KR870011129A - 디스타마이신 a 동족체 및 이의 제조방법 - Google Patents
디스타마이신 a 동족체 및 이의 제조방법 Download PDFInfo
- Publication number
- KR870011129A KR870011129A KR870004929A KR870004929A KR870011129A KR 870011129 A KR870011129 A KR 870011129A KR 870004929 A KR870004929 A KR 870004929A KR 870004929 A KR870004929 A KR 870004929A KR 870011129 A KR870011129 A KR 870011129A
- Authority
- KR
- South Korea
- Prior art keywords
- carboxamido
- pyrrole
- methyl
- compound
- unsubstituted
- Prior art date
- Legal status (The legal status 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 status listed.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Cephalosporin Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Description
Claims (9)
- 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.상기 식에서,n은 2,3 또는 4이고;및 Het-(여기서, Het는 피롤을 제외한 5원 또는 6원 헤테로모노사이클릭 환이다)으로부터 선택한 2가 라디칼이며, 이 라디칼은 C1-C6알킬, C1-C6알콕시, 시아노 및 트리플루오로메틸로부터 선택한 하나 이상의 치환제로 치환되거나 비치환되며;R1및 R2중의 하나는 수소이고, 다른 하나는 a)그룹(여기서, R3는 할로겐원자로 치환되거나 비치환된 C1-C6알킬; 페닐; 또는 사이클로헥실이다)또는 b) 그룹-CO-(CH2)m-R4(여기서, m은 0,1,2 또는 3이고, R4는 수소, 할로겐, 하이드록시, 아지리디닐 또는 옥시라닐이다)이거나, R1및 R2는 동일하고, 둘다 수소, 또는 할로겐, 하이드록시 또는 C1-C6알콕시로 치환되거나 비치환된 C1-C6알킬그룹이다.
- 제 1 항에 있어서, n이 3이고 ; A가및 그룹-Het-〔여기서, -Het-는 산소, 황 및 질소로부터 선택한 1개 또는 2개의 헤테로원자를 함유하고 C1-C6알킬로 치환되거나 비치환된 5원 또는 6원 헤테로모노사이클릭 환(단, 피롤은 제외)이다〕으로부터 선택한 2가 라디칼이며;그룹는 (i)(여기서, R3는 비치환되거나, 할로-치환된 C1-C6알킬이다) 또는(ii)〔여기서 R1′및 R2′는 동일하고, 각각 할로-치환된 C1-C6알킬이다)〕인 일반식 (Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
- 제 2 항에 있어서, 5원 또는 6원 헤테로모노 사이클릭 환이 티오펜, 티아졸, 피리딘, 이소옥사졸, 푸란. 트리아졸, 이미다졸 또는 1-메틸-이미다졸인 화합물.
- 염산염 형태의,β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-(N′-메틸-N′-니트로소우레이도벤젠)-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-(N′-(2-클로로에틸)-N′-니트로소우레이도벤젠)-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-N,N-비스(2-클로로에틸)아미노티오펜-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘;β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔4-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘, 및 β-〔1-메틸-4-〔1-메틸-4-〔1-메틸-4-〔3-N,N-비스(2-클로로에틸)아미노벤젠-1-카복스아미도〕피헤-2-카복스아미도〕피롤-2-카복스아미도〕피롤-2-카복스아미도〕프로피온아미딘으로 이루어진 그룹 중에서 선택한 화합물.
- 일반식(Ⅱ)의 화합물을 일반식(Ⅲ)의 화합물과 반응시키고, 경우에 따라 일반식(Ⅰ)의 화합물을 염화하거나 염으로부터 유리 화합물을 수득하고/하거나, 경우에 따라, 일반식(Ⅰ)의 이성체 혼합물을 단일이성체로 분리시킴을 특징으로 하여 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 염을 제조하는 방법.상기 식에서,n은 2,3 또는 4이고 ;A는및 Het-(여기서, Het는 피롤을 제외한 5원 또는 6원 헤테로모노사이클릭 환이다)으로부터 선택한 2가 라디칼이며, 이 라디칼은 C1-C6알킬, C1-C6알콕시, 시아노 및 트리플루오로메틸로부터 선택한 하나 이상의 치환제로 치환되거나 비치환되고 ;R1및 R2중의 하나는 수소이고, 다른 하나는 a) 그룹(여기서, R3는 할로겐원자로 치환되거나 비치환된 C1-C6알킬;페닐;또는 사이클로헥실이다)또는 b) 그룹--CO-(CH2)m-R4(여기서, m은 0,1,2 또는 3이고, R4는 수소, 할로겐, 하이드록시, 아지리디닐 또는 옥시라닐이다)이거나, R1및 R2는 동일하고, 둘다 수소, 또는 할로겐, 하이드록시 또는 C1-C6알콕시로 치환되거나 비치환된 C1-C6알킬그룹이며 ;X 는 하이드록시 또는 이탈그룹이다.
