JP7702866B2 - Lxrアゴニストとしての使用のためのビス-オクタヒドロフェナントレンカルボキサミド誘導体及びそのタンパク質コンジュゲート - Google Patents

Lxrアゴニストとしての使用のためのビス-オクタヒドロフェナントレンカルボキサミド誘導体及びそのタンパク質コンジュゲート Download PDF

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JP7702866B2
JP7702866B2 JP2021527836A JP2021527836A JP7702866B2 JP 7702866 B2 JP7702866 B2 JP 7702866B2 JP 2021527836 A JP2021527836 A JP 2021527836A JP 2021527836 A JP2021527836 A JP 2021527836A JP 7702866 B2 JP7702866 B2 JP 7702866B2
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グロマダ ジャスパー
グサロバ ヴィクトリア
ハン エイミー
ハジナスト ソコル
ジェイ. マーフィー アンドリュー
オルソン ウィリアム
スリーマン マシュー
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レゲネロン ファーマシューティカルス,インコーポレーテッド
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JP2021527836A 2018-11-20 2019-11-19 Lxrアゴニストとしての使用のためのビス-オクタヒドロフェナントレンカルボキサミド誘導体及びそのタンパク質コンジュゲート Active JP7702866B2 (ja)

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US201862769946P 2018-11-20 2018-11-20
US62/769,946 2018-11-20
PCT/US2019/062302 WO2020106780A1 (en) 2018-11-20 2019-11-19 Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2025138724A (ja) * 2018-11-20 2025-09-25 レゲネロン ファーマシューティカルス,インコーポレーテッド Lxrアゴニストとしての使用のためのビス-オクタヒドロフェナントレンカルボキサミド誘導体及びそのタンパク質コンジュゲート

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20250114431A (ko) 2016-11-08 2025-07-29 리제너론 파마슈티칼스 인코포레이티드 스테로이드 및 이의 단백질-접합체
KR20250008984A (ko) 2017-05-18 2025-01-16 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
CN112533951A (zh) 2018-05-09 2021-03-19 里珍纳龙药品有限公司 抗msr1抗体及其使用方法
KR20240038138A (ko) * 2020-07-13 2024-03-22 리제너론 파마슈티칼스 인코포레이티드 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도
CA3198294A1 (en) 2020-11-10 2022-05-19 Thomas Nittoli Selenium antibody conjugates
US11806405B1 (en) 2021-07-19 2023-11-07 Zeno Management, Inc. Immunoconjugates and methods
TW202320858A (zh) 2021-07-19 2023-06-01 美商薩諾管理公司 免疫接合物及方法
US20240408226A1 (en) * 2021-11-02 2024-12-12 Mabplex International Co., Ltd. Antibody drug conjugate intermediate containing sn38 and its preparation method
CN115594766A (zh) * 2021-12-30 2023-01-13 辽宁键凯科技有限公司(Cn) 一种缀合物及用其制备的抗体偶联药物
CN115505028A (zh) * 2022-09-16 2022-12-23 辽宁键凯科技有限公司 一种分支型聚乙二醇连接子及其用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003516327A (ja) 1999-12-13 2003-05-13 メルク エンド カムパニー インコーポレーテッド アテローム性動脈硬化の予防および/または治療方法
US20030125357A1 (en) 2001-06-11 2003-07-03 Adams Alan D. Therapeutic compounds for treating dyslipidemic conditions
JP2017503847A (ja) 2014-01-27 2017-02-02 ファイザー・インク 二官能性細胞毒性剤
WO2018089373A2 (en) 2016-11-08 2018-05-17 Regeneron Pharmaceuticals, Inc. Steroids and protein-conjugates thereof

