AR100006A1 - Derivados de tubulisina - Google Patents
Derivados de tubulisinaInfo
- Publication number
- AR100006A1 AR100006A1 ARP150101089A ARP150101089A AR100006A1 AR 100006 A1 AR100006 A1 AR 100006A1 AR P150101089 A ARP150101089 A AR P150101089A AR P150101089 A ARP150101089 A AR P150101089A AR 100006 A1 AR100006 A1 AR 100006A1
- Authority
- AR
- Argentina
- Prior art keywords
- derivatives
- tubulisine
- tubulisin
- chemotherapies
- ch2ch3
- Prior art date
Links
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
- 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
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- 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
- A61K47/6801—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
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
-
- 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
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
- A61K47/6817—Toxins
- A61K47/6829—Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
-
- 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
- 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
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/30—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
-
- 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
- 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
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0212—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -N-C-N-C(=0)-, e.g. retro-inverso peptides
-
- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Abstract
Se proporcionan derivados de tubulisina que son útiles como agentes citotóxicos para proveer beneficios terapéuticos en el tratamiento de varios tipos de cáncer, solos, como conjugados de fármaco o en combinación con otras quimioterapias. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1), o una sal farmacéuticamente aceptable de este, donde: R¹ es CH₃, o CH₂CH₃; R² es H o CH₃; R³ es H o NH₂; y n es 1 ó 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461978460P | 2014-04-11 | 2014-04-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR100006A1 true AR100006A1 (es) | 2016-08-31 |
Family
ID=54264545
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP150101089A AR100006A1 (es) | 2014-04-11 | 2015-04-10 | Derivados de tubulisina |
Country Status (19)
Country | Link |
---|---|
US (2) | US9427479B2 (es) |
EP (1) | EP3129362A4 (es) |
JP (1) | JP2017510661A (es) |
KR (1) | KR20160142392A (es) |
CN (1) | CN106458942A (es) |
AR (1) | AR100006A1 (es) |
AU (1) | AU2015243379B2 (es) |
CA (1) | CA2945318A1 (es) |
CL (1) | CL2016002548A1 (es) |
EA (1) | EA032203B1 (es) |
IL (1) | IL247822A0 (es) |
MA (1) | MA39862A (es) |
MX (1) | MX2016013373A (es) |
NZ (1) | NZ725131A (es) |
PH (1) | PH12016501995A1 (es) |
SG (1) | SG11201608203RA (es) |
TW (1) | TW201625662A (es) |
UY (1) | UY36075A (es) |
WO (1) | WO2015157594A1 (es) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MA39862A (fr) * | 2014-04-11 | 2017-02-15 | Lakshmaiah Gingipalli | Dérivés de tubulysine |
CN106232139A (zh) | 2014-04-11 | 2016-12-14 | 免疫医疗有限责任公司 | 双特异性her2抗体 |
US10808007B2 (en) * | 2015-02-25 | 2020-10-20 | William Marsh Rice University | Desacetoxytubulysin H and analogs thereof |
RU2710194C9 (ru) | 2015-11-10 | 2020-09-14 | МЕДИММЬЮН, ЭлЭлСи | Связывающие молекулы, специфичные в отношении asct2, и их применения |
US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
CA3006000A1 (en) | 2015-12-04 | 2017-06-08 | Seattle Genetics, Inc. | Conjugates of quaternized tubulysin compounds |
JP2019507126A (ja) * | 2016-02-01 | 2019-03-14 | ファイザー・インク | ツブリシン類似体およびこれらの調製のための方法 |
CA3020864A1 (en) | 2016-04-15 | 2017-10-19 | Macrogenics, Inc. | Novel b7-h3-binding molecules, antibody drug conjugates thereof and methods of use thereof |
JP2019534882A (ja) | 2016-10-11 | 2019-12-05 | メドイミューン・リミテッドMedImmune Limited | 免疫介在性療法薬を有する抗体−薬物コンジュゲート |
MA51447A (fr) | 2017-08-01 | 2020-06-10 | Medimmune Llc | Conjugué anticorps monoclonal-médicament dirigé contre bcma |
AU2017445144A1 (en) * | 2017-12-31 | 2020-06-18 | Hangzhou Dac Biotech Co. Ltd | A conjugate of a tubulysin analog with branched linkers |
