ES2421527T3 - Inhibidores de aspartilproteasa heterocíclica - Google Patents

Inhibidores de aspartilproteasa heterocíclica

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Publication number
ES2421527T3
ES2421527T3 ES04813947T ES04813947T ES2421527T3 ES 2421527 T3 ES2421527 T3 ES 2421527T3 ES 04813947 T ES04813947 T ES 04813947T ES 04813947 T ES04813947 T ES 04813947T ES 2421527 T3 ES2421527 T3 ES 2421527T3
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ES
Spain
Prior art keywords
alkyl
heterocycloalkylalkyl
heteroarylalkyl
cycloalkylalkyl
arylalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES04813947T
Other languages
English (en)
Inventor
Zhaoning Zhu
Brian Mckittrick
Zhong-Yue Sun
Yuanzan Ye
Corey Strickland
Elizabeth Smith
Andrew Stamford
William Greenlee
Yusheng Wu
Ulrich Iserloh
Robert Mazzola
John Caldwell
Jared Cumming
Lingyan Wang
Tao Guo
Thuy Le
Kurt Saionz
Suresh Babu
Johannes H Voigt
Rachael C Hunter
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Pharmacopeia LLC
Original Assignee
Schering Corp
Merck Sharp and Dohme LLC
Pharmacopeia LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Schering Corp, Merck Sharp and Dohme LLC, Pharmacopeia LLC filed Critical Schering Corp
Application granted granted Critical
Publication of ES2421527T3 publication Critical patent/ES2421527T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
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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
    • C07D401/12—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
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto que tiene la fórmula estructural IB: **Fórmula^** o un estereoisómero, tautómero, o sal o solvato farmacéuticamente aceptables del mismo, en la que U es -C(R6)(R7)-; R1 está seleccionado de H, alquilo, alquenilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, -OR15, -CN, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2 -N>=C(R8)2 y -N(R8)2; R2 es H o alquilo; R5 está seleccionado de H, alquilo, alquenilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, -OR15, -CN, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2 -N>=C(R8)2 y -N(R8)2; a condición de que R1 y R5 no se seleccionen ambos de -NO2 -N>=C(R8)2 y -N(R8)2; R3 y R4 están seleccionados independientemente de H, alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -CH2-O-Si(R9)(R10)(R19), -SH, -15 CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(>=NOH)R8; R6 y R7 están seleccionados independientemente de alquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -CH2-O-Si(R9)(R10)(R19), -SH, -CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -N(R11)(R12), -20 N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(>=NOH)R8; o R3 y R4 o R6 y R7 junto con el carbono al que están unidos se combinan para formar grupos multicíclicos de las siguientes fórmulas: **Fórmula**
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Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP1758907B1 (en) 2004-06-16 2009-02-18 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase
TW200602045A (en) * 2004-06-16 2006-01-16 Wyeth Corp Amino-5, 5-diphenylimidazolone derivatives for the inhibition of β-secretase
NZ554374A (en) * 2004-10-07 2010-11-26 Vitae Pharmaceuticals Inc Diaminoalkane aspartic protease inhibitors
JP2008526966A (ja) 2005-01-14 2008-07-24 ワイス β−セクレターゼの阻害のためのアミノ−イミダゾロン
BRPI0607094A2 (pt) 2005-02-01 2009-08-04 Wyeth Corp composto da fórmula i; uso do composto para o tratamento de uma doença ou distúrbio associado à atividade excessiva de bace em um paciente que dele necessita; uso do composto para modular a atividade de bace; e composição farmacêutica
CN101146769A (zh) 2005-02-14 2008-03-19 惠氏公司 作为β-分泌酶抑制剂的唑基酰基胍
AU2006259572A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
CA2610617A1 (en) * 2005-06-14 2006-12-28 Schering Corporation The preparation and use of protease inhibitors
JP2008543841A (ja) * 2005-06-14 2008-12-04 シェーリング コーポレイション 大環状複素環式アスパルチルプロテアーゼインヒビター
KR20080028881A (ko) * 2005-06-14 2008-04-02 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도
EP1896477B1 (en) 2005-06-14 2010-09-22 Schering Corporation Aspartyl protease inhibitors
WO2006138217A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
EP1896448A1 (en) * 2005-06-30 2008-03-12 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
PE20070461A1 (es) * 2005-09-26 2007-05-10 Wyeth Corp Compuestos de amino-5-[4-(difluorometoxi)fenil]-5-fenilimidazolona como inhibidores de b-secretasa
EP2597087B1 (en) 2005-10-25 2016-03-30 Shionogi&Co., Ltd. Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