- 활성 성분으로서 제 1 항에 따르는 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 염과 , 약제학적으로 허용되는 담체 및/ 또는 희석제를 합유하는 약제학적 조성물.
- 항종양제 및 항바이러스제로서 사용하기 위한 제 1 항에 따르는 일반식(Ⅰ)의 화합물.
- 항종양제 및 항바이러스제로서 사용하기 위한 제 6 항에 따르는 약제학적 조성물.
- 항종양제 및 항바이러스제로서의 활성을 갖는 제 6 항에 따르는 약제학적 조성물을 제조하기 위한 제 1 항에 따르는 일반식(Ⅰ)의 화합물의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB868612218A GB8612218D0 (en) | 1986-05-20 | 1986-05-20 | Site specific alkylating agents |
GB8612218 | 1986-05-20 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR870011129A true KR870011129A (ko) | 1987-12-21 |
KR950011408B1 KR950011408B1 (ko) | 1995-10-04 |
Family
ID=10598117
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019870004929A Expired - Fee Related KR950011408B1 (ko) | 1986-05-20 | 1987-05-19 | 디스타마이신 a 동족체의 제조방법 |
Country Status (27)
Country | Link |
---|---|
US (1) | US5017599A (ko) |
EP (1) | EP0246868B1 (ko) |
JP (1) | JPH0623193B2 (ko) |
KR (1) | KR950011408B1 (ko) |
AT (1) | ATE80617T1 (ko) |
AU (1) | AU597659B2 (ko) |
BG (1) | BG60531B2 (ko) |
BR (1) | BR1101017A (ko) |
CA (1) | CA1314551C (ko) |
CS (1) | CS413791A3 (ko) |
DE (1) | DE3781716T2 (ko) |
DK (1) | DK254587A (ko) |
ES (1) | ES2046202T3 (ko) |
FI (1) | FI86543C (ko) |
GB (1) | GB8612218D0 (ko) |
GR (1) | GR3006163T3 (ko) |
HK (1) | HK31993A (ko) |
HU (1) | HU201336B (ko) |
IE (1) | IE60198B1 (ko) |
IL (1) | IL82553A (ko) |
MX (1) | MX9203122A (ko) |
NZ (1) | NZ220361A (ko) |
PT (1) | PT84896B (ko) |
SG (1) | SG3793G (ko) |
SU (1) | SU1528316A3 (ko) |
UA (1) | UA5928A1 (ko) |
ZA (1) | ZA873593B (ko) |
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CN85103908A (zh) * | 1985-07-16 | 1986-11-05 | 法米塔利·卡洛·埃尔巴有限公司 | 制备4′-表多克索红菌素的新方法 |
GB8906709D0 (en) * | 1989-03-23 | 1989-05-10 | Creighton Andrew M | Acryloyl substituted pyrrole derivatives |
IT1262921B (it) * | 1992-01-10 | 1996-07-22 | Federico Arcamone | Agenti antitumorali analoghi di oligopeptidi pirrol-amidinici retroversi processi di preparazione e prodotti farmaceutici che li contengono |
IT1271456B (it) * | 1993-03-01 | 1997-05-28 | Menarini Farma Ind | Composti pirrol-amidinici, e loro sali farmaceuticamente accettabili, processi di preparazione e composizioni farmaceutiche che li contengono |
GB9403909D0 (en) * | 1994-03-01 | 1994-04-20 | Erba Carlo Spa | Ureido derivatives of naphthalenephosphonic acids and process for their preparation |
GB9416005D0 (en) * | 1994-08-08 | 1994-09-28 | Erba Carlo Spa | Peptidic compounds analogous to distamycin a and process for their preparation |
US5821258A (en) * | 1994-12-27 | 1998-10-13 | Mitsui Chemicals, Inc. | Phenylbenzimidazole derivatives |
EP0750913A3 (en) * | 1995-06-30 | 1997-11-05 | Takeda Chemical Industries, Ltd. | Disaccharide containing freeze-dried preparation for pharmaceutical use |
GB9514993D0 (en) * | 1995-07-21 | 1995-09-20 | Pharmacia Spa | Site specific phenyl nitrogen mustards |
US5808087A (en) | 1995-11-29 | 1998-09-15 | Mitsui Chemicals, Inc. | Sulfonium salts of pyrrolylbenzimidazoles |
JP2000503999A (ja) * | 1996-02-02 | 2000-04-04 | フアルマシア・エ・アツプジヨン・エツセ・ピー・アー | ジスタマイシン誘導体、その調製方法、および抗腫瘍および抗ウイルス剤としてのその使用 |
