PE20150754A1 - Derivados de azaindol que actuan como inhibidores de pi 3k - Google Patents

Derivados de azaindol que actuan como inhibidores de pi 3k

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Publication number
PE20150754A1
PE20150754A1 PE2015000013A PE2015000013A PE20150754A1 PE 20150754 A1 PE20150754 A1 PE 20150754A1 PE 2015000013 A PE2015000013 A PE 2015000013A PE 2015000013 A PE2015000013 A PE 2015000013A PE 20150754 A1 PE20150754 A1 PE 20150754A1
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PE
Peru
Prior art keywords
methyl
pyrrolo
pyrazol
pyrimidine
ethyl
Prior art date
Application number
PE2015000013A
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English (en)
Inventor
Edcon Chang
Wolfgang Reinhard Ludwig Notz
Michael B Wallace
Original Assignee
Takeda Pharmaceutical
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48795966&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20150754(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of PE20150754A1 publication Critical patent/PE20150754A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
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    • AHUMAN NECESSITIES
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P9/10Drugs 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
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D487/02Heterocyclic 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
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  • Chemical & Material Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Cardiology (AREA)
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  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invencion se refiere a los compuestos de la Formula 1, y una de sus sales farmaceuticamente aceptables, donde R1, R2, R3, R4, R5, R6, R7, R8, R9 y R10 se definen en la memoria. La presente revelacion tambien se refiere a los materiales y metodos para preparar compuestos de la Formula 1, a composiciones farmaceuticas que los contienen y a su empleo para tratar trastornos inmunologicos, enfermedades cardiovasculares, cancer y otros trastornos, enfermedades y afecciones que se asocian con la P13Kdelta. Son compuestos preferidos: (S)5-Cloro-N4-(1-(1-metil-6-(1-metil-1H-pirazol-5-il) -1H-pirrolo[3,2-b]piridin-5-il)etil)pirimidina-2 ,4-diamina; (S)-2 ,4-Diamino-6-((1-(1-metil-6-(1-metil-1H-pirazol-5-il)-1H-pirrolo[3,2-b]piridin-5-il)etil)amino)pirimidina-5-carbonitrilo ; (S)-2-Amino-4-metil-6-((1-(1-metil-6-(1-metil-1H-pirazol-5-il)-1H-pirrolo[3 ,2-b]piridin-5-il)etil)amino)pirimidina-5-carbonitrilo ; entre otros
PE2015000013A 2012-07-10 2013-07-08 Derivados de azaindol que actuan como inhibidores de pi 3k PE20150754A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261670116P 2012-07-10 2012-07-10

Publications (1)

Publication Number Publication Date
PE20150754A1 true PE20150754A1 (es) 2015-05-15

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ID=48795966

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Application Number Title Priority Date Filing Date
PE2015000013A PE20150754A1 (es) 2012-07-10 2013-07-08 Derivados de azaindol que actuan como inhibidores de pi 3k

Country Status (26)

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US (2) US8835420B2 (es)
EP (1) EP2872507A1 (es)
JP (1) JP2015522074A (es)
KR (1) KR20150031334A (es)
CN (1) CN104619708A (es)
AP (1) AP2015008236A0 (es)
AR (1) AR092347A1 (es)
AU (1) AU2013288895A1 (es)
BR (1) BR112015000386A2 (es)
CA (1) CA2878502A1 (es)
CO (1) CO7280475A2 (es)
CR (1) CR20150056A (es)
DO (1) DOP2015000002A (es)
EA (1) EA201590183A1 (es)
HK (1) HK1210771A1 (es)
IL (1) IL236535A0 (es)
MA (1) MA37831B1 (es)
MX (1) MX2015000107A (es)
NZ (1) NZ704160A (es)
PE (1) PE20150754A1 (es)
PH (1) PH12015500063B1 (es)
SG (1) SG11201500063UA (es)
TN (1) TN2015000005A1 (es)
TW (1) TW201414734A (es)
UY (1) UY34893A (es)
WO (1) WO2014011568A1 (es)

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DK3371165T3 (da) * 2015-11-04 2022-05-02 Merck Patent Gmbh Btk-inhibitor til anvendelse til behandling af kræft
HUE064244T2 (hu) * 2015-11-17 2024-02-28 Merck Patent Gmbh Módszerek szklerózis multiplex kezelésére BTK gátló aktivitású pirimidin- és piridin-származékokkal
WO2017155741A1 (en) * 2016-03-05 2017-09-14 Zhejiang Vimgreen Pharma Ltd. Quinoline analogs as phosphatidylinositol 3-kinase inhibitors
US10755986B2 (en) * 2016-03-29 2020-08-25 QROMIS, Inc. Aluminum nitride based Silicon-on-Insulator substrate structure
CN107964018A (zh) * 2016-10-19 2018-04-27 中国人民解放军军事医学科学院毒物药物研究所 取代嘌呤酮类衍生物及其医药用途
KR20220007111A (ko) * 2019-05-08 2022-01-18 티와이케이 메디슨즈, 인코포레이티드 키나아제 억제제로 사용되는 화합물 및 이의 응용
CN112794851B (zh) * 2021-01-26 2022-08-23 复旦大学 3-(吡啶-3基)-7-氮杂吲哚衍生物PI3Kδ抑制剂及其制备方法与应用

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