JOP20190281A1 - مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه - Google Patents
مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجهInfo
- Publication number
- JOP20190281A1 JOP20190281A1 JOP/2019/0281A JOP20190281A JOP20190281A1 JO P20190281 A1 JOP20190281 A1 JO P20190281A1 JO P20190281 A JOP20190281 A JO P20190281A JO P20190281 A1 JOP20190281 A1 JO P20190281A1
- Authority
- JO
- Jordan
- Prior art keywords
- cancer
- treatment
- same
- diphenylpyrimidin
- prevention
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 4
- 201000011510 cancer Diseases 0.000 title abstract 4
- 239000004480 active ingredient Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000002265 prevention Effects 0.000 title abstract 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 abstract 4
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 4
- 230000035772 mutation Effects 0.000 abstract 4
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 abstract 4
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 abstract 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 3
- 230000000694 effects Effects 0.000 abstract 2
- GKFFFOLFBJUEFN-UHFFFAOYSA-N 2-n,4-n-diphenylpyrimidine-2,4-diamine Chemical class C=1C=NC(NC=2C=CC=CC=2)=NC=1NC1=CC=CC=C1 GKFFFOLFBJUEFN-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/308—Foods, ingredients or supplements having a functional effect on health having an effect on cancer prevention
Abstract
يتعلق الاختراع الحالي بمشتق<span dir="LTR"> N2</span>، <span dir="LTR">N4-</span>ثنائي فينيل بيريميدين - 2، ?- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه. يُظهر المُشتق تأثير مُثبط لنشاط<span dir="LTR"> EGFR </span>ضعيف نسبيًا على النوع البري من<span dir="LTR"> EGFR</span>، قدرة تثبيط مرتفعة على طفرة<span dir="LTR"> EGFR</span>، وقدرة تثبيط مرتفعة على<span dir="LTR"> FLT3 </span>وطفرة<span dir="LTR"> FLT3 </span>أيضًا، ومن ثم يُمكن استخدامها بشكل فعال لعلاج السرطان نتيجة طفرة<span dir="LTR"> EGFR </span>أو سرطان بـ<span dir="LTR"> FLT3 </span>أو طفرة منه، ويُظهر المشتق تأثير تآزري عند زمن إعطاء التوليفة، ومن ثم يُمكن استخدامه بشكل فعال للعلاج الخاص بإعطاء توليفة<span dir="LTR">.</span>
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20170073907 | 2017-06-13 | ||
KR1020170146241A KR20180135781A (ko) | 2017-06-13 | 2017-11-03 | N2,n4-디페닐피리미딘-2,4-디아민 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
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JOP20190281A1 true JOP20190281A1 (ar) | 2019-12-02 |
Family
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JOP/2019/0281A JOP20190281A1 (ar) | 2017-06-13 | 2017-06-16 | مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه |
Country Status (17)
Country | Link |
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US (2) | US11253516B2 (ar) |
EP (1) | EP3640246B1 (ar) |
JP (1) | JP6945015B2 (ar) |
KR (2) | KR20180135781A (ar) |
CN (1) | CN110740999A (ar) |
AU (1) | AU2018286361B2 (ar) |
BR (1) | BR112019026253A2 (ar) |
CA (1) | CA3066083C (ar) |
CL (1) | CL2019003589A1 (ar) |
EA (1) | EA201992722A1 (ar) |
IL (1) | IL271291B2 (ar) |
JO (1) | JOP20190281A1 (ar) |
MX (1) | MX2019014548A (ar) |
NZ (1) | NZ760089A (ar) |
SA (1) | SA519410722B1 (ar) |
WO (1) | WO2018230934A1 (ar) |
ZA (1) | ZA201908241B (ar) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
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KR101992621B1 (ko) | 2017-12-07 | 2019-09-27 | 주식회사 온코빅스 | 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물 |
EP3941463A1 (en) | 2019-03-22 | 2022-01-26 | Sumitomo Dainippon Pharma Oncology, Inc. | Compositions comprising pkm2 modulators and methods of treatment using the same |
US20220267294A1 (en) * | 2019-06-20 | 2022-08-25 | Dana-Farber Cancer Institute, Inc. | Small molecule inhibitors of src tyrosine kinase |
JP7330546B6 (ja) * | 2019-06-20 | 2024-02-21 | オンコビクス・カンパニー・リミテッド | 癌細胞の成長を抑制するピリミジン誘導体およびその医薬用途 |
WO2021003417A1 (en) * | 2019-07-03 | 2021-01-07 | Sumitomo Dainippon Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof |
EP4079730A4 (en) * | 2019-12-16 | 2023-11-29 | Oncobix Co., Ltd. | NOVEL DEUTERIUM SUBSTITUTED PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME |
CN113896744B (zh) * | 2020-07-06 | 2024-04-16 | 成都先导药物开发股份有限公司 | 一种选择性egfr抑制剂 |
CN112390760B (zh) * | 2020-10-15 | 2022-07-29 | 北京师范大学 | 靶向fak的化合物及其制备方法和应用 |
CN112239422B (zh) * | 2020-10-16 | 2022-07-22 | 河北化工医药职业技术学院 | 一种布格替尼中间体、其盐、其制备方法以及布格替尼的制备方法 |
EP4274567A1 (en) * | 2021-01-05 | 2023-11-15 | Sumitomo Pharma Oncology, Inc. | Forms and formulations of a tyrosine kinase non-receptor 1 (tnk1) inhibitor |
