MX364558B - INHIBIDORES DE PI3K Y mTOR CONFORMACIONALMENTE RESTRINGIDOS. - Google Patents

INHIBIDORES DE PI3K Y mTOR CONFORMACIONALMENTE RESTRINGIDOS.

Info

Publication number
MX364558B
MX364558B MX2016004203A MX2016004203A MX364558B MX 364558 B MX364558 B MX 364558B MX 2016004203 A MX2016004203 A MX 2016004203A MX 2016004203 A MX2016004203 A MX 2016004203A MX 364558 B MX364558 B MX 364558B
Authority
MX
Mexico
Prior art keywords
pi3k
conformationally restricted
mtor inhibitors
compounds
mtor
Prior art date
Application number
MX2016004203A
Other languages
English (en)
Other versions
MX2016004203A (es
Inventor
Cmiljanovic Vladimir
Hebeisen Paul
Jackson Eileen
Beaufils Florent
Bohnacker Thomas
Wymann Matthias
Original Assignee
Univ Basel
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 Univ Basel filed Critical Univ Basel
Publication of MX2016004203A publication Critical patent/MX2016004203A/es
Publication of MX364558B publication Critical patent/MX364558B/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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 three hetero rings
    • C07D498/14—Ortho-condensed systems
    • 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La invención se refiere a los nuevos compuestos inhibidores de la fosfoinositida 3-quinasa (PI3K) y del blanco de la rapamicina en los mamíferos (mTOR), que tienen las fórmula (I) y (II), que están conformacionalmente restringidos y para, los cuales, el significado de los sustituyentes está enumerado en la descripción. Los compuestos preferidos son aquellos en donde X es oxígeno, R1 es un morfolino y R2 es un fenilo sustituido o heteroarilo. Estos compuestos son útiles, ya sea solos o en combinación con otros agentes terapéuticos, para el tratamiento de trastornos mediados por quinasas de lípidos. (Ver Fórmula).
MX2016004203A 2013-10-04 2014-10-03 INHIBIDORES DE PI3K Y mTOR CONFORMACIONALMENTE RESTRINGIDOS. MX364558B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13187386 2013-10-04
PCT/EP2014/071227 WO2015049369A1 (en) 2013-10-04 2014-10-03 Conformationally restricted pi3k and mtor inhibitors

Publications (2)

Publication Number Publication Date
MX2016004203A MX2016004203A (es) 2016-12-16
MX364558B true MX364558B (es) 2019-04-29

Family

ID=49303818

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016004203A MX364558B (es) 2013-10-04 2014-10-03 INHIBIDORES DE PI3K Y mTOR CONFORMACIONALMENTE RESTRINGIDOS.

Country Status (17)

Country Link
US (1) US9556203B2 (es)
EP (1) EP3052504B1 (es)
JP (1) JP6426745B2 (es)
KR (1) KR102369925B1 (es)
CN (1) CN105593231B (es)
AU (1) AU2014331049B2 (es)
BR (1) BR112016007122A2 (es)
CA (1) CA2925497C (es)
ES (1) ES2721302T3 (es)
HK (1) HK1220971A1 (es)
IL (1) IL244708B (es)
MX (1) MX364558B (es)
PH (1) PH12016500569B1 (es)
RU (1) RU2669696C2 (es)
SG (1) SG11201602602RA (es)
WO (1) WO2015049369A1 (es)
ZA (1) ZA201602084B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201804204QA (en) * 2015-12-16 2018-06-28 Genentech Inc Process for the preparation of tricyclic pi3k inhibitor compounds and methods for using the same for the treatment of cancer
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN109475560B (zh) 2016-05-18 2023-05-02 巴塞尔大学 神经病症的治疗
IL267869B2 (en) 2017-01-06 2023-10-01 Palvella Therapeutics Inc Non-aqueous preparations of mTOR inhibitors and methods of use
US11000513B2 (en) 2018-07-02 2021-05-11 Palvella Therapeutics, Inc. Anhydrous compositions of mTOR inhibitors and methods of use

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
AUPO903897A0 (en) 1997-09-08 1997-10-02 Commonwealth Scientific And Industrial Research Organisation Organic boronic acid derivatives
RU2246496C1 (ru) * 2003-09-12 2005-02-20 Тец Виктор Вениаминович Вещество с противовирусной и антибактериальной активностью на основе производных 2,8-дитиоксо-1h-пирано[2,3-d, 6,5-d`] дипиримидина и их 10-аза-аналогов
US20060188498A1 (en) * 2005-02-18 2006-08-24 Genentech, Inc. Methods of using death receptor agonists and EGFR inhibitors
WO2006125179A1 (en) * 2005-05-19 2006-11-23 Xenon Pharmaceuticals Inc. Tricyclic compounds and their uses as therapeutic agents
RU2478635C2 (ru) * 2006-10-19 2013-04-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений
FR2933983B1 (fr) * 2008-07-15 2010-08-27 Servier Lab Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
TWI378933B (en) * 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
EP2719697B1 (en) 2011-06-04 2018-08-01 Xuanzhu Pharma Co., Ltd. Pyridonaphthyridine pi3k/mtor dual inhibitors and preparation and use thereof
CN103030653A (zh) * 2011-09-30 2013-04-10 上海恒瑞医药有限公司 杂芳基并嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
RU2016112164A (ru) 2017-11-09
CN105593231B (zh) 2018-06-05
EP3052504A1 (en) 2016-08-10
KR20160067946A (ko) 2016-06-14
AU2014331049B2 (en) 2018-03-29
HK1220971A1 (zh) 2017-05-19
MX2016004203A (es) 2016-12-16
US9556203B2 (en) 2017-01-31
WO2015049369A1 (en) 2015-04-09
CA2925497A1 (en) 2015-04-09
SG11201602602RA (en) 2016-04-28
RU2016112164A3 (es) 2018-05-22
ES2721302T3 (es) 2019-07-30
ZA201602084B (en) 2017-05-31
CA2925497C (en) 2022-12-06
JP6426745B2 (ja) 2018-11-21
RU2669696C2 (ru) 2018-10-15
CN105593231A (zh) 2016-05-18
PH12016500569A1 (en) 2016-06-13
IL244708B (en) 2019-06-30
AU2014331049A1 (en) 2016-04-28
JP2016531947A (ja) 2016-10-13
PH12016500569B1 (en) 2016-06-13
NZ718614A (en) 2021-11-26
KR102369925B1 (ko) 2022-03-03
BR112016007122A2 (pt) 2017-08-01
IL244708A0 (en) 2016-04-21
EP3052504B1 (en) 2019-02-06
US20160244463A1 (en) 2016-08-25

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