BR112016007122A2 - inibidores de pi3k e mtor conformacionalmente restritos - Google Patents

inibidores de pi3k e mtor conformacionalmente restritos

Info

Publication number
BR112016007122A2
BR112016007122A2 BR112016007122A BR112016007122A BR112016007122A2 BR 112016007122 A2 BR112016007122 A2 BR 112016007122A2 BR 112016007122 A BR112016007122 A BR 112016007122A BR 112016007122 A BR112016007122 A BR 112016007122A BR 112016007122 A2 BR112016007122 A2 BR 112016007122A2
Authority
BR
Brazil
Prior art keywords
pi3k
mtor inhibitors
conformationally restricted
compounds
kinase
Prior art date
Application number
BR112016007122A
Other languages
English (en)
Inventor
Jackson Eileen
Beaufils Florent
Wymann Matthias
Hebeisen Paul
Bohnacker Thomas
Cmiljanovic Vladimir
Original Assignee
Piqur Therapeutics Ag
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 Piqur Therapeutics Ag, Univ Basel filed Critical Piqur Therapeutics Ag
Publication of BR112016007122A2 publication Critical patent/BR112016007122A2/pt

Links

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

Abstract

a invenção refere-se a novos compostos inibidores de fosfoinositida 3-cinase (pi3k) e alvo mamífero de rapamicina (mtor) de fórmula (i) e (ii), que são conformacionalmente restritos, e para os quais o significado dos substituintes são listados na descrição. compostos preferidos são aqueles em que x é oxigênio, r1 é morfolino e r2 é fenila ou heteroarila substituído. estes compostos são úteis, sozinhos ou em combinação com outros agentes terapêuticos, para tratar distúrbios mediados por lipídeo cinases.
BR112016007122A 2013-10-04 2014-10-03 inibidores de pi3k e mtor conformacionalmente restritos BR112016007122A2 (pt)

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 (1)

Publication Number Publication Date
BR112016007122A2 true BR112016007122A2 (pt) 2017-08-01

Family

ID=49303818

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016007122A BR112016007122A2 (pt) 2013-10-04 2014-10-03 inibidores de pi3k e mtor conformacionalmente restritos

Country Status (17)

Country Link
US (1) US9556203B2 (pt)
EP (1) EP3052504B1 (pt)
JP (1) JP6426745B2 (pt)
KR (1) KR102369925B1 (pt)
CN (1) CN105593231B (pt)
AU (1) AU2014331049B2 (pt)
BR (1) BR112016007122A2 (pt)
CA (1) CA2925497C (pt)
ES (1) ES2721302T3 (pt)
HK (1) HK1220971A1 (pt)
IL (1) IL244708B (pt)
MX (1) MX364558B (pt)
PH (1) PH12016500569A1 (pt)
RU (1) RU2669696C2 (pt)
SG (1) SG11201602602RA (pt)
WO (1) WO2015049369A1 (pt)
ZA (1) ZA201602084B (pt)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3389662T3 (da) * 2015-12-16 2022-02-28 Genentech Inc Fremgangsmåde til fremstilling af tricykliske PI3K-inhibitorforbindelser og fremgangsmåder til anvendelse af disse til behandling af cancer
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
EP3458067B1 (en) 2016-05-18 2020-12-30 PIQUR Therapeutics AG Treatment of neurological disorders
US10722499B2 (en) 2017-01-06 2020-07-28 Palvella Therapeutics, Inc. Anyhydrous compositions 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
KR20140104060A (ko) * 2006-10-19 2014-08-27 시그날 파마소티칼 엘엘씨 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도
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
WO2012167606A1 (zh) * 2011-06-04 2012-12-13 山东亨利医药科技有限责任公司 吡啶并萘啶类PI3K和mTOR双重抑制剂及其制备与应用
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
CA2925497A1 (en) 2015-04-09
US20160244463A1 (en) 2016-08-25
EP3052504B1 (en) 2019-02-06
SG11201602602RA (en) 2016-04-28
US9556203B2 (en) 2017-01-31
AU2014331049B2 (en) 2018-03-29
EP3052504A1 (en) 2016-08-10
WO2015049369A1 (en) 2015-04-09
CA2925497C (en) 2022-12-06
IL244708B (en) 2019-06-30
KR102369925B1 (ko) 2022-03-03
CN105593231B (zh) 2018-06-05
CN105593231A (zh) 2016-05-18
HK1220971A1 (zh) 2017-05-19
IL244708A0 (en) 2016-04-21
MX364558B (es) 2019-04-29
RU2669696C2 (ru) 2018-10-15
RU2016112164A3 (pt) 2018-05-22
MX2016004203A (es) 2016-12-16
JP2016531947A (ja) 2016-10-13
ES2721302T3 (es) 2019-07-30
RU2016112164A (ru) 2017-11-09
NZ718614A (en) 2021-11-26
PH12016500569B1 (en) 2016-06-13
AU2014331049A1 (en) 2016-04-28
KR20160067946A (ko) 2016-06-14
JP6426745B2 (ja) 2018-11-21
PH12016500569A1 (en) 2016-06-13
ZA201602084B (en) 2017-05-31

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements