KR20150027267A - LRRK2 억제제로서의 4-(치환된-아미노)-7H-피롤로[2,3-d]피리미딘 - Google Patents
LRRK2 억제제로서의 4-(치환된-아미노)-7H-피롤로[2,3-d]피리미딘 Download PDFInfo
- Publication number
- KR20150027267A KR20150027267A KR20157002334A KR20157002334A KR20150027267A KR 20150027267 A KR20150027267 A KR 20150027267A KR 20157002334 A KR20157002334 A KR 20157002334A KR 20157002334 A KR20157002334 A KR 20157002334A KR 20150027267 A KR20150027267 A KR 20150027267A
- Authority
- KR
- South Korea
- Prior art keywords
- pyrrolo
- pyrimidin
- morpholin
- benzonitrile
- pyrimidine
- 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.)
- Ceased
Links
- 0 CCCCC(C1=C(C)*(C)CC*)=C(*)[*@@](*=C)C1=*C(*)=* Chemical compound CCCCC(C1=C(C)*(C)CC*)=C(*)[*@@](*=C)C1=*C(*)=* 0.000 description 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N C1NCCOC1 Chemical compound C1NCCOC1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- AJPIFHAYBPLXFB-UHFFFAOYSA-N C[Si+](C)(C)CCOC[n]1c2ncnc(N3CCOCC3)c2c(I)c1 Chemical compound C[Si+](C)(C)CCOC[n]1c2ncnc(N3CCOCC3)c2c(I)c1 AJPIFHAYBPLXFB-UHFFFAOYSA-N 0.000 description 2
- CFOSURHAGGGJBD-UHFFFAOYSA-N CC(CCC1)CN1c1c(c(B2OC(C)(C)C(C)(C)O2)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 Chemical compound CC(CCC1)CN1c1c(c(B2OC(C)(C)C(C)(C)O2)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 CFOSURHAGGGJBD-UHFFFAOYSA-N 0.000 description 1
- TXAZMYBMOFJBSQ-UHFFFAOYSA-N CC(CCC1)CN1c1c(c(Br)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 Chemical compound CC(CCC1)CN1c1c(c(Br)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 TXAZMYBMOFJBSQ-UHFFFAOYSA-N 0.000 description 1
- SZBLLALXFOYZNM-UHFFFAOYSA-N CC1(C)OB(c2c[n](COCC[Si+](C)(C)C)c3ncnc(N4CCOCC4)c23)OC1(C)C Chemical compound CC1(C)OB(c2c[n](COCC[Si+](C)(C)C)c3ncnc(N4CCOCC4)c23)OC1(C)C SZBLLALXFOYZNM-UHFFFAOYSA-N 0.000 description 1
- JMOMEVFJRJVJNY-ZDUSSCGKSA-N C[C@@H](CCC1)CN1c1c(c(-c2cccc(CO)c2)c[nH]2)c2ncn1 Chemical compound C[C@@H](CCC1)CN1c1c(c(-c2cccc(CO)c2)c[nH]2)c2ncn1 JMOMEVFJRJVJNY-ZDUSSCGKSA-N 0.000 description 1
- HWSFRYSAIHAHSF-AWEZNQCLSA-N C[C@@H](CCC1)CN1c1c(c(I)c[n]2COCC[Si+](C)(C)C)c2ncn1 Chemical compound C[C@@H](CCC1)CN1c1c(c(I)c[n]2COCC[Si+](C)(C)C)c2ncn1 HWSFRYSAIHAHSF-AWEZNQCLSA-N 0.000 description 1
- NKYLSMIADWPFTJ-SFHVURJKSA-N C[C@@H](CCC1)[IH]N1c1c(c(-c2cccc(CO)c2)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 Chemical compound C[C@@H](CCC1)[IH]N1c1c(c(-c2cccc(CO)c2)c[n]2S(c3ccc(C)cc3)(=O)=O)c2ncn1 NKYLSMIADWPFTJ-SFHVURJKSA-N 0.000 description 1
- HGQSFSJEDYICCU-ZDUSSCGKSA-N C[C@@H]1CN(c2c(c(Br)c[n]3S(c4ccc(C)cc4)(=O)=O)c3ncn2)[IH]CC1 Chemical compound C[C@@H]1CN(c2c(c(Br)c[n]3S(c4ccc(C)cc4)(=O)=O)c3ncn2)[IH]CC1 HGQSFSJEDYICCU-ZDUSSCGKSA-N 0.000 description 1
