AR110995A1 - Combinación de inhibidores de quinasa atr con sal de radio-223 - Google Patents
Combinación de inhibidores de quinasa atr con sal de radio-223Info
- Publication number
- AR110995A1 AR110995A1 ARP180100408A ARP180100408A AR110995A1 AR 110995 A1 AR110995 A1 AR 110995A1 AR P180100408 A ARP180100408 A AR P180100408A AR P180100408 A ARP180100408 A AR P180100408A AR 110995 A1 AR110995 A1 AR 110995A1
- Authority
- AR
- Argentina
- Prior art keywords
- hours
- component
- methyl
- group
- combination
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000000335 thiazolyl group Chemical group 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 229940125775 ATR kinase inhibitor Drugs 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente abarca combinaciones de por lo menos dos componentes, el componente A y el componente B, donde el componente A es un inhibidor de quinasa ATR, y el componente B que es radio-223, particularmente una sal aceptable desde el punto de vista farmacéutico de radio- 223. Otro aspecto adicional de la presente abarca el uso de dichas combinaciones como se describe en este documento para la preparación de un medicamento para el tratamiento o la profilaxis de una enfermedad hiperproliferativa, particularmente para el tratamiento del cáncer de próstata como también su metástasis ósea. Reivindicación 3: La combinación de acuerdo con la reivindicación 1 ó 2, caracterizada porque dicho componente A se selecciona de VX-803, VX-970, AZD-67 38 y un compuesto de la fórmula (1) en la cual R¹ representa: un resto de la fórmula (2), donde * indica el punto de unión de dicho grupo con el resto de la molécula; R² representa hidrógeno, fluoro, cloro, CN, metilo, C₁₋₄-alcoxi, C₂₋₃-alquenilo, ciclopropilo, heterocicloalquilo de 3 a 6 miembros, heterocicloalquenilo de 4 a 6, fenilo, piridinilo, tiazolilo, -(SO₂)R⁹, -SR⁹, -((SO)=NR¹¹)R¹⁰, -N=(SO)R⁹R¹⁰, donde cada metilo, C₁₋₄-alcoxi, C₂₋₃-alquenilo, ciclopropilo, heterocicloalquilo de 3 a 6 miembros, fenilo, piridilo o tiazolilo está sustituido en forma opcional, una o más veces, independientemente una de otra, con fluoro, cloro, OH, -NR⁷R⁸, metilo, heterocicloalquilo de 5-miembros, -NR⁸(CO)OR⁷, -(SO₂)R⁹, -((SO)=NR¹¹)R¹⁰,- (PO)(OR⁷)₂, o con un grupo seleccionado de: los restos de fórmula (3) ó (4), donde * indica el punto de unión de dicho grupo con el resto de la molécula; donde cada heterocicloalquenilo de 4 a 6 miembros está sustituido en forma opcional, una o más veces, con metilo; R⁴ representa hidrógeno o metilo; R⁷, R⁸ representan, uno independientemente del otro, hidrógeno o C₁₋₄-alquilo; R⁹ representa C₁₋₄-alquilo; R¹⁰ representa C₁₋₄-alquilo; o R⁹ y R¹⁰ juntos, en el caso del grupo -N=(SO)R⁹R¹⁰, representan un grupo heterocicloalquilo de 6 miembros; R¹¹ representa hidrógeno, metilo, -(CO)OR⁷; o un estereoisómero, un tautómero, un N-óxido, un hidrato, un solvato o una sal aceptable desde el punto de vista farmacéutico de los anteriores, o una mezcla de los mismos. Reivindicación 5: La combinación de acuerdo con cualquiera de las reivindicaciones 1 a 4, caracterizada porque dicho componente A es 2-[(3R)-3-metilmorfolin-4-il]-4-(1-metil-1H-pirazol-5-il)-8-(1H-pirazol-5-il)-1,7-naftiridina o un tautómero, un N-óxido, un hidrato, un solvato o una sal aceptable desde el punto de vista farmacéutico de lo anterior. Reivindicación 15: La combinación para usar de acuerdo con la reivindicación 14, caracterizada porque el componente B se administra 2 horas a 96 horas, o 6 horas a 84 horas, o 12 horas a 72 horas, o 24 horas a 48 horas, o 18 horas a 30 horas, o 20 horas a 28 horas, o 22 horas a 26 horas, o 42 horas a 54 horas, o 44 horas a 52 horas, o 46 horas a 50 horas, o 24 horas, o 48 horas antes del componente A. Reivindicación 17: Un kit de acuerdo con la reivindicación 16, caracterizado porque opcionalmente todos, ambos o cualquiera de dichos componentes A y B y opcionalmente C están en forma de una composición farmacéutica que está lista para usar para administrarse simultáneamente, concurrentemente, por separado o de manera secuencial. Reivindicación 18: Una composición farmacéutica que comprende una combinación como se define en cualquiera de las reivindicaciones 1 a 7, junto con uno o más excipientes aceptables desde el punto de vista farmacéutico. Reivindicación 19: Una composición farmacéutica de acuerdo con la reivindicación 18, caracterizada porque los componentes A y B están presentes en una formulación conjunta. Reivindicación 20: Una composición farmacéutica de acuerdo con la reivindicación 18, caracterizada porque los componentes A y B están presentes en formulaciones separadas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17157764 | 2017-02-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR110995A1 true AR110995A1 (es) | 2019-05-22 |
