Shingo Matsuoka, Hironobu Nagou
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Patent number: 6713473Abstract: 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: GrantFiled: February 19, 2002Date of Patent: March 30, 2004Assignee: 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
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Publication number: 20040043965Abstract: 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: ApplicationFiled: August 20, 2002Publication date: March 4, 2004Inventors: Ling Jong, Wan-Ru Chao
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Publication number: 20030166630Abstract: The present invention relates to new derivatives of amino acids and their use as medicaments.Type: ApplicationFiled: October 31, 2002Publication date: September 4, 2003Inventors: Serge Auvin, Jeremiah Harnett, Pierre-Etienne Chabrier De Lassauniere
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Patent number: 6608098Abstract: 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: GrantFiled: February 25, 2002Date of Patent: August 19, 2003Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 6608057Abstract: 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: GrantFiled: October 24, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: 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
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Publication number: 20030064984Abstract: 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: ApplicationFiled: May 31, 2002Publication date: April 3, 2003Applicant: MEDAREX, INC.Inventors: Howard P. Ng, Danny P. C. McGee, Guoxian Wu, Jimmie Moore, Zhihong Li, Sanjeev Gangwar, Oliver L. Saunders, Irina Astafieva
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Publication number: 20030050304Abstract: The present invention provides compounds of formula (I): 1Type: ApplicationFiled: June 25, 2002Publication date: March 13, 2003Inventors: William W. McWhorter, Valentina Badescu
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Patent number: 6531598Abstract: 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: GrantFiled: August 20, 2002Date of Patent: March 11, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk
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Patent number: 6525194Abstract: 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: GrantFiled: May 24, 2002Date of Patent: February 25, 2003Assignee: Tokuyama CorporationInventors: Junji Momoda, Shingo Matsuoka, Hironobu Nagou
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Patent number: 6514968Abstract: 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: GrantFiled: August 31, 2000Date of Patent: February 4, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Ruth Elizabeth TenBrink
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Publication number: 20020107278Abstract: Disclosed are compounds of Formula (I): 1Type: ApplicationFiled: September 20, 2001Publication date: August 8, 2002Inventors: 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
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Publication number: 20020061913Abstract: The present invention provides compounds of formula (I): 1Type: ApplicationFiled: June 22, 2001Publication date: May 23, 2002Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
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Patent number: 6294112Abstract: 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: GrantFiled: December 16, 1999Date of Patent: September 25, 2001Assignee: James Robinson LimitedInventors: David A. Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Patent number: 6159995Abstract: 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: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6080859Abstract: 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: GrantFiled: July 19, 1999Date of Patent: June 27, 2000Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Rumiko Shimazawa, Yasuo Oomori, Shiro Terashima
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Patent number: 6077840Abstract: 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: GrantFiled: June 18, 1999Date of Patent: June 20, 2000Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kenichi Kurihara, Rie Shinei, Yasushi Kurata, Yuji Tabata, Kiyoshi Tanabe, Tsuneo Okonogi
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Patent number: 6040331Abstract: 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: GrantFiled: January 30, 1998Date of Patent: March 21, 2000Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ichiro Yamamoto, Manabu Itoh, Masato Shimojo, Yasunobu Yumiya, Takafumi Mukaihira, Yasushige Akada
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Patent number: 5972935Abstract: 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: GrantFiled: April 24, 1998Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 5744607Abstract: 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: GrantFiled: October 18, 1996Date of Patent: April 28, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
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Patent number: 5728709Abstract: 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: GrantFiled: November 8, 1996Date of Patent: March 17, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ikuina, Chikara Murakata, Yutaka Saitoh, Yukimasa Shiotsu, Takako Iida, Tatsuya Tamaoki, Kinya Yamashita, Shiro Akinaga
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Patent number: 5723072Abstract: 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: GrantFiled: March 18, 1997Date of Patent: March 3, 1998Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5698141Abstract: 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: GrantFiled: January 16, 1997Date of Patent: December 16, 1997Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5691334Abstract: 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: GrantFiled: August 21, 1995Date of Patent: November 25, 1997Assignee: Pharmacia & Upjohn S.p.A.Inventors: Gianfederico Doria, AnnaMaria Isetta, Marcellino Tibolla, MariaChiara Fornasiero, Mario Ferrari, Domenico Trizio
