JP3645283B2 - リソゾーム酵素開裂性抗腫瘍剤結合体 - Google Patents
リソゾーム酵素開裂性抗腫瘍剤結合体 Download PDFInfo
- Publication number
- JP3645283B2 JP3645283B2 JP10138994A JP10138994A JP3645283B2 JP 3645283 B2 JP3645283 B2 JP 3645283B2 JP 10138994 A JP10138994 A JP 10138994A JP 10138994 A JP10138994 A JP 10138994A JP 3645283 B2 JP3645283 B2 JP 3645283B2
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- compound
- doxorubicin
- group
- phenylalanyl
- 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.)
- Expired - Lifetime
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- 0 C[C@](C1[C@](C*)O)C=CCN(CC2)C1C2(C(C#I#C)N(*)c1c2)c1cc([C@@](*)(CC(CN(C1)CC3)[C@@](*)[C@@]1(C)N)C(C)=C3c1c(CC=C)cccc1)c2OC Chemical compound C[C@](C1[C@](C*)O)C=CCN(CC2)C1C2(C(C#I#C)N(*)c1c2)c1cc([C@@](*)(CC(CN(C1)CC3)[C@@](*)[C@@]1(C)N)C(C)=C3c1c(CC=C)cccc1)c2OC 0.000 description 4
- SYMBFFPUBJAOMH-UHFFFAOYSA-N CNC(OCc(cc1)ccc1NC)=O Chemical compound CNC(OCc(cc1)ccc1NC)=O SYMBFFPUBJAOMH-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/062,366 US6214345B1 (en) | 1993-05-14 | 1993-05-14 | Lysosomal enzyme-cleavable antitumor drug conjugates |
US062366 | 1993-05-14 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH0770175A JPH0770175A (ja) | 1995-03-14 |
JP3645283B2 true JP3645283B2 (ja) | 2005-05-11 |
Family
ID=22042014
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP10138994A Expired - Lifetime JP3645283B2 (ja) | 1993-05-14 | 1994-05-16 | リソゾーム酵素開裂性抗腫瘍剤結合体 |
Country Status (18)
Families Citing this family (653)
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CA2162759A1 (en) * | 1994-11-17 | 1996-05-18 | Kenji Tsujihara | Baccatin derivatives and processes for preparing the same |
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ES2195036T3 (es) * | 1995-12-22 | 2003-12-01 | Bristol Myers Squibb Co | Conectores de hidrazona ramificados. |
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US6368598B1 (en) | 1996-09-16 | 2002-04-09 | Jcrt Radiation Oncology Support Services, Inc. | Drug complex for treatment of metastatic prostate cancer |
AU739028B2 (en) * | 1996-09-27 | 2001-10-04 | Bristol-Myers Squibb Company | Hydrolyzable prodrugs for delivery of anticancer drugs to metastatic cells |
DE19640207A1 (de) * | 1996-09-30 | 1998-04-02 | Bayer Ag | Glycokonjugate von modifizierten Camptothecin-Derivaten (A- oder B-Ring-Verknüpfung) |
ATE210673T1 (de) * | 1996-09-30 | 2001-12-15 | Bayer Ag | Glycokonjugate von modifizierten camptothecin- derivaten (20-o-verknüpfung) |
US5980883A (en) * | 1996-10-02 | 1999-11-09 | Kuraray Co., Ltd. | Polymer gel for medical use |
JP2001505194A (ja) | 1996-11-05 | 2001-04-17 | ブリストル―マイヤーズ・スクイブ・カンパニー | 分枝ペプチド・リンカー |
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US6545125B1 (en) * | 1997-11-18 | 2003-04-08 | Chugai Seiyaku Kabushiki Kaisha | Compounds with antitumor activity |
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EP0624377B1 (en) | 2002-01-23 |
RU94016384A (ru) | 1996-11-10 |
FI116038B (fi) | 2005-09-15 |
CN1100426A (zh) | 1995-03-22 |
MX9403570A (es) | 1995-01-31 |
NO941819L (no) | 1994-11-15 |
HU224351B1 (hu) | 2005-08-29 |
FI942237A0 (fi) | 1994-05-13 |
HU9401507D0 (en) | 1994-09-28 |
CN1117760C (zh) | 2003-08-13 |
ATE212236T1 (de) | 2002-02-15 |
EP0624377A2 (en) | 1994-11-17 |
ES2170755T3 (es) | 2002-08-16 |
CA2123363A1 (en) | 1994-11-15 |
NZ260512A (en) | 1996-09-25 |
CZ118794A3 (en) | 1994-11-16 |
HUT66485A (en) | 1994-11-28 |
JPH0770175A (ja) | 1995-03-14 |
DK0624377T3 (da) | 2002-05-06 |
NO941819D0 (no) | 1994-05-13 |
AU687795B2 (en) | 1998-03-05 |
NO315162B1 (no) | 2003-07-21 |
CA2123363C (en) | 2005-04-12 |
AU6302694A (en) | 1994-11-17 |
FI942237A (fi) | 1994-11-15 |
DE69429689T2 (de) | 2002-10-17 |
US6214345B1 (en) | 2001-04-10 |
DE69429689D1 (de) | 2002-03-14 |
PT624377E (pt) | 2002-07-31 |
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