JO3194B1 - مشتقات البنزيميدازول كمثبطات لإنزيم pi3 كيناز - Google Patents
مشتقات البنزيميدازول كمثبطات لإنزيم pi3 كينازInfo
- Publication number
- JO3194B1 JO3194B1 JOP/2011/0306A JOP20110306A JO3194B1 JO 3194 B1 JO3194 B1 JO 3194B1 JO P20110306 A JOP20110306 A JO P20110306A JO 3194 B1 JO3194 B1 JO 3194B1
- Authority
- JO
- Jordan
- Prior art keywords
- suitably
- relates
- diseases
- benzimidazole derivatives
- pi3kβ
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/10—Radicals substituted by halogen atoms or nitro radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
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- 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
- C07D401/10—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 carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D413/10—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 carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
Abstract
يتعلق الاختراع باستخدام مشتقات البنزيميدازول لتعديل، وتحديداً لتثبيط، نشاط أو وظيفة مجموعة إنزيمات الفوسفو إينوسيتيد -3- OH- كيناز (يشار إليها فيما بعد بإنزيمات PI3 كيناز)، وبشكل مناسب إنزيمات PI3Ka و/أو PI3Kδ و/أو PI3Kβ و/أو PI3Ky. وعلى نحو مناسب، يتعلق الاختراع الحالي باستخدام البنزيميدازولات في علاج واحدة أو أكثر من الحالات المرضية المختارة من: اضطرابات المناعة الذاتية، والأمراض الالتهابية، والأمراض القلبية الوعائية، وأمراض الضمور العصبي، والحساسية، والربو، والتهاب البنكرياس، وفشل الأعضاء المتعدد، وأمراض الكلى، والأمراض الناتجة عن تجمعّ الصفيحات الدموية، والسرطان، واضطراب حركة الحيوانات المنوية، ورفض الجسم للأعضاء المنزرعة، ورفض الجسم للطعوم المنزرعة، وإصابات الرئة، وبشكل أكثر ملاءمة، يتعلق الاختراع الحالي بمركبات البنزيميدازول ذات الانتقائية تجاه إنزيم PI3Kβ. وذلك لعلاج أمراض السرطان.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US39031410P | 2010-10-06 | 2010-10-06 | |
US201161528397P | 2011-08-29 | 2011-08-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
JO3194B1 true JO3194B1 (ar) | 2018-03-08 |
Family
ID=45925614
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JOP/2011/0306A JO3194B1 (ar) | 2010-10-06 | 2011-10-04 | مشتقات البنزيميدازول كمثبطات لإنزيم pi3 كيناز |
Country Status (37)
Country | Link |
---|---|
US (10) | US20130196990A1 (ar) |
EP (2) | EP2624696B1 (ar) |
JP (1) | JP5719028B2 (ar) |
KR (1) | KR101594002B1 (ar) |
CN (1) | CN103124496B (ar) |
AR (1) | AR083296A1 (ar) |
AU (1) | AU2011312594B2 (ar) |
BR (1) | BR112013008259A2 (ar) |
CA (1) | CA2812608C (ar) |
CL (1) | CL2013000935A1 (ar) |
CO (1) | CO6700852A2 (ar) |
CR (1) | CR20130192A (ar) |
CY (1) | CY1118792T1 (ar) |
DK (1) | DK2624696T3 (ar) |
DO (1) | DOP2013000059A (ar) |
EA (1) | EA022623B1 (ar) |
ES (2) | ES2616238T3 (ar) |
HR (1) | HRP20170279T1 (ar) |
HU (1) | HUE033209T2 (ar) |
IL (1) | IL225140A (ar) |
JO (1) | JO3194B1 (ar) |
LT (1) | LT2624696T (ar) |
MA (1) | MA34591B1 (ar) |
ME (1) | ME02663B (ar) |
MX (1) | MX337662B (ar) |
MY (1) | MY170236A (ar) |
NZ (1) | NZ608069A (ar) |
