JP7728636B2 - ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート - Google Patents

ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Info

Publication number
JP7728636B2
JP7728636B2 JP2019563612A JP2019563612A JP7728636B2 JP 7728636 B2 JP7728636 B2 JP 7728636B2 JP 2019563612 A JP2019563612 A JP 2019563612A JP 2019563612 A JP2019563612 A JP 2019563612A JP 7728636 B2 JP7728636 B2 JP 7728636B2
Authority
JP
Japan
Prior art keywords
compound
solvate
pharmaceutically acceptable
acceptable salt
stereoisomer
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2019563612A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020520926A (ja
JP2020520926A5 (https=
Inventor
ハン エイミー
ジェイ． マーフィー アンドリュー
オルソン ウィリアム
Original Assignee
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=62245504&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP7728636(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 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 filed Critical 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
Publication of JP2020520926A publication Critical patent/JP2020520926A/ja
Publication of JP2020520926A5 publication Critical patent/JP2020520926A5/ja
Priority to JP2023077334A priority Critical patent/JP7843731B2/ja
Application granted granted Critical
Publication of JP7728636B2 publication Critical patent/JP7728636B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/88—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having the nitrogen atom of at least one of the carboxamide groups further acylated
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/6801—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/90—Carboxylic acid amides having nitrogen atoms of carboxamide groups further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
    • C07D295/112—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/12—Esters of phosphoric acids with hydroxyaryl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Psychology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
JP2019563612A 2017-05-18 2018-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート Active JP7728636B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023077334A JP7843731B2 (ja) 2017-05-18 2023-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762508327P 2017-05-18 2017-05-18
US62/508,327 2017-05-18
PCT/US2018/031910 WO2018213082A1 (en) 2017-05-18 2018-05-09 Bis-octahydrophenanthrene carboxamides and protein conjugates thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2023077334A Division JP7843731B2 (ja) 2017-05-18 2023-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Publications (3)

Publication Number Publication Date
JP2020520926A JP2020520926A (ja) 2020-07-16
JP2020520926A5 JP2020520926A5 (https=) 2021-08-05
JP7728636B2 true JP7728636B2 (ja) 2025-08-25

Family

ID=62245504

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2019563612A Active JP7728636B2 (ja) 2017-05-18 2018-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート
JP2023077334A Active JP7843731B2 (ja) 2017-05-18 2023-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2023077334A Active JP7843731B2 (ja) 2017-05-18 2023-05-09 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Country Status (17)

Country Link
US (3) US20180334426A1 (https=)
EP (1) EP3625209A1 (https=)
JP (2) JP7728636B2 (https=)
KR (2) KR102713173B1 (https=)
CN (1) CN111065622A (https=)
AU (1) AU2018269568B2 (https=)
BR (1) BR112019023990A2 (https=)
CA (2) CA3247217A1 (https=)
CL (2) CL2019003270A1 (https=)
CO (1) CO2019014286A2 (https=)
EA (1) EA201900562A1 (https=)
IL (1) IL270595B2 (https=)
MA (1) MA47392B1 (https=)
MX (1) MX2019013693A (https=)
PH (1) PH12019502576A1 (https=)
WO (1) WO2018213082A1 (https=)
ZA (1) ZA201907599B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023113639A (ja) * 2017-05-18 2023-08-16 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 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES3046537T3 (en) 2016-11-08 2025-12-02 Regeneron Pharma Steroids and protein-conjugates thereof
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
MX2020004691A (es) * 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
SG11202006510XA (en) 2018-01-08 2020-08-28 Regeneron Pharma Steroids and antibody-conjugates thereof
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
IL283313B2 (en) 2018-11-20 2025-08-01 Regeneron Pharma Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists
BR112021013464A2 (pt) * 2019-01-08 2021-09-21 Regeneron Pharmaceuticals, Inc. Ligantes sem traço e conjugados de proteína dos mesmos
CN115968304A (zh) 2020-04-16 2023-04-14 瑞泽恩制药公司 狄尔斯-阿尔德缀合方法
EP4172141A1 (en) * 2020-06-26 2023-05-03 Synaffix B.V. Methods for the preparation of linker payload constructs
CN116390771A (zh) * 2020-07-13 2023-07-04 瑞泽恩制药公司 与蛋白中的谷氨酰胺残基缀合的喜树碱类似物及其用途
US20220143194A1 (en) 2020-11-10 2022-05-12 Regeneron Pharmaceuticals, Inc. Selenium antibody conjugates
CN112661783B (zh) * 2020-12-28 2022-06-07 中国林业科学研究院林产化学工业研究所 一种硅氧烷二元松香基苯并环丁烯单体及其制备方法和应用
CN115006390B (zh) * 2022-06-27 2024-04-19 国药集团动物保健股份有限公司 一种病毒减毒制剂、其制备方法以及应用

Citations (3)

* 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
JP2008503547A (ja) 2004-06-24 2008-02-07 ガラパゴス・ナムローゼ・フェンノートシャップ 骨ホメオスタシスを促進させる方法及び組成物

