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tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate | 120205-52-9

分子结构分类

有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物

中文名称

——

中文别名

——

英文名称

tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate

英文别名

tert-butyl (3R,4S,5S)-4-[{N-[(benzyloxy)carbonyl]-L-valyl}(methyl)amino]-3-methoxy-5-methylheptanoate；(3R,4S,5S)-tert-butyl 4-((S)-2-(((benzyloxy)carbonyl)amino)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoate；tert-butyl (3R,4S,5S)-4-((S)-2-(((benzyloxy)carbonyl)amino)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoate；Z-Val-Dil-OBu^t；Cbz-Val-Dil-OtBu；tert-butyl (3R,4S,5S)-4-[{N-[(benzyloxy)carbonyl]-valyl}(methyl)amino]-3-methoxy-5-methylheptanoate；tert-butyl (3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]heptanoate

tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate化学式

CAS

120205-52-9

化学式

C₂₇H₄₄N₂O₆

mdl

——

分子量

492.656

InChiKey

SXCDYMWHVBJDJZ-ZXHYAQOVSA-N

BEILSTEIN

——

EINECS

——

物化性质

沸点：

601.2±55.0 °C(Predicted)
密度：

1.061±0.06 g/cm3(Predicted)

计算性质

辛醇/水分配系数(LogP)：

4.8
重原子数：

35
可旋转键数：

15
环数：

1.0
sp3杂化的碳原子比例：

0.67
拓扑面积：

94.2
氢给体数：

1
氢受体数：

6

上下游信息

上游原料

中文名称	英文名称	CAS号	化学式	分子量
(3S,4S,5S)-4-((((苄氧基)羰基)(甲基)氨基)-3-甲氧基-5-甲基庚酸叔丁	tert-Butyl (3S,4S,5S)-3-methoxy-4--5-methylheptanoate	154633-73-5	C₂₂H₃₅NO₅	393.524
——	tert-butyl (3R,4S,5S)-4-{[(benzyloxy)carbonyl](methyl)amino}-3-methoxy-5-methylheptanoate	120205-58-5	C₂₂H₃₅NO₅	393.524
——	(3R,4S,5S)-4-(Benzyloxycarbonyl-methyl-amino)-3-methoxy-5-methyl-heptanoic acid methyl ester	149664-79-9	C₁₉H₂₉NO₅	351.443
——	tert-Butyl (3S,4S,5S)-3-hydroxy-4--5-methylheptanoate	120205-57-4	C₂₁H₃₃NO₅	379.497
——	(3R,4S,5S)-4--3-methoxy-5-methylheptanoic acid	135383-56-1	C₁₈H₂₇NO₅	337.416
——	tert-butyl (3R,4S,5S)-4-[benzyl(methyl)amino]-3-methoxy-5-methyl heptanoate	——	C₂₁H₃₅NO₃	349.514