Family
ID=58185318
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180100408A AR110995A1 (es) | 2017-02-24 | 2018-02-22 | Combinación de inhibidores de quinasa atr con sal de radio-223 |
Country Status (4)
| Country | Link |
|---|---|
| AR (1) | AR110995A1 (es) |
| TW (1) | TW201840319A (es) |
| UY (1) | UY37616A (es) |
| WO (1) | WO2018153969A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| WO2017121684A1 (en) | 2016-01-14 | 2017-07-20 | Bayer Pharma Aktiengesellschaft | 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines |
| SG11202107698XA (en) * | 2019-02-11 | 2021-08-30 | Bayer Ag | The atr kinase inhibitor bay1895344 for use in the treatment of a hyper-proliferative disease |
| CN113795287A (zh) * | 2019-03-19 | 2021-12-14 | 阿布拉科斯生物科学有限公司 | 皮下施用包含mTOR抑制剂和白蛋白的纳米颗粒以治疗疾病 |
| CN112773805B (zh) * | 2019-11-11 | 2024-05-10 | 中国科学院脑科学与智能技术卓越创新中心 | 缺血性脑损伤的新型治疗药物 |
| CN114081848A (zh) * | 2021-11-19 | 2022-02-25 | 上海琪维生物科技有限公司 | 用于皮肤护理的组合物及其应用 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| NO310544B1 (no) | 1999-01-04 | 2001-07-23 | Algeta As | Opparbeidelse og anvendelse av radium-223 til fremstilling av preparat samt kit til behandling av kalsifisert vev for palliasjon, benkreft-terapi og/eller overflatebehandling av ben |
| WO2010054398A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CA3013000C (en) | 2008-12-19 | 2022-12-13 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| US20110053923A1 (en) | 2008-12-22 | 2011-03-03 | Astrazeneca | Chemical compounds 610 |
| GB201007353D0 (en) | 2010-04-30 | 2010-06-16 | Algeta Asa | Method |
| GB201007354D0 (en) | 2010-04-30 | 2010-06-16 | Algeta Asa | Method |
| NZ603478A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
| JP2013526538A (ja) | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| EP2569289A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
| NZ603477A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | Compounds useful as inhibitors of atr kinase |
| US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| SA111320519B1 (ar) | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| WO2011163527A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| KR20140027974A (ko) | 2011-04-05 | 2014-03-07 | 버텍스 파마슈티칼스 인코포레이티드 | Ｔｒａ 키나제의 억제제로서 유용한 아미노피라진 화합물 |
| WO2012178124A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| KR20140084112A (ko) | 2011-09-30 | 2014-07-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ａｔｒ 키나제의 억제제로서 유용한 화합물 |
| CN103957917A (zh) | 2011-09-30 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
| WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2776419B1 (en) | 2011-11-09 | 2016-05-11 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| WO2013071088A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| HK1205028A1 (en) | 2012-04-05 | 2015-12-11 | 沃泰克斯药物股份有限公司 | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| WO2014062604A1 (en) | 2012-10-16 | 2014-04-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| HRP20180859T1 (hr) | 2012-12-07 | 2018-07-13 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid kao inhibitor atr kinaze |
| JP2016512239A (ja) | 2013-03-15 | 2016-04-25 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な化合物 |
| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| HRP20192183T1 (hr) | 2013-12-06 | 2020-02-21 | Vertex Pharmaceuticals Inc. | Spoj 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-karboksamida koristan kao inhibitor atr kinase, njegova priprava, različiti kruti oblici te njegovi radioaktivno označeni derivati |
| EP3152212B9 (en) | 2014-06-05 | 2020-05-27 | Vertex Pharmaceuticals Inc. | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
-
2018
- 2018-02-22 AR ARP180100408A patent/AR110995A1/es unknown
- 2018-02-22 WO PCT/EP2018/054362 patent/WO2018153969A1/en not_active Ceased
- 2018-02-22 TW TW107105879A patent/TW201840319A/zh unknown
- 2018-02-22 UY UY0001037616A patent/UY37616A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201840319A (zh) | 2018-11-16 |
| UY37616A (es) | 2018-09-28 |
| WO2018153969A1 (en) | 2018-08-30 |
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Legal Events
| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |