CN102906094A - 用于治疗过度增殖性病症和与血管发生相关的疾病的氨基醇取代的2,3-二氢咪唑并[1,2-c]喹唑啉衍生物 - Google Patents

用于治疗过度增殖性病症和与血管发生相关的疾病的氨基醇取代的2,3-二氢咪唑并[1,2-c]喹唑啉衍生物 Download PDF

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CN102906094A
CN102906094A CN2011800231227A CN201180023122A CN102906094A CN 102906094 A CN102906094 A CN 102906094A CN 2011800231227 A CN2011800231227 A CN 2011800231227A CN 201180023122 A CN201180023122 A CN 201180023122A CN 102906094 A CN102906094 A CN 102906094A
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alkyl
quinazoline
glyoxalidine
methoxyl group
hydroxyl
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CN102906094B (zh
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W·斯科特
刘宁姝
M·默维斯
A·哈格巴尔特
U·门宁
U·伯默
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Bayer Intellectual Property GmbH
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Bayer Pharma AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
CN201180023122.7A 2010-11-11 2011-11-08 用于治疗过度增殖性病症和与血管发生相关的疾病的氨基醇取代的2,3-二氢咪唑并[1,2-c]喹唑啉衍生物 Active CN102906094B (zh)

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US41255610P 2010-11-11 2010-11-11
US61/412,556 2010-11-11
PCT/EP2011/069637 WO2012062748A1 (en) 2010-11-11 2011-11-08 Aminoalcohol substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis

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CN102906094A true CN102906094A (zh) 2013-01-30
CN102906094B CN102906094B (zh) 2016-06-22

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US (2) US8895549B2 (und)
EP (1) EP2638045B1 (und)
JP (1) JP6196156B2 (und)
KR (1) KR20140003436A (und)
CN (1) CN102906094B (und)
AP (1) AP3337A (und)
AR (1) AR083842A1 (und)
AU (1) AU2011328192B2 (und)
BR (1) BR112013011634A2 (und)
CA (1) CA2817317C (und)
CL (1) CL2013001295A1 (und)
CO (1) CO6761350A2 (und)
CR (1) CR20130213A (und)
CU (1) CU20130069A7 (und)
DO (1) DOP2013000105A (und)
EA (1) EA024406B1 (und)
EC (1) ECSP13012618A (und)
GT (1) GT201300121A (und)
HK (1) HK1180685A1 (und)
IL (1) IL226066A0 (und)
MA (1) MA34655B1 (und)
MX (1) MX2013005305A (und)
MY (1) MY164730A (und)
NZ (1) NZ610018A (und)
PE (1) PE20140411A1 (und)
SG (1) SG190100A1 (und)
TW (1) TW201305170A (und)
UA (1) UA113280C2 (und)
UY (1) UY33719A (und)
WO (1) WO2012062748A1 (und)
ZA (1) ZA201304244B (und)

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CN103214489A (zh) * 2013-02-25 2013-07-24 中国人民解放军第二军医大学 一类具有抗肿瘤活性的多靶点激酶抑制剂及其制备方法
CN105263497A (zh) * 2013-04-08 2016-01-20 拜耳制药股份公司 取代的2,3-二氢咪唑并[1,2-c]喹唑啉治疗淋巴瘤的用途
CN108383849A (zh) * 2018-04-26 2018-08-10 浙江大学 咪唑并喹唑啉衍生物及其在抗肿瘤抗炎中的应用
CN113518775A (zh) * 2019-03-07 2021-10-19 生物技术公司 用于制备经取代的咪唑并喹啉的方法
CN113512040A (zh) * 2021-08-25 2021-10-19 河南牧业经济学院 一种新型血根碱仿生类似物及其制备方法

