JOP20190113A1 - مثبطات بروتون تيروزين كيناز - Google Patents

مثبطات بروتون تيروزين كيناز

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JOP20190113A1
JOP20190113A1 JOP/2019/0113A JOP20190113A JOP20190113A1 JO P20190113 A1 JOP20190113 A1 JO P20190113A1 JO P20190113 A JOP20190113 A JO P20190113A JO P20190113 A1 JOP20190113 A1 JO P20190113A1
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independently
alkyl
hal
fragment
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JOP/2019/0113A
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Anna Aleksandrovna Kukushkina
Sergey Aleksandrovich Silonov
Anna Sergeevna Kushakova
Pavel Aleksandrovich Aleshunin
Natalia Vladimirovna Kozhemyakina
Alexander Moldavsky
Aleksandra Vladimirovna Popkova
Pavel Andreevich Iakovlev
Aleksey Sergeevich Gavrilov
Svetlana Leonidovna Gorbunova
Leonid Evgen`Evich Mikhaylov
Mikhail Vladimirovich Rekharsky
Svetlana Sergeevna Smirnova
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Biocad Joint Stock Co
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Publication of JOP20190113A1 publication Critical patent/JOP20190113A1/ar

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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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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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • General Chemical & Material Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

<strong>يتعلق الاختراع الحالي بمركب جديد له الصيغة </strong><span dir="LTR">I</span>: <span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image002.gif" /></span><strong> الصيغة </strong><span dir="LTR">I</span> <strong>أو ملح مقبول صيدلانيا، تذاوب أو أيزومير فراغي منه، </strong> <strong>حيث: </strong> <span dir="LTR">V<sub>1</sub></span><strong> عبارة عن </strong><span dir="LTR">C</span><strong> أو </strong><span dir="LTR">N</span><strong>، </strong> <span dir="LTR">V<sub>2</sub></span><strong> عبارة عن </strong><span dir="LTR">C(R<sub>2</sub>)</span><strong> أو </strong><span dir="LTR">N</span><strong>، </strong> <strong> حيث إذا كان </strong><span dir="LTR">V<sub>1</sub></span><strong> عبارة عن </strong><span dir="LTR">C</span><strong> فإن </strong><span dir="LTR">V<sub>2</sub></span><strong> عبارة عن </strong><span dir="LTR">N</span><strong>، </strong> <strong> إذا كان </strong><span dir="LTR">V<sub>1</sub></span><strong> عبارة عن </strong><span dir="LTR">C</span><strong> فإن </strong><span dir="LTR">V<sub>2</sub></span><strong> عبارة عن </strong><span dir="LTR">?(R<sub>2</sub>)</span><strong>، أو </strong> <strong> إذا كان </strong><span dir="LTR">V<sub>1</sub></span><strong> عبارة عن </strong><span dir="LTR">N</span><strong> فإن </strong><span dir="LTR">V<sub>2</sub></span><strong> عبارة عن </strong><span dir="LTR">?(R<sub>2</sub>)</span><strong>؛ </strong> <strong> كل من </strong><span dir="LTR">n</span><strong>، </strong><span dir="LTR">k</span><strong> تمثل على حدة </strong><strong>0</strong><strong>، 1؛ </strong> <strong> كل من </strong><span dir="LTR">R<sub>2</sub></span><strong>، </strong><span dir="LTR">R<sub>11</sub></span><strong> تمثل على حدة </strong><span dir="LTR">H</span><strong>، </strong><span dir="LTR">D</span><strong>، </strong><span dir="LTR">Hal</span><strong>، </strong><span dir="LTR">CN</span><strong>، </strong><span dir="LTR">NR’R’’</span><strong>، </strong><span dir="LTR">C(O)NR’R’’</span><strong>، </strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong> ألكوكسي؛ </strong> <span dir="LTR">R<sub>3</sub></span><strong> عبارة عن </strong><span dir="LTR">H</span><strong>، </strong><span dir="LTR">D</span><strong>، هيدروكسي، الكيل</strong><span dir="LTR"> ?(O)C<sub>1</sub>-C<sub>6</sub></span><strong>، الكينيل</strong><span dir="LTR">?(?)?<sub>2</sub>-?<sub>6</sub></span><strong>،</strong><span dir="LTR">?(?)?<sub>2</sub>-?<sub>6</sub> </span><strong>الكاينيل</strong><strong>، الكيل</strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong>؛ </strong> <span dir="LTR">R<sub>4</sub></span> <strong>عبارة عن</strong> <span dir="LTR">H</span><strong>، </strong><span dir="LTR">Hal</span><strong>، </strong><span dir="LTR">CN</span><strong>، </strong><span dir="LTR">CONR’R’’</span><strong>، هيدروكسي، الكيل </strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong>، ألكوكسي </strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong>؛ </strong> <span dir="LTR">L</span><strong> عبارة عن </strong><span dir="LTR">CH<sub>2</sub></span><strong>، </strong><span dir="LTR">NH</span><strong>، </strong><span dir="LTR">?</span><strong> أو رابطة كيميائية؛ </strong> <span dir="LTR">R<sub>1</sub></span><strong> يتم اختيارها من مجموعة أجزاء، </strong><strong>متضمنة</strong>: <span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image004.gif" /></span><strong> الجزء 1، </strong> <span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image006.gif" /></span><strong> الجزء 2، </strong> <span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image008.gif" /></span><strong> الجزء 3</strong> <strong> كل من </strong><span dir="LTR">?<sub>1</sub></span><strong>، </strong><span dir="LTR">?<sub>2</sub></span><strong>، </strong><span dir="LTR">?<sub>3</sub></span><strong>، </strong><span dir="LTR">?<sub>4</sub></span><strong> تمثل على حدة </strong><span dir="LTR">??</span><strong>، </strong><span dir="LTR">N</span><strong>، </strong><span dir="LTR">?Hal</span><strong>؛ </strong> <strong> كل من </strong><span dir="LTR">?<sub>5</sub></span><strong>، </strong><span dir="LTR">?<sub>6</sub></span><strong>، </strong><span dir="LTR">?<sub>7</sub></span><strong>، </strong><span dir="LTR">?<sub>8</sub></span><strong>، </strong><span dir="LTR">?<sub>9</sub></span><strong> تمثل على حدة </strong><span dir="LTR">?</span><strong>، </strong><span dir="LTR">?H</span><strong> أو </strong><span dir="LTR">N</span><strong>؛ </strong> <span dir="LTR">R<sub>5</sub></span><strong> عبارة عن </strong><span dir="LTR">H</span><strong>، </strong><span dir="LTR">?N</span><strong>، </strong><span dir="LTR">Hal</span><strong>، </strong><span dir="LTR">CONR’R’’</span><strong>، الكيل</strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong>، غير مستبدل أو مستبدل بواحد أو أكثر من ال</strong><strong>هالوجينات؛ </strong> <strong> كل من </strong><span dir="LTR">R’</span><strong> و </strong><span dir="LTR">R’’</span> <strong>يتم اختيارها على حدة</strong> <strong>من المجموعة</strong><strong>، المتضمنة </strong><span dir="LTR">H</span><strong>، </strong><strong>الكيل</strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub></span><strong>، </strong><span dir="LTR">C<sub>1</sub>-C<sub>6</sub> </span><strong>الكيل حلقي</strong><strong>، </strong><strong>أريل</strong><strong>؛ </strong> <span dir="LTR">R<sub>6</sub></span><strong> يتم اختيارها من المجموعة: </strong> <span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image010.gif" /></span><strong>، </strong><span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image012.gif" /></span><strong>، </strong><span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image014.gif" /></span><strong>، </strong><span dir="LTR"><img src="file:https:///C:\Users\mohammad.tw\AppData\Local\Temp\msohtmlclip1\01\clip_image016.gif" /></span><strong>؛ </strong> <strong> كل من </strong><span dir="LTR">R<sub>7</sub></span><strong>، </strong><span dir="LTR">R<sub>8</sub></span><strong>، </strong><span dir="LTR">R<sub>9</sub></span><strong>، </strong><span dir="LTR">R<sub>10</sub></span><strong> تمثل على حدة فينيل، مثيل أسيتيلين؛ </strong> <span dir="LTR">Hal</span><strong> عبارة عن </strong><span dir="LTR">Cl</span><strong>، </strong><span dir="LTR">Br</span><strong>، </strong><span dir="LTR">I</span><strong>، </strong><span dir="LTR">F</span><strong>.</strong> <strong>التي لها خواص مثبطات بروتون تيروزين كيناز (</strong><span dir="LTR">Btk</span><strong>) , للتركيبات لاصيدلانية التي تحتوي على هذه المركبات, واستخدامها كأدوية لعلاج الأمراض والاضطرابات.</strong>
JOP/2019/0113A 2016-11-18 2017-06-16 مثبطات بروتون تيروزين كيناز JOP20190113A1 (ar)

