KR102205914B1 - IL-12, IL-23 및/또는 IFNα의 조절에 유용한 알킬 아미드-치환된 피리미딘 화합물 - Google Patents

IL-12, IL-23 및/또는 IFNα의 조절에 유용한 알킬 아미드-치환된 피리미딘 화합물 Download PDF

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KR102205914B1
KR102205914B1 KR1020157011660A KR20157011660A KR102205914B1 KR 102205914 B1 KR102205914 B1 KR 102205914B1 KR 1020157011660 A KR1020157011660 A KR 1020157011660A KR 20157011660 A KR20157011660 A KR 20157011660A KR 102205914 B1 KR102205914 B1 KR 102205914B1
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KR20150079678A (ko
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조세프 비. 산텔라
리안 엠. 모슬린
데이비드 에스. 웨인스테인
스테펜 티. 로블스키
존 에스. 토카르스키
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브리스톨-마이어스 스큅 컴퍼니
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4

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  • Chemical & Material Sciences (AREA)
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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Enzymes And Modification Thereof (AREA)
KR1020157011660A 2012-11-08 2013-11-07 IL-12, IL-23 및/또는 IFNα의 조절에 유용한 알킬 아미드-치환된 피리미딘 화합물 Active KR102205914B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261723827P 2012-11-08 2012-11-08
US61/723,827 2012-11-08
PCT/US2013/068866 WO2014074670A1 (en) 2012-11-08 2013-11-07 ALKYL AMIDE-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL IN THE MODULATION OF IL-12, IL-23 AND/OR IFNα

Publications (2)

Publication Number Publication Date
KR20150079678A KR20150079678A (ko) 2015-07-08
KR102205914B1 true KR102205914B1 (ko) 2021-01-20

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KR1020157011660A Active KR102205914B1 (ko) 2012-11-08 2013-11-07 IL-12, IL-23 및/또는 IFNα의 조절에 유용한 알킬 아미드-치환된 피리미딘 화합물

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US (1) US9540333B2 (enExample)
EP (1) EP2917186B1 (enExample)
JP (1) JP6266639B2 (enExample)
KR (1) KR102205914B1 (enExample)
CN (1) CN104903301B (enExample)
AU (1) AU2013341195B2 (enExample)
BR (1) BR112015009798A2 (enExample)
CA (1) CA2890935A1 (enExample)
EA (1) EA028052B1 (enExample)
ES (1) ES2648226T3 (enExample)
IL (1) IL238605A (enExample)
MX (1) MX2015005561A (enExample)
SG (1) SG11201503395TA (enExample)
WO (1) WO2014074670A1 (enExample)

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EP2922846B1 (en) 2012-11-08 2018-10-03 Bristol-Myers Squibb Company Amide-substituted heterocyclic compounds useful as modulators of il-12, il-23 and/or ifn-alpha
TWI582077B (zh) 2013-11-07 2017-05-11 必治妥美雅史谷比公司 作爲IL-12、IL-23及/或IFNα反應調節劑之經烷基-醯胺取代之吡啶化合物
CN105992768B (zh) 2013-12-10 2018-04-20 百时美施贵宝公司 用作IL‑12、IL‑23和/或IFNα响应的调节剂的咪唑并哒嗪化合物
KR102477063B1 (ko) * 2016-10-28 2022-12-12 브리스톨-마이어스 스큅 컴퍼니 Il-12, il-23 및/또는 ifn 알파 반응의 조정제로서 유용한 헤테로비시클릭 화합물
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
CN107857754B (zh) * 2018-01-15 2018-11-09 泰山医学院 一种化合物及其在制备预防/治疗类风湿性关节炎药物中的应用
AR117398A1 (es) 2018-03-12 2021-08-04 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa 2
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CN114269336A (zh) 2019-04-30 2022-04-01 细胞基因公司 包含阿普斯特和tyk2抑制剂的联合疗法
EP3944859A1 (en) 2020-07-30 2022-02-02 Assistance Publique Hôpitaux de Paris Method for treating immune toxicities induced by immune checkpoint inhibitors
TW202246232A (zh) 2021-02-19 2022-12-01 英商蘇多生物科學有限公司 Tyk2抑制劑及其用途
TW202246233A (zh) 2021-02-19 2022-12-01 英商蘇多生物科學有限公司 Tyk2抑制劑及其用途
CA3236262A1 (en) 2021-10-25 2023-05-04 Isaac Marx Tyk2 degraders and uses thereof
WO2024257023A1 (en) 2023-06-14 2024-12-19 Alembic Pharmaceuticals Limited Tyk2 pseudokinase ligands and uses thereof

