JOP20190058B1 - مشتقات كرومان، أيزوكرومان وداي هيدرو أيزو بنزوفوران كمُعدلات تفارغية سالبة mGluR2، تركيبات، واستخدامها - Google Patents

مشتقات كرومان، أيزوكرومان وداي هيدرو أيزو بنزوفوران كمُعدلات تفارغية سالبة mGluR2، تركيبات، واستخدامها

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JOP20190058B1
JOP20190058B1 JOP/2019/0058A JOP20190058A JOP20190058B1 JO P20190058 B1 JOP20190058 B1 JO P20190058B1 JO P20190058 A JOP20190058 A JO P20190058A JO P20190058 B1 JOP20190058 B1 JO P20190058B1
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mglur2
pharmaceutically acceptable
disorders
compounds
acceptable salt
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JOP/2019/0058A
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English (en)
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Arasappan Ashok
Demong Duane
R Wilkening Robert
B Hoyt Scott
K Sebhat Iyassu
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Merck Sharp And Dohme Llc
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    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
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Abstract

يتعلق الاختراع الحالي بتوفير مركبات كرومان، أيزوكرومان، وداي هيدرو أيزو بنزوفوران مستبدلة معينة من الصيغة (I) أو ملح مقبول صيدلانياً منها، حيث تكون الحلقة A عبارة عن شطر تم اختياره من: (II)،(III)،(IV)،(V) وتكون الحلقة B، n، R1، R2، R2A، R3، R3A كما تحدد هنا. تكون مركبات الاختراع مفيدة بوصفها مثبطات mGluR2، أو مُعدلات تفارغية سالبة mGluR2 (NAMs)، وقد تكون مفيدة في طرق لعلاج مريض من أمراض أو اضطرابات يتدخل فيها المستقبل mGluR2-NAM، مثلا مرض الزهايمر، الخلل الإدراكي، الخلل الإدراكي البسيط، الفصام واضطرابات مزاجية أخرى، اضطرابات الألم واضطرابات النوم، عن طريق إعطاء المريض كمية فعّالة علاجياً من مركب الاختراع، أو ملح مقبول صيدلانياً منه. يتعلق الاختراع أيضاً بتركيبات صيدلانية تشتمل على مركب من الاختراع، أو ملح مقبول صيدلانياً منه (اختيارياً في توليفة مع واحد أو أكثر من المقومات النشطة الإضافية)، ومادة حاملة مقبولة صيدلانياً، واستخدام المركبات والتركيبات الصيدلانية من الاختراع في علاج هذه الأمراض.
JOP/2019/0058A 2016-09-27 2017-09-25 مشتقات كرومان، أيزوكرومان وداي هيدرو أيزو بنزوفوران كمُعدلات تفارغية سالبة mGluR2، تركيبات، واستخدامها JOP20190058B1 (ar)

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US201662400150P 2016-09-27 2016-09-27
PCT/US2017/053155 WO2018063955A1 (en) 2016-09-27 2017-09-25 CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

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JOP20190058A1 JOP20190058A1 (ar) 2019-03-24
JOP20190058B1 true JOP20190058B1 (ar) 2023-09-17

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ECSP19020742A (es) 2019-04-30
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EA038627B1 (ru) 2021-09-24
AU2017334870A1 (en) 2019-03-28
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PL3519416T3 (pl) 2021-09-06
US10335399B2 (en) 2019-07-02
CN109983022A (zh) 2019-07-05
DOP2019000076A (es) 2019-07-15
MY196807A (en) 2023-05-03
US20190247374A1 (en) 2019-08-15
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JP6992109B2 (ja) 2022-02-15
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MA46342A (fr) 2019-08-07
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