下游产品

中文名称	英文名称	CAS号	化学式	分子量
——	tert-butyl (3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]butanoyl]amino]heptanoate	173441-12-8	C₃₂H₅₃N₃O₇	591.789
——	Cbz-MeVal-Val-Dil-OtBu	173441-13-9	C₃₃H₅₅N₃O₇	605.816
——	(3R,4S,5S)-4-(N-((2S)-((2S)-N-benzyloxycarbonylamino-3-methylbutanoyl)-3-methylbutanoyl)-N-methylamino)-3-methoxy-5-methylheptanoic acid	716371-64-1	C₂₈H₄₅N₃O₇	535.681
——	(5S,8S,11S,12R)-11-((S)-sec-butyl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-1-phenyl-2-oxa-4,7,10-triazatetradecan-14-oic acid	920017-22-7	C₂₉H₄₇N₃O₇	549.708
——	tert-butyl (3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]heptanoate	173441-14-0	C₂₄H₄₆N₂O₅	442.64
——	(3R,4S,5S)-4-{[(S)-2-(2-Dimethylamino-acetylamino)-3-methyl-butyryl]-methyl-amino}-3-methoxy-5-methyl-heptanoic acid tert-butyl ester	149606-68-8	C₂₃H₄₅N₃O₅	443.627
N,N-二甲基-L-缬氨酰-N-[(1S,2R)-4-(1,1-二甲基乙氧基)-2-甲氧基-1-	Dov-Val-Dil-OBu-t	120205-53-0	C₂₆H₅₁N₃O₅	485.708
——	tert-butyl (3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)propanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoate	149606-61-1	C₂₄H₄₇N₃O₅	457.654
——	Dov-Dil-OBu^t	173441-22-0	C₂₁H₄₂N₂O₄	386.575
——	tert-butyl (3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-hydroxy-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoate	173441-15-1	C₂₄H₄₆N₂O₆	458.639
——	tert-butyl (3R,4S,5S)-3-methoxy-5-methyl-4-[methyl(L-valyl)amino]heptanoate	177423-00-6	C₁₉H₃₈N₂O₄	358.522
——	N-[(benzyloxy)carbonyl]-N-methyl-L-threonyl-N-[(2R,3S,4S)-1-carboxy-2-methoxy-4-methylhexan-3-yl]-N-methyl-L-valinamide	——	C₂₈H₄₅N₃O₈	551.681
——	(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]heptanoic acid	1053615-81-8	C₂₀H₃₈N₂O₅	386.532
——	(3R,4S,5S)-4-[[(2S)-2-[[2-(dimethylamino)acetyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoic acid	1054613-46-5	C₁₉H₃₇N₃O₅	387.52
海兔毒素中间体	(3R,4S,5S)-4-((S)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoic acid	133120-89-5	C₂₂H₄₃N₃O₅	429.601
——	(3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)propanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoic acid	1053465-14-7	C₂₀H₃₉N₃O₅	401.547
——	(3R,4S,5S)-4-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoic acid	1054782-94-3	C₁₇H₃₄N₂O₄	330.468
——	Dov-Val-Dil-Dap-OBzl	163768-52-3	C₃₈H₆₄N₄O₇	688.949
——	tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate	1375415-93-2	C₃₄H₄₈N₂O₆	580.765
——	Dov-Val-Dil-Dap	163768-53-4	C₃₁H₅₈N₄O₇	598.824
(5S,8S,11S,12R)-11-((S)-仲丁基)-1-(9H-芴-9-基)-5,8-	N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-tert-butoxy-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide	474645-25-5	C₄₀H₅₉N₃O₇	693.924
——	(3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoic acid	1438851-41-2	C₃₀H₄₀N₂O₆	524.657
——	N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(1S)-1-carboxy-2-phenylethyl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide	1369427-27-9	C₄₄H₇₃N₅O₁₀	832.091
(2S)-2-[[(2S)-2-二甲基氨基-3-甲基丁酰基]氨基]-N-[(3R,4R,5S)-3-甲氧基-1-[(2S)-2-[(1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(2-苯基乙基氨基)丙基]吡咯烷-1-基]-5-甲基-1-氧代庚烷-4-基]-N,3-二甲基丁酰胺	TZT-1027	149606-27-9	C₃₉H₆₇N₅O₆	701.991
(5S,9S,11S,12R)-11-((S)-仲丁基)-1-(9H-芴-9-基)-5,9-	(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid	863971-44-2	C₃₆H₅₁N₃O₇	637.817
一甲基澳瑞他汀E	MMAE	474645-27-7	C₃₉H₆₇N₅O₇	717.99
——	Z-Val-Val-Dil-Dap-Doe	173441-24-2	C₄₈H₇₀N₆O₈S	891.185
——	N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-tert-butoxy-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide	——	C₄₀H₅₉N₃O₇	693.924
——	Z-N-Me-Val-Val-Dil-Dap-Doe	173441-25-3	C₄₉H₇₂N₆O₈S	905.212
——	methyl (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-amino-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate	669074-47-9	C₃₄H₅₆N₄O₇	632.841
——	N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(2R,3S,4S)-1-carboxy-2-methoxy-4-methylhexan-3-yl]-N-methyl-L-valinamide	——	C₃₆H₅₁N₃O₇	637.817
——	(S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-((4-aminophenyl)sulfonamido)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamide	——	C₃₇H₆₄N₆O₈S	753.017
——	methyl (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate	1438852-21-1	C₄₉H₆₆N₄O₉	855.084
单甲基澳瑞他汀D	monomethyl dolastatin 10	203849-91-6	C₄₁H₆₆N₆O₆S	771.078
(S)-2-((S)-2-(二甲基氨基)-3-甲基丁酰氨基)-N-((3R,4S,5S)-3-甲氧基-1-((s)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基）乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚烷-4-基)-N,3-二甲基丁酰胺	dolastatin 10	110417-88-4	C₄₂H₆₈N₆O₆S	785.105
——	(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2S)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide	130272-92-3	C₄₂H₆₈N₆O₆S	785.105
——	tert-Butyl (2S)-2-[(1R,2R)-3-{[(2S)-3,3-dimethyl-1-(1,2-oxazinan-2-yl)-1-oxobutan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidine-1-carboxylate	1352202-01-7	C₂₄H₄₃N₃O₆	469.622
——	(S)-N-(4-(N-((2R,3R)-3-((S)-1-((3R,4S)-4-((S)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)sulfamoyl)phenyl)-2-((S)-1-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-14-isopropyl-12-oxo-3,6,9-trioxa-13-azapentadecanamido)-5-ureidopentanamide	1800462-96-7	C₆₁H₁₀₁N₁₁O₁₇S	1292.6

