JP2015518473A - ツブリシン誘導体およびその複合体の製造方法 - Google Patents
ツブリシン誘導体およびその複合体の製造方法 Download PDFInfo
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- JP2015518473A JP2015518473A JP2015503659A JP2015503659A JP2015518473A JP 2015518473 A JP2015518473 A JP 2015518473A JP 2015503659 A JP2015503659 A JP 2015503659A JP 2015503659 A JP2015503659 A JP 2015503659A JP 2015518473 A JP2015518473 A JP 2015518473A
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- 0 *[C@@]1C(C2)C=CCC2C1 Chemical compound *[C@@]1C(C2)C=CCC2C1 0.000 description 18
- ZFONFELJYOQMNL-UHFFFAOYSA-N CCCC(OCNC)=O Chemical compound CCCC(OCNC)=O ZFONFELJYOQMNL-UHFFFAOYSA-N 0.000 description 1
- STCYGGMJLKXDAN-UHFFFAOYSA-N CCCCOCNO Chemical compound CCCCOCNO STCYGGMJLKXDAN-UHFFFAOYSA-N 0.000 description 1
- DXUHGVJOVNEWTM-BDAKNGLRSA-N CCC[C@@H](C)C[C@]1(C)SC[IH]N1 Chemical compound CCC[C@@H](C)C[C@]1(C)SC[IH]N1 DXUHGVJOVNEWTM-BDAKNGLRSA-N 0.000 description 1
- WKJOQYHMXRVQDK-UHFFFAOYSA-N CN(C)CC(N)=O Chemical compound CN(C)CC(N)=O WKJOQYHMXRVQDK-UHFFFAOYSA-N 0.000 description 1
- NBFVMBGIPAJCJQ-UHFFFAOYSA-N CN(CCCC1)C1C(N)=O Chemical compound CN(CCCC1)C1C(N)=O NBFVMBGIPAJCJQ-UHFFFAOYSA-N 0.000 description 1
- ACSBWMJRTPCPOB-UHFFFAOYSA-N CNCCCCCC(N)=O Chemical compound CNCCCCCC(N)=O ACSBWMJRTPCPOB-UHFFFAOYSA-N 0.000 description 1
- OQZVMPVNJOEVEG-ONEGZZNKSA-N CS/C=C(\N)/[O]=C Chemical compound CS/C=C(\N)/[O]=C OQZVMPVNJOEVEG-ONEGZZNKSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C241/00—Preparation of compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
- C07C241/02—Preparation of hydrazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/70—Sulfur atoms
- C07D213/71—Sulfur atoms to which a second hetero atom is attached
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/76—Nitrogen atoms to which a second hetero atom is attached
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/188—Preparation; Treatments not provided for in C07F7/20 by reactions involving the formation of Si-O linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261617386P | 2012-03-29 | 2012-03-29 | |
| US61/617,386 | 2012-03-29 | ||
| US201261684450P | 2012-08-17 | 2012-08-17 | |
| US61/684,450 | 2012-08-17 | ||
| US201361771451P | 2013-03-01 | 2013-03-01 | |
| US61/771,451 | 2013-03-01 | ||
| US201361794720P | 2013-03-15 | 2013-03-15 | |
| US61/794,720 | 2013-03-15 | ||
| PCT/US2013/034672 WO2013149185A1 (en) | 2012-03-29 | 2013-03-29 | Processes for preparing tubulysin derivatives and conjugates thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015518473A true JP2015518473A (ja) | 2015-07-02 |
| JP2015518473A5 JP2015518473A5 (https=) | 2016-05-19 |
Family
ID=49261307
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503659A Pending JP2015518473A (ja) | 2012-03-29 | 2013-03-29 | ツブリシン誘導体およびその複合体の製造方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US20140080175A1 (https=) |
| EP (1) | EP2831059B1 (https=) |
| JP (1) | JP2015518473A (https=) |
| CA (1) | CA2868494A1 (https=) |
| WO (1) | WO2013149185A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017533887A (ja) * | 2014-09-17 | 2017-11-16 | ジェネンテック, インコーポレイテッド | ピロロベンゾジアゼピン類及びその抗体ジスルフィドコンジュゲート |
| JP2022516427A (ja) * | 2018-12-21 | 2022-02-28 | レゲネロン ファーマシューティカルス,インコーポレーテッド | ツブリシン及びタンパク質-ツブリシンコンジュゲート |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5149620B2 (ja) | 2004-07-23 | 2013-02-20 | エンドサイト,インコーポレイテッド | 2価リンカーおよびその結合体 |
| CN104127878A (zh) | 2007-03-14 | 2014-11-05 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| BRPI0812970A2 (pt) | 2007-06-25 | 2019-09-24 | Endocyte Inc | conjugados contendo espaçadores hidrofílicos |
| US10080805B2 (en) | 2012-02-24 | 2018-09-25 | Purdue Research Foundation | Cholecystokinin B receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| EP2908818A4 (en) | 2012-10-16 | 2016-07-13 | Endocyte Inc | CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE |
| BR112015011118B1 (pt) | 2012-11-15 | 2022-12-13 | Endocyte, Inc | Conjugado; composição farmacêutica; e uso de um conjugado |
| US20140249315A1 (en) * | 2013-03-01 | 2014-09-04 | Endocyte, Inc. | Processes for preparing tubulysins |
| WO2015113760A1 (en) * | 2014-01-28 | 2015-08-06 | Tube Pharmaceuticals Gmbh | Cytotoxic tubulysin compounds for conjugation |
| EP3131587A4 (en) * | 2014-04-14 | 2017-11-01 | Endocyte, Inc. | Drug delivery conjugates for treating resistant cancer and for use in combination therapy |
| HK1248069A1 (zh) * | 2015-02-25 | 2018-10-12 | William Marsh Rice University | 去乙酰氧基微管溶素h及其类似物 |
| WO2017031209A1 (en) * | 2015-08-18 | 2017-02-23 | Endocyte, Inc. | Tubulysin analogs and methods |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| CN108367043A (zh) | 2015-12-04 | 2018-08-03 | 西雅图基因公司 | 季铵化的微管溶素化合物的缀合物 |
| US11274124B2 (en) | 2017-11-29 | 2022-03-15 | William Marsh Rice University | Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010521485A (ja) * | 2007-03-14 | 2010-06-24 | エンドサイト,インコーポレイテッド | 結合性リガンドが結合したツブリシンの薬剤送達結合体 |
| JP2011500835A (ja) * | 2007-10-25 | 2011-01-06 | エンドサイト,インコーポレイテッド | チューブリシン類および調製プロセス |
| WO2011069116A1 (en) * | 2009-12-04 | 2011-06-09 | Endocyte, Inc. | Binding ligand linked drug delivery conjugates of tubulysins |
| WO2011106639A1 (en) * | 2010-02-25 | 2011-09-01 | Purdue Research Foundation | Psma binding ligand-linker conjugates and methods for using |
| WO2012019123A1 (en) * | 2010-08-06 | 2012-02-09 | Endocyte, Inc. | Processes for preparing tubulysins |
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Also Published As
| Publication number | Publication date |
|---|---|
| EP2831059A1 (en) | 2015-02-04 |
| WO2013149185A1 (en) | 2013-10-03 |
| US20140080175A1 (en) | 2014-03-20 |
| EP2831059A4 (en) | 2015-09-02 |
| EP2831059B1 (en) | 2017-11-29 |
| CA2868494A1 (en) | 2013-10-03 |
| US9505747B2 (en) | 2016-11-29 |
| US20150051399A1 (en) | 2015-02-19 |
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