ES2543567T3 - Métodos de utilización de inhibidores de ALK - Google Patents
Métodos de utilización de inhibidores de ALK Download PDFInfo
- Publication number
- ES2543567T3 ES2543567T3 ES12703670.5T ES12703670T ES2543567T3 ES 2543567 T3 ES2543567 T3 ES 2543567T3 ES 12703670 T ES12703670 T ES 12703670T ES 2543567 T3 ES2543567 T3 ES 2543567T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- methods
- formula
- alk inhibitors
- alk
- 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.)
- Active
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 239000002146 L01XE16 - Crizotinib Substances 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 abstract 1
- 229960005061 crizotinib Drugs 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- VOASCOSDVNWJEV-UHFFFAOYSA-N 5-chloro-2-n-(5-methyl-4-piperidin-2-yl-2-propan-2-yloxyphenyl)-4-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCCCN1 VOASCOSDVNWJEV-UHFFFAOYSA-N 0.000 description 1
- IGUPHIBNKHHSSE-UHFFFAOYSA-N 5-chloro-2-n-(5-methyl-4-piperidin-3-yl-2-propan-2-yloxyphenyl)-4-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCCNC1 IGUPHIBNKHHSSE-UHFFFAOYSA-N 0.000 description 1
- VOASCOSDVNWJEV-JOCHJYFZSA-N 5-chloro-2-n-[5-methyl-4-[(2r)-piperidin-2-yl]-2-propan-2-yloxyphenyl]-4-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1[C@H]1CCCCN1 VOASCOSDVNWJEV-JOCHJYFZSA-N 0.000 description 1
- VOASCOSDVNWJEV-QFIPXVFZSA-N 5-chloro-2-n-[5-methyl-4-[(2s)-piperidin-2-yl]-2-propan-2-yloxyphenyl]-4-n-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1[C@@H]1CCCCN1 VOASCOSDVNWJEV-QFIPXVFZSA-N 0.000 description 1
- VERWOWGGCGHDQE-UHFFFAOYSA-N ceritinib Chemical compound CC=1C=C(NC=2N=C(NC=3C(=CC=CC=3)S(=O)(=O)C(C)C)C(Cl)=CN=2)C(OC(C)C)=CC=1C1CCNCC1 VERWOWGGCGHDQE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto de fórmula (I)**Fórmula** o una sal farmacéuticamente aceptable del mismo; en donde R1 es halo; R2 es H; R3 is SO2R7 en donde R7 es C1-6 alquilo; R4 es C1-6 alcoxi; R5 es piperidinilo opcionalmente sustituido con C1-6 alquilo; R6 es C1-6 alquilo; o R5 y R6 junto con los átomos de carbono al cual están unidos forman un anillo heterocíclico de 5-6 miembros que comprende tener 1-2 heteroátomos seleccionados de N, O y S, para uso en un método para tratar un cáncer de pulmón de células no pequeñas EML4-ALK+, y opcionalmente resistente a crizotinib.
Description
E12703670
23-07-2015
- Compuesto
- 1
- 5-cloro-N2-(2-isopropoxi-5-metil-4-(piperidin-4-il)fenil)-N4-[2-(propano-2-sulfonil)-fenil] -pirimidin2,4-diamina;
- 2
- 5-cloro-N2-(2-isopropoxi-5-metil-4-(piperidin-2-il)fenil)-N4-(2-(isopropilsulfonil)fenil)pirimidin-2,4diamina;
- 3
- (S)-5-cloro-N2-(2-isopropoxi-5-metil-4-(piperidin-2-il)fenil)-N4-(2-(isopropilsulfonil)fenil)pirimidin-2,4diamina;
- 4
- (R)-5-cloro-N2-(2-isopropoxi-5-metil-4-(piperidin-2-il)fenil)-N4-(2-(isopropilsulfonil)fenil)pirimidin-2,4diamina;
- 5
- 5-cloro-N2-(2-isopropoxi-5-metil-4-(piperidin-3-il)fenil)-N4-(2-(isopropilsulfonil) fenil)pirimidin-2,4diamina; y
3
Claims (1)
-
imagen1 imagen2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161438878P | 2011-02-02 | 2011-02-02 | |
| US201161438878P | 2011-02-02 | ||
| PCT/US2012/023669 WO2012106540A1 (en) | 2011-02-02 | 2012-02-02 | Methods of using alk inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2543567T3 true ES2543567T3 (es) | 2015-08-20 |
