MX2017011024A - Desacetoxitubulisina h y analogos de esta. - Google Patents
Desacetoxitubulisina h y analogos de esta.Info
- Publication number
- MX2017011024A MX2017011024A MX2017011024A MX2017011024A MX2017011024A MX 2017011024 A MX2017011024 A MX 2017011024A MX 2017011024 A MX2017011024 A MX 2017011024A MX 2017011024 A MX2017011024 A MX 2017011024A MX 2017011024 A MX2017011024 A MX 2017011024A
- Authority
- MX
- Mexico
- Prior art keywords
- present disclosure
- analogs
- desacetoxytubulysin
- provides
- compounds disclosed
- Prior art date
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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
- C07K5/06—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
-
- 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
- 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
- C07D417/02—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
- 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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
En un aspecto, la presente invención proporciona análogos de tubulisina de la fórmula: (ver Fórmula) en donde R1, R2, R3, R4, X1, X2, X3, y A1 son como se definen en la presente descripción. En otro aspecto, la presente invención proporciona, además, métodos para preparar los compuestos descritos en en la presente descripción. En otro aspecto, la presente invención proporciona, además, composiciones farmacéuticas y métodos de uso de los compuestos descritos en en la presente descripción.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562120613P | 2015-02-25 | 2015-02-25 | |
US201662275667P | 2016-01-06 | 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 |
---|---|
MX2017011024A true MX2017011024A (es) | 2017-10-20 |
Family
ID=56789084
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2017011024A MX2017011024A (es) | 2015-02-25 | 2016-02-25 | Desacetoxitubulisina h y analogos de esta. |
Country Status (22)
Country | Link |
---|---|
US (1) | US10808007B2 (es) |
EP (1) | EP3261443B1 (es) |
JP (1) | JP2018509404A (es) |
KR (1) | KR20170137725A (es) |
CN (1) | CN107529754A (es) |
AU (1) | AU2016222575A1 (es) |
BR (1) | BR112017018305A2 (es) |
CA (1) | CA2977589A1 (es) |
CL (1) | CL2017002170A1 (es) |
CO (1) | CO2017008600A2 (es) |
CR (1) | CR20170438A (es) |
DO (1) | DOP2017000202A (es) |
EA (1) | EA201791896A1 (es) |
EC (1) | ECSP17057131A (es) |
GT (1) | GT201700190A (es) |
HK (1) | HK1248069A1 (es) |
IL (1) | IL254089A0 (es) |
MX (1) | MX2017011024A (es) |
PE (1) | PE20180355A1 (es) |
PH (1) | PH12017501539A1 (es) |
SG (1) | SG11201706820RA (es) |
WO (1) | WO2016138288A1 (es) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2017049140A2 (en) | 2015-09-18 | 2017-03-23 | 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 |
US20210145771A1 (en) * | 2017-07-03 | 2021-05-20 | Glaxosmithkline Intellectual Property Development Limited | N-(3-(2-(4-chlorophenoxy)acetamido)bicyclo[1.1.1] pentan-1-yl)-2-cyclobutane-1- carboxamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases |
CR20200054A (es) | 2017-08-09 | 2020-03-21 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
US11389543B2 (en) * | 2017-09-08 | 2022-07-19 | Seagen Inc. | Process for the preparation of tubulysins and intermediates thereof |
WO2019108685A1 (en) * | 2017-11-29 | 2019-06-06 | William March Rice University | Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith |
EA202191769A1 (ru) | 2018-12-21 | 2021-12-08 | Регенерон Фармасьютикалз, Инк. | Тубулизины и конъюгаты белок-тубулизин |
CA3129609A1 (en) | 2019-02-13 | 2020-08-20 | Denali Therapeutics Inc. | Eukaryotic initiation factor 2b modulators |
CN112209938B (zh) * | 2019-07-11 | 2021-06-11 | 苏州亚盛药业有限公司 | 2-吲哚啉螺环酮类化合物的制备方法及其中间体 |
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 |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1523493B1 (de) | 2002-07-09 | 2013-09-04 | Dömling, Alexander | Neue tubulysinanaloga |
AU2003253048A1 (en) | 2002-07-09 | 2004-01-23 | Morphochem Aktiengellschaft Fur Kombinatorische Chemie | Tubulysin conjugates |
