RU2017118792A - Конъюгаты антитела к staphylococcus aureus с рифамицином и их применение - Google Patents
Конъюгаты антитела к staphylococcus aureus с рифамицином и их применение Download PDFInfo
- Publication number
- RU2017118792A RU2017118792A RU2017118792A RU2017118792A RU2017118792A RU 2017118792 A RU2017118792 A RU 2017118792A RU 2017118792 A RU2017118792 A RU 2017118792A RU 2017118792 A RU2017118792 A RU 2017118792A RU 2017118792 A RU2017118792 A RU 2017118792A
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- Prior art keywords
- antibody
- antibiotic
- conjugate
- compound
- formula
- Prior art date
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- 241000191967 Staphylococcus aureus Species 0.000 title claims 3
- 229940127121 immunoconjugate Drugs 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 36
- 230000003115 biocidal effect Effects 0.000 claims 35
- 239000003242 anti bacterial agent Substances 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 229910052799 carbon Inorganic materials 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000005647 linker group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000004452 carbocyclyl group Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 108091005804 Peptidases Proteins 0.000 claims 5
- 239000004365 Protease Substances 0.000 claims 5
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 5
- 108090000765 processed proteins & peptides Proteins 0.000 claims 5
- HJYYPODYNSCCOU-ODRIEIDWSA-N rifamycin SV Chemical group OC1=C(C(O)=C2C)C3=C(O)C=C1NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)\C=C\O[C@@]1(C)OC2=C3C1=O HJYYPODYNSCCOU-ODRIEIDWSA-N 0.000 claims 5
- 125000003003 spiro group Chemical group 0.000 claims 4
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 241000191963 Staphylococcus epidermidis Species 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000000816 peptidomimetic Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- DKQPFCGUMYBORR-UHFFFAOYSA-N 4-[[(2-bromoacetyl)amino]-[(2-iodoacetyl)amino]methyl]benzenesulfonic acid Chemical compound C1=CC(=CC=C1C(NC(=O)CBr)NC(=O)CI)S(=O)(=O)O DKQPFCGUMYBORR-UHFFFAOYSA-N 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- HAXFWIACAGNFHA-UHFFFAOYSA-N aldrithiol Chemical compound C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical group 0.000 claims 1
- FNXLCIKXHOPCKH-UHFFFAOYSA-N bromamine Chemical compound BrN FNXLCIKXHOPCKH-UHFFFAOYSA-N 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001268 conjugating effect Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- -1 glidant Substances 0.000 claims 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- SGHWBDUXKUSFOP-KYALZUAASA-N rifalazil Chemical group O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)N=C2C(=O)C=3C(O)=C4C)C)OC)C4=C1C=3C(NC1=C(O)C=3)=C2OC1=CC=3N1CCN(CC(C)C)CC1 SGHWBDUXKUSFOP-KYALZUAASA-N 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
Classifications
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/12—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria
- C07K16/1267—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria
- C07K16/1271—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria from Micrococcaceae (F), e.g. Staphylococcus
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Organic Chemistry (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462087213P | 2014-12-03 | 2014-12-03 | |
| US62/087,213 | 2014-12-03 | ||
| PCT/US2015/063515 WO2016090040A1 (en) | 2014-12-03 | 2015-12-02 | Anti-staphylococcus aureus antibody rifamycin conjugates and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017118792A true RU2017118792A (ru) | 2019-01-09 |
| RU2017118792A3 RU2017118792A3 (enExample) | 2019-06-14 |
Family
ID=55022690
