JOP20190181B1 - مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل - Google Patents

مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل

Info

Publication number
JOP20190181B1
JOP20190181B1 JOP/2019/0181A JOP20190181A JOP20190181B1 JO P20190181 B1 JOP20190181 B1 JO P20190181B1 JO P20190181 A JOP20190181 A JO P20190181A JO P20190181 B1 JOP20190181 B1 JO P20190181B1
Authority
JO
Jordan
Prior art keywords
cathepsin
phenyldifluoromethyl
present
useful
inhibitory effect
Prior art date
Application number
JOP/2019/0181A
Other languages
English (en)
Inventor
Nakajima Yutaka
Yamamoto Eriko
Imada Sunao
Matsumoto Shunichiro
Tsuchiya Kazuyuki
Harayama Yu
Original Assignee
Astellas Pharma Inc
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 Astellas Pharma Inc filed Critical Astellas Pharma Inc
Publication of JOP20190181A1 publication Critical patent/JOP20190181A1/ar
Application granted granted Critical
Publication of JOP20190181B1 publication Critical patent/JOP20190181B1/ar

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

[المشكلة] توفير مركب مفيد كمثبط كاثيبسين S [وسيلة الحل] لقد فحص المخترعون الحاليون مركباً له تأثير ثبيطي على كاثيبسين S ويعد مفيداً كمكون فعال لتركيبة صيدلانية للوقاية من و/أوعلاج مرض مناعة ذاتية يشمل ذئبة حمراء جهازية (SLE)، والتهاب كلية ذئبي، أنواع حساسية، أو رفض طعم لعضو، نخاع عظم أو نسيج، ووجدوا أن مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل للاختراع الحالي له تأثير تثبيطي على كاثبيسين S، وبالتالي أكملوا الاختراع الحالي. مركب برولين أميد الذي به استبدال بواسطة فينيل داي فلوروميثيل للاختراع الحالي له تأثير تثبيطي على كاثيبسين S ويعد مفيداً كعامل للوقاية من و/أوعلاج مرض مناعة ذاتية يشمل يشمل SLE والتهاب كلية، أنواع حساسية، أو رفض طعم لعضو، نخاع عظم أو نسيج.
JOP/2019/0181A 2017-01-24 2018-01-23 مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل JOP20190181B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2017010321 2017-01-24
PCT/JP2018/001927 WO2018139438A1 (ja) 2017-01-24 2018-01-23 フェニルジフルオロメチル置換プロリンアミド化合物

Publications (2)

Publication Number Publication Date
JOP20190181A1 JOP20190181A1 (ar) 2019-07-22
JOP20190181B1 true JOP20190181B1 (ar) 2023-09-17

Family

ID=62979051

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2019/0181A JOP20190181B1 (ar) 2017-01-24 2018-01-23 مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل

Country Status (31)

