KR102252925B1 - 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 - Google Patents

마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 Download PDF

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KR102252925B1
KR102252925B1 KR1020167008038A KR20167008038A KR102252925B1 KR 102252925 B1 KR102252925 B1 KR 102252925B1 KR 1020167008038 A KR1020167008038 A KR 1020167008038A KR 20167008038 A KR20167008038 A KR 20167008038A KR 102252925 B1 KR102252925 B1 KR 102252925B1
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formula
compound
diastereomer
iib
chiral carbon
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KR20160045146A (ko
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토마스 니톨리
나레시쿠마르 에프. 자인
토마스 패트릭 마르코탄
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리제너론 파마슈티칼스 인코포레이티드
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    • 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
    • A61K31/537—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 spiro-condensed or forming part of bridged ring systems
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    • 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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
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    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
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    • 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
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
KR1020167008038A 2013-08-26 2014-08-26 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 Active KR102252925B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361869954P 2013-08-26 2013-08-26
US61/869,954 2013-08-26
US201461934313P 2014-01-31 2014-01-31
US61/934,313 2014-01-31
PCT/US2014/052757 WO2015031396A1 (en) 2013-08-26 2014-08-26 Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses

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KR20160045146A KR20160045146A (ko) 2016-04-26
KR102252925B1 true KR102252925B1 (ko) 2021-05-18

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US (3) US20160354482A1 (https=)
EP (1) EP3038624B1 (https=)
JP (1) JP6608823B2 (https=)
KR (1) KR102252925B1 (https=)
CN (1) CN105530942B (https=)
AU (1) AU2014311361B2 (https=)
BR (1) BR112016004023A2 (https=)
CA (1) CA2921412C (https=)
CL (1) CL2016000408A1 (https=)
EA (1) EA038192B1 (https=)
ES (1) ES2989322T3 (https=)
IL (1) IL244203B (https=)
MX (1) MX373528B (https=)
PH (1) PH12016500380A1 (https=)
SG (1) SG11201601230RA (https=)
WO (1) WO2015031396A1 (https=)
ZA (1) ZA201601534B (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX379256B (es) 2013-03-15 2025-03-10 Regeneron Pharma Moleculas biologicamente activas, conjugados de las mismas, y usos terapeuticos.
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
EA034950B1 (ru) * 2015-03-27 2020-04-09 Регенерон Фармасьютикалз, Инк. Производные майтанзиноида, их конъюгаты и способы использования
MY189159A (en) 2015-07-06 2022-01-29 Regeneron Pharma Multispecific antigen-binding molecules and uses thereof
WO2017132173A1 (en) 2016-01-25 2017-08-03 Regeneron Pharmaceuticals, Inc. Maytansinoid derivatives, conjugates thereof, and methods of use
WO2017190079A1 (en) 2016-04-28 2017-11-02 Regeneron Pharmaceuticals, Inc. Methods of making multispecific antigen-binding molecules
MX2019003325A (es) 2016-09-23 2019-08-05 Regeneron Pharma Anticuerpos anti-steap2, conjugados anticuerpo-farmaco, y moleculas de fijacion al antigeno biespecificas que se fijan a steap2 y cd3, y usos de estos.
MY194596A (en) 2016-09-23 2022-12-06 Regeneron Pharma Bi Specific Anti-Muc16-CD3 Antibodies And Anti-Muc16 Drug Conjugates
TWI782930B (zh) * 2016-11-16 2022-11-11 美商再生元醫藥公司 抗ｍｅｔ抗體，結合ｍｅｔ之雙特異性抗原結合分子及其使用方法
WO2018102304A1 (en) 2016-11-29 2018-06-07 Regeneron Pharmaceuticals, Inc. Methods of treating prlr positive breast cancer
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
FI3635009T3 (fi) 2017-06-07 2026-04-07 Regeneron Pharma Koostumuksia ja menetelmiä entsyymien internalisoimiseksi
MX2020004691A (es) 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
MX2020011487A (es) 2018-04-30 2020-12-07 Regeneron Pharma Anticuerpos y moleculas biespecificas de union al antigeno que se unen a her2 y/o aplp2, conjugados y usos de estos.
EP3793591A1 (en) 2018-05-17 2021-03-24 Regeneron Pharmaceuticals, Inc. Anti-cd63 antibodies, conjugates, and uses thereof
WO2020047231A1 (en) * 2018-08-31 2020-03-05 Osteoanalgesia Llc Diastereomeric conjugate compositions and methods of making and using same
US20220040319A1 (en) 2019-02-21 2022-02-10 Regeneron Pharmaceuticals, Inc. Methods of treating ocular cancer using anti-met antibodies and bispecific antigen binding molecules that bind met
US11896682B2 (en) 2019-09-16 2024-02-13 Regeneron Pharmaceuticals, Inc. Radiolabeled MET binding proteins for immuno-PET imaging and methods of use thereof
US11814428B2 (en) 2019-09-19 2023-11-14 Regeneron Pharmaceuticals, Inc. Anti-PTCRA antibody-drug conjugates and uses thereof
AU2020381495A1 (en) 2019-11-15 2022-05-19 Seagen Inc. Methods of treating HER2 positive breast cancer with tucatinib in combination with an anti-HER2 antibody-drug conjugate
IL295312A (en) 2020-02-28 2022-10-01 Regeneron Pharma Bispecific antigen binding molecules that bind her2, and methods of use thereof
IL319200A (en) 2020-04-16 2025-04-01 Regeneron Pharma Antibody-drug conjugates prepared using Diels-Alder compression methods
KR20240038138A (ko) 2020-07-13 2024-03-22 리제너론 파마슈티칼스 인코포레이티드 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도
AU2021366691B2 (en) 2020-10-22 2024-06-06 Regeneron Pharmaceuticals, Inc. Anti-FGFR2 antibodies and methods of use thereof
CA3198294A1 (en) 2020-11-10 2022-05-19 Thomas Nittoli Selenium antibody conjugates
CN115215780B (zh) * 2022-04-22 2023-08-08 上海格苓凯生物科技有限公司 一种利用n,n-二琥珀酰亚胺基碳酸酯制备异双功能交联剂smcc的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010126551A1 (en) 2009-04-30 2010-11-04 Immunogen, Inc. Potent conjugates and hydrophilic linkers
CN103254311A (zh) 2013-05-09 2013-08-21 齐鲁制药有限公司 一种制备抗体-美登素类生物碱药物偶联物的方法