US6090947A (en) * | 1996-02-26 | 2000-07-18 | California Institute Of Technology | Method for the synthesis of pyrrole and imidazole carboxamides on a solid support |
US6143901A (en) * | 1996-07-31 | 2000-11-07 | Genesoft, Inc. | Complex formation between dsDNA and pyrrole imidazole polyamides |
US6506906B1 (en) | 1996-02-26 | 2003-01-14 | California Institute Of Technology | Preparation and use of bifunctional molecules having DNA sequence binding specificity |
US6555692B1 (en) | 1996-02-26 | 2003-04-29 | California Institute Of Technology | Preparation and use of bifunctional molecules having DNA sequence binding specificity |
EP0968186A1 (en) | 1996-02-26 | 2000-01-05 | California Institute Of Technology | Improved polyamides for binding in the minor groove of double stranded dna |
US6635417B1 (en) | 1996-07-31 | 2003-10-21 | California Institute Of Technology | Complex formation between DSDNA and oligomer of cyclic heterocycles |
AU6757698A (en) | 1996-02-26 | 1998-10-30 | California Institute Of Technology | Stereochemical control of the dna binding affinity, sequence specificity, and orientation-preference of chiral hairpin polyamides in the minor groove |
GB9610079D0 (en) * | 1996-05-14 | 1996-07-17 | Pharmacia Spa | Distamycin deriratives process for preparing them and their use as antitumor and antiviral agents |
GB9615692D0 (en) * | 1996-07-25 | 1996-09-04 | Pharmacia Spa | Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents |
US5998140A (en) * | 1996-07-31 | 1999-12-07 | The Scripps Research Institute | Complex formation between dsDNA and oligomer of cyclic heterocycles |
GB9623522D0 (en) * | 1996-11-11 | 1997-01-08 | Pharmacia & Upjohn Spa | Benzoheterocycle distamycin derivatives process for preparing them and their use as antitumour and antiviral agents |
US20040072889A1 (en) * | 1997-04-21 | 2004-04-15 | Pharmacia Corporation | Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia |
GB9806692D0 (en) | 1998-03-27 | 1998-05-27 | Pharmacia & Upjohn Spa | Benzoheterocyclic distamycin derivatives, process for preparing them and their use as antitumour agents |
GB9816652D0 (en) * | 1998-07-30 | 1998-09-30 | Pharmacia & Upjohn Spa | Sulfurated distamycin derivatives process for preparing them and their use as antitumor agents |
GB9816653D0 (en) * | 1998-07-30 | 1998-09-30 | Pharmacia & Upjohn Spa | Oxidised sulfurated distamycin derivatives process for preparing them and their use as antitumor agents |
KR20010063274A (ko) * | 1999-12-22 | 2001-07-09 | 성재갑 | 〔1-{〔1-(1,3-벤조디옥솔-5-일메틸-1h-이미다졸-5-일〕메틸}-4-(1-나프틸)-1h-피롤-3-일〕(4-메틸-1-피페라지닐)메타논의 약학적 조성물 |
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JP2003529609A (ja) | 2000-03-16 | 2003-10-07 | ジーンソフト インコーポレイティッド | 核酸結合部分を含む荷電した化合物およびその利用法 |
GB0011059D0 (en) | 2000-05-08 | 2000-06-28 | Pharmacia & Upjohn Spa | Use of substituted acryloyl distamycin derivatives in the treatment of tumours associated with high levels of glutathione |
GB0015447D0 (en) | 2000-06-23 | 2000-08-16 | Pharmacia & Upjohn Spa | Combined therapy against tumors comprising substituted acryloyl derivates and alkylating agents |
GB0015446D0 (en) | 2000-06-23 | 2000-08-16 | Pharmacia & Upjohn Spa | Combined therapy against tumors comprising substituted acryloyl distamycin derivates,taxanes and/or antimetabolites |
