KR960037682A - 축합 6환 화합물 및 그의 제조방법 - Google Patents
축합 6환 화합물 및 그의 제조방법 Download PDFInfo
- Publication number
- KR960037682A KR960037682A KR1019960010291A KR19960010291A KR960037682A KR 960037682 A KR960037682 A KR 960037682A KR 1019960010291 A KR1019960010291 A KR 1019960010291A KR 19960010291 A KR19960010291 A KR 19960010291A KR 960037682 A KR960037682 A KR 960037682A
- Authority
- KR
- South Korea
- Prior art keywords
- methanesulfonic acid
- rti
- protecting group
- compound
- methanesulfonate
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Abstract
본 발명은 식(2)로 표시되는 화합물을 메탄술폰산으로 처리한 후, 재결정하여 식(1)로 표시되는 화합물의 제조방법 및 이렇게 얻어진 화합물(1)을 개시한다.
본 화합물(1)은 흡습하지 않고, 여과성 및 용해성이 우수하고, 취급이 용이하다. 더욱이 본 발명의 제조방법에 따라 불필요한 이성체를 목적 이성체로 변환시킬 수 있고, 재결정함으로써 목적물을 쉽게 분리할 수 있다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 본 발명과 비교품의 흡수에 의한 중량변화를 나타내는 도면이다.
Claims (7)
- 다음 식(1)로 표시되는 캄프토테신 유도체의 메탄술폰산염 또는 그의 수화물.
- 다음 식(1)로 표시되는 캄프토테신 유도체의 메탄술폰산염 또는 그의 수화물과 약학적으로 허용되는 염을 함유하는 의약 조성물.
- 제2항에 있어서, 항종양 의약 조성물인 조성물.
- 다음 식(2)(식중, X는 메탄술폰산에 의해 제거될 수 있는 보호기를 나타낸다.)로 표시되는 화합물을 메탄술폰산으로 처리한 후, 재결정함을 특징으로 하는 다음 식(1)로 표시되는 캄프토테신 유도체의 메탄술폰산염의 제조방법.
- 다음 식(3)(식중, X는 메탄술폰산에 의해 제거될 수 있는 보호기를 나타낸다.)로 표시되는 화합물의 아미노기를 메탄술폰산에 의해 제거될 수 있는 보호기로 보호하고, 메탄술폰산으로 처리한 후, 재결정함을 특징으로 하는 다음 식(1)로 표시되는 캄프토테신 유도체의 메탄술폰산염의 제조방법.
- 제4항 또는 제5항에 있어서, 메탄술폰산에 의해 제거될 수 있는 보호기가 아세틸기인 것이 특징인 방법.
- 제4항, 제5항 또는 제16항에 있어서, 재결정에 사용되는 용매가 물과 알코올의 혼합 용매인 것이 특징인 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP83717/1995 | 1995-04-10 | ||
JP8371795 | 1995-04-10 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960037682A true KR960037682A (ko) | 1996-11-19 |
KR100400941B1 KR100400941B1 (ko) | 2003-12-24 |
Family
ID=13810270
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019960010291A KR100400941B1 (ko) | 1995-04-10 | 1996-04-04 | 축합6환화합물및그의제조방법 |
Country Status (13)
Country | Link |
---|---|
US (2) | US6504029B1 (ko) |
EP (1) | EP0737686B1 (ko) |
KR (1) | KR100400941B1 (ko) |
CN (1) | CN1050131C (ko) |
AT (1) | ATE181919T1 (ko) |
CA (1) | CA2173671A1 (ko) |
DE (1) | DE69603117T2 (ko) |
DK (1) | DK0737686T3 (ko) |
EA (1) | EA000036B1 (ko) |
ES (1) | ES2136338T3 (ko) |
GR (1) | GR3031400T3 (ko) |
NO (1) | NO314085B1 (ko) |
TW (1) | TW382630B (ko) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2273841T3 (es) | 2000-02-28 | 2007-05-16 | Pfizer Enterprises Sarl | Combinacion sinergica para el tratamiento de cancer colorrectal. |
US6545010B2 (en) | 2000-03-17 | 2003-04-08 | Aventis Pharma S.A. | Composition comprising camptothecin or a camptothecin derivative and a platin derivative for the treatment of cancer |
US6548488B2 (en) | 2000-03-17 | 2003-04-15 | Aventis Pharma S.A. | Composition comprising camptothecin or a camptothecin derivative and an alkylating agent for the treatment of cancer |
AR030207A1 (es) * | 2000-04-07 | 2003-08-13 | Daiichi Seiyaku Co | Composicion farmaceutica que contiene un derivado de camptotecina y procedimiento de preparacion de la misma |
US6486320B2 (en) | 2000-09-15 | 2002-11-26 | Aventis Pharma S.A. | Preparation of camptothecin and of its derivatives |
PL365685A1 (en) | 2000-10-27 | 2005-01-10 | Aventis Pharma S.A. | A combination comprising camptothecin and a stilbene derivative for the treatment of cancer |
WO2006069344A2 (en) | 2004-12-22 | 2006-06-29 | Rutgers, The State University Of New Jersey | Controlled release hydrogels |
