CL2017001825A1 - Dímeros de benzodiazepina unidos con puentes de heteroarileno, conjugados de estos, y sus métodos de preparación y uso. - Google Patents
Dímeros de benzodiazepina unidos con puentes de heteroarileno, conjugados de estos, y sus métodos de preparación y uso.Info
- Publication number
- CL2017001825A1 CL2017001825A1 CL2017001825A CL2017001825A CL2017001825A1 CL 2017001825 A1 CL2017001825 A1 CL 2017001825A1 CL 2017001825 A CL2017001825 A CL 2017001825A CL 2017001825 A CL2017001825 A CL 2017001825A CL 2017001825 A1 CL2017001825 A1 CL 2017001825A1
- Authority
- CL
- Chile
- Prior art keywords
- heteroarylene
- conjugates
- bridges
- preparation
- methods
- Prior art date
Links
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 title 1
- 239000000611 antibody drug conjugate Substances 0.000 abstract 2
- 229940049595 antibody-drug conjugate Drugs 0.000 abstract 2
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- C07K5/06052—Val-amino acid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Cell Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
<p>DÍMEROS DE BENZODIAZEPINA QUE TIENEN UNA ESTRUCTURA REPRESENTADA, EN DONDE X COMPRENDE UNA PORCIÓN HETEROAROMÁTICA Y ES COMO SE DEFINE EN MAYOR DETALLE EN LA SOLICITUD; R1 ES Y LAS OTRAS VARIABLES EN LAS FORMULAS (I), (IA) Y (IB) SON COMO SE DEFINEN EN LA SOLICITUD. ESTOS DÍMEROS SON ÚTILES COMO AGENTES ANTINEOPLÁSICOS, ESPECIAL, CUANDO SE USAN EN UN CONJUGADO ANTICUERPO-FÁRMACO (ADC).</p>
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562103157P | 2015-01-14 | 2015-01-14 | |
| US201562215938P | 2015-09-09 | 2015-09-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2017001825A1 true CL2017001825A1 (es) | 2018-02-09 |
Family
ID=55272673
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2017001825A CL2017001825A1 (es) | 2015-01-14 | 2017-07-13 | Dímeros de benzodiazepina unidos con puentes de heteroarileno, conjugados de estos, y sus métodos de preparación y uso. |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US9526801B2 (es) |
| EP (1) | EP3245207B1 (es) |
| JP (1) | JP6676058B2 (es) |
| KR (1) | KR20170102981A (es) |
| CN (1) | CN107231804B (es) |
| AU (1) | AU2016206808A1 (es) |
| BR (1) | BR112017014937A2 (es) |
| CA (1) | CA2973355A1 (es) |
| CL (1) | CL2017001825A1 (es) |
| CO (1) | CO2017008086A2 (es) |
| EA (1) | EA201791461A1 (es) |
| ES (1) | ES2747386T3 (es) |
| IL (1) | IL253401A0 (es) |
| MX (1) | MX2017009144A (es) |
| PE (1) | PE20171185A1 (es) |
| SG (1) | SG11201705645YA (es) |
| TW (1) | TW201632532A (es) |
| WO (1) | WO2016115201A1 (es) |
| ZA (1) | ZA201704739B (es) |
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| US9504694B2 (en) | 2015-03-19 | 2016-11-29 | Cellerant Therapeutics, Inc. | Isoquinolidinobenzodiazepines |
| GB201510010D0 (en) | 2015-06-09 | 2015-07-22 | King S College London | PDD and BPD compounds |
| US20180339985A1 (en) | 2015-08-21 | 2018-11-29 | Femtogenix Limited | Pdd compounds |
| GB201514928D0 (en) | 2015-08-21 | 2015-10-07 | King S College London | PDD compounds |
| BR112019000071A2 (pt) | 2016-07-07 | 2019-07-02 | Bolt Biotherapeutics Inc | conjugados adjuvantes de anticorpo |
| US20190218294A1 (en) | 2016-09-09 | 2019-07-18 | Bristol-Myers Squibb Company | Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment |
| CN110049780A (zh) * | 2016-10-10 | 2019-07-23 | 塞勒兰特治疗公司 | 异喹啉并苯并二氮杂卓(iqb)-1(氯甲基)-2,3-二氢-1h-苯并[e]吲哚(cbi)二聚体 |
| US10738338B2 (en) | 2016-10-18 | 2020-08-11 | The Research Foundation for the State University | Method and composition for biocatalytic protein-oligonucleotide conjugation and protein-oligonucleotide conjugate |
| US10398783B2 (en) | 2016-10-20 | 2019-09-03 | Bristol-Myers Squibb Company | Antiproliferative compounds and conjugates made therefrom |
