CN104024255B - 作为btk活性的抑制剂的烷基化哌嗪化合物 - Google Patents

作为btk活性的抑制剂的烷基化哌嗪化合物 Download PDF

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Publication number: CN104024255B
Authority: CN; China
Prior art keywords: methyl; cancer; pyridin; oxo; mmol
Prior art date: 2011-11-03
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

CN201280065838.8A

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English (en)

Chinese (zh)

Other versions

CN104024255A (zh

Inventor

J.J.克劳福德

W.B.扬

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.)

F Hoffmann La Roche AG

Original Assignee

F Hoffmann La Roche AG

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.)

2011-11-03

Filing date

2012-11-02

Publication date

2017-01-18

2012-11-02 Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG

2014-09-03 Publication of CN104024255A publication Critical patent/CN104024255A/zh

2017-01-18 Application granted granted Critical

2017-01-18 Publication of CN104024255B publication Critical patent/CN104024255B/zh

Status Expired - Fee Related legal-status Critical Current

2032-11-02 Anticipated expiration legal-status Critical

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0 CCC(C)(CN(*)CC1)CN1c1*(C)cc(N)nc1 Chemical compound CCC(C)(CN(*)CC1)CN1c1*(C)cc(N)nc1 0.000 description 11
LCKGWMCJLOFBAO-UHFFFAOYSA-N CCC(CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(CCc4c5cc6[n]4CCCC6)C5=O)c3COC(C)=O)=CN(C)C2=O)nc1 Chemical compound CCC(CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(CCc4c5cc6[n]4CCCC6)C5=O)c3COC(C)=O)=CN(C)C2=O)nc1 LCKGWMCJLOFBAO-UHFFFAOYSA-N 0.000 description 1
BHMXKIZQZAPSSG-LBPRGKRZSA-O CC[C@@H](CN(CC1)C(OC(C)(C)C)=O)N1c(cn1)ccc1[NH+]=O Chemical compound CC[C@@H](CN(CC1)C(OC(C)(C)C)=O)N1c(cn1)ccc1[NH+]=O BHMXKIZQZAPSSG-LBPRGKRZSA-O 0.000 description 1
VGRKPWHLVRPNAO-CYBMUJFWSA-N C[C@H](CN(CC1)C2COC2)N1c(cc1)cnc1NC1=CC(Br)=CN(C)C1=O Chemical compound C[C@H](CN(CC1)C2COC2)N1c(cc1)cnc1NC1=CC(Br)=CN(C)C1=O VGRKPWHLVRPNAO-CYBMUJFWSA-N 0.000 description 1
CPBJGJJJTCBMEG-UHFFFAOYSA-N C[I](C(COC1)C2)C1C[I]2S(c1ccccc1)(=C)=O Chemical compound C[I](C(COC1)C2)C1C[I]2S(c1ccccc1)(=C)=O CPBJGJJJTCBMEG-UHFFFAOYSA-N 0.000 description 1
OKLIUUXZPLEMNE-UHFFFAOYSA-N O=C1NN=Cc2c1cc1[n]2CCCC1 Chemical compound O=C1NN=Cc2c1cc1[n]2CCCC1 OKLIUUXZPLEMNE-UHFFFAOYSA-N 0.000 description 1

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- C—CHEMISTRY; METALLURGY
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
- 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
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- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- C07D495/04—Ortho-condensed systems
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- C07D498/02—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 two hetero rings
- C07D498/08—Bridged systems
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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
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General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Immunology (AREA)
Pulmonology (AREA)
Dermatology (AREA)
Hematology (AREA)
Heart & Thoracic Surgery (AREA)
Diabetes (AREA)
Cardiology (AREA)
Rheumatology (AREA)
Oncology (AREA)
Vascular Medicine (AREA)
Transplantation (AREA)
Obesity (AREA)
Ophthalmology & Optometry (AREA)
Virology (AREA)
Communicable Diseases (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Pain & Pain Management (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Urology & Nephrology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

CN201280065838.8A 2011-11-03 2012-11-02 作为btk活性的抑制剂的烷基化哌嗪化合物 Expired - Fee Related CN104024255B (zh)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201161555395P	2011-11-03	2011-11-03
US61/555,395		2011-11-03
PCT/US2012/063198 WO2013067277A1 (en)	2011-11-03	2012-11-02	Alkylated piperazine compounds as inhibitors of btk activity

Publications (2)

Publication Number	Publication Date
CN104024255A CN104024255A (zh)	2014-09-03
CN104024255B true CN104024255B (zh)	2017-01-18

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Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CN201280065838.8A Expired - Fee Related CN104024255B (zh)	2011-11-03	2012-11-02	作为btk活性的抑制剂的烷基化哌嗪化合物

