PE20180355A1 - Desacetoxitubulisina h y analogos de esta - Google Patents
Desacetoxitubulisina h y analogos de estaInfo
- Publication number
- PE20180355A1 PE20180355A1 PE2017001465A PE2017001465A PE20180355A1 PE 20180355 A1 PE20180355 A1 PE 20180355A1 PE 2017001465 A PE2017001465 A PE 2017001465A PE 2017001465 A PE2017001465 A PE 2017001465A PE 20180355 A1 PE20180355 A1 PE 20180355A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- compounds
- methylpentil
- methylpiperidine
- acetoxy
- Prior art date
Links
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- NBFVMBGIPAJCJQ-ZCFIWIBFSA-N (2r)-1-methylpiperidine-2-carboxamide Chemical compound CN1CCCC[C@@H]1C(N)=O NBFVMBGIPAJCJQ-ZCFIWIBFSA-N 0.000 abstract 2
- -1 THIAZOL-4-CARBOXAMIDO Chemical class 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000004982 aromatic amines Chemical class 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229960005190 phenylalanine Drugs 0.000 abstract 1
Classifications
-
- 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)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562120613P | 2015-02-25 | 2015-02-25 | |
| US201662275667P | 2016-01-06 | 2016-01-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20180355A1 true PE20180355A1 (es) | 2018-02-21 |
Family
ID=56789084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017001465A PE20180355A1 (es) | 2015-02-25 | 2016-02-25 | Desacetoxitubulisina h y analogos de esta |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US10808007B2 (enExample) |
| EP (1) | EP3261443B1 (enExample) |
| JP (1) | JP2018509404A (enExample) |
| KR (1) | KR20170137725A (enExample) |
| CN (1) | CN107529754A (enExample) |
| AU (1) | AU2016222575A1 (enExample) |
| BR (1) | BR112017018305A2 (enExample) |
| CA (1) | CA2977589A1 (enExample) |
| CL (1) | CL2017002170A1 (enExample) |
| CO (1) | CO2017008600A2 (enExample) |
| CR (1) | CR20170438A (enExample) |
| DO (1) | DOP2017000202A (enExample) |
| EA (1) | EA201791896A1 (enExample) |
| EC (1) | ECSP17057131A (enExample) |
| GT (1) | GT201700190A (enExample) |
| HK (1) | HK1248069A1 (enExample) |
| IL (1) | IL254089A0 (enExample) |
| MX (1) | MX2017011024A (enExample) |
| PE (1) | PE20180355A1 (enExample) |
| PH (1) | PH12017501539A1 (enExample) |
| SG (1) | SG11201706820RA (enExample) |
| WO (1) | WO2016138288A1 (enExample) |
Families Citing this family (14)
| 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 |
| WO2019008506A1 (en) * | 2017-07-03 | 2019-01-10 | 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 THE TREATMENT OF CANCER AND OTHER DISEASES |
| IL301709B2 (en) | 2017-08-09 | 2025-07-01 | Denali Therapeutics Inc | Compounds, compositions and methods |
| TW201920129A (zh) | 2017-09-01 | 2019-06-01 | 美商戴納立製藥公司 | 化合物、組合物及方法 |
| MA50124A (fr) * | 2017-09-08 | 2020-07-15 | Seattle Genetics Inc | Procédé de préparation de tubulysines et d'intermédiaires de celles-ci |
| 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 |
| WO2020132658A2 (en) | 2018-12-21 | 2020-06-25 | Regeneron Pharmaceuticals, Inc. | Tubulysins and protein-tubulysin conjugates |
| EP3924341A4 (en) | 2019-02-13 | 2022-11-02 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| CR20210426A (es) | 2019-02-13 | 2021-09-30 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| WO2021004516A1 (en) * | 2019-07-11 | 2021-01-14 | Ascentage Pharma (Suzhou) Co., Ltd. | Method for preparing 2-indolinospirone compound 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) |
