JP7624922B2 - 胃腸疾患の治療のためのjak1経路阻害剤 - Google Patents

胃腸疾患の治療のためのjak1経路阻害剤 Download PDF

Info

Publication number
JP7624922B2
JP7624922B2 JP2021535585A JP2021535585A JP7624922B2 JP 7624922 B2 JP7624922 B2 JP 7624922B2 JP 2021535585 A JP2021535585 A JP 2021535585A JP 2021535585 A JP2021535585 A JP 2021535585A JP 7624922 B2 JP7624922 B2 JP 7624922B2
Authority
JP
Japan
Prior art keywords
azetidin
acetonitrile
pharma
pyrimidin
trifluoromethyl
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
JP2021535585A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022514089A (ja
JPWO2020132210A5 (enExample
Inventor
イェレスワラム,クリシュナスワミー
スミス,ポール
エフ ホリス,グレゴリー
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Incyte Corp
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of JP2022514089A publication Critical patent/JP2022514089A/ja
Publication of JPWO2020132210A5 publication Critical patent/JPWO2020132210A5/ja
Application granted granted Critical
Publication of JP7624922B2 publication Critical patent/JP7624922B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021535585A 2018-12-19 2019-12-19 胃腸疾患の治療のためのjak1経路阻害剤 Active JP7624922B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862781877P 2018-12-19 2018-12-19
US62/781,877 2018-12-19
US201962854801P 2019-05-30 2019-05-30
US62/854,801 2019-05-30
US201962901377P 2019-09-17 2019-09-17
US62/901,377 2019-09-17
PCT/US2019/067418 WO2020132210A1 (en) 2018-12-19 2019-12-19 Jak1 pathway inhibitors for the treatment of gastrointestinal disease

Publications (3)

Publication Number Publication Date
JP2022514089A JP2022514089A (ja) 2022-02-09
JPWO2020132210A5 JPWO2020132210A5 (enExample) 2022-12-26
JP7624922B2 true JP7624922B2 (ja) 2025-01-31

Family

ID=69326646

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021535585A Active JP7624922B2 (ja) 2018-12-19 2019-12-19 胃腸疾患の治療のためのjak1経路阻害剤

Country Status (14)

Country Link
US (2) US11596632B2 (enExample)
EP (1) EP3897627A1 (enExample)
JP (1) JP7624922B2 (enExample)
KR (1) KR20210116487A (enExample)
CN (1) CN113692278A (enExample)
AU (1) AU2019403304B2 (enExample)
CA (1) CA3123596A1 (enExample)
IL (1) IL284034A (enExample)
MA (1) MA54544A (enExample)
MX (1) MX2021007260A (enExample)
PH (1) PH12021551455A1 (enExample)
SG (1) SG11202106470TA (enExample)
TW (1) TWI884142B (enExample)
WO (1) WO2020132210A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
US11021482B2 (en) 2018-08-10 2021-06-01 Adaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
KR20210109522A (ko) 2018-10-31 2021-09-06 인사이트 코포레이션 혈액 질환의 치료를 위한 병용 요법
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제
IL285999B1 (en) 2019-03-05 2025-09-01 Incyte Corp JAK1 inhibitor pathway for the treatment of chronic lung allograft dysfunction
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
US20240307396A1 (en) * 2021-06-07 2024-09-19 The Regents Of The University Of California Compositions and methods for treating celiac disease
WO2024102778A1 (en) * 2022-11-08 2024-05-16 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of itk mediated conditions
WO2025144781A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Crystalline polymorph of an itk inhibitor
CN120699157B (zh) * 2025-07-16 2025-12-16 安康市中心医院 一种治疗溃疡性结肠炎的恢复肠屏障功能抗体及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013522214A (ja) 2010-03-10 2013-06-13 インサイト・コーポレイション Jak1阻害剤としてのピペリジン−4−イルアゼチジン誘導体
WO2017091544A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
WO2018112245A1 (en) 2016-12-14 2018-06-21 Progenity Inc. Treatment of a disease of the gastrointestinal tract with a jak inhibitor and devices