Family
ID=45582065
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12703670.5T Active ES2543567T3 (es) | 2011-02-02 | 2012-02-02 | Métodos de utilización de inhibidores de ALK |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8703787B2 (es) |
| EP (1) | EP2670401B1 (es) |
| JP (1) | JP5837095B2 (es) |
| KR (1) | KR101521861B1 (es) |
| CN (1) | CN103458881B (es) |
| AU (1) | AU2012212142B2 (es) |
| BR (1) | BR112013019643B1 (es) |
| CA (1) | CA2824092C (es) |
| CY (1) | CY1116662T1 (es) |
| DK (1) | DK2670401T3 (es) |
| EA (1) | EA023404B1 (es) |
| ES (1) | ES2543567T3 (es) |
| HR (1) | HRP20150946T1 (es) |
| HU (1) | HUE025395T2 (es) |
| ME (1) | ME02200B (es) |
| MX (1) | MX2013008791A (es) |
| PL (1) | PL2670401T3 (es) |
| PT (1) | PT2670401E (es) |
| RS (1) | RS54189B1 (es) |
| SI (1) | SI2670401T1 (es) |
| SM (1) | SMT201500300B (es) |
| WO (1) | WO2012106540A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2890006C (en) | 2012-11-06 | 2021-11-23 | Shanghai Fochon Pharmaceutical Co Ltd | Alk kinase inhibitors |
| KR20150081344A (ko) * | 2012-11-07 | 2015-07-13 | 노파르티스 아게 | 조합 요법 |
| CN104109149B (zh) | 2013-04-22 | 2018-09-28 | 苏州泽璟生物制药有限公司 | 氘代的二氨基嘧啶化合物以及包含该化合物的药物组合物 |
| ITMI20131124A1 (it) * | 2013-07-04 | 2015-01-05 | Univ Milano Bicocca | 2-acilamminotiazoli per il trattamento del cancro |
| JP6510510B2 (ja) * | 2013-07-11 | 2019-05-08 | ベータ ファーマシューティカルズ カンパニー リミテッド | プロテインチロシンキナーゼモジュレーター及び使用方法 |
| ES2674361T3 (es) * | 2013-08-28 | 2018-06-29 | Novartis Ag | Combinación de un inhibidor de ALK y un inhibidor de CDK para el tratamiento de enfermedades celulares proliferativas |
| CN104672214B (zh) * | 2013-12-03 | 2019-04-12 | 上海翰森生物医药科技有限公司 | 具有alk抑制活性的化合物及其制备与用途 |
| KR20160100975A (ko) * | 2013-12-23 | 2016-08-24 | 노파르티스 아게 | 제약 조합물 |
| CN104876914B (zh) * | 2014-02-28 | 2017-04-19 | 山东轩竹医药科技有限公司 | 嘧啶衍生物类间变性淋巴瘤激酶抑制剂 |
| KR101656382B1 (ko) * | 2014-02-28 | 2016-09-09 | 한국화학연구원 | 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 |
| JP6622726B2 (ja) * | 2014-06-17 | 2019-12-18 | コリア リサーチ インスティチュート オブ ケミカル テクノロジーＫｏｒｅａ Ｒｅｓｅａｒｃｈ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｃｈｅｍｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ | ピリミジン‐２，４‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物 |
| CN105524045B (zh) * | 2014-10-22 | 2020-04-10 | 山东轩竹医药科技有限公司 | 四环类间变性淋巴瘤激酶抑制剂 |
| CN106146525B (zh) * | 2015-04-10 | 2018-11-02 | 山东轩竹医药科技有限公司 | 三并环类间变性淋巴瘤激酶抑制剂 |
| CN111440189B (zh) | 2015-04-24 | 2022-08-09 | 广州再极医药科技有限公司 | 稠环嘧啶氨基衍生物、其制备方法、中间体、药物组合物及应用 |
| CN106699743B (zh) | 2015-11-05 | 2020-06-12 | 湖北生物医药产业技术研究院有限公司 | 嘧啶类衍生物及其用途 |
| CN106220608B (zh) * | 2016-07-25 | 2018-11-27 | 安润医药科技（苏州）有限公司 | 二苯氨基嘧啶及三嗪化合物、其药用组合物及用途 |
| CN107698603B (zh) * | 2016-08-09 | 2022-04-08 | 南京红云生物科技有限公司 | 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用 |
| SG11201901251SA (en) * | 2016-08-29 | 2019-03-28 | Univ Michigan Regents | Aminopyrimidines as alk inhibitors |
| CN111484484B (zh) * | 2020-04-13 | 2021-11-23 | 沈阳药科大学 | 含芳杂环的2,4-二芳氨基嘧啶衍生物及其制备与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9301192D0 (en) | 1993-06-09 | 1993-06-09 | Trott Francis W | Flower shaped mechanised table |
| GB0305929D0 (en) * | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| TWI378923B (en) * | 2003-08-15 | 2012-12-11 | Novartis Ag | Pyrimidine derivatives |