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4307016A (en) 1978-03-24 1981-12-22 Takeda Chemical Industries, Ltd. Demethyl maytansinoids
JPS5566585A (en) 1978-11-14 1980-05-20 Takeda Chem Ind Ltd Novel maytansinoid compound and its preparation
CA2026147C (en) 1989-10-25 2006-02-07 Ravi J. Chari Cytotoxic agents comprising maytansinoids and their therapeutic use
US5208020A (en) 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
US5714586A (en) 1995-06-07 1998-02-03 American Cyanamid Company Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates
US6596541B2 (en) 2000-10-31 2003-07-22 Regeneron Pharmaceuticals, Inc. Methods of modifying eukaryotic cells
US20070258987A1 (en) 2000-11-28 2007-11-08 Seattle Genetics, Inc. Recombinant Anti-Cd30 Antibodies and Uses Thereof
EP1258255A1 (en) 2001-05-18 2002-11-20 Boehringer Ingelheim International GmbH Conjugates of an antibody to CD44 and a maytansinoid
US20090068178A1 (en) * 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
US8088387B2 (en) 2003-10-10 2012-01-03 Immunogen Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
CN102558352A (zh) 2003-06-27 2012-07-11 艾默根佛蒙特有限公司 针对表皮生长因子受体的缺失突变体的抗体及其使用
GB0316294D0 (en) 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
AR048098A1 (es) 2004-03-15 2006-03-29 Wyeth Corp Conjugados de caliqueamicina
KR20120064120A (ko) 2004-06-01 2012-06-18 제넨테크, 인크. 항체 약물 접합체 및 방법
EP1817341A2 (en) 2004-11-29 2007-08-15 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
PL1819359T3 (pl) 2004-12-09 2015-08-31 Janssen Biotech Inc Immunokoniugaty skierowane przeciw integrynie, metody ich wytwarzania oraz ich zastosowanie
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
KR20140116546A (ko) 2006-10-27 2014-10-02 제넨테크, 인크. 항체 및 면역접합체 및 이들의 용도
WO2008122039A2 (en) 2007-04-02 2008-10-09 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Selenocysteine mediated hybrid antibody molecules
EP2144628B1 (en) 2007-05-08 2012-10-17 Genentech, Inc. Cysteine engineered anti-muc16 antibodies and antibody drug conjugates
JP2010528285A (ja) 2007-05-23 2010-08-19 ベンタナ・メデイカル・システムズ・インコーポレーテツド 免疫組織化学およびｉｎｓｉｔｕハイブリダーゼーションのためのポリマー担体
NZ602675A (en) * 2008-03-18 2014-03-28 Genentech Inc Combinations of an anti-her2 antibody-drug conjugate and chemotherapeutic agents, and methods of use
EP2276506A4 (en) 2008-04-30 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER
EP2374481B1 (en) 2008-07-21 2015-11-04 Polytherics Limited Novel reagents and method for conjugating biological molecules
US9005598B2 (en) 2009-03-04 2015-04-14 Polytherics Limited Conjugated proteins and peptides
JP5954789B2 (ja) 2009-08-10 2016-07-20 ユーシーエル ビジネス パブリック リミテッド カンパニー 機能的分子の可逆的共有結合
TW201116297A (en) 2009-10-02 2011-05-16 Sanofi Aventis Antibodies that specifically bind to the EphA2 receptor
AR078471A1 (es) 2009-10-02 2011-11-09 Sanofi Aventis COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOS
US8501692B2 (en) 2009-12-14 2013-08-06 The Regents Of The University Of Michigan Compositions and methods for altering cocaine esterase activity
DK2528625T3 (da) 2010-04-15 2013-10-14 Spirogen Sarl Pyrrolobenzodiazepiner og konjugater deraf
US20130244905A1 (en) 2010-07-06 2013-09-19 Ed Grabczyk Reporter for RNA Polymerase II Termination
SG10201912639SA (en) 2010-08-02 2020-02-27 Regeneron Pharma Mice that make binding proteins comprising vl domains
MY162780A (en) 2010-09-01 2017-07-14 Bayer Ip Gmbh N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and use thereof as herbicides