| TW202241857A (zh) | 2020-12-18 | 2022-11-01 | 美商戴納立製藥公司 | 化合物之固體形式 |
| 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 |
|---|---|---|---|---|
| EP1521769B1 (de) | 2002-07-09 | 2015-09-09 | Dömling, Alexander | Tubulysinkonjugate |
| US7816377B2 (en) | 2002-07-09 | 2010-10-19 | R&D-Biopharmaceuticals Gmbh | Tubulysin analogues |
| 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 |
| EP2148886B1 (en) | 2007-05-10 | 2014-02-19 | R & D Biopharmaceuticals Gmbh | Tubulysine derivatives |
| EP2181101A2 (en) | 2007-07-20 | 2010-05-05 | Helmholtz-Zentrum für Infektionsforschung GmbH | Tubulysin d analogues |
| EP2209374B1 (en) * | 2007-10-25 | 2014-12-03 | 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 |
| DK2956173T3 (en) | 2013-02-14 | 2017-07-17 | Bristol Myers Squibb Co | TUBULYSIS RELATIONSHIPS, METHODS OF PRODUCING AND USING THEREOF |
| CA2945318A1 (en) * | 2014-04-11 | 2015-10-15 | Medimmune, Llc | Tubulysin derivatives |
-
2016
- 2016-02-25 KR KR1020177027116A patent/KR20170137725A/ko not_active Withdrawn
- 2016-02-25 WO PCT/US2016/019604 patent/WO2016138288A1/en not_active Ceased
- 2016-02-25 US US15/553,674 patent/US10808007B2/en active Active
- 2016-02-25 JP JP2017545239A patent/JP2018509404A/ja active Pending
- 2016-02-25 HK HK18107653.3A patent/HK1248069A1/zh unknown
- 2016-02-25 EP EP16756378.2A patent/EP3261443B1/en active Active
- 2016-02-25 AU AU2016222575A patent/AU2016222575A1/en not_active Abandoned
- 2016-02-25 MX MX2017011024A patent/MX2017011024A/es unknown
- 2016-02-25 PE PE2017001465A patent/PE20180355A1/es unknown
- 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 BR BR112017018305A patent/BR112017018305A2/pt not_active Application Discontinuation
- 2016-02-25 CR CR20170438A patent/CR20170438A/es unknown
- 2016-02-25 CA CA2977589A patent/CA2977589A1/en not_active Abandoned
-
2017
- 2017-08-22 IL IL254089A patent/IL254089A0/en unknown
- 2017-08-25 PH PH12017501539A patent/PH12017501539A1/en unknown
- 2017-08-25 GT GT201700190A patent/GT201700190A/es unknown
- 2017-08-25 CO CONC2017/0008600A patent/CO2017008600A2/es unknown
- 2017-08-25 DO DO2017000202A patent/DOP2017000202A/es unknown
- 2017-08-25 CL CL2017002170A patent/CL2017002170A1/es unknown
- 2017-08-30 EC ECIEPI201757131A patent/ECSP17057131A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016138288A1 (en) | 2016-09-01 |
| GT201700190A (es) | 2018-11-26 |
| CL2017002170A1 (es) | 2018-06-08 |
| JP2018509404A (ja) | 2018-04-05 |
| CR20170438A (es) | 2018-01-30 |
| EP3261443A1 (en) | 2018-01-03 |
| IL254089A0 (en) | 2017-10-31 |
| EP3261443A4 (en) | 2018-09-26 |
| US20180127463A1 (en) | 2018-05-10 |
| AU2016222575A1 (en) | 2017-09-07 |
| US10808007B2 (en) | 2020-10-20 |
| CA2977589A1 (en) | 2016-09-01 |
| BR112017018305A2 (pt) | 2018-04-17 |
| CO2017008600A2 (es) | 2018-02-09 |
| PH12017501539A1 (en) | 2018-02-05 |
| CN107529754A (zh) | 2018-01-02 |
| SG11201706820RA (en) | 2017-09-28 |
| DOP2017000202A (es) | 2017-09-29 |
| KR20170137725A (ko) | 2017-12-13 |
| EP3261443B1 (en) | 2021-04-28 |
| MX2017011024A (es) | 2017-10-20 |
| EA201791896A1 (ru) | 2018-02-28 |
| ECSP17057131A (es) | 2019-03-29 |
| HK1248069A1 (zh) | 2018-10-12 |
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