反应信息

作为反应物：

描述：

tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate 在氰基磷酸二乙酯、 palladium on activated charcoal 、四丁基氟化铵、氢气、碳酸氢钠、 N,N-二异丙基乙胺、三氟乙酸作用下，以 1,4-二氧六环、乙醇、二氯甲烷、水、 N,N-二甲基甲酰胺为溶剂，反应 8.0h，生成 methyl (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-amino-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

参考文献：

名称：

[EN] CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER
[FR] CONJUGUÉ DE MONOMÉTHYLE AURISTATINE F ET DE TRASTUZUMAB ET SON UTILISATION POUR LE TRAITEMENT DU CANCER

摘要：

本发明涉及一种抗体药物偶联物。从一方面来说，该发明涉及一种抗体药物偶联物，包括由曲妥珠单抗组成的抗体，所述抗体与至少一种由单甲基奥瑞他汀F衍生物组成的药物偶联。该发明还包括治疗方法和使用所述抗体药物偶联物治疗癌症的方法。

公开号：

WO2016173682A1
作为产物：

描述：

醋酸叔丁酯在盐酸、正丁基锂、 palladium on activated charcoal 、氢气、 trifluoroborane diethyl ether 、 N,N-二异丙基乙胺、 bromo-tris(1-pyrrolidinyl)phosphonium hexafluorophosphate 作用下，以四氢呋喃、乙醇、二氯甲烷、 N,N-二甲基甲酰胺为溶剂，反应 45.66h，生成 tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate

参考文献：

名称：

[EN] COMPOSITION FOR THE TREATMENT OF IGF-1R EXPRESSING CANCER
[FR] COMPOSITION POUR LE TRAITEMENT D'UN CANCER EXPRIMANT IGF-1R

摘要：

本发明涉及一种用于治疗表达IGF-IR的癌症的方法，以及用于所述治疗的组合物和试剂盒。从一方面来说，发明涉及第一抗体用于确定癌症的IGF-IR状态和第二抗体作为ADC用于治疗所述癌症的联合使用。

公开号：

WO2017072196A1
作为试剂：

描述：

N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(adamantan-1-ylmethoxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide trifluoroacetate 、琥珀半醛、、氰基硼氢化钠、盐酸以 tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate 为溶剂，反应 5.0h，以18.5 mg (73% of theory) of the title compound were thus obtained的产率得到N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(adamantan-1-ylmethoxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

参考文献：

名称：

NEW BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF

摘要：

本申请涉及一种新的N，N-二烷基月桂酰基链霉素（ADC）结合物，其针对C4.4a靶标，以及这些ADC的活性代谢物，制备这些ADC的方法，使用这些ADC治疗和/或预防疾病，以及使用这些ADC制造治疗和/或预防疾病的药物，尤其是高增殖和/或血管生成性疾病，如癌症等。这种治疗可以作为单一疗法，也可以与其他药物或进一步治疗措施结合使用。

公开号：

US20130066055A1

点击查看最新优质反应信息

文献信息

[EN] ANTIBODY-DRUG-CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER<br/>[FR] CONJUGUÉ ANTICORPS-MÉDICAMENT ET SON UTILISATION POUR LE TRAITEMENT DU CANCER

申请人：PF MEDICAMENT

公开号：WO2015162293A1

公开（公告）日：2015-10-29

The present invention relates to an antibody-drug-conjugate. From one aspect, the invention relates to an antibody-drug-conjugate comprising an antibody capable of binding to a Target, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said antibody-drug-conjugate for the treatment of cancer.

