CN102361872B - 作为akt抑制剂的稠合嘧啶 - Google Patents

作为akt抑制剂的稠合嘧啶 Download PDF

Info

Publication number
CN102361872B
CN102361872B CN201080012970.3A CN201080012970A CN102361872B CN 102361872 B CN102361872 B CN 102361872B CN 201080012970 A CN201080012970 A CN 201080012970A CN 102361872 B CN102361872 B CN 102361872B
Authority
CN
China
Prior art keywords
compound
compounds
alkyl
formula
hydrogen
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201080012970.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN102361872A (zh
Inventor
M·芬内曼
T·贝尔
T·迈尔
S·赫尔德
G·贝内克
F·德默尔
A·齐尔希
A·施特鲁布
T·贝克尔斯
S·英斯
H·雷温克尔
刘宁姝
U·伯默
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Bayer Pharma AG
Bayer Intellectual Property GmbH
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 Bayer Pharma AG, Bayer Intellectual Property GmbH filed Critical Bayer Pharma AG
Publication of CN102361872A publication Critical patent/CN102361872A/zh
Application granted granted Critical
Publication of CN102361872B publication Critical patent/CN102361872B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201080012970.3A 2009-02-13 2010-02-05 作为akt抑制剂的稠合嘧啶 Expired - Fee Related CN102361872B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09152805 2009-02-13
EP09152805.9 2009-02-13
PCT/EP2010/000717 WO2010091824A1 (en) 2009-02-13 2010-02-05 Fused pyrimidines as akt inhibitors

Publications (2)

Publication Number Publication Date
CN102361872A CN102361872A (zh) 2012-02-22
CN102361872B true CN102361872B (zh) 2014-12-03

Family

ID=42019301

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080012970.3A Expired - Fee Related CN102361872B (zh) 2009-02-13 2010-02-05 作为akt抑制剂的稠合嘧啶

Country Status (7)

Country Link
US (1) US20130310362A1 (https=)
EP (1) EP2396331B1 (https=)
JP (1) JP5667085B2 (https=)
CN (1) CN102361872B (https=)
CA (1) CA2752114C (https=)
ES (1) ES2435804T3 (https=)
WO (1) WO2010091824A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA38287B1 (fr) 2013-01-23 2018-08-31 Astrazeneca Ab Nouveaux dérivés aminopyrazine pour le traitement ou la prévention du cancer
CA3206628A1 (en) 2013-09-12 2015-03-19 Dana-Farber Cancer Institute, Inc. Methods for evaluating and treating waldenstrom's macroglobulinemia
MX373103B (es) 2014-02-13 2020-04-17 Incyte Holdings Corp Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1).
SI3105218T1 (sl) 2014-02-13 2019-11-29 Incyte Corp Ciklopropilamini kot inhibitorji LSD1
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP2907811A1 (en) 2014-02-14 2015-08-19 Actelion Pharmaceuticals Ltd. Process for manufacturing pyrimidine sulfamide derivatives
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1668619A (zh) * 2002-04-19 2005-09-14 细胞基因组公司 咪唑并[1,2－а]吡嗪－8－基胺,其制备方法及使用方法
CN1809354A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
CN101242834A (zh) * 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005233584B2 (en) 2004-04-09 2010-12-09 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7544677B2 (en) 2004-08-23 2009-06-09 Merck & Co., Inc. Inhibitors of Akt activity
ATE479687T1 (de) * 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
CN101115479A (zh) 2005-02-14 2008-01-30 默克公司 Akt活性抑制剂
US8008317B2 (en) 2005-06-10 2011-08-30 Merck Sharp & Dohme Corp. Inhibitors of akt activtiy
DE102007012645A1 (de) * 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
UY31292A1 (es) * 2007-08-14 2009-03-31 Imidazoles biciclicos fusionados
PT2188291E (pt) * 2007-08-14 2012-12-20 Bayer Ip Gmbh Pirimidinas bicíclicas fundidas

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1668619A (zh) * 2002-04-19 2005-09-14 细胞基因组公司 咪唑并[1,2－а]吡嗪－8－基胺,其制备方法及使用方法
CN1809354A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
CN101242834A (zh) * 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Rapid assembly of diverse and potent allosteric Akt inhibitors;Zhicai Wu，等;《Bioorganic & Medicinal Chemistry Letters》;20071017;第18卷(第6期);第2212页第1栏Scheme 1 *

Also Published As

Publication number Publication date
CA2752114C (en) 2017-06-20
JP2012517965A (ja) 2012-08-09
EP2396331A1 (en) 2011-12-21
ES2435804T3 (es) 2013-12-23
EP2396331B1 (en) 2013-10-16
JP5667085B2 (ja) 2015-02-12
WO2010091824A1 (en) 2010-08-19
HK1166984A1 (en) 2012-11-16
US20130310362A1 (en) 2013-11-21
CA2752114A1 (en) 2010-08-19
CN102361872A (zh) 2012-02-22

Similar Documents

Publication Publication Date Title
CN102361872B (zh) 作为akt抑制剂的稠合嘧啶
CN102317291B (zh) 稠合嘧啶
JP5327652B2 (ja) 癌処理のための融合されたイミダゾール
TWI439272B (zh) 稠合雙環嘧啶
HK1166984B (en) Fused pyrimidines as akt inhibitors
HK1165423B (en) Fused pyrimidines
EP2062893A1 (en) Fused imidazoles for cancer treatment
EP2050748A1 (en) Novel fused pyrimidines

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1166984

Country of ref document: HK

ASS Succession or assignment of patent right

Owner name: BAYER INTELLECTUAL PROPERTY GMBH

Free format text: FORMER OWNER: BAYER PHARMA AG

Effective date: 20130725

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20130725

Address after: German Monheim

Applicant after: Bayer Pharma Aktiengesellschaft

Address before: Berlin

Applicant before: Bayer Pharma AG

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1166984

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20141203

Termination date: 20180205

CF01 Termination of patent right due to non-payment of annual fee