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DK0763529T3 - Uracilderivater og antitumorvirkningspotentiator og antitumormiddel indeholdende samme - Google Patents

Uracilderivater og antitumorvirkningspotentiator og antitumormiddel indeholdende samme

Info

Publication number
DK0763529T3
DK0763529T3 DK96907693T DK96907693T DK0763529T3 DK 0763529 T3 DK0763529 T3 DK 0763529T3 DK 96907693 T DK96907693 T DK 96907693T DK 96907693 T DK96907693 T DK 96907693T DK 0763529 T3 DK0763529 T3 DK 0763529T3
Authority
DK
Denmark
Prior art keywords
group
lower alkyl
substituted
hydrogen atom
alkyl group
Prior art date
Application number
DK96907693T
Other languages
English (en)
Inventor
Shingo Yano
Yukio Tada
Hideki Kazuno
Tsutomu Sato
Junichi Yamashita
Norihiko Suzuki
Tomohiro Emura
Masakazu Fukushima
Tetsuji Asao
Original Assignee
Taiho Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Taiho Pharmaceutical Co Ltd filed Critical Taiho Pharmaceutical Co Ltd
Application granted granted Critical
Publication of DK0763529T3 publication Critical patent/DK0763529T3/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Organic Insulating Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)
DK96907693T 1995-03-29 1996-03-28 Uracilderivater og antitumorvirkningspotentiator og antitumormiddel indeholdende samme DK0763529T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP7166795 1995-03-29
PCT/JP1996/000828 WO1996030346A1 (en) 1995-03-29 1996-03-28 Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same

Publications (1)

Publication Number Publication Date
DK0763529T3 true DK0763529T3 (da) 2003-11-10

Family

ID=13467185

Family Applications (1)

Application Number Title Priority Date Filing Date
DK96907693T DK0763529T3 (da) 1995-03-29 1996-03-28 Uracilderivater og antitumorvirkningspotentiator og antitumormiddel indeholdende samme

Country Status (14)