Country Status (23)

Country	Link
US (3)	US8729072B2 (2)
EP (1)	EP2773639B1 (2)
JP (2)	JP5976828B2 (2)
KR (1)	KR101716011B1 (2)
CN (1)	CN104024255B (2)
AR (1)	AR088642A1 (2)
AU (1)	AU2012332368A1 (2)
BR (1)	BR112014010439A2 (2)
CA (1)	CA2853970A1 (2)
CL (1)	CL2014001158A1 (2)
CO (1)	CO6950475A2 (2)
CR (1)	CR20140187A (2)
EA (1)	EA027561B1 (2)
IL (1)	IL232280A0 (2)
IN (1)	IN2014CN03265A (2)
MA (1)	MA35725B1 (2)
MX (1)	MX2014005289A (2)
PE (1)	PE20141686A1 (2)
PH (1)	PH12014500966A1 (2)
SG (1)	SG11201401993RA (2)
TW (1)	TW201326171A (2)
WO (1)	WO2013067277A1 (2)
ZA (1)	ZA201403158B (2)

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WO2015000949A1 (en)	2013-07-03	2015-01-08	F. Hoffmann-La Roche Ag	Heteroaryl pyridone and aza-pyridone amide compounds
WO2015082583A1 (en)	2013-12-05	2015-06-11	F. Hoffmann-La Roche Ag	Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
CA2932353A1 (en)	2013-12-13	2015-06-18	Steven P. Treon	Methods to treat lymphoplasmacytic lymphoma
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WO2015151006A1 (en)	2014-03-29	2015-10-08	Lupin Limited	Substituted purine compounds as btk inhibitors
SG11201608303QA (en)	2014-04-04	2016-11-29	Del Mar Pharmaceuticals	Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2015170266A1 (en)	2014-05-07	2015-11-12	Lupin Limited	Substituted pyrimidine compounds as btk inhibitors
CN106922146B (zh)	2014-10-02	2020-05-26	豪夫迈·罗氏有限公司	用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物
EP3715346B1 (en)	2014-10-22	2024-01-03	Dana-Farber Cancer Institute, Inc.	Thiazolyl-containing compounds for treating proliferative diseases
JP6368043B2 (ja)	2014-10-27	2018-08-01	エフ．ホフマン−ラロシュアーゲーＦ．Ｈｏｆｆｍａｎｎ−ＬａＲｏｃｈｅＡｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ	三環式ラクタム化合物の製造法
CN105837576B (zh)	2015-01-14	2019-03-26	湖北生物医药产业技术研究院有限公司	Btk抑制剂
KR102894264B1 (ko) *	2015-03-10	2025-12-02	오리진 온콜로지 리미티드	면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
WO2017148837A1 (en)	2016-02-29	2017-09-08	F. Hoffmann-La Roche Ag	Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
CA3045339A1 (en)	2016-12-03	2018-06-07	Juno Therapeutics, Inc.	Methods and compositions for use of therapeutic t cells in combination with kinase inhibitors
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AR088642A1 (es)	2014-06-25
CO6950475A2 (es)	2014-05-20
BR112014010439A2 (pt)	2017-04-18
IL232280A0 (en)	2014-06-30
US8729072B2 (en)	2014-05-20
WO2013067277A1 (en)	2013-05-10
PH12014500966A1 (en)	2014-06-09
US9115152B2 (en)	2015-08-25
KR20140090227A (ko)	2014-07-16
IN2014CN03265A (2)	2015-07-03
TW201326171A (zh)	2013-07-01
JP2014532763A (ja)	2014-12-08
SG11201401993RA (en)	2014-05-29
PE20141686A1 (es)	2014-11-08
CA2853970A1 (en)	2013-05-10
CN104024255A (zh)	2014-09-03
ZA201403158B (en)	2017-09-27
MA35725B1 (fr)	2014-12-01
AU2012332368A1 (en)	2014-05-22
CL2014001158A1 (es)	2014-09-12
EP2773639A1 (en)	2014-09-10
KR101716011B1 (ko)	2017-03-13
MX2014005289A (es)	2014-05-30
CR20140187A (es)	2014-06-20
EA201490859A1 (ru)	2014-09-30
US20140221365A1 (en)	2014-08-07
EA027561B1 (ru)	2017-08-31
JP5976828B2 (ja)	2016-08-24
JP2016028045A (ja)	2016-02-25
US8946213B2 (en)	2015-02-03
US20130116245A1 (en)	2013-05-09
EP2773639B1 (en)	2017-04-26
US20150094302A1 (en)	2015-04-02

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