PE (1) | PE20140192A1 (ar) |
PL (1) | PL2624696T3 (ar) |
PT (1) | PT2624696T (ar) |
RS (1) | RS55662B1 (ar) |
SG (1) | SG188974A1 (ar) |
SI (1) | SI2624696T1 (ar) |
TW (1) | TWI513690B (ar) |
UY (1) | UY33648A (ar) |
WO (1) | WO2012047538A1 (ar) |
ZA (1) | ZA201301951B (ar) |
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EA022623B1 (ru) | 2010-10-06 | 2016-02-29 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Производные бензимидазола в качестве ингибиторов pi3-киназ |
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RU2015132907A (ru) * | 2013-01-09 | 2017-02-14 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Комбинация |
US20160228446A1 (en) * | 2013-09-19 | 2016-08-11 | GlaxoSmithKline LLCC | Combination Drug Therapy |
WO2015042027A1 (en) * | 2013-09-19 | 2015-03-26 | Glaxosmithkline Llc | Combination drug therapy |
CN106831721B (zh) * | 2013-10-16 | 2019-10-22 | 上海璎黎药业有限公司 | 稠合杂环化合物、其制备方法、药物组合物和用途 |
CN103910682B (zh) * | 2013-11-28 | 2016-03-02 | 大连理工大学 | 一种基于邻苯二胺环化的苯并咪唑类化合物制备方法 |
WO2015095838A2 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of mek type i and erk inhibitors |
CN106573922A (zh) | 2014-06-13 | 2017-04-19 | 吉利德科学公司 | 磷脂酰肌醇3‑激酶抑制剂 |
NZ726608A (en) | 2014-06-13 | 2018-04-27 | Gilead Sciences Inc | Phosphatidylinositol 3-kinase inhibitors |
NZ726052A (en) | 2014-06-13 | 2018-04-27 | Gilead Sciences Inc | Phosphatidylinositol 3-kinase inhibitors |
EA201692266A1 (ru) | 2014-06-13 | 2017-06-30 | Джилид Сайэнс, Инк. | Ингибиторы фосфатидилинозитол-3-киназы |
MA40059A (fr) | 2014-06-13 | 2015-12-17 | Gilead Sciences Inc | Inhibiteurs de la phosphatidylinositol 3-kinase |
WO2016097359A1 (en) | 2014-12-19 | 2016-06-23 | Janssen Pharmaceutica Nv | Heterocyclyl linked imidazopyridazine derivatives as pi3kbeta inhibitors |
LT3233862T (lt) * | 2014-12-19 | 2019-09-10 | Janssen Pharmaceutica Nv | Imidazopiridazino dariniai, kaip pi3kbeta slopikliai |
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CA3011189C (en) * | 2016-01-14 | 2024-02-20 | Bayer Pharma Aktiengesellschaft | 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines |
EA037361B1 (ru) | 2016-06-16 | 2021-03-18 | Янссен Фармацевтика Нв | Производные бициклического пиридина, пиразина и пиримидина в качестве ингибиторов pi3k бета |
JP7158286B2 (ja) | 2016-06-16 | 2022-10-21 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのアザベンゾイミダゾール誘導体 |
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JP5791150B2 (ja) | 2009-12-15 | 2015-10-07 | 塩野義製薬株式会社 | 血管内皮リパーゼ阻害活性を有するオキサジアゾール誘導体 |
ES2362337B1 (es) | 2009-12-17 | 2012-05-16 | Consejo Superior De Investigaciones Cient�?Ficas (Csic) | Derivados de aminociclitoles, procedimiento de obtencion y usos. |
EA022623B1 (ru) * | 2010-10-06 | 2016-02-29 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Производные бензимидазола в качестве ингибиторов pi3-киназ |
WO2015053091A1 (ja) | 2013-10-11 | 2015-04-16 | ユニ・チャーム株式会社 | ペットフード |
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