HK1248069A1 - 去乙酰氧基微管溶素h及其類似物 - Google Patents

去乙酰氧基微管溶素h及其類似物 Download PDF

Info

Publication number: HK1248069A1
Authority: HK; Hong Kong
Prior art keywords: present disclosure; analogs; desacetoxytubulysin; provides; compounds disclosed
Prior art date: 2015-02-25

Application number

HK18107653.3A

Other languages

English (en)

Inventor

Kyriacos C. Nicolaou

Dionosios VOURLOUMIS

Jun Yin

Rohan ERANDE

Debashis MANDAL

Philipp KLAHN

Original Assignee

William Marsh Rice University

Priority date (The priority date 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 date listed.)

2015-02-25

Filing date

2016-02-25

Publication date

2018-10-12

2016-02-25 Application filed by William Marsh Rice University filed Critical William Marsh Rice University

2018-10-12 Publication of HK1248069A1 publication Critical patent/HK1248069A1/zh

Classifications

- 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
- 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
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- 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
- 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
- A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- 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
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Biochemistry (AREA)
Biophysics (AREA)
Genetics & Genomics (AREA)
Molecular Biology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Crystallography & Structural Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Immunology (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Cell Biology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Peptides Or Proteins (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Medicinal Preparation (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

HK18107653.3A 2015-02-25 2016-02-25 去乙酰氧基微管溶素h及其類似物 HK1248069A1 (zh)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US201562120613P	2015-02-25	2015-02-25
US62/120,613		2015-02-25
US201662275667P	2016-01-06	2016-01-06
US62/275,667		2016-01-06
PCT/US2016/019604 WO2016138288A1 (en)	2015-02-25	2016-02-25	Desacetoxytubulysin h and analogs thereof

Publications (1)

Publication Number	Publication Date
HK1248069A1 true HK1248069A1 (zh)	2018-10-12

Family

ID=56789084

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
HK18107653.3A HK1248069A1 (zh)	2015-02-25	2016-02-25	去乙酰氧基微管溶素h及其類似物

Country Status (22)

Country	Link
US (1)	US10808007B2 (zh)
EP (1)	EP3261443B1 (zh)
JP (1)	JP2018509404A (zh)
KR (1)	KR20170137725A (zh)
CN (1)	CN107529754A (zh)
AU (1)	AU2016222575A1 (zh)
BR (1)	BR112017018305A2 (zh)
CA (1)	CA2977589A1 (zh)
CL (1)	CL2017002170A1 (zh)
CO (1)	CO2017008600A2 (zh)
CR (1)	CR20170438A (zh)
DO (1)	DOP2017000202A (zh)
EA (1)	EA201791896A1 (zh)
EC (1)	ECSP17057131A (zh)
GT (1)	GT201700190A (zh)
HK (1)	HK1248069A1 (zh)
IL (1)	IL254089A0 (zh)
MX (1)	MX2017011024A (zh)
PE (1)	PE20180355A1 (zh)
PH (1)	PH12017501539A1 (zh)
SG (1)	SG11201706820RA (zh)
WO (1)	WO2016138288A1 (zh)

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US10829519B2 (en)	2015-09-18	2020-11-10	Wake Forest University Health Sciences	Angiotensin (1-7) analogs and methods relating thereto
CA2914601A1 (en) *	2015-12-11	2017-06-11	Wake Forest University Health Sciences	Angiotensin-(1-7) analogs and methods relating thereto
JP2020525513A (ja) *	2017-07-03	2020-08-27	グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅＩｎｔｅｌｌｅｃｔｕａｌＰｒｏｐｅｒｔｙＤｅｖｅｌｏｐｍｅｎｔＬｉｍｉｔｅｄ	癌および他の疾患を治療するためのａｔｆ４阻害剤としてのｎ−（３−（２−（４−クロロフェノキシ）アセトアミドビシクロ［１．１．１］ペンタン−１−イル）−２−シクロブタン−１−カルボキサミド誘導体および関連化合物
EP3665156A4 (en)	2017-08-09	2021-04-28	Denali Therapeutics Inc.	COMPOUNDS, COMPOSITIONS, AND PROCEDURES
DK3676297T3 (da)	2017-09-01	2023-08-14	Denali Therapeutics Inc	Forbindelser, sammensætninger og fremgangsmåder
BR112020004495A2 (pt) *	2017-09-08	2020-09-08	Seattle Genetics, Inc.	composto, composição, e, método para preparar uma composição.
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
CA3124106A1 (en)	2018-12-21	2020-06-25	Regeneron Pharmaceuticals, Inc.	Tubulysins and protein-tubulysin conjugates
TWI877136B (zh)	2019-02-13	2025-03-21	美商戴納立製藥公司	化合物、組合物及方法
US12091392B2 (en)	2019-02-13	2024-09-17	Denali Therapeutics Inc.	Compounds, compositions and methods
EP3814358A4 (en) *	2019-07-11	2022-04-06	Ascentage Pharma (Suzhou) Co., Ltd.	PROCESS FOR THE PREPARATION OF 2-INDOLINOSPIRONE COMPOUNDS AND INTERMEDIATE THEREOF
US11694341B2 (en)	2019-12-23	2023-07-04	Texas Instmments Incorporated	Cascaded architecture for disparity and motion prediction with block matching and convolutional neural network (CNN)
CN112645833A (zh) *	2021-01-29	2021-04-13	上海吉奉生物科技有限公司	一种(s)-2,6-二氨基-5-氧己酸的合成方法