CN109456212A (zh) * | 2018-12-03 | 2019-03-12 | 康化(上海)新药研发有限公司 | 一种沙库比曲中间体的合成方法 |
TWI753252B (zh) * | 2019-05-03 | 2022-01-21 | 中國大陸商杭州多禧生物科技有限公司 | 含支鏈連接體的Tubulysin同系物偶聯物 |
WO2020257998A1 (en) * | 2019-06-24 | 2020-12-30 | Hangzhou Dac Biotech Co., Ltd | A conjugate of a cytotoxic agent to a cell binding molecule with branched linkers |
US20230069722A1 (en) * | 2020-06-24 | 2023-03-02 | Regeneron Pharmaceuticals, Inc. | Tubulysins and protein-tubulysin conjugates |
AR123480A1 (es) | 2020-09-11 | 2022-12-07 | Medimmune Ltd | Moléculas de unión terapéuticas |
WO2023083846A1 (en) | 2021-11-10 | 2023-05-19 | Astrazeneca Ab | Antibody molecules and conjugates |
GB202117928D0 (en) | 2021-12-11 | 2022-01-26 | Cancer Research Tech Ltd | Immunotherapy for cancer |
WO2024002938A1 (en) | 2022-06-27 | 2024-01-04 | Astrazeneca Ab | Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7064211B2 (en) * | 2002-03-22 | 2006-06-20 | Eisai Co., Ltd. | Hemiasterlin derivatives and uses thereof |
JP2008522624A (ja) * | 2004-12-09 | 2008-07-03 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘミアスタリン(hemiasterlin)アナログを使用する癌治療におけるチューブリンのアイソタイプのスクリーニング |
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 |
ES2657014T3 (es) * | 2011-11-17 | 2018-03-01 | Pfizer Inc. | Péptidos citotóxicos y conjugados de fármaco anticuerpo de los mismos |
EP2793585A4 (en) * | 2011-12-05 | 2015-12-09 | Igenica Biotherapeutics Inc | Antibody-Agent Conjugates and Related Compounds, Compositions and Methods |
DK2956173T3 (en) * | 2013-02-14 | 2017-07-17 | Bristol Myers Squibb Co | TUBULYSIS RELATIONSHIPS, METHODS OF PRODUCING AND USING THEREOF |
MA39862A (fr) * | 2014-04-11 | 2017-02-15 | Lakshmaiah Gingipalli | Dérivés de tubulysine |
WO2015155345A1 (en) | 2014-04-11 | 2015-10-15 | Medimmune Limited | Antibodies and antibody-drug conjugates |
CN106232139A (zh) * | 2014-04-11 | 2016-12-14 | 免疫医疗有限责任公司 | 双特异性her2抗体 |
-
2015
- 2015-04-10 MA MA039862A patent/MA39862A/fr unknown
- 2015-04-10 SG SG11201608203RA patent/SG11201608203RA/en unknown
- 2015-04-10 US US14/683,196 patent/US9427479B2/en not_active Expired - Fee Related
- 2015-04-10 CN CN201580031041.XA patent/CN106458942A/zh active Pending
- 2015-04-10 AR ARP150101089A patent/AR100006A1/es unknown
- 2015-04-10 EA EA201691963A patent/EA032203B1/ru not_active IP Right Cessation
- 2015-04-10 KR KR1020167031176A patent/KR20160142392A/ko unknown
- 2015-04-10 TW TW104111700A patent/TW201625662A/zh unknown
- 2015-04-10 CA CA2945318A patent/CA2945318A1/en not_active Abandoned
- 2015-04-10 AU AU2015243379A patent/AU2015243379B2/en not_active Ceased
- 2015-04-10 UY UY0001036075A patent/UY36075A/es not_active Application Discontinuation
- 2015-04-10 MX MX2016013373A patent/MX2016013373A/es unknown
- 2015-04-10 WO PCT/US2015/025235 patent/WO2015157594A1/en active Application Filing
- 2015-04-10 EP EP15777523.0A patent/EP3129362A4/en not_active Withdrawn
- 2015-04-10 JP JP2017504616A patent/JP2017510661A/ja active Pending
- 2015-04-10 NZ NZ725131A patent/NZ725131A/en not_active IP Right Cessation
-
2016
- 2016-08-08 US US15/230,918 patent/US10159745B2/en not_active Expired - Fee Related
- 2016-09-14 IL IL247822A patent/IL247822A0/en unknown
- 2016-10-06 CL CL2016002548A patent/CL2016002548A1/es unknown
- 2016-10-07 PH PH12016501995A patent/PH12016501995A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
IL247822A0 (en) | 2016-11-30 |
TW201625662A (zh) | 2016-07-16 |
KR20160142392A (ko) | 2016-12-12 |
WO2015157594A1 (en) | 2015-10-15 |
US9427479B2 (en) | 2016-08-30 |
EA201691963A1 (ru) | 2017-06-30 |
CN106458942A (zh) | 2017-02-22 |
US20150291657A1 (en) | 2015-10-15 |
AU2015243379A1 (en) | 2016-11-03 |
MX2016013373A (es) | 2017-05-02 |
EP3129362A1 (en) | 2017-02-15 |
NZ725131A (en) | 2018-03-23 |
US20160339114A1 (en) | 2016-11-24 |
PH12016501995A1 (en) | 2017-01-09 |
US10159745B2 (en) | 2018-12-25 |
AU2015243379B2 (en) | 2018-02-01 |
UY36075A (es) | 2015-10-30 |
CL2016002548A1 (es) | 2017-02-24 |
JP2017510661A (ja) | 2017-04-13 |
EP3129362A4 (en) | 2017-08-23 |
CA2945318A1 (en) | 2015-10-15 |
EA032203B1 (ru) | 2019-04-30 |
MA39862A (fr) | 2017-02-15 |
SG11201608203RA (en) | 2016-10-28 |
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