- OYQMYAFIMOBAJA-UHFFFAOYSA-N C[Si+](C)(C)CCOCCl Chemical compound C[Si+](C)(C)CCOCCl OYQMYAFIMOBAJA-UHFFFAOYSA-N 0.000 description 1
- HGFUNLMSHQSFAL-UHFFFAOYSA-N C[Si+](C)(C)CCOC[n]1c2ncnc(Cl)c2c(I)c1 Chemical compound C[Si+](C)(C)CCOC[n]1c2ncnc(Cl)c2c(I)c1 HGFUNLMSHQSFAL-UHFFFAOYSA-N 0.000 description 1
- PLKRSMDMXVKCAM-UHFFFAOYSA-N Cc1nc(Cl)c(c(I)c[nH]2)c2n1 Chemical compound Cc1nc(Cl)c(c(I)c[nH]2)c2n1 PLKRSMDMXVKCAM-UHFFFAOYSA-N 0.000 description 1
- ZXLAKPNNQOCGSR-UHFFFAOYSA-N Cc1nc(Cl)c(c(I)c[n]2COCC[Si+](C)(C)C)c2n1 Chemical compound Cc1nc(Cl)c(c(I)c[n]2COCC[Si+](C)(C)C)c2n1 ZXLAKPNNQOCGSR-UHFFFAOYSA-N 0.000 description 1
- HCFJHJBEGJJOMO-UHFFFAOYSA-N Cc1nc(Cl)c(cc[nH]2)c2n1 Chemical compound Cc1nc(Cl)c(cc[nH]2)c2n1 HCFJHJBEGJJOMO-UHFFFAOYSA-N 0.000 description 1
- XTIGQBGLUHGYQF-UHFFFAOYSA-N Cc1nc(N2CCOCC2)c(c(-c2cccc(C#N)c2)c[nH]2)c2n1 Chemical compound Cc1nc(N2CCOCC2)c(c(-c2cccc(C#N)c2)c[nH]2)c2n1 XTIGQBGLUHGYQF-UHFFFAOYSA-N 0.000 description 1
- JGAFRSZMEXADGP-UHFFFAOYSA-N Cc1nc(N2CCOCC2)c(c(-c2cccc(C#N)c2)c[n]2C[U]CC[Si+](C)(C)C)c2n1 Chemical compound Cc1nc(N2CCOCC2)c(c(-c2cccc(C#N)c2)c[n]2C[U]CC[Si+](C)(C)C)c2n1 JGAFRSZMEXADGP-UHFFFAOYSA-N 0.000 description 1
- CBWBJFJMNBPWAL-UHFFFAOYSA-N Clc1c(c(I)c[nH]2)c2ncn1 Chemical compound Clc1c(c(I)c[nH]2)c2ncn1 CBWBJFJMNBPWAL-UHFFFAOYSA-N 0.000 description 1
- XDBHWPLGGBLUHH-UHFFFAOYSA-N N#Cc1cccc(B(O)O)c1 Chemical compound N#Cc1cccc(B(O)O)c1 XDBHWPLGGBLUHH-UHFFFAOYSA-N 0.000 description 1
- LQZMLBORDGWNPD-UHFFFAOYSA-N O=C(CCC1=O)N1I Chemical compound O=C(CCC1=O)N1I LQZMLBORDGWNPD-UHFFFAOYSA-N 0.000 description 1
- HGTDLKXUWVKLQX-UHFFFAOYSA-N OB(c1cc(CO)ccc1)O Chemical compound OB(c1cc(CO)ccc1)O HGTDLKXUWVKLQX-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/535—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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261666299P | 2012-06-29 | 2012-06-29 | |
| US61/666,299 | 2012-06-29 | ||
| US201361820828P | 2013-05-08 | 2013-05-08 | |
| US61/820,828 | 2013-05-08 | ||
| PCT/IB2013/055039 WO2014001973A1 (en) | 2012-06-29 | 2013-06-19 | NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20150027267A true KR20150027267A (ko) | 2015-03-11 |
Family
ID=49029142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR20157002334A Ceased KR20150027267A (ko) | 2012-06-29 | 2013-06-19 | LRRK2 억제제로서의 4-(치환된-아미노)-7H-피롤로[2,3-d]피리미딘 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US9156845B2 (https=) |
| EP (2) | EP2867236B1 (https=) |
| JP (3) | JP6189948B2 (https=) |
| KR (1) | KR20150027267A (https=) |
| CN (2) | CN105732639A (https=) |
