KR890006244A - Ll- e33288 항종양제의 이황 유사물과 그 제조 방법 및 이용 - Google Patents
Ll- e33288 항종양제의 이황 유사물과 그 제조 방법 및 이용 Download PDFInfo
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- KR890006244A KR890006244A KR1019880014245A KR880014245A KR890006244A KR 890006244 A KR890006244 A KR 890006244A KR 1019880014245 A KR1019880014245 A KR 1019880014245A KR 880014245 A KR880014245 A KR 880014245A KR 890006244 A KR890006244 A KR 890006244A
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- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
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- C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
- A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
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- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- C—CHEMISTRY; METALLURGY
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- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/20—Carbocyclic rings
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Abstract
내용 없음
Description
제1도는 LL-E33288r2-Ⅰ의 자외선 스펙트럼이다.
제2도는 LL-E33288r2-Ⅰ의 핵자기 공명 스펙트럼이다.
제Ⅲ도는 LL-E33288r2-Ⅰ의 적외선 스펙트럼이다.
제Ⅳ도는 LL-E33288r2-Ⅰ의 질량 스펙트럼이다.
제Ⅴ도는 LL-E33288r2-Ⅰ의 핵자기 공명 스펙트럼이다.
제Ⅵ도는 LL-E33288r2-Ⅰ의 질량 스펙트럼이다.
본 내용은 요부 건이므로 전문 내용을 수록하지 않음
Claims (10)
- 하기 a)-d)를 갖는 항종양제 LL-E33288r2-Ⅰ:a)제1도에 보여진 바와같은 자외선 스펙트럼; b)제2도에 보여진 바와같은 핵자기공명 스펙트럼; c)제Ⅲ도에 보여진 바와 같은 적외선 스펙트럼; 및 d) 제Ⅳ도에 보여진 바와같은 질량 스펙트럼.
- 항종양제 LL-E33288r2-Ⅰ-Br
- 하기 일반식의 항생물질 CL-1724-1577E,CL-1577D,CL-1577B,CL-1577A,PD 115028,PD114759, FR-900406, FR-900405, BBm-1675, LL-E33288 a₁-Br, a₁-Ⅰ,a₂-Br a₂-Ⅰ,a₃-Br, a₃-Ⅰ,a₃-Br ,a₃- I, a₄-Br, β₁-Br, β₁- I,β<SB<2>/SB>I ,₩1Br, r₁Ⅰ,∂1-I 의 치환 이황화물 유사물;X는 요오드 또는 브롬이고; Sp는 직체 또는 측쇄이가(C₁-C₁8)라디칼; 이가 아릴 또는 헤테로아릴 라디칼, 이가(C₁-C₁8)시클로아킬 또는 헤테로시클로알킬 라디칼, 이가 (C₁-C₁8)아릴알킬 헤테로 아릴알킬 라디칼, 이가 (C₁-C₁8)시클로알킬알킬 또는 헤테로시클로 알킬알킬 라디칼, 또는 이가 (C₁-C₁8)불포화아킬 라디칼이며; Q는 수소, 할로겐, 아미노, 알킬아미노, 디알킬아미노, 피페리디노, 피롤리디노, 피페라지노, 카르복실, 카르복스알데히드; 저급 알콕시, 히드록시, 티올, 저급 알킬디카르복실, -CONHNH₂-NHCONHNH₂,-CSNHNH₂-NHCSNHNH₂또는 -ONH₂이다; (단, Sp가 에틸리덴일때, Q가 수소이면 안된다.)
- LL-E33288r₁-Ⅰ의 이황화에틸 유사물.
- 제Ⅵ도에 보여진 바와같은 질량 스펙트럼과 제Ⅴ도에 보여진 바와같은 핵자기 공명 스펙트럼을 갖는 LL-E33288r₁-Ⅰ의 Ⅰ-메틸-1 프로필 이황화물 유사물.
- LL-E33288r₁-Ⅰ의 Ⅰ-메틸-Ⅰ-프로필 이황화물 유사물.
- 제3항에 있어서, 헤테로 아릴알킬 라디칼이 7-아미노--4-메틸-쿠마린인 화합물.
- 하기의 삼황화알킬 항생물질을 1-48시간동안 -10℃내지 -30℃, 아세토니트릴내에서 적적히 치환된 메르캅탄과 반응시키는 것을 포함하는, 하기 일반식의 항생물질 CL-1724-1577E,CL-1577D,CL-1577B,CL-1577A,PD 115028,PD114759, FR-900406, FR-900405, BBm-1675, LL-E33288 Br ,a₃- I, a₄-Br, β₁-Br, β₁- I,β<SB<2>/SB>I ,₩1Br, r₁Ⅰ,∂1-I 의 치환 이황화물 유사물을 제조하는 방법.X는 요오드 또는 브롬이고; Sp는 직쇄 또는 측쇄이가(C₁-C18)라디칼; 이가 아릴 또는 헤테로아릴 라디칼, 이가(C₁-C18)시클로알킬 또는 헤테로시클로알킬 라디칼, 이가(C₁-C18)아릴알킬 헤테로 아릴알킬 라디칼, 이가 (C₁-C18)시클로알킬알킬 똔든 헤테로시클로 알킬알킬 라디칼, 또는 이가 (C₁-C18)불포화 알킬 라디칼이며; Q는 수소, 할로겐, 아미노, 알킬아미노, 디알킬아미노, 피페리디노, 피롤리디노, 리페라지노, 카르복실, 카르복스알데히디; 저급 알콕시, 히드록시, 티올, 저급 알킬디카르복실 - CONHNH₂-NHCONHNH₂-CSNHNH₂또는 -ONH₂이다; (단, Sp가 에틸리덴일때, Q가 수소이면 안된다.)