Country Link
US (2) US10322997B2 (ar)
EP (1) EP3575284B1 (ar)
JP (1) JP7001068B2 (ar)
KR (1) KR102553613B1 (ar)
CN (2) CN111574422B (ar)
AR (1) AR110767A1 (ar)
AU (1) AU2018211735B2 (ar)
BR (1) BR112019014788A2 (ar)
CA (1) CA3050224A1 (ar)
CO (1) CO2019009090A2 (ar)
CY (1) CY1124906T1 (ar)
DK (1) DK3575284T3 (ar)
ES (1) ES2892400T3 (ar)
HR (1) HRP20211613T1 (ar)
HU (1) HUE056920T2 (ar)
IL (1) IL268060B (ar)
JO (1) JOP20190181B1 (ar)
LT (1) LT3575284T (ar)
MA (1) MA47380A (ar)
MX (1) MX379651B (ar)
MY (1) MY195587A (ar)
PH (1) PH12019501645A1 (ar)
PL (1) PL3575284T3 (ar)
PT (1) PT3575284T (ar)
RS (1) RS62477B1 (ar)
SG (1) SG11201906777TA (ar)
SI (1) SI3575284T1 (ar)
TW (1) TWI764976B (ar)
UA (1) UA124036C2 (ar)
WO (1) WO2018139438A1 (ar)
ZA (1) ZA201904741B (ar)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2312861C2 (ru) * 2002-03-05 2007-12-20 Мерк Фросст Кэнада Лтд. Ингибиторы катепсин-цистеинпротеазы
JP2010121918A (ja) 2008-11-17 2010-06-03 Hiroyoshi Asada 鍋等の取っ手部分の焼き焦げ防止具。
MX2011011094A (es) * 2009-04-20 2011-11-04 Hoffmann La Roche Derivados de prolina como inhibidores de catepsina.
US7893099B2 (en) * 2009-06-11 2011-02-22 Hoffman-La Roche Inc. Cyclopentane derivatives
JP2012059507A (ja) 2010-09-08 2012-03-22 Panasonic Corp 基板間接続コネクタ構造
US8524710B2 (en) 2010-11-05 2013-09-03 Hoffmann-La Roche Inc. Pyrrolidine derivatives
AU2012334123B2 (en) * 2011-11-11 2016-12-15 F. Hoffmann-La Roche Ag Process for the preparation of 1-acyl-4-phenylsulfonylprolinamide derivatives and new intermediates
CN104114549A (zh) * 2012-02-17 2014-10-22 霍夫曼-拉罗奇有限公司 新型吡咯烷衍生物
SG11201500900YA (en) 2012-08-21 2015-03-30 Hoffmann La Roche Novel pyridine derivatives
RU2692799C2 (ru) * 2013-10-08 2019-06-27 Мерк Шарп И Доум Корп. Ингибиторы цистеинпротеаз катепсинов
WO2015051479A1 (en) * 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
SI3419970T1 (sl) 2016-02-26 2020-04-30 F. Hoffmann-La Roche Ag Novi pirolidinski derivati

Also Published As

Publication number Publication date
EP3575284A1 (en) 2019-12-04
KR102553613B1 (ko) 2023-07-07
WO2018139438A1 (ja) 2018-08-02
AU2018211735A1 (en) 2019-08-01
PH12019501645A1 (en) 2020-03-09
EP3575284B1 (en) 2021-08-25
SI3575284T1 (sl) 2021-11-30
PL3575284T3 (pl) 2021-12-27
CY1124906T1 (el) 2023-01-05
US20190071398A1 (en) 2019-03-07
US10322997B2 (en) 2019-06-18
MY195587A (en) 2023-02-02
IL268060A (en) 2019-09-26
AR110767A1 (es) 2019-05-02
CN110248925A (zh) 2019-09-17
DK3575284T3 (da) 2021-10-18
RS62477B1 (sr) 2021-11-30
JPWO2018139438A1 (ja) 2019-11-07
MX379651B (es) 2025-03-11
US10532979B2 (en) 2020-01-14
CN111574422B (zh) 2023-09-08
EP3575284A4 (en) 2020-08-12
KR20190110549A (ko) 2019-09-30
CN110248925B (zh) 2020-07-17
CO2019009090A2 (es) 2019-08-30
PT3575284T (pt) 2021-10-01
MA47380A (fr) 2021-03-17
AU2018211735B2 (en) 2021-08-12
JOP20190181A1 (ar) 2019-07-22
TW201840531A (zh) 2018-11-16
ZA201904741B (en) 2020-12-23
LT3575284T (lt) 2021-10-25
JP7001068B2 (ja) 2022-01-19
TWI764976B (zh) 2022-05-21
MX2019008756A (es) 2019-09-11
HUE056920T2 (hu) 2022-03-28
SG11201906777TA (en) 2019-08-27
ES2892400T3 (es) 2022-02-04
HRP20211613T1 (hr) 2022-02-04
RU2019122734A (ru) 2021-02-26
IL268060B (en) 2021-09-30
BR112019014788A2 (pt) 2020-02-27
US20190248738A1 (en) 2019-08-15
UA124036C2 (uk) 2021-07-07
CN111574422A (zh) 2020-08-25
RU2019122734A3 (ar) 2021-05-31
CA3050224A1 (en) 2018-08-02

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