本发明涉及一种抗体药物偶联物。从一方面来说，该发明涉及一种抗体药物偶联物，包括一种能够与靶标结合的抗体，所述抗体与至少一种选自多拉司汀10衍生物和奥里司汀衍生物的药物偶联。该发明还包括治疗方法以及使用所述抗体药物偶联物治疗癌症的应用。
CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER

申请人：Pierre Fabre Medicament

公开号：US20170112943A1

公开（公告）日：2017-04-27

The present invention relates to an antibody-drug-conjugate or pharmaceutical composition comprising the same. From one aspect, the invention relates to an antibody-drug-conjugate (ADC) comprising an antibody consisting of the Trastuzumab or a biosimilar thereof, said antibody being conjugated to at least one drug consisting of a monomethyl auristatin F derivative. The invention also comprises method of treatment of cancer comprising administering to the subject an effective amount of said antibody-drug-conjugate or composition comprising the same.

本发明涉及一种抗体药物偶联物或包含该偶联物的药物组合物。从一方面来说，该发明涉及一种抗体药物偶联物（ADC），包括一种由曲妥珠单抗或其生物类似物组成的抗体，所述抗体与至少一种由单甲基奥瑞他汀F衍生物组成的药物偶联。该发明还包括一种治疗癌症的方法，包括向受试者施用有效量的所述抗体药物偶联物或包含该偶联物的组合物。
NEW ANTIBODY DRUG CONJUGATES (ADCS) AND THE USE THEREOF

申请人：SEATTLE GENETICS, INC.

公开号：US20150023989A1

公开（公告）日：2015-01-22

The present application relates to new antibody drug conjugates (ADCs) of N,N dialkylauristatins directed against the target FGFR2, drug metabolites of said ADCs, a method for producing said ADCs, the use of said ADCs for the treatment and/or prevention of illnesses as well as the use of said ADCs for producing pharmaceuticals for the treatment and/or prevention of illnesses, particularly of hyperproliferative and/or angiogenic diseases such as carcinosis. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.

本申请涉及针对FGFR2靶点的新抗体药物结合物（ADCs），所述ADCs的药物代谢产物，生产所述ADCs的方法，利用所述ADCs治疗和/或预防疾病以及利用所述ADCs生产用于治疗和/或预防疾病的药物，特别是治疗高增殖和/或血管生成性疾病如癌症。这种治疗可以作为单药疗法进行，也可以与其他药物或额外的治疗措施结合使用。
NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME

申请人：SEATTLE GENETICS, INC.

公开号：US20150246136A1

公开（公告）日：2015-09-03

The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.

本专利申请涉及针对靶向表皮生长因子受体（EGFR，基因ID 1956）的新型结合物-药物共轭物（ADCs）N，N-二烷基月桂酰基蛋白酶抑制剂，这些ADCs的有效代谢物，生产这些ADCs的方法，利用这些ADCs治疗和/或预防疾病，以及利用这些ADCs生产用于治疗和/或预防疾病的药物，特别是治疗高增殖和/或血管生成性疾病，如癌症。这种治疗可以作为单药疗法或与其他药物或其他治疗措施联合使用。
[EN] AURISTATIN DERIVATIVES AND CONJUGATES THEREOF<br/>[FR] DÉRIVÉS D'AURISTATINE ET CONJUGUÉS DE CEUX-CI

申请人：NOVARTIS AG

公开号：WO2015189791A1

公开（公告）日：2015-12-17

Disclosed herein are novel compounds of formula (I) as described herein, and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

本文披露了如下所述的化合物(I)的新颖化合物，以及在制备免疫结合物（即抗体药物结合物）中使用这些肽的用途。本文还描述了包括这种新颖化合物与抗原结合基团（如抗体）连接的免疫结合物（即抗体药物结合物），这些免疫结合物可用于治疗细胞增殖性疾病。该发明还提供了包括这些免疫结合物的药物组合物，包括与治疗性辅助剂一起的免疫结合物的组合物，以及使用这些免疫结合物和组合物治疗细胞增殖性疾病的方法。