- 하기 일반식의 CL-1724-1577E,CL-1577D,CL-1577B,CL-1577A,PD 115028,PD114759, FR-900406, FR-900405, BBm-1675, LL-E33288 Br ,a₃- I, a₄-Br, β₁-Br, β₁- I,β<SB<2>/SB>I ,₩1Br, r₁Ⅰ,∂1-I 의 치환 이황화물 유사물로부터 선택된 화합물 향균적으로 효과적인 양을 온혈 동물에게 투여하는 것을 포함하는 온혈동물의 세균 감염의 치료방법;X는 요오드 또는 브롬이고; Sp는 직쇄 또는 측쇄이가(C₁-C18)라디칼; 이가 아릴 또는 헤테로아릴 라디칼, 이가(C₁-C18)시클로알킬 또는 헤테로시클로알킬 라디칼, 이가(C₁-C18)아릴알킬 헤테로 아릴알킬 라디칼, 이가 (C₁-C18)시클로알킬알킬 똔든 헤테로시클로 알킬알킬 라디칼, 또는 이가 (C₁-C18)불포화 알킬 라디칼이며; Q는 수소, 할로겐, 아미노, 알킬아미노, 디알킬아미노, 피페리디노, 피롤리디노, 리페라지노, 카르복실, 카르복스알데히디; 저급 알콕시, 히드록시, 티올, 저급 알킬디카르복실 - CONHNH₂-NHCONHNH₂-CSNHNH₂또는 -ONH₂이다; (단, Sp가 에틸리덴일때, Q가 수소이면 안된다.)
- 하기 일반식의 CL-1724-1577E,CL-1577D,CL-1577B,CL-1577A,PD 115028,PD114759, FR-900406, FR-900405, BBm-1675, LL-E33288 Br ,a₃- I, a₄-Br, β₁-Br, β₁- I,β<SB<2>/SB>I ,₩1Br, r₁Ⅰ,∂1-I 의 치환 이호아화물 유사물로부터 선택된 화합물의 종양학적(oncolytic)양을 포유 동물에게 투여하는 것을 포함하는, 포유동물의 종양의 성장 저지 방법.X는 요오드 또는 브롬이고; Sp는 직쇄 또는 측쇄이가(C₁-C18)라디칼; 이가 아릴 또는 헤테로아릴 라디칼, 이가(C₁-C18)시클로알킬 또는 헤테로시클로알킬 라디칼, 이가(C₁-C18)아릴알킬 헤테로 아릴알킬 라디칼, 이가 (C₁-C18)시클로알킬알킬 똔든 헤테로시클로 알킬알킬 라디칼, 또는 이가 (C₁-C18)불포화 알킬 라디칼이며; Q는 수소, 할로겐, 아미노, 알킬아미노, 디알킬아미노, 피페리디노, 피롤리디노, 리페라지노, 카르복실, 카르복스알데히디; 저급 알콕시, 히드록시, 티올, 저급 알킬디카르복실 - CONHNH₂-NHCONHNH₂-CSNHNH₂또는 -ONH₂로부터 선택된 기이다.; (단, Sp가 에틸리덴일때, Q가 수소이면 안된다.)※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11494087A | 1987-10-30 | 1987-10-30 | |
US114,940 | 1987-10-30 | ||
US07/114,940 | 1987-10-30 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR890006244A true KR890006244A (ko) | 1989-06-12 |
KR970011385B1 KR970011385B1 (ko) | 1997-07-10 |
Family
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880014246A KR0133130B1 (ko) | 1987-10-30 | 1988-10-30 | 메틸트리티오 항종양제의 표적형태인 약제-담체 결합제와 그 제조방법 |
KR1019880014245A KR970011385B1 (ko) | 1987-10-30 | 1988-10-30 | Ll-e33288 항종양제의 이황 유사물과 그 제조 방법 및 이용 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019880014246A KR0133130B1 (ko) | 1987-10-30 | 1988-10-30 | 메틸트리티오 항종양제의 표적형태인 약제-담체 결합제와 그 제조방법 |
Country Status (19)
Country | Link |
---|---|
EP (2) | EP0313874B1 (ko) |
JP (2) | JP2820256B2 (ko) |
KR (2) | KR0133130B1 (ko) |
AR (1) | AR246083A1 (ko) |
AT (2) | ATE112172T1 (ko) |
AU (2) | AU612714B2 (ko) |
BR (1) | BR1100939A (ko) |
CA (1) | CA1321582C (ko) |
DE (2) | DE3889063T2 (ko) |
DK (2) | DK602488A (ko) |
ES (2) | ES2061586T3 (ko) |
FI (2) | FI95204C (ko) |
HK (2) | HK131897A (ko) |
IE (2) | IE65053B1 (ko) |
IL (2) | IL87947A (ko) |
NO (2) | NO176480C (ko) |
NZ (2) | NZ226727A (ko) |
PT (2) | PT88882B (ko) |
ZA (2) | ZA888123B (ko) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5079233A (en) * | 1987-01-30 | 1992-01-07 | American Cyanamid Company | N-acyl derivatives of the LL-E33288 antitumor antibiotics, composition and methods for using the same |
US5606040A (en) * | 1987-10-30 | 1997-02-25 | American Cyanamid Company | Antitumor and antibacterial substituted disulfide derivatives prepared from compounds possessing a methyl-trithio group |
IL115770A (en) * | 1989-04-14 | 1999-03-12 | American Cyanamid Co | Substituted disulfides of formula q-sp-ss-w their preparation and use for inhibiting the growth of tumours and for treating bacterial infections |
GB9007384D0 (en) * | 1990-04-02 | 1990-05-30 | Duncan Ruth | Coupling between polymers and other organic molecular entities utilising thiol-specific reactive groups |
