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PT2877467T - 2-(azaindol-2-il)benzimidazóis como inibidores de pad4 - Google Patents

2-(azaindol-2-il)benzimidazóis como inibidores de pad4

Info

Publication number
PT2877467T
PT2877467T PT127405819T PT12740581T PT2877467T PT 2877467 T PT2877467 T PT 2877467T PT 127405819 T PT127405819 T PT 127405819T PT 12740581 T PT12740581 T PT 12740581T PT 2877467 T PT2877467 T PT 2877467T
Authority
PT
Portugal
Prior art keywords
azaindol
benzimidazoles
pad4 inhibitors
pad4
inhibitors
Prior art date
Application number
PT127405819T
Other languages
English (en)
Inventor
David Barker Michael
Liddle John
Louise Walker Ann
Matthew Wilson David
John Atkinson Stephen
Campbell Matthew
Diallo Hawa
Douault Clement
Stuart Garton Neil
John Sheppard Robert
Wellaway Christopher
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PT2877467T publication Critical patent/PT2877467T/pt

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
    • A61K31/435Heterocyclic 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
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PT127405819T 2012-07-26 2012-07-26 2-(azaindol-2-il)benzimidazóis como inibidores de pad4 PT2877467T (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12740581.9A EP2877467B1 (en) 2012-07-26 2012-07-26 2-(azaindol-2-yl)benzimidazoles as pad4 inhibitors
PCT/EP2012/064649 WO2014015905A1 (en) 2012-07-26 2012-07-26 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors

Publications (1)

Publication Number Publication Date
PT2877467T true PT2877467T (pt) 2017-01-02

Family

ID=49996626

Family Applications (1)

Application Number Title Priority Date Filing Date
PT127405819T PT2877467T (pt) 2012-07-26 2012-07-26 2-(azaindol-2-il)benzimidazóis como inibidores de pad4

Country Status (22)

Country Link
US (4) US9127003B2 (pt)
EP (1) EP2877467B1 (pt)
JP (1) JP6063567B2 (pt)
KR (1) KR101916443B1 (pt)
CN (1) CN104470919B (pt)
AU (1) AU2012386257B2 (pt)
BR (1) BR112015001545B1 (pt)
CA (1) CA2879341C (pt)
CY (1) CY1118524T1 (pt)
DK (1) DK2877467T3 (pt)
ES (1) ES2609126T3 (pt)
HR (1) HRP20161530T1 (pt)
HU (1) HUE033294T2 (pt)
IN (1) IN2014KN02935A (pt)
LT (1) LT2877467T (pt)
PL (1) PL2877467T3 (pt)
PT (1) PT2877467T (pt)
RS (1) RS55684B1 (pt)
RU (1) RU2611010C2 (pt)
SI (1) SI2877467T1 (pt)
SM (2) SMT201700052T1 (pt)
WO (1) WO2014015905A1 (pt)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180005250A (ko) * 2015-05-21 2018-01-15 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Pad4 억제제로서의 벤조이미다졸 유도체
AR107032A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
AR107030A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
ES2770102T3 (es) 2016-02-23 2020-06-30 Padlock Therapeutics Inc Inhibidores de heteroarilo de PAD4
CN107188867A (zh) * 2016-03-14 2017-09-22 中国科学院天津工业生物技术研究所 精氨酸脱亚氨酶4的抑制剂
JP6987843B2 (ja) * 2016-07-27 2022-01-05 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の共有結合性阻害剤
KR102502992B1 (ko) * 2016-09-12 2023-02-24 패들락 테라퓨틱스, 인코포레이티드 Pad4의 헤테로아릴 억제제
WO2018102262A1 (en) * 2016-12-02 2018-06-07 University Of Massachusetts Inhibitors of protein arginine deiminases (pads) and methods of preparation and use thereof
CN108689946B (zh) * 2017-04-12 2022-10-18 中国科学院上海药物研究所 2-取代硫基乙酰胺类化合物及其制备方法和应用
WO2019058393A1 (en) * 2017-09-22 2019-03-28 Jubilant Biosys Limited HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PAD
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
EP3707135A1 (en) 2017-11-06 2020-09-16 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
DK3704120T3 (da) 2017-11-24 2024-05-21 Jubilant Episcribe Llc Heterocykliske forbindelser som prmt5-inhibitorer
EP3760628A4 (en) * 2018-02-26 2021-10-13 Nanjing Transthera Biosciences Co., Ltd. PEPTIDYLARGININE DEIMINASE INHIBITOR AND ITS USES
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
KR20210042933A (ko) * 2018-08-08 2021-04-20 브리스톨-마이어스 스큅 컴퍼니 Pad 효소의 벤즈이미다졸 억제제
ES2929200T3 (es) 2018-08-08 2022-11-25 Bristol Myers Squibb Co Tienopirroles sustituidos como inhibidores de PAD4
CN112805066A (zh) * 2018-08-08 2021-05-14 百时美施贵宝公司 作为pad4抑制剂的经取代的苯并咪唑
EP3833440A1 (en) 2018-08-08 2021-06-16 Bristol-Myers Squibb Company Indole and azaindole inhibitors of pad enzymes
CN109369513B (zh) * 2018-11-20 2020-08-25 都创(上海)医药科技有限公司 一种fbdd常用分子片段的制备方法
WO2020132045A1 (en) 2018-12-19 2020-06-25 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
EP3994128A4 (en) * 2019-07-03 2022-12-07 University of Massachusetts INHIBITORS OF PROTEIN ARGININE DEIMINASE 1, AND PROCESSES FOR THEIR PREPARATION AND USE
WO2021057910A1 (zh) * 2019-09-27 2021-04-01 南京药捷安康生物科技有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
WO2021158840A1 (en) * 2020-02-06 2021-08-12 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
CN111265526B (zh) * 2020-04-09 2021-03-19 黑龙江中医药大学 一种治疗胃癌的药物及其制备方法
IL296923A (en) 2020-04-30 2022-12-01 Gilead Sciences Inc Macrocyclic inhibitors of peptidylarginine deiminases
EP4211171A2 (en) 2020-09-10 2023-07-19 Precirix N.V. Antibody fragment against fap
EP4215534A4 (en) 2020-09-18 2024-10-02 Carna Biosciences, Inc. AMINE DERIVATIVE
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
JP2024543517A (ja) 2021-11-15 2024-11-21 レゴー・ファーマシューティカルズ,インコーポレーテッド Pad4阻害剤及びその使用
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting
WO2023230609A1 (en) * 2022-05-26 2023-11-30 Celgene Corporation Heterocyclic pad4 inhibitors
TW202434605A (zh) * 2022-11-24 2024-09-01 大陸商蘇州華明道康生物醫藥有限公司 含硒雜環化合物及其用途
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators

