JP7657151B2 - 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド - Google Patents

代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド Download PDF

Info

Publication number
JP7657151B2
JP7657151B2 JP2021529386A JP2021529386A JP7657151B2 JP 7657151 B2 JP7657151 B2 JP 7657151B2 JP 2021529386 A JP2021529386 A JP 2021529386A JP 2021529386 A JP2021529386 A JP 2021529386A JP 7657151 B2 JP7657151 B2 JP 7657151B2
Authority
JP
Japan
Prior art keywords
phe
ala
glu
ser
gly
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
JP2021529386A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022509184A5 (https=
JP2022509184A (ja
Inventor
ネイサンソン フライヤー，アレク
アレクサンドロヴィチ ゴロソフ，アンドレィ
グロッシュ，フィリップ
ルイス，イアン
ユェジン リゥ，ユージーン
マージンジク，アンドレアス
ギルクリスト モノヴィチ，ローレン
オットル，ヨハンズ
ジェイプラカシュ パテル，タジェシュ
クロフォード リード，パトリック
シーパーソード，モヒンドラ
Original Assignee
ノバルティス アーゲー
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
Application filed by ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2022509184A publication Critical patent/JP2022509184A/ja
Publication of JP2022509184A5 publication Critical patent/JP2022509184A5/ja
Application granted granted Critical
Publication of JP7657151B2 publication Critical patent/JP7657151B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2021529386A 2018-11-27 2019-11-26 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド Active JP7657151B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862772033P 2018-11-27 2018-11-27
US62/772,033 2018-11-27
PCT/IB2019/060203 WO2020110011A1 (en) 2018-11-27 2019-11-26 Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders

Publications (3)

Publication Number Publication Date
JP2022509184A JP2022509184A (ja) 2022-01-20
JP2022509184A5 JP2022509184A5 (https=) 2022-12-06
JP7657151B2 true JP7657151B2 (ja) 2025-04-04

Family

ID=68808461

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021529386A Active JP7657151B2 (ja) 2018-11-27 2019-11-26 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド

Country Status (5)

Country Link
US (1) US12209144B2 (https=)
EP (1) EP3887388A1 (https=)
JP (1) JP7657151B2 (https=)
CN (1) CN113166204B (https=)
WO (1) WO2020110011A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021156792A1 (en) * 2020-02-07 2021-08-12 Novartis Ag Targeted plasma protein degradation
KR20250025685A (ko) * 2022-06-15 2025-02-24 머크 샤프 앤드 돔 엘엘씨 인터류킨-1 베타를 포획하기 위한 시클릭 펩티드

