JOP20190181A1 - مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل - Google Patents

مركب برولين أميد به استبدال بواسطة فينيل داي فلوروميثيل

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Publication number
JOP20190181A1
JOP20190181A1 JOP/2019/0181A JOP20190181A JOP20190181A1 JO P20190181 A1 JOP20190181 A1 JO P20190181A1 JO P20190181 A JOP20190181 A JO P20190181A JO P20190181 A1 JOP20190181 A1 JO P20190181A1
Authority
JO
Jordan
Prior art keywords
cathepsin
compound
phenyldifluoromethyl
present
inhibitory effect
Prior art date
Application number
JOP/2019/0181A
Other languages
English (en)
Inventor
Matsumoto Shunichiro
Harayama Yu
Yamamoto Eriko
Tsuchiya Kazuyuki
Imada Sunao
Nakajima Yutaka
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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (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 true JOP20190181A1 (ar) 2019-07-22
JOP20190181B1 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) CN110248925B (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
WO2018119142A1 (en) 2016-12-21 2018-06-28 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
US7375134B2 (en) * 2002-03-05 2008-05-20 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
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。
SI2421826T1 (sl) * 2009-04-20 2014-02-28 F. Hoffmann-La Roche Ag Derivati prolina kot inhibitorji katepsina
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
CN103930400B (zh) * 2011-11-11 2016-04-20 霍夫曼-拉罗奇有限公司 制备1-酰基-4-苯基磺酰基脯氨酰胺衍生物的方法及中间体
CA2859928A1 (en) * 2012-02-17 2013-08-22 F. Hoffmann-La Roche Ag Novel pyrrolidine derivatives
TW201412728A (zh) 2012-08-21 2014-04-01 Hoffmann La Roche 新穎吡啶衍生物
WO2015051479A1 (en) * 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015054089A1 (en) * 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
DK3419970T3 (da) 2016-02-26 2020-03-02 H Hoffmann La Roche Ag Hidtil ukendte pyridinderivater

Also Published As

Publication number Publication date
AU2018211735B2 (en) 2021-08-12
SI3575284T1 (sl) 2021-11-30
AU2018211735A1 (en) 2019-08-01
ZA201904741B (en) 2020-12-23
CA3050224A1 (en) 2018-08-02
EP3575284B1 (en) 2021-08-25
SG11201906777TA (en) 2019-08-27
RU2019122734A3 (ar) 2021-05-31
EP3575284A1 (en) 2019-12-04
CN110248925A (zh) 2019-09-17
BR112019014788A2 (pt) 2020-02-27
IL268060B (en) 2021-09-30
UA124036C2 (uk) 2021-07-07
US10322997B2 (en) 2019-06-18
HUE056920T2 (hu) 2022-03-28
TW201840531A (zh) 2018-11-16
JOP20190181B1 (ar) 2023-09-17
CN110248925B (zh) 2020-07-17
MA47380A (fr) 2021-03-17
KR102553613B1 (ko) 2023-07-07
PL3575284T3 (pl) 2021-12-27
US20190071398A1 (en) 2019-03-07
US10532979B2 (en) 2020-01-14
LT3575284T (lt) 2021-10-25
ES2892400T3 (es) 2022-02-04
TWI764976B (zh) 2022-05-21
CO2019009090A2 (es) 2019-08-30
CN111574422B (zh) 2023-09-08
CN111574422A (zh) 2020-08-25
PT3575284T (pt) 2021-10-01
JP7001068B2 (ja) 2022-01-19
MY195587A (en) 2023-02-02
MX2019008756A (es) 2019-09-11
DK3575284T3 (da) 2021-10-18
PH12019501645A1 (en) 2020-03-09
WO2018139438A1 (ja) 2018-08-02
CY1124906T1 (el) 2023-01-05
KR20190110549A (ko) 2019-09-30
RU2019122734A (ru) 2021-02-26
IL268060A (en) 2019-09-26
JPWO2018139438A1 (ja) 2019-11-07
MX379651B (es) 2025-03-11
HRP20211613T1 (hr) 2022-02-04
AR110767A1 (es) 2019-05-02
RS62477B1 (sr) 2021-11-30
EP3575284A4 (en) 2020-08-12
US20190248738A1 (en) 2019-08-15

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