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017118792A RU2017118792A (ru) | 2014-12-03 | 2015-12-02 | Конъюгаты антитела к staphylococcus aureus с рифамицином и их применение |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20180125995A1 (enExample) |
| EP (1) | EP3226908A1 (enExample) |
| JP (1) | JP6751393B2 (enExample) |
| KR (1) | KR20170086542A (enExample) |
| CN (1) | CN107249642A (enExample) |
| BR (1) | BR112017011478A2 (enExample) |
| CA (1) | CA2966211A1 (enExample) |
| HK (1) | HK1244230A1 (enExample) |
| MX (1) | MX2017007231A (enExample) |
| RU (1) | RU2017118792A (enExample) |
| WO (1) | WO2016090040A1 (enExample) |
Families Citing this family (14)
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| EA201691023A1 (ru) | 2013-12-16 | 2016-10-31 | Дженентек, Инк. | Пептидомиметические соединения и их конъюгаты антитела с лекарственным средством |
| CN105848685B (zh) | 2013-12-16 | 2020-09-22 | 健泰科生物技术公司 | 拟肽化合物及其抗体药物偶联物 |
| WO2016205176A1 (en) | 2015-06-15 | 2016-12-22 | Genentech, Inc. | Antibodies and immunoconjugates |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| SG10202010590UA (en) | 2015-12-04 | 2020-12-30 | Seattle Genetics Inc | Conjugates of quaternized tubulysin compounds |
| SG11201807537RA (en) * | 2016-03-04 | 2018-09-27 | Genentech Inc | Process for the preparation of an antibody-rifamycin conjugate |
| KR102835535B1 (ko) | 2016-11-08 | 2025-07-18 | 리제너론 파마슈티칼스 인코포레이티드 | 스테로이드 및 이의 단백질-접합체 |
| CN110944718A (zh) | 2017-05-18 | 2020-03-31 | 里珍纳龙药品有限公司 | 环糊精蛋白质药物偶联物 |
| AU2018365946B2 (en) * | 2017-11-07 | 2025-08-28 | Regeneron Pharmaceuticals, Inc. | Hydrophilic linkers for antibody drug conjugates |
| MX2020006994A (es) | 2018-01-08 | 2020-11-06 | Regeneron Pharma | Esteroides y conjugados de anticuerpos de los mismos. |
| CN118955710A (zh) | 2018-05-09 | 2024-11-15 | 里珍纳龙药品有限公司 | 抗msr1抗体及其使用方法 |
| CN111939256B (zh) * | 2020-07-06 | 2022-05-31 | 中国药科大学 | 一种具有细菌调理特性的抗菌辅助材料及其制备方法和应用 |
| US20250082761A1 (en) * | 2021-08-20 | 2025-03-13 | Rutgers, The State University Of New Jersey | Dual-targeted rna polymerase inhibitors: conjugates of benzoxazino- and spiro-rifamycins with n alpha-aroyl-n-aryl-phenylalaninamides |
| US20250319024A1 (en) * | 2021-08-27 | 2025-10-16 | University Of Georgia Research Foundation, Inc. | Targeted nanoparticles and their uses related to infectious disease |
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-
2015
- 2015-12-02 JP JP2017528877A patent/JP6751393B2/ja not_active Expired - Fee Related
- 2015-12-02 CA CA2966211A patent/CA2966211A1/en not_active Abandoned
- 2015-12-02 EP EP15816304.8A patent/EP3226908A1/en not_active Withdrawn
- 2015-12-02 MX MX2017007231A patent/MX2017007231A/es unknown
- 2015-12-02 CN CN201580075250.4A patent/CN107249642A/zh active Pending
- 2015-12-02 HK HK18103816.6A patent/HK1244230A1/zh unknown
- 2015-12-02 BR BR112017011478-0A patent/BR112017011478A2/pt not_active Application Discontinuation
- 2015-12-02 KR KR1020177015225A patent/KR20170086542A/ko not_active Withdrawn
- 2015-12-02 WO PCT/US2015/063515 patent/WO2016090040A1/en not_active Ceased
- 2015-12-02 RU RU2017118792A patent/RU2017118792A/ru not_active Application Discontinuation
-
2017
- 2017-06-02 US US15/612,193 patent/US20180125995A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP6751393B2 (ja) | 2020-09-02 |
| CN107249642A (zh) | 2017-10-13 |
| US20180125995A1 (en) | 2018-05-10 |
| HK1244230A1 (zh) | 2018-08-03 |
| MX2017007231A (es) | 2017-11-08 |
| KR20170086542A (ko) | 2017-07-26 |
| WO2016090040A9 (en) | 2017-06-29 |
| CA2966211A1 (en) | 2016-06-09 |
| RU2017118792A3 (enExample) | 2019-06-14 |
| JP2018507166A (ja) | 2018-03-15 |
| WO2016090040A1 (en) | 2016-06-09 |
| BR112017011478A2 (pt) | 2018-02-27 |
| EP3226908A1 (en) | 2017-10-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20201210 |