CN105399831A (zh) 2010-10-29 2016-03-16 伊缪诺金公司 非拮抗性egfr结合分子及其免疫偶联物
CN103269712B (zh) 2010-11-03 2016-09-21 伊缪诺金公司 包含新型安丝菌素衍生物的细胞毒性剂
JP6215194B2 (ja) 2011-05-16 2017-10-18 コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． 生体直交型薬物活性化
KR20140037105A (ko) 2011-05-27 2014-03-26 암브룩스, 인코포레이티드 비-천연 아미노산 연결된 돌라스타틴 유도체를 함유하는 조성물, 이를 수반하는 방법, 및 용도
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
CN103648532A (zh) 2011-06-21 2014-03-19 伊缪诺金公司 具有肽连接子的新型美登木素生物碱衍生物及其偶联物
CA2850096C (en) 2011-10-14 2018-07-03 Spirogen Sarl Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines
CA2850103C (en) 2011-10-14 2019-09-10 Spirogen Sarl Pyrrolobenzodiazepines
ES2945932T3 (es) 2011-10-14 2023-07-10 Seagen Inc Pirrolobenzodiazepinas y conjugados dirigidos
WO2013055993A1 (en) 2011-10-14 2013-04-18 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
CN104244718A (zh) 2011-12-05 2014-12-24 伊格尼卡生物治疗公司 抗体-药物缀合物以及相关化合物、组合物和方法
GB201210770D0 (en) 2012-06-18 2012-08-01 Polytherics Ltd Novel conjugation reagents
MX2014015682A (es) 2012-06-19 2015-07-23 Polytherics Ltd Proceso novedoso para preparacion de conjugados de anticuerpo y conjugados de anticuerpo novedosos.
FI2911699T4 (fi) 2012-10-23 2025-12-09 Synaffix Bv Muokattu vasta-aine, vasta-ainekonjugaatti ja menetelmä niiden valmistamiseksi
NO2789793T3 (https=) 2012-10-24 2018-01-27
US10131682B2 (en) 2012-11-24 2018-11-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
TW201425336A (zh) * 2012-12-07 2014-07-01 Amgen Inc Ｂｃｍａ抗原結合蛋白質
CN103254213B (zh) 2012-12-21 2015-02-25 百奥泰生物科技(广州)有限公司 类美登素酯的制备方法及用于所述方法的组合物
CN104688740A (zh) 2012-12-21 2015-06-10 百奥泰生物科技(广州)有限公司 类美登素衍生物及其制备方法和用途
MX379256B (es) 2013-03-15 2025-03-10 Regeneron Pharma Moleculas biologicamente activas, conjugados de las mismas, y usos terapeuticos.
WO2014194030A2 (en) 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
SG11201509982UA (https=) 2013-06-06 2016-04-28 Igenica Biotherapeutics Inc
WO2014197871A2 (en) 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Antibody-drug conjugates, compositions and methods of use
US10781259B2 (en) 2013-06-06 2020-09-22 Magenta Therapeutics, Inc. Modified antibodies and related compounds, compositions, and methods of use
US11229711B2 (en) 2013-06-06 2022-01-25 Magenta Therapeutics, Inc. Linkers for antibody-drug conjugates and related compounds, compositions, and methods of use
US9545451B2 (en) 2013-08-21 2017-01-17 Regeneron Pharmaceuticals, Inc. Anti-PRLR antibodies and methods for killing PRLR-expressing cells
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
WO2015081282A1 (en) 2013-11-27 2015-06-04 Redwood Bioscience, Inc. Hydrazinyl-pyrrolo compounds and methods for producing a conjugate
US9562059B2 (en) 2013-12-02 2017-02-07 Hong Kong Baptist University Anticancer maytansinoids with two fused macrocyclic rings
CA2950155C (en) 2014-06-02 2021-11-23 Regeneron Pharmaceuticals, Inc. Biologically active molecule conjugates, reagents and methods of manufacture, and therapeutic uses
EA034950B1 (ru) 2015-03-27 2020-04-09 Регенерон Фармасьютикалз, Инк. Производные майтанзиноида, их конъюгаты и способы использования
WO2017132173A1 (en) 2016-01-25 2017-08-03 Regeneron Pharmaceuticals, Inc. Maytansinoid derivatives, conjugates thereof, and methods of use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010126551A1 (en) 2009-04-30 2010-11-04 Immunogen, Inc. Potent conjugates and hydrophilic linkers
CN103254311A (zh) 2013-05-09 2013-08-21 齐鲁制药有限公司 一种制备抗体-美登素类生物碱药物偶联物的方法

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