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01013458A (es) 1999-06-25 2002-07-30 Genentech Inc Anticuerpos humanizados anti-erbb2 y tratamiento con anticuerpos anti-erbb2.
ES2225624T3 (es) 2000-06-28 2005-03-16 Smithkline Beecham Plc Procedimiento de molienda por via humeda.
US20040132101A1 (en) 2002-09-27 2004-07-08 Xencor Optimized Fc variants and methods for their generation
EP2263691B1 (en) 2002-07-15 2012-08-29 F.Hoffmann-La Roche Ag Treatment of cancer with the recombinant humanized monoclonal anti-erbb2 antibody 2C4 (rhuMAb 2C4)
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
BR112015009942A2 (pt) 2012-11-01 2017-07-11 Incyte Corp derivados de tiofeno fundidos tricíclicos como inibidores de jak
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備jak抑制劑之方法及中間物
WO2014186706A1 (en) 2013-05-17 2014-11-20 Incyte Corporation Bipyrazole derivatives as jak inhibitors
MX394928B (es) 2013-08-07 2025-03-24 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
WO2018111327A1 (en) * 2016-12-14 2018-06-21 Progenity Inc. Methods and ingestible devices for the regio-specific release of jak inhibitors at the site of gastrointestinal tract disease
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013522214A (ja) 2010-03-10 2013-06-13 インサイト・コーポレイション Jak1阻害剤としてのピペリジン−4−イルアゼチジン誘導体
WO2017091544A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
WO2018112245A1 (en) 2016-12-14 2018-06-21 Progenity Inc. Treatment of a disease of the gastrointestinal tract with a jak inhibitor and devices

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MARJORIE ARGOLLO; ET AL,NOVEL THERAPEUTIC TARGETS FOR INFLAMMATORY BOWEL DISEASE,JOURNAL OF AUTOIMMUNITY,2017年07月12日,VOL:85,PAGE(S):103-116,http://dx.doi.org/10.1016/j.jaut.2017.07.004
WILLIAM J. SANDBORN; ET AL,TOFACITINIB, AN ORAL JANUS KINASE INHIBITOR, IN ACTIVE ULCERATIVE COLITIS,THE NEW ENGLAND JOURNAL OF MEDICINE,米国,MASSACHUSETTS MEDICAL SOCIETY,2012年07月31日,VOL:367, NR:7,PAGE(S):616-624,http://dx.doi.org/10.1056/NEJMoa1112168

Also Published As

Publication number Publication date
TW202038944A (zh) 2020-11-01
WO2020132210A1 (en) 2020-06-25
SG11202106470TA (en) 2021-07-29
US20230172939A1 (en) 2023-06-08
US20200197399A1 (en) 2020-06-25
KR20210116487A (ko) 2021-09-27
EP3897627A1 (en) 2021-10-27
JP2022514089A (ja) 2022-02-09
US12150943B2 (en) 2024-11-26
TWI884142B (zh) 2025-05-21
AU2019403304A1 (en) 2021-07-08
AU2019403304B2 (en) 2025-09-04
PH12021551455A1 (en) 2022-04-18
US11596632B2 (en) 2023-03-07
MX2021007260A (es) 2021-09-08
MA54544A (fr) 2021-10-27
CN113692278A (zh) 2021-11-23
CA3123596A1 (en) 2020-06-25
IL284034A (en) 2021-08-31

Similar Documents

Publication Publication Date Title
JP7624922B2 (ja) 胃腸疾患の治療のためのjak1経路阻害剤
KR102830476B1 (ko) 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
US11844801B2 (en) Oral compositions of MK2 pathway inhibitor for treatment of immune conditions
JP2025087734A (ja) 慢性肺同種移植片機能不全の治療のためのjak1経路阻害剤
JP2022533368A (ja) Mk2媒介性障害の治療方法
JP2016516815A (ja) 1−エチル−7−(2−メチル−6−(1H−1,2,4−トリアゾール−3−イル)ピリジン−3−イル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オンに関する医薬製剤、プロセス、固形形態、及び使用方法
EP3508487A1 (en) PYRAZOLO[1,5-a]PYRIMIDINE COMPOUND
JP2023506118A (ja) 皮膚エリテマトーデス及び扁平苔癬(lp)の治療のためのjak1阻害剤の使用
KR20240009964A (ko) 결절성 양진 치료를 위한 jak1 경로 억제제
EA048119B1 (ru) Ингибиторы пути jak1 для лечения заболевания желудочно-кишечного тракта
US20240307353A1 (en) Jak1 pathway inhibitors for the treatment of asthma
CN119816304A (zh) Nlrp3抑制剂的给药方案
EA042956B1 (ru) Ингибиторы пути jak1, предназначенные для лечения связанных с цитокинами нарушений
JP2004083499A (ja) 早産防止剤

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221216

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20221216

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240109

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20240408

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240606

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240827

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20241126

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: 20250114

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20250121

R150 Certificate of patent or registration of utility model

Ref document number: 7624922

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150