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
US7238791B1 (en) * 2005-12-16 2007-07-03 Roche Diagnostics Operations, Inc. 6-monoacetylmorphine derivatives useful in immunoassay
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
EP2167963B1 (en) 2007-05-23 2019-04-17 Ventana Medical Systems, Inc. Polymeric carriers for immunohistochemistry and in situ hybridization
SG189817A1 (en) 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers
SI2528625T1 (sl) 2010-04-15 2013-11-29 Spirogen Sarl Pirolobenzodiazepini in njihovi konjugati
US20130244905A1 (en) 2010-07-06 2013-09-19 Ed Grabczyk Reporter for RNA Polymerase II Termination
EA201390575A1 (ru) 2010-10-29 2014-01-30 Иммьюноджен, Инк. Неантагонистические egfr-связывающие молекулы и их иммуноконъюгаты
CN110078789A (zh) 2011-05-27 2019-08-02 Ambrx 公司 含有非天然氨基酸连接的海兔毒素衍生物的组合物、涉及该海兔毒素衍生物的方法及其用途
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
BR112014009070B1 (pt) 2011-10-14 2021-11-23 Medimmune Limited Método de síntese e intermediários úteis na preparação de pirrolobenzo-diazepinas
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
CN103997893B (zh) 2011-10-14 2019-04-12 西雅图基因公司 吡咯并苯并二氮杂卓和靶向结合物
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
CN105142672B (zh) 2012-10-23 2019-04-05 西纳福克斯股份有限公司 经修饰的抗体、抗体-缀合物及其制备方法
CN105814083A (zh) * 2013-10-15 2016-07-27 加州生物医学研究所 嵌合抗原受体t细胞开关和其用途
WO2015189478A1 (en) 2014-06-13 2015-12-17 Glykos Finland Oy Payload-polymer-protein conjugates
US10588980B2 (en) * 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
US20160324981A1 (en) * 2015-05-08 2016-11-10 The California Institute For Biomedical Research Liver x receptor agonists and uses thereof
EP3419670A2 (en) 2016-02-26 2019-01-02 Regeneron Pharmaceuticals, Inc. Optimized transglutaminase site-specific antibody conjugation
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
WO2018213082A1 (en) * 2017-05-18 2018-11-22 Regeneron Pharmaceuticals, Inc. Bis-octahydrophenanthrene carboxamides and protein conjugates thereof
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

Patent Citations (3)

* 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
JP2008503547A (ja) 2004-06-24 2008-02-07 ガラパゴス・ナムローゼ・フェンノートシャップ 骨ホメオスタシスを促進させる方法及び組成物

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Bioorg.Med.Chem.Lett.,(2005),15,pp.2824-2828
CAN.J.CHEM.,(1973),51,pp.3236-3241
DATABASE REGISTRY [online] CHEMICAL ABSTRACT SERVICE, US; Retrieved from STN,1984年11月16日,RN=53404-26-5
J.Med.Chem.,(2014),57,pp.7182-7205
Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii),(1999),35(1),pp.41-55

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023113639A (ja) * 2017-05-18 2023-08-16 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 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート
JP7843731B2 (ja) 2017-05-18 2026-04-10 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 ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート

Also Published As

Publication number Publication date
CA3063872A1 (en) 2018-11-22
US20250270163A1 (en) 2025-08-28
JP2020520926A (ja) 2020-07-16
KR20240150809A (ko) 2024-10-16
MX2019013693A (es) 2020-01-27
KR20200008579A (ko) 2020-01-28
KR102713173B1 (ko) 2024-10-07
AU2018269568A1 (en) 2020-01-16
WO2018213082A1 (en) 2018-11-22
US20180334426A1 (en) 2018-11-22
IL270595A (https=) 2019-12-31
EA201900562A1 (ru) 2020-05-12
CN111065622A (zh) 2020-04-24
CL2019003270A1 (es) 2020-05-08
US12338199B2 (en) 2025-06-24
JP2023113639A (ja) 2023-08-16
MA47392B1 (fr) 2021-09-30
US20220112158A1 (en) 2022-04-14
JP7843731B2 (ja) 2026-04-10
IL270595B2 (en) 2023-09-01
PH12019502576A1 (en) 2020-09-28
AU2018269568B2 (en) 2022-03-24
MA47392A1 (fr) 2020-10-28
ZA201907599B (en) 2026-01-28
CO2019014286A2 (es) 2020-04-01
CL2024002173A1 (es) 2024-12-20
IL270595B1 (en) 2023-05-01
EP3625209A1 (en) 2020-03-25
CA3247217A1 (en) 2025-11-29
BR112019023990A2 (pt) 2020-06-16

Similar Documents

Publication Publication Date Title
JP7843731B2 (ja) ビス－オクタヒドロフェナントレンカルボキサミド及びそのタンパク質コンジュゲート
JP7702866B2 (ja) 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
JP7824992B2 (ja) 抗ｍｓｒ１抗体及びその使用方法
JP7426931B2 (ja) 抗体薬物コンジュゲートのための親水性リンカー
JP7617974B2 (ja) シクロデキストリンタンパク質薬物コンジュゲート
JP2025069133A (ja) 無痕跡型リンカー及びそのタンパク質－コンジュゲート
JP7590328B2 (ja) ツブリシン及びタンパク質－ツブリシンコンジュゲート
JP2023533218A (ja) ツブリシン及びタンパク質－ツブリシンコンジュゲート
KR20260038273A (ko) 링커-약물 분자 및 항체 약물 접합체, 이의 제조 방법 및 용도
HK40116735A (en) Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof
EA049882B1 (ru) Производные бис-октагидрофенантренкарбоксамида и их белковые конъюгаты
HK40060716B (en) Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists
HK40060716A (en) Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists
EA047045B1 (ru) Бис-октагидрофенантрена карбоксамиды и их белковые конъюгаты

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200318

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210507

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210507

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210517

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220217

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220329

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220622

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220928

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20230110

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230509

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20230510

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20230526

A912 Re-examination (zenchi) completed and case transferred to appeal board

Free format text: JAPANESE INTERMEDIATE CODE: A912

Effective date: 20230714

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250131

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250529

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250813

R150 Certificate of patent or registration of utility model

Ref document number: 7728636

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150