BR112017014937A2 - dímeros de benzodiazepina ligados em ponte a heteroarileno, conjugados dos mesmos, e métodos de preparação e uso - Google Patents
dímeros de benzodiazepina ligados em ponte a heteroarileno, conjugados dos mesmos, e métodos de preparação e usoInfo
- Publication number
- BR112017014937A2 BR112017014937A2 BR112017014937A BR112017014937A BR112017014937A2 BR 112017014937 A2 BR112017014937 A2 BR 112017014937A2 BR 112017014937 A BR112017014937 A BR 112017014937A BR 112017014937 A BR112017014937 A BR 112017014937A BR 112017014937 A2 BR112017014937 A2 BR 112017014937A2
- Authority
- BR
- Brazil
- Prior art keywords
- heteroarylene
- conjugates
- bridged
- preparation
- methods
- Prior art date
Links
Classifications
-
- 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
- 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
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical 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)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
Abstract
a presente invenção refere-se aos dímeros de benzodiazepina, tendo uma estrutura representada por em que x compreende uma porção heteroaromática e é como também definido no pedido; r1 é ou ; e as outras variáveis nas fórmulas (i), (ia), e (ib) são como definido no pedido. tais dímeros são úteis como agentes anticâncer, especialmente quando usados em um conjugado de anticorpo-fármaco (adc).
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562103157P | 2015-01-14 | 2015-01-14 | |
US201562215938P | 2015-09-09 | 2015-09-09 | |
PCT/US2016/013154 WO2016115201A1 (en) | 2015-01-14 | 2016-01-13 | Heteroarylene-bridged benzodiazepine dimers, conjugates thereof, and methods of making and using |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112017014937A2 true BR112017014937A2 (pt) | 2018-03-13 |
Family
ID=55272673
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017014937A BR112017014937A2 (pt) | 2015-01-14 | 2016-01-13 | dímeros de benzodiazepina ligados em ponte a heteroarileno, conjugados dos mesmos, e métodos de preparação e uso |
Country Status (19)
Country | Link |
---|---|
US (4) | US9526801B2 (pt) |
EP (1) | EP3245207B1 (pt) |
JP (1) | JP6676058B2 (pt) |
KR (1) | KR20170102981A (pt) |
CN (1) | CN107231804B (pt) |
AU (1) | AU2016206808A1 (pt) |
BR (1) | BR112017014937A2 (pt) |
CA (1) | CA2973355A1 (pt) |
CL (1) | CL2017001825A1 (pt) |
CO (1) | CO2017008086A2 (pt) |
EA (1) | EA201791461A1 (pt) |
ES (1) | ES2747386T3 (pt) |
IL (1) | IL253401A0 (pt) |
MX (1) | MX2017009144A (pt) |
PE (1) | PE20171185A1 (pt) |
SG (1) | SG11201705645YA (pt) |
TW (1) | TW201632532A (pt) |
WO (1) | WO2016115201A1 (pt) |
ZA (1) | ZA201704739B (pt) |
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WO2018009916A1 (en) | 2016-07-07 | 2018-01-11 | The Board Of Trustees Of The Leland Stanford Junior University | Antibody adjuvant conjugates |
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 |
EP3522932A4 (en) * | 2016-10-10 | 2020-06-24 | Cellerant Therapeutics, Inc. | ISOCHINOLIDINOBENZODIAZEPINE (IQB) -1 (CHLORMETHYL) -2,3-DIHYDRO-1-H-BENZO [E] INDOL (CBI) DIMERS |
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BR112021008354A2 (pt) * | 2018-10-31 | 2021-08-03 | Intocell, Inc. | derivados de benzodiazepina heterocíclica fundida e usos dos mesmos |
WO2020092631A1 (en) * | 2018-10-31 | 2020-05-07 | Fred Hutchinson Cancer Research Center | Compositions and methods for detecting and treating cancers characterized by expression of mesothelin |
JP7389803B2 (ja) | 2018-11-30 | 2023-11-30 | ブリストル-マイヤーズ スクイブ カンパニー | グルタミンを含有する軽鎖c末端に伸長部分を含む抗体およびそのコンジュゲートならびにその方法および用途 |
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- 2016-01-13 US US14/994,378 patent/US9526801B2/en active Active
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- 2016-01-13 WO PCT/US2016/013154 patent/WO2016115201A1/en active Application Filing
- 2016-01-13 AU AU2016206808A patent/AU2016206808A1/en not_active Abandoned
- 2016-01-13 KR KR1020177022246A patent/KR20170102981A/ko not_active Application Discontinuation
- 2016-01-13 CN CN201680006152.XA patent/CN107231804B/zh active Active
- 2016-01-13 SG SG11201705645YA patent/SG11201705645YA/en unknown
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- 2016-01-13 EP EP16702266.4A patent/EP3245207B1/en active Active
- 2016-01-13 JP JP2017537229A patent/JP6676058B2/ja active Active
- 2016-01-13 BR BR112017014937A patent/BR112017014937A2/pt not_active Application Discontinuation
- 2016-01-13 CA CA2973355A patent/CA2973355A1/en not_active Abandoned
- 2016-01-13 PE PE2017001217A patent/PE20171185A1/es unknown
- 2016-01-13 TW TW105100988A patent/TW201632532A/zh unknown
- 2016-11-15 US US15/351,955 patent/US9676775B2/en active Active
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- 2017-07-13 ZA ZA2017/04739A patent/ZA201704739B/en unknown
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KR20170102981A (ko) | 2017-09-12 |
CA2973355A1 (en) | 2016-07-21 |
PE20171185A1 (es) | 2017-08-22 |
US20160199510A1 (en) | 2016-07-14 |
ES2747386T3 (es) | 2020-03-10 |
US20180037581A1 (en) | 2018-02-08 |
US9822112B2 (en) | 2017-11-21 |
SG11201705645YA (en) | 2017-08-30 |
WO2016115201A1 (en) | 2016-07-21 |
EP3245207B1 (en) | 2019-08-21 |
JP6676058B2 (ja) | 2020-04-08 |
US20170057959A1 (en) | 2017-03-02 |
CN107231804A (zh) | 2017-10-03 |
CN107231804B (zh) | 2019-11-26 |
IL253401A0 (en) | 2017-09-28 |
JP2018502131A (ja) | 2018-01-25 |
EP3245207A1 (en) | 2017-11-22 |
MX2017009144A (es) | 2017-11-22 |
CO2017008086A2 (es) | 2017-11-10 |
ZA201704739B (en) | 2019-02-27 |
US9676775B2 (en) | 2017-06-13 |
EA201791461A1 (ru) | 2017-11-30 |
CL2017001825A1 (es) | 2018-02-09 |
US20170233392A1 (en) | 2017-08-17 |
AU2016206808A1 (en) | 2017-08-31 |
TW201632532A (zh) | 2016-09-16 |
US9526801B2 (en) | 2016-12-27 |
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