| GB0419161D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| ES2533575T3 (es) | 2006-07-10 | 2015-04-13 | Goji Limited | Método y sistema para calentamiento con microondas de multifrecuencia |
| CA2598893C (en) * | 2006-10-11 | 2012-04-10 | Astellas Pharma Inc. | Eml4-alk fusion gene |
| BRPI0722383A2 (pt) * | 2006-12-08 | 2012-06-05 | Irm Llc | compostos inibidores de proteìna quinase, composições contendo os mesmos bem como seus usos |
| WO2008073687A2 (en) | 2006-12-08 | 2008-06-19 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US8592432B2 (en) * | 2008-04-07 | 2013-11-26 | Bei Chen | Compounds and compositions as protein kinase inhibitors |
-
2012
- 2012-02-02 HU HUE12703670A patent/HUE025395T2/en unknown
- 2012-02-02 MX MX2013008791A patent/MX2013008791A/es unknown
- 2012-02-02 CN CN201280007465.9A patent/CN103458881B/zh active Active
- 2012-02-02 JP JP2013552637A patent/JP5837095B2/ja active Active
- 2012-02-02 DK DK12703670.5T patent/DK2670401T3/en active
- 2012-02-02 CA CA2824092A patent/CA2824092C/en active Active
- 2012-02-02 EP EP12703670.5A patent/EP2670401B1/en active Active
- 2012-02-02 ME MEP-2015-127A patent/ME02200B/me unknown
- 2012-02-02 SI SI201230285T patent/SI2670401T1/sl unknown
- 2012-02-02 BR BR112013019643-2A patent/BR112013019643B1/pt active IP Right Grant
- 2012-02-02 WO PCT/US2012/023669 patent/WO2012106540A1/en not_active Ceased
- 2012-02-02 PT PT127036705T patent/PT2670401E/pt unknown
- 2012-02-02 US US13/981,046 patent/US8703787B2/en active Active
- 2012-02-02 KR KR1020137023001A patent/KR101521861B1/ko active Active
- 2012-02-02 HR HRP20150946TT patent/HRP20150946T1/hr unknown
- 2012-02-02 PL PL12703670T patent/PL2670401T3/pl unknown
- 2012-02-02 AU AU2012212142A patent/AU2012212142B2/en active Active
- 2012-02-02 EA EA201391114A patent/EA023404B1/ru not_active IP Right Cessation
- 2012-02-02 RS RS20150563A patent/RS54189B1/sr unknown
- 2012-02-02 ES ES12703670.5T patent/ES2543567T3/es active Active
-
2015
- 2015-08-28 CY CY20151100758T patent/CY1116662T1/el unknown
- 2015-11-30 SM SM201500300T patent/SMT201500300B/it unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2824092A1 (en) | 2012-08-09 |
| CN103458881A (zh) | 2013-12-18 |
| AU2012212142B2 (en) | 2015-09-24 |
| KR101521861B1 (ko) | 2015-05-21 |
| HUE025395T2 (en) | 2016-02-29 |
| ME02200B (me) | 2016-02-20 |
| SMT201500300B (it) | 2016-01-08 |
| WO2012106540A1 (en) | 2012-08-09 |
| PL2670401T3 (pl) | 2015-11-30 |
| JP2014504646A (ja) | 2014-02-24 |
| CN103458881B (zh) | 2015-08-12 |
| JP5837095B2 (ja) | 2015-12-24 |
| HRP20150946T1 (hr) | 2015-10-09 |
| AU2012212142A1 (en) | 2013-08-15 |
| CA2824092C (en) | 2020-06-30 |
| CY1116662T1 (el) | 2017-03-15 |
| US20130296357A1 (en) | 2013-11-07 |
| EP2670401B1 (en) | 2015-06-10 |
| BR112013019643A2 (pt) | 2016-10-04 |
| EA023404B1 (ru) | 2016-05-31 |
| EP2670401A1 (en) | 2013-12-11 |
| DK2670401T3 (en) | 2015-09-07 |
| SI2670401T1 (sl) | 2015-10-30 |
| EA201391114A1 (ru) | 2013-12-30 |
| MX2013008791A (es) | 2013-10-07 |
| RS54189B1 (sr) | 2015-12-31 |
| US8703787B2 (en) | 2014-04-22 |
| KR20130121174A (ko) | 2013-11-05 |
| BR112013019643B1 (pt) | 2022-04-19 |
| PT2670401E (pt) | 2015-10-12 |
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