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US (1) US20190352276A1 (ar)
EP (1) EP3541811A1 (ar)
JP (1) JP2019537611A (ar)
KR (1) KR20190104516A (ar)
CN (1) CN110177781A (ar)
AU (1) AU2017362066A1 (ar)
BR (1) BR112019009945A2 (ar)
CA (1) CA3043297A1 (ar)
CL (1) CL2019001330A1 (ar)
CR (1) CR20190261A (ar)
EA (1) EA201990902A1 (ar)
EC (1) ECSP19043231A (ar)
JO (1) JOP20190113A1 (ar)
MA (1) MA45888A1 (ar)
MX (1) MX2019005706A (ar)
PE (1) PE20191082A1 (ar)
PH (1) PH12019550083A1 (ar)
WO (1) WO2018092047A1 (ar)
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KR20230053661A (ko) * 2020-08-17 2023-04-21 베타 파머수티컬 컴퍼니 리미티드 비사이클 화합물과 비사이클 화합물을 포함하는 조성물 및 이들의 용도
CN114478519B (zh) * 2020-10-23 2024-06-11 励缔(杭州)医药科技有限公司 吡唑并吡啶类化合物或其盐及其制备方法和用途
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US20190352276A1 (en) 2019-11-21
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AU2017362066A1 (en) 2019-05-30
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MX2019005706A (es) 2019-07-08
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