US20100047841A1 (en) | 2007-02-27 | 2010-02-25 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Synthesis of desacetoxytubulysin h and analogs thereof |
CA2723671C (en) * | 2007-05-10 | 2018-06-19 | R & D Biopharmaceuticals Gmbh | Tubulysine derivatives |
WO2009012958A2 (en) | 2007-07-20 | 2009-01-29 | Helmholtz-Zentrum für Infektionsforschung GmbH | Tubulysin d analogues |
AU2008316835B2 (en) * | 2007-10-25 | 2015-07-16 | Endocyte, Inc. | Tubulysins and processes for preparing |
EP2174947A1 (en) * | 2008-09-25 | 2010-04-14 | Universität des Saarlandes | Bioactive pre-tubulysins and use thereof |
IT1394860B1 (it) | 2009-07-22 | 2012-07-20 | Kemotech S R L | Composti farmaceutici |
US8394922B2 (en) | 2009-08-03 | 2013-03-12 | Medarex, Inc. | Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof |
EP2322537A1 (en) | 2009-11-12 | 2011-05-18 | R & D Biopharmaceuticals Gmbh | Tubulin inhibitors |
WO2011069116A1 (en) * | 2009-12-04 | 2011-06-09 | Endocyte, Inc. | Binding ligand linked drug delivery conjugates of tubulysins |
EP2409983A1 (en) | 2010-07-19 | 2012-01-25 | Leibniz-Institut für Pflanzenbiochemie (IPB) | Tubulysin analogues |
US8889880B2 (en) * | 2010-08-06 | 2014-11-18 | Endocyte, Inc. | Processes for preparing tubulysins |
US20140080175A1 (en) * | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
SG11201506243XA (en) | 2013-02-14 | 2015-09-29 | Bristol Myers Squibb Co | Tubulysin compounds, methods of making and use |
US9427479B2 (en) * | 2014-04-11 | 2016-08-30 | Medimmune Llc | Tubulysin derivatives |
-
2016
- 2016-02-25 CA CA2977589A patent/CA2977589A1/en not_active Abandoned
- 2016-02-25 KR KR1020177027116A patent/KR20170137725A/ko unknown
- 2016-02-25 EP EP16756378.2A patent/EP3261443B1/en active Active
- 2016-02-25 SG SG11201706820RA patent/SG11201706820RA/en unknown
- 2016-02-25 EA EA201791896A patent/EA201791896A1/ru unknown
- 2016-02-25 CN CN201680023813.XA patent/CN107529754A/zh active Pending
- 2016-02-25 CR CR20170438A patent/CR20170438A/es unknown
- 2016-02-25 MX MX2017011024A patent/MX2017011024A/es unknown
- 2016-02-25 BR BR112017018305A patent/BR112017018305A2/pt not_active Application Discontinuation
- 2016-02-25 JP JP2017545239A patent/JP2018509404A/ja active Pending
- 2016-02-25 AU AU2016222575A patent/AU2016222575A1/en not_active Abandoned
- 2016-02-25 WO PCT/US2016/019604 patent/WO2016138288A1/en active Application Filing
- 2016-02-25 PE PE2017001465A patent/PE20180355A1/es unknown
- 2016-02-25 US US15/553,674 patent/US10808007B2/en active Active
-
2017
- 2017-08-22 IL IL254089A patent/IL254089A0/en unknown
- 2017-08-25 CL CL2017002170A patent/CL2017002170A1/es unknown
- 2017-08-25 CO CONC2017/0008600A patent/CO2017008600A2/es unknown
- 2017-08-25 DO DO2017000202A patent/DOP2017000202A/es unknown
- 2017-08-25 PH PH12017501539A patent/PH12017501539A1/en unknown
- 2017-08-25 GT GT201700190A patent/GT201700190A/es unknown
- 2017-08-30 EC ECIEPI201757131A patent/ECSP17057131A/es unknown
-
2018
- 2018-06-13 HK HK18107653.3A patent/HK1248069A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
IL254089A0 (en) | 2017-10-31 |
KR20170137725A (ko) | 2017-12-13 |
PH12017501539A1 (en) | 2018-02-05 |
US10808007B2 (en) | 2020-10-20 |
AU2016222575A1 (en) | 2017-09-07 |
US20180127463A1 (en) | 2018-05-10 |
CN107529754A (zh) | 2018-01-02 |
JP2018509404A (ja) | 2018-04-05 |
CL2017002170A1 (es) | 2018-06-08 |
CR20170438A (es) | 2018-01-30 |
ECSP17057131A (es) | 2019-03-29 |
EP3261443A1 (en) | 2018-01-03 |
CO2017008600A2 (es) | 2018-02-09 |
BR112017018305A2 (pt) | 2018-04-17 |
HK1248069A1 (zh) | 2018-10-12 |
WO2016138288A1 (en) | 2016-09-01 |
SG11201706820RA (en) | 2017-09-28 |
EP3261443B1 (en) | 2021-04-28 |
EA201791896A1 (ru) | 2018-02-28 |
GT201700190A (es) | 2018-11-26 |
CA2977589A1 (en) | 2016-09-01 |
DOP2017000202A (es) | 2017-09-29 |
EP3261443A4 (en) | 2018-09-26 |
PE20180355A1 (es) | 2018-02-21 |
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