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20070258987A1 (en) 2000-11-28 2007-11-08 Seattle Genetics, Inc. Recombinant Anti-Cd30 Antibodies and Uses Thereof
EP1398032A1 (en) 2002-09-10 2004-03-17 PheneX Pharmaceuticals AG 4-Oxo-quinazolines as LXR nuclear receptor binding compounds
AR048098A1 (es) 2004-03-15 2006-03-29 Wyeth Corp Conjugados de caliqueamicina
EP1758651A2 (en) 2004-06-24 2007-03-07 Galapagos N.V. Lxr agonists to promote bone homeostasis
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
KR20090094125A (ko) * 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Lxr 및 fxr 조절자
US8993628B2 (en) * 2007-02-23 2015-03-31 City Of Hope Synthetic ligands selective for LXRβ over LXRα, identification and methods of use thereof
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
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
EP2276506A4 (en) 2008-04-30 2014-05-07 Immunogen Inc EFFICIENT CONJUGATES AND HYDROPHILIC BINDER
KR101000067B1 (ko) 2008-12-30 2010-12-10 엘지전자 주식회사 고효율 태양전지용 레이저 소성장치 및 고효율 태양전지 제조방법
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
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
CA2850103C (en) 2011-10-14 2019-09-10 Spirogen Sarl Pyrrolobenzodiazepines
CA2850096C (en) 2011-10-14 2018-07-03 Spirogen Sarl Synthesis method and intermediates useful in the preparation of 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
FI2911699T4 (fi) 2012-10-23 2025-12-09 Synaffix Bv Muokattu vasta-aine, vasta-ainekonjugaatti ja menetelmä niiden valmistamiseksi
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
KR102399277B1 (ko) 2014-04-10 2022-05-18 다이이찌 산쿄 가부시키가이샤 항her3 항체-약물 콘주게이트
US20160324981A1 (en) * 2015-05-08 2016-11-10 The California Institute For Biomedical Research Liver x receptor agonists and uses thereof
CA3001938A1 (en) * 2015-11-04 2017-05-11 Borealis Ag A process for producing a multilayer laminate
WO2017147542A2 (en) 2016-02-26 2017-08-31 Regeneron Pharmaceuticals, Inc. Optimized transglutaminase site-specific antibody conjugation
WO2018213082A1 (en) 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Bis-octahydrophenanthrene carboxamides and protein conjugates thereof
CN112533951A (zh) 2018-05-09 2021-03-19 里珍纳龙药品有限公司 抗msr1抗体及其使用方法
MA53455B1 (fr) * 2018-11-20 2022-11-30 Regeneron Pharma Dérivés de bis-octahydrophénanthrène carboxamide et leurs conjugués protéiques destinés à être utilisés en tant qu'agonistes de lxr

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003516327A (ja) 1999-12-13 2003-05-13 メルク エンド カムパニー インコーポレーテッド アテローム性動脈硬化の予防および/または治療方法
US20030125357A1 (en) 2001-06-11 2003-07-03 Adams Alan D. Therapeutic compounds for treating dyslipidemic conditions
JP2017503847A (ja) 2014-01-27 2017-02-02 ファイザー・インク 二官能性細胞毒性剤
WO2018089373A2 (en) 2016-11-08 2018-05-17 Regeneron Pharmaceuticals, Inc. Steroids and protein-conjugates thereof

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
COLIN M TICE,THE MEDICINAL CHEMISTRY OF LIVER X RECEPTOR (LXR) MODULATORS,JOURNAL OF MEDICINAL CHEMISTRY,2014年09月11日,VOL:57, NR:17,,PAGE(S):7182 - 7205,http://dx.doi.org/10.1021/jm500442z
COLIN, M. T. et al.,THE MEDICINAL CHEMISTRY OF LIVER X RECEPTOR (LXR) MODULATORS,JOURNAL OF MEDICINAL CHEMISTRY,2014年09月11日,Vol.57, No.17,pp.7182 - 7205,DOI:10.1021/jm500442z
SINGH S B,DISCOVERY AND DEVELOPMENT OF DIMERIC PODOCARPIC ACID LEADS AS POTENT AGONISTS OF LIVER X RECEPTOR WITH HDL CHOLESTEROL RAISING ACTIVITY IN MICE AND HAMSTERS,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,NL,PERGAMON,2005年06月02日,VOL:15, NR:11,,PAGE(S):2824 - 2828,http://doi.org/10.1016/j.bmcl.2005.03.100
SINGH S B,DISCOVERY AND DEVELOPMENT OF DIMERIC PODOCARPIC ACID LEADS AS POTENT AGONISTS 以下備考,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,NL,PERGAMON,2005年06月02日,VOL:15, NR:11,,PAGE(S):2824 - 2828,http://doi.org/10.1016/j.bmcl.2005.03.100,OF LIVER X RECEPTOR WITH HDL CHOLESTEROL RAISING ACTIVITY IN MICE AND HAMSTERS
SINGH, S. B. et al.,DISCOVERY AND DEVELOPMENT OF DIMERIC PODOCARPIC ACID LEADS AS POTENT AGONISTS OF LIVER X RECEPTOR WITH HDL CHOLESTEROL RAISING ACTIVITY IN MICE AND HAMSTERS,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,NL,PERGAMON,2005年06月02日,Vol.15, No.11,pp.2824 - 2828,DOI:10.1016/j.bmcl.2005.03.100
SINGH, S. B. et al.,DISCOVERY AND DEVELOPMENT OF DIMERIC PODOCARPIC ACID LEADS AS POTENT AGONISTS OF LIVER X RECEPTOR WITH HDL CHOLESTEROL RAISING ACTIVITY IN MICE AND HAMSTERS,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,PERGAMON,2005年06月02日,Vol.15, No.11,pp.2824 - 2828,DOI:10.1016/j.bmcl.2005.03.100

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2025138724A (ja) * 2018-11-20 2025-09-25 レゲネロン ファーマシューティカルス,インコーポレーテッド Lxrアゴニストとしての使用のためのビス-オクタヒドロフェナントレンカルボキサミド誘導体及びそのタンパク質コンジュゲート

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