US8410045B2 (en) | 2006-03-30 | 2013-04-02 | Drais Pharmaceuticals, Inc. | Camptothecin-peptide conjugates and pharmaceutical compositions containing the same |
US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
TW201031675A (en) | 2008-12-23 | 2010-09-01 | Pharmasset Inc | Synthesis of purine nucleosides |
US8551973B2 (en) | 2008-12-23 | 2013-10-08 | Gilead Pharmasset Llc | Nucleoside analogs |
AU2009329867B2 (en) | 2008-12-23 | 2015-01-29 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
HUE026235T2 (en) | 2010-03-31 | 2016-06-28 | Gilead Pharmasset Llc | Crystalline (S) -isopropyl 2 - (((S) - (((2R, 3R, 4R, 5R) -5- (2,4-dioxo-3,4-dihydropyrimidin-1 (2H) -IL) - 4-Fluoro-3-hydroxy-4-methyltetrahydrofuran-2-IL) methoxy) (phenoxy) phosphoryl) amino) propanoate |
US20140086975A1 (en) | 2010-10-15 | 2014-03-27 | Rutgers, The State University Of New Jersey | Hydrogel formulation for dermal and ocular delivery |
BR122021014365B1 (pt) | 2012-10-11 | 2022-07-05 | Daiichi Sankyo Company, Limited | Conjugado de anticorpo-fármaco, fármacos e composição farmacêutica compreendendo os mesmos, e uso |
WO2014061277A1 (ja) | 2012-10-19 | 2014-04-24 | 第一三共株式会社 | 親水性構造を含むリンカーで結合させた抗体-薬物コンジュゲート |
PL3088419T3 (pl) | 2013-12-25 | 2019-03-29 | Daiichi Sankyo Company, Limited | Koniugat lek-przeciwciało anty-trop2 |
CA2928794C (en) | 2014-01-31 | 2019-08-13 | Daiichi Sankyo Company, Limited | Anti-her2 antibody-drug conjugate |
KR102186027B1 (ko) | 2014-04-10 | 2020-12-03 | 다이이치 산쿄 유럽 게엠베하 | 항her3 항체-약물 콘주게이트 |
EP3130608B1 (en) | 2014-04-10 | 2019-09-04 | Daiichi Sankyo Co., Ltd. | (anti-her2 antibody)-drug conjugate |
WO2017002776A1 (ja) | 2015-06-29 | 2017-01-05 | 第一三共株式会社 | 抗体-薬物コンジュゲートの選択的製造方法 |
EP3552626A4 (en) | 2016-12-12 | 2020-06-10 | Daiichi Sankyo Company, Limited | ASSOCIATION OF AN ANTIBODY DRUG CONJUGATE AND AN IMMUNE CONTROL POINT INHIBITOR |
WO2018135501A1 (ja) | 2017-01-17 | 2018-07-26 | 第一三共株式会社 | 抗gpr20抗体及び抗gpr20抗体-薬物コンジュゲート |
TW202330036A (zh) | 2017-05-15 | 2023-08-01 | 日商第一三共股份有限公司 | 抗體-藥物結合物之製造方法 |
US11318212B2 (en) | 2017-08-31 | 2022-05-03 | Daiichi Sankyo Company, Limited | Method for producing antibody-drug conjugate |
AU2018327171B2 (en) | 2017-08-31 | 2023-03-09 | Daiichi Sankyo Company, Limited | Improved method for producing antibody-drug conjugate |
US20210187118A1 (en) | 2018-05-18 | 2021-06-24 | Daiichi Sankyo Co., Ltd. | Anti-muc1 antibody-drug conjugate |
CA3114137A1 (en) | 2018-09-26 | 2020-04-02 | Jiangsu Hengrui Medicine Co., Ltd. | Ligand-drug conjugate of exatecan analogue, preparation method therefor and application thereof |
AU2019351427A1 (en) | 2018-09-30 | 2021-04-15 | Changzhou Hansoh Pharmaceutical Co., Ltd. | Anti-B7H3 antibody-exatecan analog conjugate and medicinal use thereof |
JP7210770B2 (ja) | 2019-03-29 | 2023-01-23 | メドイミューン・リミテッド | 化合物及びその複合体 |
AU2020309570A1 (en) | 2019-07-10 | 2022-02-03 | Cybrexa 2, Inc. | Peptide conjugates of cytotoxins as therapeutics |
JP2022541747A (ja) | 2019-07-10 | 2022-09-27 | サイブレクサ 3,インコーポレイテッド | 治療薬としての微小管標的化剤のペプチドコンジュゲート |
KR20220113728A (ko) | 2019-12-12 | 2022-08-16 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 항 클라우딘 항체 약물 접합체 및 그 의약 용도 |
MX2022008474A (es) | 2020-01-22 | 2022-08-02 | Jiangsu Hengrui Medicine Co | Conjugado de anticuerpo anti-trop-2-analogo de exatecan y uso medico del mismo. |
CN115103691A (zh) | 2020-03-25 | 2022-09-23 | 江苏恒瑞医药股份有限公司 | 一种含抗体药物偶联物的药物组合物及其用途 |