Citations (3)

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WO2004002964A1 (ja) 2002-06-28 2004-01-08 Yamanouchi Pharmaceutical Co., Ltd. ジアミノピリミジンカルボキサミド誘導体
WO2006035069A1 (en) 2004-09-30 2006-04-06 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-substituted pyrimidines
WO2011065800A2 (ko) * 2009-11-30 2011-06-03 주식회사 오스코텍 피리미딘 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물

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GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
KR20050019797A (ko) * 2002-06-28 2005-03-03 야마노우치세이야쿠 가부시키가이샤 디아미노피리미딘카르복사미드 유도체
ATE540035T1 (de) * 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
ES2465666T3 (es) * 2006-03-30 2014-06-06 Janssen R&D Ireland Pirimidinas 5-amido-sustituidas inhibidoras del HIV
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
EP2321283B1 (en) * 2008-04-16 2016-07-13 Portola Pharmaceuticals, Inc. 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
CA2728893C (en) * 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. Inhibitors of syk protein kinase
US20110071158A1 (en) * 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
AR076550A1 (es) * 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (jak)
EP2440204B1 (en) * 2009-06-12 2013-12-18 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
AU2012245387C1 (en) * 2011-04-22 2016-05-05 Signal Pharmaceuticals, Llc Substituted Diaminocarboxamide and Diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
WO2014074660A1 (en) 2012-11-08 2014-05-15 Bristol-Myers Squibb Company ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNα RESPONSES
EP2922846B1 (en) 2012-11-08 2018-10-03 Bristol-Myers Squibb Company Amide-substituted heterocyclic compounds useful as modulators of il-12, il-23 and/or ifn-alpha
TWI582077B (zh) 2013-11-07 2017-05-11 必治妥美雅史谷比公司 作爲IL-12、IL-23及/或IFNα反應調節劑之經烷基-醯胺取代之吡啶化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004002964A1 (ja) 2002-06-28 2004-01-08 Yamanouchi Pharmaceutical Co., Ltd. ジアミノピリミジンカルボキサミド誘導体
WO2006035069A1 (en) 2004-09-30 2006-04-06 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-substituted pyrimidines
WO2011065800A2 (ko) * 2009-11-30 2011-06-03 주식회사 오스코텍 피리미딘 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물

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Publication number Publication date
EP2917186A1 (en) 2015-09-16
JP6266639B2 (ja) 2018-01-24
SG11201503395TA (en) 2015-05-28
AU2013341195B2 (en) 2017-09-21
IL238605A (en) 2017-05-29
MX2015005561A (es) 2015-07-23
AU2013341195A1 (en) 2015-07-02
BR112015009798A2 (pt) 2017-07-11
EA201590911A1 (ru) 2015-10-30
JP2016501185A (ja) 2016-01-18
EP2917186B1 (en) 2017-10-18
US9540333B2 (en) 2017-01-10
US20150299139A1 (en) 2015-10-22
ES2648226T3 (es) 2017-12-29
KR20150079678A (ko) 2015-07-08
WO2014074670A1 (en) 2014-05-15
CN104903301A (zh) 2015-09-09
EA028052B1 (ru) 2017-10-31
IL238605A0 (en) 2015-06-30
CA2890935A1 (en) 2014-05-15
CN104903301B (zh) 2017-08-29

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