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EP3129362A4 (en) *	2014-04-11	2017-08-23	Medimmune, LLC	Tubulysin derivatives

2016
- 2016-02-25 CR CR20170438A patent/CR20170438A/es unknown
- 2016-02-25 US US15/553,674 patent/US10808007B2/en active Active
- 2016-02-25 WO PCT/US2016/019604 patent/WO2016138288A1/en active Application Filing
- 2016-02-25 BR BR112017018305A patent/BR112017018305A2/pt not_active Application Discontinuation
- 2016-02-25 CN CN201680023813.XA patent/CN107529754A/zh active Pending
- 2016-02-25 CA CA2977589A patent/CA2977589A1/en not_active Abandoned
- 2016-02-25 PE PE2017001465A patent/PE20180355A1/es unknown
- 2016-02-25 SG SG11201706820RA patent/SG11201706820RA/en unknown
- 2016-02-25 KR KR1020177027116A patent/KR20170137725A/ko not_active Withdrawn
- 2016-02-25 HK HK18107653.3A patent/HK1248069A1/zh unknown
- 2016-02-25 AU AU2016222575A patent/AU2016222575A1/en not_active Abandoned
- 2016-02-25 MX MX2017011024A patent/MX2017011024A/es unknown
- 2016-02-25 JP JP2017545239A patent/JP2018509404A/ja active Pending
- 2016-02-25 EP EP16756378.2A patent/EP3261443B1/en active Active
- 2016-02-25 EA EA201791896A patent/EA201791896A1/ru unknown
2017
- 2017-08-22 IL IL254089A patent/IL254089A0/en unknown
- 2017-08-25 CL CL2017002170A patent/CL2017002170A1/es unknown
- 2017-08-25 DO DO2017000202A patent/DOP2017000202A/es unknown
- 2017-08-25 CO CONC2017/0008600A patent/CO2017008600A2/es unknown
- 2017-08-25 GT GT201700190A patent/GT201700190A/es unknown
- 2017-08-25 PH PH12017501539A patent/PH12017501539A1/en unknown
- 2017-08-30 EC ECIEPI201757131A patent/ECSP17057131A/es unknown

Also Published As

Publication number	Publication date
EA201791896A1 (ru)	2018-02-28
IL254089A0 (en)	2017-10-31
EP3261443A4 (en)	2018-09-26
KR20170137725A (ko)	2017-12-13
CA2977589A1 (en)	2016-09-01
BR112017018305A2 (pt)	2018-04-17
CN107529754A (zh)	2018-01-02
SG11201706820RA (en)	2017-09-28
EP3261443B1 (en)	2021-04-28
WO2016138288A1 (en)	2016-09-01
PE20180355A1 (es)	2018-02-21
US10808007B2 (en)	2020-10-20
MX2017011024A (es)	2017-10-20
CL2017002170A1 (es)	2018-06-08
CO2017008600A2 (es)	2018-02-09
ECSP17057131A (es)	2019-03-29
AU2016222575A1 (en)	2017-09-07
PH12017501539A1 (en)	2018-02-05
DOP2017000202A (es)	2017-09-29
US20180127463A1 (en)	2018-05-10
EP3261443A1 (en)	2018-01-03
CR20170438A (es)	2018-01-30
GT201700190A (es)	2018-11-26
JP2018509404A (ja)	2018-04-05

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