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CN103339133B (zh) * 2010-11-11 2016-06-15 拜耳知识产权有限责任公司 烷氧基取代的2,3-二氢咪唑并[1,2-c]喹唑啉
UA113280C2 (xx) * 2010-11-11 2017-01-10 АМІНОСПИРТЗАМІЩЕНІ ПОХІДНІ 2,3-ДИГІДРОІМІДАЗО$1,2-c]ХІНАЗОЛІНУ, ПРИДАТНІ ДЛЯ ЛІКУВАННЯ ГІПЕРПРОЛІФЕРАТИВНИХ ПОРУШЕНЬ І ЗАХВОРЮВАНЬ, ПОВ'ЯЗАНИХ З АНГІОГЕНЕЗОМ
JP5940078B2 (ja) * 2010-11-11 2016-06-29 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH アリールアミノアルコール−置換2,3−ジヒドロイミダゾ[1,2−c]キノリン
EP2508525A1 (en) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
WO2015082376A2 (en) 2013-12-03 2015-06-11 Bayer Pharma Aktiengesellschaft Use of pi3k-inhibitors
US10124007B2 (en) 2013-12-03 2018-11-13 Bayer Pharma Aktiengesellschaft Combination of PI3K-inhibitors
EP3077002B1 (en) 2013-12-03 2020-04-22 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
WO2016071380A1 (en) * 2014-11-07 2016-05-12 Bayer Pharma Aktiengesellschaft Synthesis of pi3k inhibitor and salts thereof
WO2016071382A1 (en) * 2014-11-07 2016-05-12 Bayer Pharma Aktiengesellschaft Synthesis of pi3k inhibitor and salts thereof
WO2016087488A1 (en) * 2014-12-03 2016-06-09 Bayer Pharma Aktiengesellschaft Administration regime for aminoalcohol substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives
WO2016087490A1 (en) * 2014-12-03 2016-06-09 Bayer Pharma Aktiengesellschaft Combination of pi3k-inhibitors
CN108884159A (zh) 2015-11-07 2018-11-23 茂体外尔公司 用于癌症治疗的包含肿瘤抑制基因治疗和免疫检查点阻断的组合物
CN109729716B (zh) 2016-09-23 2022-03-15 拜耳制药股份公司 Pi3k-抑制剂的组合产品
WO2018111902A1 (en) 2016-12-12 2018-06-21 Multivir Inc. Methods and compositions comprising viral gene therapy and an immune checkpoint inhibitor for treatment and prevention of cancer and infectious diseases
WO2018215282A1 (en) 2017-05-26 2018-11-29 Bayer Pharma Aktiengesellschaft Combination of bub1 and pi3k inhibitors
US11185549B2 (en) 2017-06-28 2021-11-30 Bayer Consumer Care Ag Combination of a PI3K-inhibitor with an androgen receptor antagonist
WO2020036635A2 (en) 2018-03-19 2020-02-20 Multivir Inc. Methods and compositions comprising tumor suppressor gene therapy and cd122/cd132 agonists for the treatment of cancer
CN115315424A (zh) * 2019-10-15 2022-11-08 拜耳公司 2-甲基-氮杂-喹唑啉
WO2021113644A1 (en) 2019-12-05 2021-06-10 Multivir Inc. Combinations comprising a cd8+ t cell enhancer, an immune checkpoint inhibitor and radiotherapy for targeted and abscopal effects for the treatment of cancer
WO2021260443A1 (en) 2020-06-24 2021-12-30 Bayer Aktiengesellschaft Combinations of 2,3-dihydroimidazo[1,2-c]quinazolines
WO2023205680A1 (en) * 2022-04-20 2023-10-26 Synnovation Therapeutics, Inc. PI3Kα INHIBITORS
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Cited By (9)

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Publication number Priority date Publication date Assignee Title
CN103214489A (zh) * 2013-02-25 2013-07-24 中国人民解放军第二军医大学 一类具有抗肿瘤活性的多靶点激酶抑制剂及其制备方法
CN103214489B (zh) * 2013-02-25 2016-10-26 中国人民解放军第二军医大学 一类具有抗肿瘤活性的多靶点激酶抑制剂及其制备方法
CN105263497A (zh) * 2013-04-08 2016-01-20 拜耳制药股份公司 取代的2,3-二氢咪唑并[1,2-c]喹唑啉治疗淋巴瘤的用途
CN105263497B (zh) * 2013-04-08 2019-04-30 拜耳制药股份公司 取代的2,3-二氢咪唑并[1,2-c]喹唑啉治疗淋巴瘤的用途
CN108383849A (zh) * 2018-04-26 2018-08-10 浙江大学 咪唑并喹唑啉衍生物及其在抗肿瘤抗炎中的应用
CN108383849B (zh) * 2018-04-26 2020-11-06 浙江大学 咪唑并喹唑啉衍生物及其在抗肿瘤抗炎中的应用
CN113518775A (zh) * 2019-03-07 2021-10-19 生物技术公司 用于制备经取代的咪唑并喹啉的方法
CN113512040A (zh) * 2021-08-25 2021-10-19 河南牧业经济学院 一种新型血根碱仿生类似物及其制备方法
CN113512040B (zh) * 2021-08-25 2023-10-13 河南牧业经济学院 一种血根碱仿生化合物及其制备方法

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CL2013001295A1 (es) 2013-10-04
HK1180685A1 (zh) 2013-10-25
AU2011328192B2 (en) 2016-09-01
ECSP13012618A (es) 2013-07-31
MY164730A (en) 2018-01-30
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EA201300556A1 (ru) 2013-10-30
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CN102906094B (zh) 2016-06-22
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