US20240051940A1 (en) * | 2021-02-08 | 2024-02-15 | Accutar Biotechnology Inc. | Sulfonamides with egfr inhibition activities and their use thereof |
AU2022250976A1 (en) * | 2021-04-01 | 2023-08-17 | Industry-Academic Cooperation Foundation, Yonsei University | Pyrimidine derivative having protein kinase inhibitory activity, and therapeutic pharmaceutical composition comprising same |
IL310020A (en) * | 2021-07-13 | 2024-03-01 | Korea Res Inst Chemical Tech | Innovative 2,4-pyrimidine-diamine derivatives, their preparation method and pharmaceutical preparations containing them as an active substance for the prevention and treatment of cancer |
WO2023201024A1 (en) * | 2022-04-15 | 2023-10-19 | Bridge Biotherapeutics, Inc. | Composition and treatment for cancer with mutations |
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MXPA06001759A (es) * | 2003-08-15 | 2006-05-12 | Novartis Ag | 2,4-pirimidinadiaminas utiles en el tratamiento de enfermedades neoplasticas, desordenes del sistema inmune e inflamatorios. |
RS53588B1 (en) | 2006-12-08 | 2015-02-27 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS |
WO2009127642A2 (en) * | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
EA029131B1 (ru) | 2008-05-21 | 2018-02-28 | Ариад Фармасьютикалз, Инк. | Фосфорсодержащие производные в качестве ингибиторов киназы |
ES2698298T3 (es) * | 2012-03-15 | 2019-02-04 | Celgene Car Llc | Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico |
KR101656382B1 (ko) | 2014-02-28 | 2016-09-09 | 한국화학연구원 | 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물 |
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 |
US10053458B2 (en) | 2014-06-17 | 2018-08-21 | Korea Research Institute Of Chemical Technology | Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient |
EP3195866B1 (en) | 2014-08-22 | 2020-11-18 | FUJIFILM Corporation | Pharmaceutical composition for treating flt3 mutation-positive cancer, mutant flt3 inhibitor and uses thereof |
KR101789934B1 (ko) | 2015-07-31 | 2017-10-26 | 중앙대학교 산학협력단 | 상피세포성장인자수용체 변이체를 가진 종양 진단 및 종양 성장 억제 활성을 갖는 신규 화합물 및 이를 포함하는 의학적 용도 |
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2017
- 2017-06-16 JO JOP/2019/0281A patent/JOP20190281A1/ar unknown
- 2017-11-03 KR KR1020170146241A patent/KR20180135781A/ko active Search and Examination
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2018
- 2018-06-12 NZ NZ760089A patent/NZ760089A/en unknown
- 2018-06-12 BR BR112019026253-9A patent/BR112019026253A2/pt active Search and Examination
- 2018-06-12 CN CN201880039329.5A patent/CN110740999A/zh active Pending
- 2018-06-12 EP EP18816671.4A patent/EP3640246B1/en active Active
- 2018-06-12 JP JP2019568682A patent/JP6945015B2/ja active Active
- 2018-06-12 EA EA201992722A patent/EA201992722A1/ru unknown
- 2018-06-12 KR KR1020180067349A patent/KR102023156B1/ko active IP Right Grant
- 2018-06-12 US US16/622,057 patent/US11253516B2/en active Active
- 2018-06-12 WO PCT/KR2018/006644 patent/WO2018230934A1/ko unknown
- 2018-06-12 MX MX2019014548A patent/MX2019014548A/es unknown
- 2018-06-12 CA CA3066083A patent/CA3066083C/en active Active
- 2018-06-12 AU AU2018286361A patent/AU2018286361B2/en active Active
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- 2019-12-03 SA SA519410722A patent/SA519410722B1/ar unknown
- 2019-12-06 CL CL2019003589A patent/CL2019003589A1/es unknown
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2022
- 2022-02-18 US US17/675,917 patent/US20220249482A1/en active Pending
Also Published As
Publication number | Publication date |
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EP3640246A1 (en) | 2020-04-22 |
NZ760089A (en) | 2022-10-28 |
IL271291B2 (en) | 2023-02-01 |
MX2019014548A (es) | 2020-02-07 |
CA3066083A1 (en) | 2018-12-20 |
EA201992722A1 (ru) | 2020-04-02 |
EP3640246A4 (en) | 2020-08-05 |
EP3640246C0 (en) | 2023-11-01 |
CN110740999A (zh) | 2020-01-31 |
JP2020523360A (ja) | 2020-08-06 |
SA519410722B1 (ar) | 2023-03-15 |
IL271291A (en) | 2020-01-30 |
ZA201908241B (en) | 2021-04-28 |
AU2018286361B2 (en) | 2020-11-19 |
EP3640246B1 (en) | 2023-11-01 |
CL2019003589A1 (es) | 2020-07-03 |
US11253516B2 (en) | 2022-02-22 |
US20200179384A1 (en) | 2020-06-11 |
WO2018230934A1 (ko) | 2018-12-20 |
CA3066083C (en) | 2021-11-30 |
US20220249482A1 (en) | 2022-08-11 |
BR112019026253A2 (pt) | 2020-06-23 |
KR20180135815A (ko) | 2018-12-21 |
JP6945015B2 (ja) | 2021-10-06 |
KR20180135781A (ko) | 2018-12-21 |
KR102023156B1 (ko) | 2019-09-19 |
IL271291B (en) | 2022-10-01 |
AU2018286361A1 (en) | 2020-01-16 |
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