| AU2018236272B2 (en) | 2017-03-15 | 2022-03-31 | Silverback Therapeutics, Inc. | Benzazepine compounds, conjugates, and uses thereof |
| EP3612533A1 (en) | 2017-04-20 | 2020-02-26 | Immunogen, Inc. | Methods of preparing indolinobenzodiazepine derivatives |
| GB201714115D0 (en) | 2017-09-04 | 2017-10-18 | Femtogenix Ltd | Cytotoxic agents |
| GB201806022D0 (en) * | 2018-04-12 | 2018-05-30 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| CN112166115A (zh) * | 2018-05-29 | 2021-01-01 | 尹图赛利有限公司 | 新型苯二氮杂*衍生物及其用途 |
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| GB201814281D0 (en) * | 2018-09-03 | 2018-10-17 | Femtogenix Ltd | Cytotoxic agents |
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| US20240377413A1 (en) | 2019-09-16 | 2024-11-14 | Bristol-Myers Squibb Company | Dual capture method for analysis of antibody-drug conjugates |
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| KR20230047361A (ko) | 2020-07-01 | 2023-04-07 | 아르스 파마슈티컬스 인크. | 항-asgr1 항체 접합체 및 이의 용도 |
| CN113203780B (zh) * | 2021-05-13 | 2022-05-31 | 桂林电子科技大学 | 一种非诊断目的无标记适配体传感器检测gpc3的方法 |
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-
2016
- 2016-01-13 CN CN201680006152.XA patent/CN107231804B/zh not_active Expired - Fee Related
- 2016-01-13 WO PCT/US2016/013154 patent/WO2016115201A1/en not_active Ceased
- 2016-01-13 AU AU2016206808A patent/AU2016206808A1/en not_active Abandoned
- 2016-01-13 EA EA201791461A patent/EA201791461A1/ru unknown
- 2016-01-13 CA CA2973355A patent/CA2973355A1/en not_active Abandoned
- 2016-01-13 JP JP2017537229A patent/JP6676058B2/ja not_active Expired - Fee Related
- 2016-01-13 EP EP16702266.4A patent/EP3245207B1/en active Active
- 2016-01-13 PE PE2017001217A patent/PE20171185A1/es unknown
- 2016-01-13 ES ES16702266T patent/ES2747386T3/es active Active
- 2016-01-13 BR BR112017014937A patent/BR112017014937A2/pt not_active Application Discontinuation
- 2016-01-13 TW TW105100988A patent/TW201632532A/zh unknown
- 2016-01-13 SG SG11201705645YA patent/SG11201705645YA/en unknown
- 2016-01-13 KR KR1020177022246A patent/KR20170102981A/ko active Pending
- 2016-01-13 US US14/994,378 patent/US9526801B2/en active Active
- 2016-01-13 MX MX2017009144A patent/MX2017009144A/es unknown
- 2016-11-15 US US15/351,955 patent/US9676775B2/en active Active
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2017
- 2017-05-05 US US15/587,679 patent/US9822112B2/en active Active
- 2017-07-10 IL IL253401A patent/IL253401A0/en unknown
- 2017-07-13 ZA ZA2017/04739A patent/ZA201704739B/en unknown
- 2017-07-13 CL CL2017001825A patent/CL2017001825A1/es unknown
- 2017-08-10 CO CONC2017/0008086A patent/CO2017008086A2/es unknown
- 2017-10-17 US US15/785,608 patent/US20180037581A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US9526801B2 (en) | 2016-12-27 |
| WO2016115201A1 (en) | 2016-07-21 |
| JP2018502131A (ja) | 2018-01-25 |
| US20170233392A1 (en) | 2017-08-17 |
| KR20170102981A (ko) | 2017-09-12 |
| CO2017008086A2 (es) | 2017-11-10 |
| ZA201704739B (en) | 2019-02-27 |
| CN107231804A (zh) | 2017-10-03 |
| EP3245207A1 (en) | 2017-11-22 |
| PE20171185A1 (es) | 2017-08-22 |
| US9822112B2 (en) | 2017-11-21 |
| EA201791461A1 (ru) | 2017-11-30 |
| CA2973355A1 (en) | 2016-07-21 |
| BR112017014937A2 (pt) | 2018-03-13 |
| EP3245207B1 (en) | 2019-08-21 |
| US9676775B2 (en) | 2017-06-13 |
| US20160199510A1 (en) | 2016-07-14 |
| SG11201705645YA (en) | 2017-08-30 |
| US20180037581A1 (en) | 2018-02-08 |
| IL253401A0 (en) | 2017-09-28 |
| CN107231804B (zh) | 2019-11-26 |
| AU2016206808A1 (en) | 2017-08-31 |
| MX2017009144A (es) | 2017-11-22 |
| TW201632532A (zh) | 2016-09-16 |
| ES2747386T3 (es) | 2020-03-10 |
| JP6676058B2 (ja) | 2020-04-08 |
| US20170057959A1 (en) | 2017-03-02 |
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