BR112015001695A2 - compostos de heteroarila e heterociclo, composições e métodos - Google Patents

compostos de heteroarila e heterociclo, composições e métodos

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Publication number
BR112015001695A2
BR112015001695A2 BR112015001695A BR112015001695A BR112015001695A2 BR 112015001695 A2 BR112015001695 A2 BR 112015001695A2 BR 112015001695 A BR112015001695 A BR 112015001695A BR 112015001695 A BR112015001695 A BR 112015001695A BR 112015001695 A2 BR112015001695 A2 BR 112015001695A2
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BR
Brazil
Prior art keywords
methods
heteroaryl
compositions
heterocycle compounds
cancer
Prior art date
Application number
BR112015001695A
Other languages
English (en)
Inventor
Dai Guangxiu
Jia Hong
Diane Venable Jennifer
Xiao Kun
Damian Bembenek Scott
Su Wei-Guo
Chai Wenying
Zhang Zhulin
Original Assignee
Hutchison Medipharma Ltd
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Publication date
Application filed by Hutchison Medipharma Ltd filed Critical Hutchison Medipharma Ltd
Publication of BR112015001695A2 publication Critical patent/BR112015001695A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • 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
    • 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
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

novel heteroaryl and heterocycle compounds, compositions and methods abstract the invention relates to novel heteroaryl and heterocycle compounds of formula i-1, i-2 or i-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of pi3k and for treating inflammatory and autoimmune diseases and cancer. ************************** tradução do resumo resumo patente de invenção: "compostos de heteroarila e heterociclo, composições e métodos". a invenção refere-se a novos compostos de heteroarila e heterociclo de fórmula i-1, i-2 ou i-3 e composições farmacêuticas compreendendo-os, usos e métodos dos mesmos para inibir a atividade de pi3k e para tratar doenças inflamatórias e autoimunes e câncer. 1/1
BR112015001695A 2012-07-27 2013-07-26 compostos de heteroarila e heterociclo, composições e métodos BR112015001695A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2012/079290 WO2014015523A1 (en) 2012-07-27 2012-07-27 Novel heteroaryl and heterocycle compounds, compositions and methods
PCT/CN2013/072686 WO2014015675A1 (en) 2012-07-27 2013-03-15 Novel heteroaryl and heterocycle compounds, compositions and methods
PCT/CN2013/080195 WO2014015830A1 (en) 2012-07-27 2013-07-26 Novel heteroaryl and heterocycle compounds, composition and methods thereof

Publications (1)

Publication Number Publication Date
BR112015001695A2 true BR112015001695A2 (pt) 2017-07-04

Family

ID=49996522

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015001695A BR112015001695A2 (pt) 2012-07-27 2013-07-26 compostos de heteroarila e heterociclo, composições e métodos

Country Status (12)

Country Link
US (2) US20150291593A1 (pt)
EP (1) EP2877472A4 (pt)
JP (1) JP5976933B2 (pt)
KR (1) KR20150036738A (pt)
AU (1) AU2013295906B2 (pt)
BR (1) BR112015001695A2 (pt)
CA (1) CA2880251C (pt)
EA (1) EA201590281A1 (pt)
IN (1) IN2015DN00827A (pt)
MX (1) MX2015001207A (pt)
TW (1) TW201404779A (pt)
WO (3) WO2014015523A1 (pt)

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CN107501275B (zh) 2012-12-07 2019-11-22 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物
WO2014143242A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2970286A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
RU2720408C2 (ru) 2013-12-06 2020-04-29 Вертекс Фармасьютикалз Инкорпорейтед Способ получения ингибиторов atr киназы (варианты)
AU2015271030B2 (en) 2014-06-05 2019-05-16 Vertex Pharmaceuticals Incorporated Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof
ES2733847T3 (es) 2014-06-17 2019-12-03 Vertex Pharma Método para tratar cáncer usando una combinación de inhibidores de CHK1 y ATR
CU24428B1 (es) 2014-07-04 2019-06-04 Lupin Ltd Derivados de quinolizinona como inhibidores de pi3k
DK3177612T3 (da) * 2014-08-04 2022-05-16 Nuevolution As Eventuelt fusionerede heterocyclylsubstituerede derivater af pyrimidin, der er anvendelige til behandling af inflammatoriske, metaboliske, onkologiske og autoimmune sygdomme
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TW201639845A (zh) * 2015-01-29 2016-11-16 和記黃埔醫藥（上海）有限公司 新的雜芳基和雜環化合物、其組成物及方法
JP6861166B2 (ja) * 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
KR101845931B1 (ko) * 2015-06-18 2018-04-05 한국화학연구원 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
WO2016204429A1 (ko) * 2015-06-18 2016-12-22 한국화학연구원 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물.
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