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Patent number: 5654298Abstract: 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: GrantFiled: April 16, 1991Date of Patent: August 5, 1997Assignee: Imperial Chemical IndustriesInventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
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Patent number: 5651923Abstract: 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: GrantFiled: December 12, 1995Date of Patent: July 29, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5641780Abstract: 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: GrantFiled: December 15, 1995Date of Patent: June 24, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Nobuyoshi Amishiro, Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Akihiko Okamoto, Katsushige Gomi
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Patent number: 5639756Abstract: 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: GrantFiled: October 28, 1994Date of Patent: June 17, 1997Assignee: Adir et CompagnieInventors: Vera Alekseevna Anisimova, Margarita Valentinovna Levchenko, Tatyana Borisovna Korochina, Alexander Alexeyevich Spasov, Sergei Gennadyevich Kovalev, Galina Petrovna Dudchenko
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Patent number: 5639874Abstract: 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: GrantFiled: June 28, 1994Date of Patent: June 17, 1997Assignee: Li-Cor, Inc.Inventors: Lyle Richard Middendorf, Gabor Patonay
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Patent number: 5541340Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 30, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard L. Hamer, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang
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Patent number: 5536721Abstract: 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: GrantFiled: March 14, 1995Date of Patent: July 16, 1996Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Anders Kanstrup, Peter Faarup, Preben H. Olesen
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Patent number: 5514700Abstract: 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: GrantFiled: June 7, 1995Date of Patent: May 7, 1996Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Gerard J. O'Malley, Michael C. Merriman, Mark G. Palermo
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Patent number: 5498727Abstract: 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: GrantFiled: July 19, 1994Date of Patent: March 12, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, Cindy L. Palmer, Judy G. Deal
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Patent number: 5470853Abstract: 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: GrantFiled: March 30, 1994Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: Michael E. Flaugh, Michael J. Martinelli
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Patent number: 5462913Abstract: 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: GrantFiled: October 21, 1993Date of Patent: October 31, 1995Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Christoph Erdelen, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5424451Abstract: 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: GrantFiled: January 4, 1994Date of Patent: June 13, 1995Assignee: 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
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Patent number: 5380746Abstract: 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: GrantFiled: March 9, 1993Date of Patent: January 10, 1995Assignee: Goedecke AktiengesellschaftInventors: Hubert Barth, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hans-Jurgen Betche, Reinhard Reck, Hartmut Osswald
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Patent number: 5350762Abstract: 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: GrantFiled: March 8, 1993Date of Patent: September 27, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Lawrence L. Martin, Larry Davis
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Patent number: 5318967Abstract: 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: GrantFiled: September 3, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
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Patent number: 5314889Abstract: 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: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5302593Abstract: 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: GrantFiled: June 23, 1993Date of Patent: April 12, 1994Assignee: 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
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Patent number: 5302612Abstract: 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: GrantFiled: May 27, 1993Date of Patent: April 12, 1994Assignee: Eli Lilly and CompanyInventors: Michael E. Flaugh, Michael J. Martinelli
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Patent number: 5258383Abstract: 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: GrantFiled: June 25, 1992Date of Patent: November 2, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Satoru Nagamura, Hiromitsu Saito, Eiji Kobayashi, Katsushige Gomi
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Patent number: 5252560Abstract: 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: GrantFiled: June 29, 1992Date of Patent: October 12, 1993Assignee: Glaxo Inc.Inventors: Peter L. Myers, Andrew B. McElroy, Michael Gregson, Peter J. Brown, Howard G. Davies, David H. Drewry, Michael A. Foley
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Patent number: 5248692Abstract: 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: GrantFiled: March 1, 1993Date of Patent: September 28, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiromitsu Saito, Akira Asai, Satoru Nagamura, Eiji Kobayashi, Katsushige Gomi