US5712374A (en) * | 1995-06-07 | 1998-01-27 | American Cyanamid Company | Method for the preparation of substantiallly monomeric calicheamicin derivative/carrier conjugates |
US5714586A (en) * | 1995-06-07 | 1998-02-03 | American Cyanamid Company | Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates |
US20040009535A1 (en) | 1998-11-27 | 2004-01-15 | Celltech R&D, Inc. | Compositions and methods for increasing bone mineralization |
PT2261335T (pt) | 1998-11-27 | 2017-09-08 | Ucb Pharma Sa | Composições e métodos para aumentar a mineralização óssea |
NZ511705A (en) * | 2001-05-14 | 2004-03-26 | Horticulture & Food Res Inst | Methods and rapid immunoassay device for detecting progesterone and other steroids |
MEP2808A (xx) | 2003-06-16 | 2010-02-10 | Celltech R & D Inc | Antitijela specifična za sklerositin i metode za povećanje mineralizacije kostiju |
US8841092B2 (en) * | 2006-08-30 | 2014-09-23 | Wisconsin Alumni Research Foundation | Reversible natural product glycosyltransferase-catalyzed reactions, compounds and related methods |
KR100979928B1 (ko) * | 2008-07-16 | 2010-09-03 | 한주학 | 수직축형 부력풍차 |
SI3066074T1 (sl) * | 2013-11-04 | 2020-03-31 | Pfizer Inc. | Intermediati in postopki za sintetizacijo derivatov kaliheamicina |
EP3573995A1 (en) * | 2017-01-24 | 2019-12-04 | Pfizer Inc. | Calicheamicin derivatives and antibody drug conjugates thereof |
EP3924387A2 (en) * | 2019-02-15 | 2021-12-22 | University Of Southern California | Lym-1 and lym-2 antibody compositions and improved car constructs |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2430943A1 (fr) * | 1978-07-13 | 1980-02-08 | Toyo Jozo Kk | Nouveaux derives disulfures |
DE3175151D1 (en) * | 1980-05-21 | 1986-09-25 | Teijin Ltd | Reactive polymer and process for the preparation thereof |
US4530835A (en) * | 1983-07-08 | 1985-07-23 | Warner-Lambert Company | CL-1577 Antibiotic compounds and their production |
CA1314245C (en) * | 1984-05-23 | 1993-03-09 | Franz Jansen | Process for the preparation of conjugates in which a monovalent carboxylic ionophore is associated by means of a covalent bond with a macromolecule, which are useful as immunotoxin potentiators |
DE3588213T2 (de) * | 1984-11-16 | 1999-09-30 | American Cyanamid Co | Antitumorale Antibiotika (Komplex LL-E-33288) |
EP0330874A3 (en) * | 1988-02-29 | 1989-10-18 | American Cyanamid Company | Antibacterial and antitumor agents LL-E33288 epsilon-I and LL-E33288-epsilonBr, with processes and intermediates for producing said agents |
EP0342341A3 (en) * | 1988-05-17 | 1991-07-24 | American Cyanamid Company | Process for producing antitumor antibiotic ll-e33288gamma2 |
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1988
- 1988-10-03 DE DE3889063T patent/DE3889063T2/de not_active Expired - Lifetime
- 1988-10-03 EP EP88116339A patent/EP0313874B1/en not_active Expired - Lifetime
- 1988-10-03 ES ES88116339T patent/ES2061586T3/es not_active Expired - Lifetime
- 1988-10-03 ES ES88116338T patent/ES2059464T3/es not_active Expired - Lifetime
- 1988-10-03 EP EP88116338A patent/EP0313873B1/en not_active Expired - Lifetime
- 1988-10-03 AT AT88116338T patent/ATE112172T1/de not_active IP Right Cessation
- 1988-10-03 AT AT88116339T patent/ATE104309T1/de not_active IP Right Cessation
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