| AP (1) | AP3902A (https=) |
| AR (1) | AR091628A1 (https=) |
| AU (1) | AU2013282869B2 (https=) |
| BR (1) | BR112014032913A2 (https=) |
| CA (1) | CA2878054C (https=) |
| CL (1) | CL2014003566A1 (https=) |
| CO (1) | CO7160063A2 (https=) |
| CR (1) | CR20140566A (https=) |
| DO (1) | DOP2014000303A (https=) |
| EA (1) | EA025186B1 (https=) |
| ES (1) | ES2637245T3 (https=) |
| GE (1) | GEP201706620B (https=) |
| GT (1) | GT201400301A (https=) |
| IL (1) | IL236294A (https=) |
| MD (1) | MD20140130A2 (https=) |
| MX (1) | MX2014015769A (https=) |
| NI (1) | NI201400151A (https=) |
| NZ (1) | NZ702571A (https=) |
| PE (1) | PE20150153A1 (https=) |
| PH (1) | PH12014502886A1 (https=) |
| SG (1) | SG11201408044QA (https=) |
| TN (1) | TN2014000537A1 (https=) |
| TW (1) | TWI482774B (https=) |
| UY (1) | UY34883A (https=) |
| WO (1) | WO2014001973A1 (https=) |
| ZA (1) | ZA201409136B (https=) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019221566A1 (ko) * | 2018-05-18 | 2019-11-21 | 재단법인 대구경북첨단의료산업진흥재단 | 외상성 뇌손상 또는 뇌졸중의 예방 또는 치료용 약학적 조성물 |
| WO2020040591A1 (ko) * | 2018-08-23 | 2020-02-27 | 재단법인 대구경북첨단의료산업진흥재단 | Lrrk 키나아제 저해제를 유효성분으로 함유하는 피리미딘 유도체의 신규용도 |
| WO2025170397A1 (ko) * | 2024-02-07 | 2025-08-14 | 노보렉스 주식회사 | Lrrk2 단백질 키나제 도메인 억제제로서 신규한 화합물 |
| KR20250123656A (ko) * | 2024-02-07 | 2025-08-18 | 노보렉스 주식회사 | Lrrk2 단백질 키나제 도메인 억제제로서 신규한 화합물 |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2617339T3 (es) | 2010-12-16 | 2017-06-16 | Calchan Limited | Derivados de pirrolopirimidina inhibidores de ASK1 |
| CA2868302A1 (en) | 2012-03-23 | 2013-09-26 | Dennis M. Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| EP2867236B1 (en) * | 2012-06-29 | 2017-06-14 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| US8963597B1 (en) * | 2013-10-02 | 2015-02-24 | Nanya Technology Corporation | Cross-domain enablement method and electronic apparatus |
| EP3083618B1 (en) | 2013-12-17 | 2018-02-21 | Pfizer Inc | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
| RU2016134751A (ru) | 2014-01-29 | 2018-03-02 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения |
| MA39219B1 (fr) * | 2014-01-29 | 2018-11-30 | Glaxosmithkline Ip Dev Ltd | Nouveaux composés inhibiteurs de la kinase lrrk2 utilisés pour le traitement du parkinson, de l’alzheimer et de la sclérose latérale amyotrophique |
| US10058559B2 (en) | 2014-05-15 | 2018-08-28 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Treatment or prevention of an intestinal disease or disorder |
| CN104086553B (zh) * | 2014-06-13 | 2016-04-27 | 南京药石科技股份有限公司 | 一种制备7-溴咪唑并[2,1-f][1,2,4]三嗪-4-胺的方法 |