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4889861A (en) 1982-12-21 1989-12-26 Ciba-Geigy Corp. Substituted imidazo[1,5-a]pyridine derivatives and other substituted bicyclic derivatives and their use as aromatase inhibitors
US4617307A (en) 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
US5118666A (en) 1986-05-05 1992-06-02 The General Hospital Corporation Insulinotropic hormone
US5114946A (en) 1987-06-12 1992-05-19 American Cyanamid Company Transdermal delivery of pharmaceuticals
US4818541A (en) 1987-08-19 1989-04-04 Schering Corporation Transdermal delivery of enantiomers of phenylpropanolamine
ATE164852T1 (de) 1990-01-24 1998-04-15 Douglas I Buckley Glp-1-analoga verwendbar in der diabetesbehandlung
US5155100A (en) 1991-05-01 1992-10-13 Ciba-Geigy Corporation Phosphono/biaryl substituted dipeptide derivatives
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5705483A (en) 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
IT1291776B1 (it) 1997-02-07 1999-01-21 Menarini Ricerche Spa Composti monociclici a quattro residui bifunzionali, aventi azione nk-2 antagonista
IT1304888B1 (it) 1998-08-05 2001-04-05 Menarini Ricerche Spa Composti monociclici ad azione nk-2 antagonista e formulazioni che licontengono
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
IT1307809B1 (it) 1999-10-21 2001-11-19 Menarini Ricerche Spa Composti monociclici basici ad azione nk-2 antagonista, processi difabbricazione e formulazioni che li contengono.
HUP0301335A3 (en) 2000-04-12 2006-02-28 Novartis Ag Combination of organic compounds
EP1297826A1 (en) 2001-09-27 2003-04-02 Menarini Ricerche S.p.A. Nasal pharmaceutical compositions containing a NK-2 antagonist
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
WO2003104200A1 (en) 2002-06-07 2003-12-18 Glaxo Group Limited N-mercaptoacyl phenyalanine derivatives, process for their preparation, and pharmaceutical compositions containing them
DK1537114T3 (da) 2002-08-07 2006-11-13 Novartis Ag Organiske forbindelser som midler til behandling af aldosteronmedierede tilstande
CN100447142C (zh) 2002-11-18 2008-12-31 诺瓦提斯公司 咪唑并[1,5a]吡啶衍生物及治疗醛固酮所介导疾病的方法
CA2525764C (en) 2003-05-20 2012-07-17 Novartis Ag N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
CA2568164A1 (en) 2004-05-28 2005-12-15 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
JP5179174B2 (ja) 2004-05-28 2013-04-10 ノバルティス ファーマ アーゲー アルドステロンシンターゼ阻害剤としてのテトラヒドロ−イミダゾ［１，５−ａ］ピリジン誘導体
US7612088B2 (en) 2004-05-28 2009-11-03 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
WO2006005726A2 (en) 2004-07-09 2006-01-19 Speedel Experimenta Ag Heterocyclic compounds
TW200716636A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
TW200716105A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Imidazole compounds
TW200716634A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
TW200804378A (en) 2005-12-09 2008-01-16 Speedel Experimenta Ag Organic compounds
EP2418202B1 (en) 2006-03-31 2014-01-29 Novartis AG (4-[4-[5-(substituted amino)-pyridin-2-yl]phenyl]-cyclohexyl)-acetic acid derivatives as DGAT inhibitors
US20090156875A1 (en) 2006-04-04 2009-06-18 Takafumi Tomioka Methane separation method, methane separation apparatus, and methane utilization system
TW200808813A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808812A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
EP1886695A1 (en) 2006-06-27 2008-02-13 Speedel Experimenta AG Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist
CA2660701A1 (en) 2006-08-25 2008-03-06 Novartis Ag Fused imidazole derivatives for the treatment of disorders mediated by aldosterone synthase and/or 11-beta-hydroxylase and/or aromatase
EA200900811A1 (ru) 2006-12-18 2009-12-30 Новартис Аг Имидазолы в качестве ингибиторов альдостеронсинтазы
EP2094669A2 (en) 2006-12-18 2009-09-02 Novartis AG 1-substituted imidazole derivatives and their use as aldosterone synthase inhibitors
KR20090090395A (ko) 2006-12-18 2009-08-25 노파르티스 아게 4-이미다졸릴-1,2,3,4-테트라히드로퀴놀린 유도체 및 알도스테론/11-베타-히드록실라제 억제제로서의 그의 용도
RU2009139811A (ru) 2007-03-29 2011-05-10 Новартис АГ (CH) Гетероциклические спиросоединения
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
WO2009035543A1 (en) 2007-09-07 2009-03-19 Theravance, Inc. Dual-acting antihypertensive agents
AR066169A1 (es) 2007-09-28 2009-07-29 Novartis Ag Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat
EP2297113A1 (en) 2008-04-29 2011-03-23 Theravance, Inc. Dual-acting antihypertensive agents
AR072297A1 (es) 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
ES2627377T3 (es) 2008-10-23 2017-07-27 Steba Biotech S.A. Peptidomiméticos que contienen RGD y sus usos
WO2010048582A1 (en) 2008-10-24 2010-04-29 Irm Llc Biosynthetically generated pyrroline-carboxy-lysine and site specific protein modifications via chemical derivatization of pyrroline-carboxy-lysine and pyrrolysine residues
NZ596302A (en) 2009-05-15 2014-01-31 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
SG176009A1 (en) 2009-05-28 2011-12-29 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
JP5466759B2 (ja) 2009-05-28 2014-04-09 ノバルティス アーゲー ネプリライシン阻害剤としての置換アミノ酪酸誘導体
JP5640091B2 (ja) 2009-10-01 2014-12-10 カディラ・ヘルスケア・リミテッド 脂質異常症および関連疾患の治療のための化合物
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
JP5999702B2 (ja) 2009-11-23 2016-09-28 パラティン テクノロジーズ, インコーポレイテッドPalatin Technologies, Inc. メラノコルチン−１受容体特異的環状ペプチド
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
HUE028051T2 (hu) 2010-12-15 2016-11-28 Theravance Biopharma R&D Ip Llc Neprilizin inhibitorok
JP5959065B2 (ja) 2011-02-17 2016-08-02 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤としての置換アミノ酪酸誘導体
CN103748070B (zh) 2011-05-31 2015-06-24 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
JP5959074B2 (ja) 2011-05-31 2016-08-02 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
SMT201700306T1 (it) 2012-06-08 2017-07-18 Theravance Biopharma R&D Ip Llc Inibitori di neprilisina
DE102012014480A1 (de) 2012-07-21 2014-01-23 Daimler Ag Aufbau eines Innendekors
MX366149B (es) 2012-08-08 2019-06-28 Theravance Biopharma R&D Ip Llc Inhibidores de neprilisina.
TR201808541T4 (tr) 2013-02-14 2018-07-23 Novartis Ag Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri.
DK2964616T3 (en) 2013-03-05 2017-08-28 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
CN105473141A (zh) 2013-03-15 2016-04-06 实发生物医学公司 治疗和/或预防心血管疾病的抗pcsk9化合物和方法
CA2934898A1 (en) 2014-01-30 2015-08-06 Theravance Biopharma R&D Ip, Llc 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
CA2934936A1 (en) 2014-01-30 2015-08-06 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
TW201823222A (zh) 2016-12-23 2018-07-01 財團法人生物技術開發中心 化合物、醫藥組成物及其用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Circulation，2015年，Vol.132，pp.1648-1666