Family Cites Families (21)

* 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
PT820279E (pt) 1995-04-14 2002-11-29 Smithkline Beecham Corp Inalador de doses calibradas para albuterol
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
ES2253930T3 (es) * 1998-09-18 2006-06-01 ABBOTT GMBH & CO. KG 4-aminopirrolopirimidinas como inhibidores de quinasa.
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
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
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
ATE290865T1 (de) * 1999-10-19 2005-04-15 Merck & Co Inc Tyrosin kinase inhibitoren
OA12514A (en) 1999-12-24 2006-05-29 Aventis Pharma Ltd Azaindoles.
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003000690A1 (en) 2001-06-25 2003-01-03 Aventis Pharmaceuticals Inc. Synthesis of heterocyclic compounds employing microwave technology
WO2005044354A1 (en) 2003-11-03 2005-05-19 Glaxo Group Limited A fluid dispensing device
EP1687309A1 (en) 2003-11-17 2006-08-09 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
FR2862971B1 (fr) * 2003-11-28 2006-03-24 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament
US7429611B2 (en) * 2004-09-23 2008-09-30 Bristol-Myers Squibb Company Indole inhibitors of 15-lipoxygenase
EP2205085A1 (en) * 2007-09-25 2010-07-14 Merck Sharp & Dohme Corp. 2-aryl or heteroaryl indole derivatives
WO2009155042A1 (en) 2008-05-28 2009-12-23 Wyeth 3-substituted-1h-indole compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
RU2011106786A (ru) * 2008-07-23 2012-08-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы пиразолопиридинкиназы
MY159575A (en) * 2009-04-02 2017-01-13 Merck Serono Sa Dihydroorotate dehydrogenase inhibitors
WO2010118208A1 (en) 2009-04-09 2010-10-14 Exelixis, Inc. Benzoxazepin-4- (5h) -yl derivatives and their use to treat cancer

Also Published As

Publication number Publication date
US9518054B2 (en) 2016-12-13
IN2014KN02935A (pt) 2015-05-08
KR101916443B1 (ko) 2018-11-08
CN104470919A (zh) 2015-03-25
SI2877467T1 (sl) 2017-02-28
DK2877467T3 (en) 2017-02-13
ES2609126T3 (es) 2017-04-18
US20170119750A1 (en) 2017-05-04
HRP20161530T1 (hr) 2017-02-10
JP2015522628A (ja) 2015-08-06
RU2611010C2 (ru) 2017-02-17
BR112015001545B1 (pt) 2022-07-05
PL2877467T3 (pl) 2017-08-31
RS55684B1 (sr) 2017-07-31
US9833449B2 (en) 2017-12-05
US20160009716A1 (en) 2016-01-14
KR20150038438A (ko) 2015-04-08
SMT201700052T1 (it) 2017-03-08
CA2879341C (en) 2019-06-11
BR112015001545A2 (pt) 2017-07-04
CY1118524T1 (el) 2017-07-12
AU2012386257A1 (en) 2015-03-12
WO2014015905A1 (en) 2014-01-30
US10039755B2 (en) 2018-08-07
CA2879341A1 (en) 2014-01-30
JP6063567B2 (ja) 2017-01-18
US20150175600A1 (en) 2015-06-25
LT2877467T (lt) 2017-01-10
CN104470919B (zh) 2016-07-06
US20180161316A1 (en) 2018-06-14
EP2877467B1 (en) 2016-11-02
US9127003B2 (en) 2015-09-08
HUE033294T2 (en) 2017-11-28
EP2877467A1 (en) 2015-06-03
AU2012386257B2 (en) 2016-09-08
RU2014152456A (ru) 2016-09-20
SMT201700052B (it) 2017-03-08

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