JP5946768B2 - ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 - Google Patents

３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 Download PDF

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Publication number: JP5946768B2
Authority: JP; Japan
Prior art keywords: compound; pyrrolo; pyrimidin; pyrazol; disease
Prior art date: 2009-10-09
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.): Active

Application number

JP2012533354A

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English (en)

Japanese (ja)

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JP2013507390A (ja

Inventor

ジェイムズ・ディ・ロジャース

アダム・シリング

アーギリオス・ジー・アーバニティス

ステイシー・シェパード

ローリン・ジー・ガルヤ

メイ・リー

フランク・エム・ネザ

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.)

Incyte Holdings Corp

Original Assignee

Incyte Holdings Corp

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.)

2009-10-09

Filing date

2010-10-08

Publication date

2016-07-06

2010-10-08 Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp

2013-03-04 Publication of JP2013507390A publication Critical patent/JP2013507390A/ja

2016-07-06 Application granted granted Critical

2016-07-06 Publication of JP5946768B2 publication Critical patent/JP5946768B2/ja

Status Active legal-status Critical Current

2030-10-08 Anticipated expiration legal-status Critical

Links

0 CO[C@@](CCC1)[C@]1C=* Chemical compound CO[C@@](CCC1)[C@]1C=* 0.000 description 2
BOFXVYGDIRCHEQ-UHFFFAOYSA-N COC(C(C(C1O)O)O)OC1C(O)=O Chemical compound COC(C(C(C1O)O)O)OC1C(O)=O BOFXVYGDIRCHEQ-UHFFFAOYSA-N 0.000 description 1
OBYLXIZDTJLUTM-UHFFFAOYSA-N N#CCC(C1CCCC1)[n](cc1-c2c(cc[nH]3)c3ncn2)nc1O Chemical compound N#CCC(C1CCCC1)[n](cc1-c2c(cc[nH]3)c3ncn2)nc1O OBYLXIZDTJLUTM-UHFFFAOYSA-N 0.000 description 1
WBDZJBCZCBJJQQ-UHFFFAOYSA-N N#CCC(C1CCCC1)[n]1ncc(-c2c(c(O)c[nH]3)c3ncn2)c1 Chemical compound N#CCC(C1CCCC1)[n]1ncc(-c2c(c(O)c[nH]3)c3ncn2)c1 WBDZJBCZCBJJQQ-UHFFFAOYSA-N 0.000 description 1
ZVOWMVHSOALPOW-UHFFFAOYSA-N N#CCC(C1CCCC1)[n]1ncc(-c2c(cc([nH]3)O)c3ncn2)c1 Chemical compound N#CCC(C1CCCC1)[n]1ncc(-c2c(cc([nH]3)O)c3ncn2)c1 ZVOWMVHSOALPOW-UHFFFAOYSA-N 0.000 description 1
HHNARICGCSVDAS-UHFFFAOYSA-N N#CCC(C1CCCC1)[n]1ncc(-c2c(cc[nH]3)c3nc(O)n2)c1 Chemical compound N#CCC(C1CCCC1)[n]1ncc(-c2c(cc[nH]3)c3nc(O)n2)c1 HHNARICGCSVDAS-UHFFFAOYSA-N 0.000 description 1
ZHZLDCAFBCJTDF-UHFFFAOYSA-N N#CCC(C1CCCC1)[n]1ncc(-c2c(cc[nH]3)c3ncn2)c1O Chemical compound N#CCC(C1CCCC1)[n]1ncc(-c2c(cc[nH]3)c3ncn2)c1O ZHZLDCAFBCJTDF-UHFFFAOYSA-N 0.000 description 1

Classifications

- 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
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/02—Antineoplastic agents specific for leukemia
- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
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- 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
- A—HUMAN NECESSITIES
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms

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Organic Chemistry (AREA)
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Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
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Engineering & Computer Science (AREA)
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Neurology (AREA)
Diabetes (AREA)
Neurosurgery (AREA)
Endocrinology (AREA)
Physical Education & Sports Medicine (AREA)
Dermatology (AREA)
Rheumatology (AREA)
Orthopedic Medicine & Surgery (AREA)
Oncology (AREA)
Hematology (AREA)
Transplantation (AREA)
Psychiatry (AREA)
Reproductive Health (AREA)
Hospice & Palliative Care (AREA)
Pain & Pain Management (AREA)
Obesity (AREA)
Urology & Nephrology (AREA)
Emergency Medicine (AREA)