Also Published As

Publication number Publication date
CN113166204B (zh) 2025-01-28
US12209144B2 (en) 2025-01-28
CN113166204A (zh) 2021-07-23
EP3887388A1 (en) 2021-10-06
WO2020110011A1 (en) 2020-06-04
US20220024981A1 (en) 2022-01-27
JP2022509184A (ja) 2022-01-20

Similar Documents

Publication Publication Date Title
JP7607615B2 (ja) Ｐｃｓｋ９アンタゴニスト化合物
JP6595553B2 (ja) 心不全治療用の合成アペリン模倣物
TW202333563A (zh) 用於治療疾病或障礙之二胺基環戊基吡啶衍生物
KR20070102544A (ko) 유기 화합물의 조합물
JP2019502659A (ja) 大環状広域抗生物質
JP7657151B2 (ja) 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド
KR20070106677A (ko) 유기 화합물의 조합물
JP2022507958A (ja) 代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物
EP3247405B1 (en) Synthetic apelin fatty acid conjugates with improved half-life
US11813306B2 (en) Cyclic tetramer compounds as proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors for the treatment of metabolic disorders
JP2021531308A (ja) 腎障害の処置で使用するための化合物
CN119451944A (zh) Prep结合配体

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221125

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20221125

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230912

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20231208

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20240213

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240312

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240702

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20241001

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20241127

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20241226

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20250311

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250325

R150 Certificate of patent or registration of utility model

Ref document number: 7657151

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150