CN107849015B - 作为pad4抑制剂的苯并咪唑衍生物 - Google Patents

作为pad4抑制剂的苯并咪唑衍生物 Download PDF

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CN107849015B
CN107849015B CN201680042358.8A CN201680042358A CN107849015B CN 107849015 B CN107849015 B CN 107849015B CN 201680042358 A CN201680042358 A CN 201680042358A CN 107849015 B CN107849015 B CN 107849015B
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methyl
indol
ethyl
benzo
imidazol
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CN107849015A (zh
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D·阿曼斯
S·J·阿特金森
M·D·巴克
M·坎贝尔
H·迪亚洛
C·杜阿特
N·S·加顿
J·利德尔
J·F·勒诺
R·J·谢伯德
A·L·瓦尔克
C·R·维拉威
D·M·威尔逊
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GlaxoSmithKline Intellectual Property Development Ltd
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    • 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
    • C07D401/14Heterocyclic 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 three or more hetero 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
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    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Materials For Medical Uses (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
CN201680042358.8A 2015-05-21 2016-05-19 作为pad4抑制剂的苯并咪唑衍生物 Active CN107849015B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562164906P 2015-05-21 2015-05-21
US62/164,906 2015-05-21
PCT/IB2016/000761 WO2016185279A1 (en) 2015-05-21 2016-05-19 Benzoimidazole derivatives as pad4 inhibitors

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CN107849015A CN107849015A (zh) 2018-03-27
CN107849015B true CN107849015B (zh) 2021-03-19