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US6969592B2 (en) | 2001-09-26 | 2005-11-29 | Pharmacia Italia S.P.A. | Method for predicting the sensitivity to chemotherapy |
ATE425753T1 (de) | 2002-08-02 | 2009-04-15 | Genesoft Pharmaceuticals Inc | Biaryl-verbindungen mit antiinfektiver wirkung |
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GB202114032D0 (en) * | 2021-09-30 | 2021-11-17 | Univ Strathclyde | Antivirals |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
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FR86210E (ko) * | 1963-04-04 | 1966-03-23 | ||
FR141F (ko) * | 1963-07-26 | |||
BR6461040D0 (pt) * | 1963-07-26 | 1973-08-02 | Farmaceutici Italia | Processo para preparar novos derivados de pirrol |
DE1795539A1 (de) * | 1963-07-26 | 1972-01-13 | Farmaceutici Italia | Verfahren zur Herstellung von neuen Pyrrolderivaten und ihren Salzen |
NL130086C (ko) * | 1964-07-14 | 1970-06-15 | ||
CN85103908A (zh) * | 1985-07-16 | 1986-11-05 | 法米塔利·卡洛·埃尔巴有限公司 | 制备4′-表多克索红菌素的新方法 |
GB8517922D0 (en) * | 1985-07-16 | 1985-08-21 | Erba Farmitalia | Carboxamido derivatives |
-
1986
- 1986-05-20 GB GB868612218A patent/GB8612218D0/en active Pending
-
1987
- 1987-05-14 HU HU872168A patent/HU201336B/hu not_active IP Right Cessation
- 1987-05-18 AU AU73163/87A patent/AU597659B2/en not_active Ceased
- 1987-05-18 IL IL82553A patent/IL82553A/xx unknown
- 1987-05-18 UA UA4202591A patent/UA5928A1/uk unknown
- 1987-05-18 IE IE129287A patent/IE60198B1/en not_active IP Right Cessation
- 1987-05-18 FI FI872173A patent/FI86543C/fi not_active IP Right Cessation
- 1987-05-18 SU SU874202591A patent/SU1528316A3/ru active
- 1987-05-19 NZ NZ220361A patent/NZ220361A/en unknown
- 1987-05-19 CA CA000537338A patent/CA1314551C/en not_active Expired - Fee Related
- 1987-05-19 AT AT87304442T patent/ATE80617T1/de not_active IP Right Cessation
- 1987-05-19 KR KR1019870004929A patent/KR950011408B1/ko not_active Expired - Fee Related
- 1987-05-19 ZA ZA873593A patent/ZA873593B/xx unknown
- 1987-05-19 PT PT84896A patent/PT84896B/pt not_active IP Right Cessation
- 1987-05-19 DK DK254587A patent/DK254587A/da not_active Application Discontinuation
- 1987-05-19 DE DE8787304442T patent/DE3781716T2/de not_active Expired - Fee Related
- 1987-05-19 JP JP62122375A patent/JPH0623193B2/ja not_active Expired - Lifetime
- 1987-05-19 EP EP87304442A patent/EP0246868B1/en not_active Expired - Lifetime
- 1987-05-19 ES ES198787304442T patent/ES2046202T3/es not_active Expired - Lifetime
-
1990
- 1990-02-21 US US07/485,847 patent/US5017599A/en not_active Expired - Fee Related
-
1991
- 1991-12-30 CS CS914137A patent/CS413791A3/cs unknown
-
1992
- 1992-06-22 MX MX9203122A patent/MX9203122A/es unknown
- 1992-11-05 GR GR920402483T patent/GR3006163T3/el unknown
-
1993
- 1993-01-08 SG SG37/93A patent/SG3793G/en unknown
- 1993-04-01 HK HK319/93A patent/HK31993A/en not_active IP Right Cessation
-
1994
- 1994-02-22 BG BG098518A patent/BG60531B2/bg unknown
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1997
- 1997-05-14 BR BR1101017-7A patent/BR1101017A/pt active IP Right Grant
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