| US10004751B2 (en) | 2014-07-10 | 2018-06-26 | The J. David Gladstone Institutes | Compositions and methods for treating Dengue virus infection |
| KR102562866B1 (ko) | 2014-11-14 | 2023-08-04 | 네르비아노 메디칼 사이언시스 에스.알.엘. | 단백질 키나아제 억제제로서의 6-아미노-7-바이사이클로-7-데아자-퓨린 유도체 |
| RU2722149C1 (ru) | 2015-09-14 | 2020-05-27 | Пфайзер Инк. | Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2 |
| FR3041640B1 (fr) * | 2015-09-30 | 2019-05-17 | Les Laboratoires Servier | NOUVEAUX DERIVES DE PYRROLO[2,3-d]PYRIMIDINE, LEUR PROCEDE DE PREPRATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT |
| AR107032A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| JP2019534266A (ja) | 2016-10-14 | 2019-11-28 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 5員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用 |
| RU2761626C2 (ru) * | 2017-02-03 | 2021-12-13 | Лео Фарма А/С | ПРОИЗВОДНЫЕ 5-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-5-АЗАСПИРО[2.5]ОКТАН-8-КАРБОНОВОЙ КИСЛОТЫ В КАЧЕСТВЕ НОВЫХ ИНГИБИТОРОВ JAK-КИНАЗЫ |
| CN106831790B (zh) * | 2017-02-17 | 2019-07-26 | 四川大学华西医院 | 7H-吡咯并[2,3-d]嘧啶衍生物 |
| KR101923852B1 (ko) | 2017-02-24 | 2018-11-29 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| KR101990739B1 (ko) * | 2018-07-24 | 2019-06-19 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
| KR101992059B1 (ko) * | 2018-08-23 | 2019-06-21 | 재단법인 대구경북첨단의료산업진흥재단 | 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물 |
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| WO2020167624A1 (en) | 2019-02-13 | 2020-08-20 | Ptc Therapeutics, Inc. | Pyrrolo[2,3-d]pyrimidine compounds for treating familial dysautonomia |
| CA3139277A1 (en) | 2019-05-08 | 2020-11-12 | Vimalan Biosciences, Inc. | Jak inhibitors |
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| BR112022007680A2 (pt) | 2019-10-25 | 2022-08-09 | Merck Sharp & Dohme | Derivados de n-(heteroaril)quinazolin-2-amina como inibidores de lrrk2, composições farmacêuticas, e usos dos mesmos |
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| CN111671757A (zh) * | 2020-07-16 | 2020-09-18 | 福建医科大学附属协和医院 | 3-[4-(4-吗啉基)-7h-吡咯并[2,3-d]嘧啶-5-基]苯甲腈制药用途 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019221566A1 (ko) * | 2018-05-18 | 2019-11-21 | 재단법인 대구경북첨단의료산업진흥재단 | 외상성 뇌손상 또는 뇌졸중의 예방 또는 치료용 약학적 조성물 |
| WO2020040591A1 (ko) * | 2018-08-23 | 2020-02-27 | 재단법인 대구경북첨단의료산업진흥재단 | Lrrk 키나아제 저해제를 유효성분으로 함유하는 피리미딘 유도체의 신규용도 |
| WO2025170397A1 (ko) * | 2024-02-07 | 2025-08-14 | 노보렉스 주식회사 | Lrrk2 단백질 키나제 도메인 억제제로서 신규한 화합물 |
| KR20250123656A (ko) * | 2024-02-07 | 2025-08-18 | 노보렉스 주식회사 | Lrrk2 단백질 키나제 도메인 억제제로서 신규한 화합물 |
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