BR112018011633A2 - inibidores de aza-benzimidazol de pad4 - Google Patents

inibidores de aza-benzimidazol de pad4

Info

Publication number
BR112018011633A2
BR112018011633A2 BR112018011633A BR112018011633A BR112018011633A2 BR 112018011633 A2 BR112018011633 A2 BR 112018011633A2 BR 112018011633 A BR112018011633 A BR 112018011633A BR 112018011633 A BR112018011633 A BR 112018011633A BR 112018011633 A2 BR112018011633 A2 BR 112018011633A2
Authority
BR
Brazil
Prior art keywords
pad4
aza
benzimidazole inhibitors
inhibitors
benzimidazole
Prior art date
Application number
BR112018011633A
Other languages
English (en)
Inventor
Kotey Adrian
Lecci Cristina
Kumaravel Gnanasambandam
Tye Heather
Wigginton Ian
Gleave Laura
Devraj Rajesh
Krulle Thomas
Original Assignee
Padlock Therapeutics 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 Padlock Therapeutics Inc filed Critical Padlock Therapeutics Inc
Publication of BR112018011633A2 publication Critical patent/BR112018011633A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

Abstract

a presente invenção refere-se aos compostos úteis como inibidores de pad4, as composições dos mesmos e aos métodos de tratamento de distúrbios relacionadas com pad4.
BR112018011633A 2015-12-09 2016-12-09 inibidores de aza-benzimidazol de pad4 BR112018011633A2 (pt)

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PCT/US2016/065865 WO2017100601A1 (en) 2015-12-09 2016-12-09 Aza-benzimidazole inhibitors of pad4

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CN109071497B (zh) 2016-02-23 2021-10-22 帕德罗科治疗公司 Pad4杂芳基抑制剂
US10703741B2 (en) 2016-07-27 2020-07-07 Padlock Therapeutics, Inc. Covalent inhibitors of PAD4
EP3510025B1 (en) 2016-09-12 2022-06-29 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
AU2019319835A1 (en) * 2018-08-08 2021-03-25 Bristol-Myers Squibb Company Indole and azaindole inhibitors of PAD enzymes
MX2021001471A (es) * 2018-08-08 2021-04-28 Bristol Myers Squibb Co Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4).
JP2023512557A (ja) * 2020-02-06 2023-03-27 ブリストル－マイヤーズ スクイブ カンパニー 免疫抑制剤として有用な大環状ｐａｄ４阻害剤
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
EP4143189A1 (en) 2020-04-30 2023-03-08 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases

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US6087380A (en) * 1949-11-24 2000-07-11 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions
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FR2826653B1 (fr) 2001-06-29 2005-10-14 Servier Lab Nouveaux derives de pyrido-pyrido-pyrrolo[3,2-g]pyrrolo [3,4-e]-indole et pyrido-pyrrolo[2,3-a]pyrrolo[3,4-c] carbazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
BR0213562A (pt) * 2001-10-26 2004-08-31 Aventis Pharma Inc Benzimidazóis e análogos e seu uso como inibidores de cinases de proteìna
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
EP2358202B1 (en) * 2008-11-03 2016-06-15 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
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CA3007954A1 (en) 2017-06-15
US20170166592A1 (en) 2017-06-15
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US9765093B2 (en) 2017-09-19
EP3386505A1 (en) 2018-10-17
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TW201726689A (zh) 2017-08-01
CN108601770B (zh) 2021-06-04
AR107030A1 (es) 2018-03-14
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IL259796A (en) 2018-07-31
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