Country Link
US (3) US5744475A (da)
EP (1) EP0763529B1 (da)
JP (1) JP3088757B2 (da)
KR (1) KR100424934B1 (da)
AT (1) ATE245631T1 (da)
AU (1) AU681321B2 (da)
CA (1) CA2191340C (da)
DE (1) DE69629156T2 (da)
DK (1) DK0763529T3 (da)
ES (1) ES2203683T3 (da)
HU (1) HU227726B1 (da)
NO (1) NO308033B1 (da)
PT (1) PT763529E (da)
WO (1) WO1996030346A1 (da)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
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EP0763529B1 (en) 1995-03-29 2003-07-23 Taiho Pharmaceutical Company Limited Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same
PT884051E (pt) * 1996-09-24 2005-03-31 Taiho Pharmaceutical Co Ltd Inibidores de metasteses cancerosas contendo derivados de uracilo
US6235776B1 (en) 1998-11-12 2001-05-22 Cell Pathways, Inc. Method for treating a patient with neoplasia by treatment with a paclitaxel derivative
US6235782B1 (en) 1998-11-12 2001-05-22 Rifat Pamukcu Method for treating a patient with neoplasia by treatment with a platinum coordination complex
JP4049477B2 (ja) * 1999-03-23 2008-02-20 大鵬薬品工業株式会社 副作用軽減剤
WO2000073281A1 (de) * 1999-05-31 2000-12-07 Discovery Technologies Ag Antiviral und antitumoral wirksame thymin-derivate
JP4110347B2 (ja) * 1999-11-05 2008-07-02 大鵬薬品工業株式会社 抗hiv剤
US6906067B2 (en) * 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
ES2363766T3 (es) 2002-08-21 2011-08-16 Albert Einstein College Of Medicine Of Yeshiva University Inhibidores de nucleosidasas y fosforilasas de nucleosidos.
US20070275988A1 (en) * 2003-09-05 2007-11-29 Schramm Vern L Transition state structure and inhibitors of thymidine phosphorylases
US7622580B2 (en) * 2004-08-13 2009-11-24 Xerox Corporation Colorant compounds
US7211131B2 (en) * 2004-08-13 2007-05-01 Xerox Corporation Phase change inks
US7799783B2 (en) 2005-01-26 2010-09-21 Taiho Pharmaceutical Co., Ltd. Method of administrating an anticancer drug containing α, α, α-trifluorothymidine and thymidine phosphorylase inhibitor
PT1849470T (pt) * 2005-01-26 2017-09-22 Taiho Pharmaceutical Co Ltd Fármaco anticancro contendo alfa, alfa, alfa-trifluorotimidina e inibidor da timidina-fosforilase
JP5058156B2 (ja) * 2006-04-13 2012-10-24 大鵬薬品工業株式会社 炎症性腸疾患治療薬
US8148381B2 (en) * 2006-06-30 2012-04-03 Taiho Pharmaceutical Co., Ltd. Potentiator of radiation therapy
AU2008310734B2 (en) 2007-10-10 2014-06-05 Parion Sciences, Inc. Delivering osmolytes by nasal cannula
TWI435725B (zh) * 2007-10-11 2014-05-01 Taiho Pharmaceutical Co Ltd The use of a uracil compound for a prophylactic or therapeutic composition for the preparation of cystitis and hepatitis
TWI429439B (zh) * 2007-10-11 2014-03-11 Taiho Pharmaceutical Co Ltd And a therapeutic agent for inflammatory bowel disease using a uracil derivative as an active ingredient
PL2295414T3 (pl) * 2008-06-03 2013-02-28 Taiho Pharmaceutical Co Ltd Związek uracylu o aktywności hamującej ludzką trifosfatazę deoksyurydyny lub jego sól
NZ590757A (en) 2008-07-01 2014-05-30 Univ Gifu Novel imino derivative, process for production of the same, and pesticide comprising the same
JP2010202591A (ja) * 2009-03-04 2010-09-16 Hokkaido Univ 増殖性疾患の内用放射線治療剤
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
CN103732213A (zh) 2011-06-07 2014-04-16 帕里昂科学公司 治疗方法
TWI503122B (zh) 2012-02-15 2015-10-11 Taiho Pharmaceutical Co Ltd Oral administration of pharmaceutical compositions
TWI526210B (zh) * 2012-02-15 2016-03-21 Taiho Pharmaceutical Co Ltd Oral pharmaceutical composition
DK2979700T3 (da) 2013-03-27 2019-01-21 Taiho Pharmaceutical Co Ltd Antitumormiddel, der indbefatter en lav irinotecanhydrochloridhydrat
NZ712584A (en) 2013-03-27 2018-03-23 Taiho Pharmaceutical Co Ltd Antitumor agent including irinotecan hydrochloride hydrate
TWI595879B (zh) 2013-05-17 2017-08-21 Taiho Pharmaceutical Co Ltd Prediction of therapeutic effect in patients with colorectal cancer with TK1 protein hyperactivity
PT3012255T (pt) * 2013-06-17 2021-11-30 Taiho Pharmaceutical Co Ltd Forma de cristal estável de cloridrato de tipiracilo e método de cristalização para o mesmo
WO2015034032A1 (ja) 2013-09-06 2015-03-12 大鵬薬品工業株式会社 抗腫瘍剤及び抗腫瘍効果増強剤
CN104744443A (zh) * 2013-12-26 2015-07-01 江苏豪森药业股份有限公司 嘧啶二酮类化合物盐酸盐新晶型及其制备方法
CN106333952A (zh) * 2014-02-19 2017-01-18 齐鲁制药有限公司 一种胸苷磷酸化酶抑制剂的结晶形式及其制备方法
CN104945384B (zh) * 2014-03-25 2018-10-16 江苏豪森药业集团有限公司 5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1h,3h)-嘧啶二酮或其盐的制备方法
CN104945385A (zh) * 2014-03-31 2015-09-30 江苏豪森药业股份有限公司 Tipracil盐酸盐的新晶型及其制备方法
NZ725067A (en) 2014-04-04 2019-01-25 Taiho Pharmaceutical Co Ltd Anti-tumor agent containing anti-tumor platinum complex, and anti-tumor effect enhancer
CN106317028A (zh) * 2015-11-03 2017-01-11 江苏悦兴药业有限公司 抗肿瘤药物盐酸替比拉西的制备方法及其关键中间体
CN105906573A (zh) * 2015-12-23 2016-08-31 嘉实(湖南)医药科技有限公司 一种替吡嘧啶中间体的制备方法
AU2017205531B2 (en) 2016-01-08 2021-05-13 Les Laboratoires Servier Anti-tumor agent containing immunomodulator and anti-tumor effect potentiator
JP6882205B2 (ja) 2016-02-05 2021-06-02 大鵬薬品工業株式会社 重度腎機能障害を有する癌患者に対する治療方法
US11654157B2 (en) 2017-01-09 2023-05-23 Shuttle Pharmaceuticals, Inc. Methods and compositions for cancer therapies that include delivery of halogenated thymidines and thymidine phosphorylase inhibitors in combination with radiation
CN106831607A (zh) * 2017-02-14 2017-06-13 山东创新药物研发有限公司 一种6‑氯甲基尿嘧啶的合成方法
CN106892902A (zh) * 2017-03-01 2017-06-27 国药心制药有限公司 一种盐酸替匹嘧啶及其中间体6‑氯甲基尿嘧啶的合成方法
TWI671072B (zh) 2017-03-17 2019-09-11 法商施維雅藥廠 曲氟尿苷(trifluridine)/替匹拉希(tipiracil)鹽酸鹽、抗腫瘤鉑錯合物及免疫檢查點調節子之間的新穎組合
WO2019002407A1 (en) 2017-06-28 2019-01-03 Amneal Pharmaceuticals Company Gmbh PROCESS FOR THE PREPARATION OF TIPIRACIL CHLORHYDRATE
US11149026B2 (en) * 2017-09-07 2021-10-19 Msn Laboratories Private Limited, R&D Center Solid state forms of 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4-(1H,3H)-dione hydrochloride and their processes for the preparation thereof
ES2987509T3 (es) * 2017-11-02 2024-11-15 Procos Spa Proceso para la preparación de la forma cristalina III de clorhidrato de tipiracilo
US10866219B2 (en) 2017-12-22 2020-12-15 Taiho Pharmaceutical Co., Ltd. Method for detecting trifluridine- and/or tipiracil-related substance
WO2019124544A1 (ja) 2017-12-22 2019-06-27 大鵬薬品工業株式会社 トリフルリジン及び/又はチピラシル由来の類縁物質の検出方法
WO2019135405A1 (ja) 2018-01-05 2019-07-11 大鵬薬品工業株式会社 トリフルリジン由来の類縁物質の検出方法
US10816517B2 (en) 2018-01-05 2020-10-27 Taiho Pharmaceutical Co., Ltd. Method for detecting trifluridine-related substance by high-performance liquid chromatography
WO2019171394A1 (en) 2018-03-03 2019-09-12 Natco Pharma Limited Stable pharmaceutical compositions comprising trifluridine and tipiracil hydrochloride
WO2020121334A1 (en) 2018-12-15 2020-06-18 Natco Pharma Limited An improved process for the preparation of tipiracil hydrochloride and intermediates thereof
CN109796441B (zh) * 2019-02-19 2020-10-16 北京民康百草医药科技有限公司 一种盐酸替比嘧啶的杂质a的制备方法
CN114057697B (zh) * 2020-08-07 2025-02-25 鲁南制药集团股份有限公司 一种替吡嘧啶中间体的制备方法
AR127893A1 (es) 2021-12-10 2024-03-06 Servier Lab Terapia del cáncer dirigida a egfr