JP2012533354A 2009-10-09 2010-10-08 ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 Active JP5946768B2 (ja)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US25038709P	2009-10-09	2009-10-09
US61/250,387		2009-10-09
US31621810P	2010-03-22	2010-03-22
US61/316,218		2010-03-22
PCT/US2010/052011 WO2011044481A1 (en)	2009-10-09	2010-10-08	Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Related Child Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2015246515A Division JP6251232B2 (ja)	2009-10-09	2015-12-17	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体

Publications (2)

Publication Number	Publication Date
JP2013507390A JP2013507390A (ja)	2013-03-04
JP5946768B2 true JP5946768B2 (ja)	2016-07-06

Family

ID=43037845

Family Applications (3)

Application Number	Title	Priority Date	Filing Date
JP2012533354A Active JP5946768B2 (ja)	2009-10-09	2010-10-08	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
JP2015246515A Active JP6251232B2 (ja)	2009-10-09	2015-12-17	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
JP2017172989A Pending JP2017226695A (ja)	2009-10-09	2017-09-08	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体

Family Applications After (2)

Application Number	Title	Priority Date	Filing Date
JP2015246515A Active JP6251232B2 (ja)	2009-10-09	2015-12-17	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
JP2017172989A Pending JP2017226695A (ja)	2009-10-09	2017-09-08	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体

Country Status (13)

Country	Link
US (3)	US8486902B2 (2)
EP (1)	EP2486041B1 (2)
JP (3)	JP5946768B2 (2)
KR (3)	KR20180126619A (2)
CN (2)	CN102596960B (2)
BR (1)	BR112012008267B1 (2)
CA (1)	CA2777114C (2)
EA (1)	EA021478B1 (2)
ES (1)	ES2435491T3 (2)
MX (1)	MX2012004180A (2)
PL (1)	PL2486041T3 (2)
PT (1)	PT2486041E (2)
WO (1)	WO2011044481A1 (2)

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SG10202003901UA (en)	2005-12-13	2020-05-28	Incyte Holdings Corp	Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
CL2008001709A1 (es)	2007-06-13	2008-11-03	Incyte Corp	Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20150036210A (ko)	2007-06-13	2015-04-07	인사이트 코포레이션	야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
CL2009001884A1 (es) *	2008-10-02	2010-05-14	Incyte Holdings Corp	Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
TWI720517B (zh)	2009-01-15	2021-03-01	美商英塞特公司	製造ｊａｋ抑制劑之方法及相關中間化合物
AR076794A1 (es)	2009-05-22	2011-07-06	Incyte Corp	Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) *	2009-05-22	2019-11-29	Incyte Holdings Corp	3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
TW201113285A (en)	2009-09-01	2011-04-16	Incyte Corp	Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) *	2009-10-09	2015-06-30	Инсайт Корпорейшн	ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
JP5858434B2 (ja) *	2010-02-18	2016-02-10	インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅＨｏｌｄｉｎｇｓＣｏｒｐｏｒａｔｉｏｎ	Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
EP3354652B1 (en)	2010-03-10	2020-05-06	Incyte Holdings Corporation	Piperidin-4-yl azetidine derivatives as jak1 inhibitors
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BR112012008267B1 (pt)	2022-10-04
EA021478B1 (ru)	2015-06-30
KR20170098334A (ko)	2017-08-29
WO2011044481A1 (en)	2011-04-14
JP6251232B2 (ja)	2017-12-20
CA2777114A1 (en)	2011-04-14
PT2486041E (pt)	2013-11-14
KR101805936B1 (ko)	2017-12-07
BR112012008267A2 (2)	2021-11-03
US20110086810A1 (en)	2011-04-14
JP2016056183A (ja)	2016-04-21
US20130345157A1 (en)	2013-12-26
CA2777114C (en)	2018-10-23
US20140378400A1 (en)	2014-12-25
MX2012004180A (es)	2012-07-17
AU2010303245A1 (en)	2012-05-10
CN102596960A (zh)	2012-07-18
EP2486041A1 (en)	2012-08-15
PL2486041T3 (pl)	2014-01-31
KR101921850B1 (ko)	2018-11-23
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US9512161B2 (en)	2016-12-06
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US8486902B2 (en)	2013-07-16
US8748401B2 (en)	2014-06-10
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Publication	Publication Date	Title
JP6251232B2 (ja)	2017-12-20	３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
CA2689158C (en)	2015-10-06	Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
AU2010303245B2 (en)	2016-04-28	Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
HK1174899B (en)	2014-02-14	Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
HK1141020B (en)	2014-07-11	Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d] pyrimidin-4-yl)-lh-pyrazol-l-yl)-3-cyclopentylpropanenitrile