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US (2) US10407407B2 (enExample)
EP (1) EP3298003B1 (enExample)
JP (1) JP6703553B2 (enExample)
KR (1) KR20180005250A (enExample)
CN (1) CN107849015B (enExample)
AR (1) AR106863A1 (enExample)
AU (1) AU2016264958B2 (enExample)
BR (1) BR112017024678A2 (enExample)
CA (2) CA2986199C (enExample)
EA (1) EA033680B1 (enExample)
ES (1) ES2945314T3 (enExample)
IL (2) IL255666A (enExample)
MX (1) MX387321B (enExample)
TW (1) TW201706263A (enExample)
WO (1) WO2016185279A1 (enExample)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR107032A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
JP6926126B2 (ja) 2016-02-23 2021-08-25 パドロック・セラピューティクス・インコーポレイテッドPadlock Therapeutics, Inc. Pad4のヘテロアリール阻害剤
CN109790162B (zh) * 2016-07-27 2022-06-28 帕德罗科治疗公司 Pad4的共价抑制剂
EP3510025B1 (en) 2016-09-12 2022-06-29 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
IL273428B2 (en) * 2017-09-22 2023-09-01 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
CN111225915B (zh) * 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
BR112020008851A2 (pt) 2017-11-06 2020-10-20 Jubilant Prodel LLC composto da fórmula i, processo de preparação de compostos da fórmula i, composição farmacêutica, método para o tratamento e/ou prevenção de várias doenças, uso, método para o tratamento de câncer, método de tratamento de câncer e método para o tratamento e/ou prevenção de câncer e doenças infecciosas
JP7368369B2 (ja) 2017-11-24 2023-10-24 ジュビラント・エピスクライブ・エルエルシー Prmt5阻害剤としてのヘテロ環式化合物
CN111566105A (zh) 2018-01-08 2020-08-21 豪夫迈·罗氏有限公司 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物
US11453676B2 (en) 2018-02-02 2022-09-27 Forward Therapeutics, Inc. Inhibitors of protein arginine deiminases
JP7279063B6 (ja) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Pd1/pd-l1相互作用/活性化の阻害剤としての二環式化合物
ES2942319T3 (es) 2018-03-22 2023-05-31 Hoffmann La Roche Inhibidores de oxacina monoacilglicerol lipasa (MAGL)
WO2020033490A1 (en) 2018-08-08 2020-02-13 Bristol-Myers Squibb Company Substituted thienopyrroles as pad4 inhibitors
JP7434281B2 (ja) * 2018-08-08 2024-02-20 ブリストル-マイヤーズ スクイブ カンパニー Pad酵素のベンズイミダゾール阻害剤
AU2019318415A1 (en) * 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Substituted benzimidazoles as PAD4 inhibitors
MX2021001565A (es) 2018-08-08 2021-04-19 Bristol Myers Squibb Co Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).
WO2020035425A1 (en) 2018-08-13 2020-02-20 F. Hoffmann-La Roche Ag New heterocyclic compounds as monoacylglycerol lipase inhibitors
HUE067912T2 (hu) 2018-08-13 2024-11-28 Hoffmann La Roche Új heterociklusos vegyületek, mint monoacil-glicerin-lipáz inhibitorok
KR20210094540A (ko) 2018-11-22 2021-07-29 에프. 호프만-라 로슈 아게 헤테로사이클릭 화합물
US20210094971A1 (en) 2019-09-09 2021-04-01 Hoffmann-La Roche Inc. Heterocyclic compounds
CA3151516A1 (en) 2019-09-12 2021-03-18 F. Hoffmann-La Roche Ag 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors
BR112022005472A2 (pt) 2019-09-24 2022-06-14 Hoffmann La Roche Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica
US20210094972A1 (en) 2019-09-24 2021-04-01 Hoffmann-La Roche Inc. Heterocyclic compounds
EP4034602A1 (en) 2019-09-24 2022-08-03 F. Hoffmann-La Roche AG Fluorescent probes for monoacylglycerol lipase (magl)
TW202115083A (zh) * 2019-09-27 2021-04-16 大陸商南京藥捷安康生物科技有限公司 肽醯精胺酸脫亞胺酶抑制劑及其用途
EP4100405A1 (en) 2020-02-06 2022-12-14 Bristol-Myers Squibb Company Macrocyclic pad4 inhibitors useful as immunosuppressant
TW202140477A (zh) * 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑
WO2021174024A1 (en) 2020-02-28 2021-09-02 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
PE20230488A1 (es) * 2020-04-30 2023-03-21 Gilead Sciences Inc Inhibidores macrociclicos de las peptidilarginina deiminasas
JP2023538018A (ja) * 2020-08-12 2023-09-06 ジュビラント・エピパッド・エルエルシー ネトーシスの処置及び/又は予防における使用のための方法及び化合物
CA3190277A1 (en) 2020-09-03 2022-03-10 Joerg Benz Heterocyclic compounds
US12240862B2 (en) 2020-12-22 2025-03-04 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
EP4267562A1 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
US20250136607A1 (en) * 2021-11-15 2025-05-01 Regor Pharmaceuticals, Inc. Pad4 inhibitors and use thereof
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104470919A (zh) * 2012-07-26 2015-03-25 葛兰素集团有限公司 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU570439B2 (en) 1983-03-28 1988-03-17 Compression Labs, Inc. A combined intraframe and interframe transform coding system
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
DE69637257T2 (de) 1995-04-14 2008-06-12 Smithkline Beecham Corp. Verfahren zur Herstellung eines Dosierinhalators
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6448281B1 (en) * 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
EP1441725A1 (en) * 2001-10-26 2004-08-04 Aventis Pharmaceuticals Inc. Benzimidazoles and analogues and their use as protein kinases inhibitors
ES2388434T3 (es) 2003-11-03 2012-10-15 Glaxo Group Limited Dispositivo de administración de fluido
US7429611B2 (en) * 2004-09-23 2008-09-30 Bristol-Myers Squibb Company Indole inhibitors of 15-lipoxygenase
UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
SG10201401169QA (en) * 2009-04-02 2014-05-29 Merck Serono Sa Dihydroorotate dehydrogenase inhibitors
LT3001903T (lt) * 2009-12-21 2018-01-10 Samumed, Llc 1h-pirazolo[3,4-b]piridinai ir jų terapinis panaudojimas
AR107032A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104470919A (zh) * 2012-07-26 2015-03-25 葛兰素集团有限公司 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Inhibition of PADPAD4 activity is sufficient to disrupt mouse and human NET formation;Huw D Lewis,等;《NATURE CHEMICAL BIOLOGY》;20150126;第11卷(第3期);第189-194页,以及补充信息S1第1-33页,S2第1-25页 *

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AR106863A1 (es) 2018-02-28
IL278916A (en) 2021-01-31
US10407407B2 (en) 2019-09-10
CA2986199C (en) 2023-07-18
EP3298003B1 (en) 2023-04-19
JP2018520105A (ja) 2018-07-26
EA201792517A1 (ru) 2018-04-30
EP3298003A1 (en) 2018-03-28
BR112017024678A2 (pt) 2018-07-31
CA3199601A1 (en) 2016-11-24
US20200095227A1 (en) 2020-03-26
TW201706263A (zh) 2017-02-16
EA033680B1 (ru) 2019-11-15
WO2016185279A1 (en) 2016-11-24
ES2945314T3 (es) 2023-06-30
AU2016264958A1 (en) 2017-12-07
JP6703553B2 (ja) 2020-06-03
MX2017014714A (es) 2018-01-25
CN107849015A (zh) 2018-03-27
US10815218B2 (en) 2020-10-27
US20180297983A1 (en) 2018-10-18
IL255666A (en) 2018-01-31
CA2986199A1 (en) 2016-11-24
MX387321B (es) 2025-03-11
AU2016264958B2 (en) 2020-10-29
KR20180005250A (ko) 2018-01-15

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