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US4820712A (en) * 1986-08-27 1989-04-11 Stichting Katholieke Universiteit Sparsomycin (SC-RS) compounds having antitumor activity, a process for their preparation and pharmaceutical compositions containing sparsomycin (SC-RS) compounds
JPH0751567B2 (ja) * 1989-09-29 1995-06-05 三菱化学株式会社 6―置換アシクロピリミジンヌクレオシド誘導体及び該誘導体を有効成分とする抗ウイルス剤
KR0155168B1 (ko) * 1989-09-29 1998-11-16 미우라 아끼라 6-치환된 아시클로피리미딘 뉴클레오시드 유도체 및 이를 활성성분으로 함유하는 항비루스제
JPH075570B2 (ja) * 1990-03-29 1995-01-25 三菱化学株式会社 ピリミジンヌクレオシド誘導体及び該誘導体を有効成分とする抗ウイルス剤
CA2039039C (en) * 1990-03-29 2001-05-15 Tadashi Miyasaka Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient
EP0763529B1 (en) * 1995-03-29 2003-07-23 Taiho Pharmaceutical Company Limited Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same

Also Published As

Publication number Publication date
HUP9603280A3 (en) 2001-04-28
WO1996030346A1 (en) 1996-10-03
HUP9603280A2 (hu) 1998-01-28
ATE245631T1 (de) 2003-08-15
US5744475A (en) 1998-04-28
CA2191340C (en) 2001-04-17
EP0763529B1 (en) 2003-07-23
ES2203683T3 (es) 2004-04-16
EP0763529A1 (en) 1997-03-19
DE69629156T2 (de) 2004-05-06
NO308033B1 (no) 2000-07-10
HU227726B1 (en) 2012-01-30
JP3088757B2 (ja) 2000-09-18
US6294535B1 (en) 2001-09-25
CA2191340A1 (en) 1996-10-03
NO965083L (no) 1997-01-27
AU5121696A (en) 1996-10-16
US6159969A (en) 2000-12-12
KR970703326A (ko) 1997-07-03
KR100424934B1 (ko) 2004-07-27
AU681321B2 (en) 1997-08-21
PT763529E (pt) 2003-12-31
EP0763529A4 (en) 1998-07-08
DE69629156D1 (de) 2003-08-28
NO965083D0 (no) 1996-11-28

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