WO2021190583A1 (zh) | 2020-03-25 | 2021-09-30 | 江苏恒瑞医药股份有限公司 | 抗psma抗体-依喜替康类似物偶联物及其医药用途 |
CA3175048A1 (en) | 2020-03-25 | 2021-09-30 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Preparation method for antibody medicament conjugate |
WO2023030364A1 (zh) * | 2021-09-01 | 2023-03-09 | 上海弼领生物技术有限公司 | 一种喜树碱类化合物、其制备方法和用途 |
Family Cites Families (9)
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JPS6087746A (ja) * | 1983-10-17 | 1985-05-17 | Hakubakumai Kk | 即席麺ないしは焼そば用蒸し麺の製造方法 |
US4939255A (en) * | 1987-06-24 | 1990-07-03 | Daiichi Pharmaceutical Co., Ltd. | Hexa-cyclic camptothecin derivatives |
US4943579A (en) * | 1987-10-06 | 1990-07-24 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Water soluble prodrugs of camptothecin |
US5004758A (en) * | 1987-12-01 | 1991-04-02 | Smithkline Beecham Corporation | Water soluble camptothecin analogs useful for inhibiting the growth of animal tumor cells |
JP3008226B2 (ja) * | 1991-01-16 | 2000-02-14 | 第一製薬株式会社 | 六環性化合物 |
US5658920A (en) * | 1991-01-16 | 1997-08-19 | Daiichi Pharmaceutical Co., Ltd. | Substituted 1H,12H-benz-[DE]pyrano[3',4':6,7] indolizino[1,2-B]quinoline-10,13(9H,15H)-dione compound |
JP3359955B2 (ja) * | 1992-07-16 | 2002-12-24 | 第一製薬株式会社 | 抗腫瘍剤 |
IS4152A (is) * | 1993-04-29 | 1994-10-30 | Glaxo Inc. | Vatnsuppleysanlegar Camptothecin afleiður og aðferð til framleiðslu þeirra |
GB9319944D0 (en) * | 1993-09-28 | 1993-11-17 | Erba Carlo Spa | Process for the preparation of 9-amino camptothecin |
-
1995
- 1995-07-13 US US08/501,933 patent/US6504029B1/en not_active Expired - Fee Related
- 1995-09-18 CN CN95116111A patent/CN1050131C/zh not_active Expired - Fee Related
-
1996
- 1996-04-04 KR KR1019960010291A patent/KR100400941B1/ko not_active IP Right Cessation
- 1996-04-09 EA EA199600018A patent/EA000036B1/ru not_active IP Right Cessation
- 1996-04-09 NO NO19961405A patent/NO314085B1/no unknown
- 1996-04-09 CA CA002173671A patent/CA2173671A1/en not_active Abandoned
- 1996-04-09 TW TW085104156A patent/TW382630B/zh not_active IP Right Cessation
- 1996-04-10 EP EP96105661A patent/EP0737686B1/en not_active Expired - Lifetime
- 1996-04-10 ES ES96105661T patent/ES2136338T3/es not_active Expired - Lifetime
- 1996-04-10 AT AT96105661T patent/ATE181919T1/de not_active IP Right Cessation
- 1996-04-10 DK DK96105661T patent/DK0737686T3/da active
- 1996-04-10 DE DE69603117T patent/DE69603117T2/de not_active Expired - Fee Related
-
1999
- 1999-09-30 GR GR990402491T patent/GR3031400T3/el unknown
-
2001
- 2001-06-11 US US09/876,945 patent/US6552197B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
DE69603117D1 (de) | 1999-08-12 |
EA000036B1 (ru) | 1998-02-26 |
ES2136338T3 (es) | 1999-11-16 |
DK0737686T3 (da) | 1999-11-22 |
EA199600018A2 (ru) | 1996-10-01 |
ATE181919T1 (de) | 1999-07-15 |
GR3031400T3 (en) | 2000-01-31 |
EA199600018A3 (ru) | 1997-03-31 |
US6504029B1 (en) | 2003-01-07 |
CA2173671A1 (en) | 1996-10-11 |
US20010034446A1 (en) | 2001-10-25 |
TW382630B (en) | 2000-02-21 |
AU5056696A (en) | 1996-10-24 |
EP0737686A1 (en) | 1996-10-16 |
KR100400941B1 (ko) | 2003-12-24 |
DE69603117T2 (de) | 1999-10-28 |
US6552197B2 (en) | 2003-04-22 |
CN1050131C (zh) | 2000-03-08 |
NO961405D0 (no) | 1996-04-09 |
AU692078B2 (en) | 1998-05-28 |
EP0737686B1 (en) | 1999-07-07 |
NO961405L (no) | 1996-10-11 |
CN1133290A (zh) | 1996-10-16 |
NO314085B1 (no) | 2003-01-27 |
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