EP1940828B1 (en) 2005-10-27 2010-08-18 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7560451B2 (en) 2005-10-31 2009-07-14 Schering Corporation Aspartyl protease inhibitors
CN101360720A (zh) * 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶酮衍生物及其用途
JP2009520686A (ja) * 2005-11-21 2009-05-28 アストラゼネカ・アクチエボラーグ 新規な２−アミノ−イミダゾール−４−オン化合物並びに認知障害、アルツハイマー病、神経変性及び認知症の治療に使用する医薬の製造におけるその使用
TW200734311A (en) * 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
CA2634037A1 (en) * 2005-12-19 2007-07-12 Wyeth 2-amino-5-piperidinylimidazolone compounds and use thereof for .beta.-secretase modulation
AR058381A1 (es) * 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
WO2007100536A1 (en) 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
JP5191155B2 (ja) * 2006-03-27 2013-04-24 大塚製薬株式会社 カルボスチリル化合物からなる医薬
WO2007114771A1 (en) * 2006-04-05 2007-10-11 Astrazeneca Ab 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR TREATING OR PREVENTING Aβ-RELATED PATHOLOGIES
CA2653650A1 (en) * 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
US7700606B2 (en) 2006-08-17 2010-04-20 Wyeth Llc Imidazole amines as inhibitors of β-secretase
WO2008063114A1 (en) * 2006-11-20 2008-05-29 Astrazeneca Ab Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia
CN101668751A (zh) * 2006-12-12 2010-03-10 先灵公司 天冬氨酰蛋白酶抑制剂
TW200831484A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
WO2008076044A1 (en) * 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
TW200831091A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
AR065814A1 (es) 2007-03-23 2009-07-01 Wyeth Corp Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados.
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
CA2683887A1 (en) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein
UY31083A1 (es) * 2007-05-15 2009-01-05 Astrazeneca Ab Derivados de sulfoximinas para la inhibicion de b-secretasa
MX2010002674A (es) 2007-09-06 2010-03-25 Schering Corp Moduladores de gamma secretasa.
CN101910178A (zh) 2007-11-05 2010-12-08 先灵公司 γ分泌酶调节剂
CA2708300A1 (en) 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
CN101910143B (zh) 2008-01-18 2013-08-21 卫材R&D管理有限公司 稠合的氨基二氢噻嗪衍生物
EP2288613B1 (en) 2008-04-22 2016-07-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
ES2433223T3 (es) 2008-07-28 2013-12-10 Eisai R&D Management Co., Ltd. Derivados de espiroaminodihidrotiazina
WO2010013302A1 (ja) * 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
EP2324032B1 (en) 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
WO2010030954A1 (en) 2008-09-11 2010-03-18 Amgen Inc. Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
KR20110076965A (ko) 2008-09-30 2011-07-06 에자이 알앤드디 매니지먼트 가부시키가이샤 신규한 축합 아미노 디하이드로티아진 유도체
WO2010047372A1 (ja) * 2008-10-22 2010-04-29 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体
AU2009314049B2 (en) 2008-11-13 2015-03-05 Merck Sharp & Dohme Corp. Gamma secretase modulators
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010105179A2 (en) 2009-03-13 2010-09-16 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
JPWO2010113848A1 (ja) 2009-03-31 2012-10-11 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
EP2443118A1 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
EP2281824A1 (en) 2009-08-07 2011-02-09 Noscira, S.A. Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
BR112012013854A2 (pt) 2009-12-11 2019-09-24 Shionogi & Co derivados de oxazina.
JPWO2011071109A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
US8889703B2 (en) 2010-02-24 2014-11-18 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
MX2012010658A (es) 2010-03-15 2012-12-05 Amgen Inc Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa.
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
WO2012069428A1 (en) 2010-11-22 2012-05-31 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
US8957083B2 (en) 2010-11-23 2015-02-17 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
SG10201601516QA (en) 2011-01-21 2016-03-30 Eisai R&D Man Co Ltd Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
EP2675810A1 (en) 2011-02-15 2013-12-25 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
JP2014524472A (ja) * 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
EP3607946B1 (en) 2012-03-19 2023-02-22 Buck Institute for Research on Aging App specific bace inhibitors (asbis) and uses thereof
CN104394862A (zh) 2012-05-30 2015-03-04 科门蒂斯公司 色满化合物
GB201209587D0 (en) 2012-05-30 2012-07-11 Takeda Pharmaceutical Therapeutic compounds
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β－分泌酶抑制劑
EP2900650A1 (en) 2012-09-28 2015-08-05 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9489013B2 (en) 2012-12-20 2016-11-08 Merck Sharp & Dohme Corp. C6-azaspiro iminothiadiazine dioxides as bace inhibitors, compositions, and their use
EP2934534B1 (en) 2012-12-21 2017-12-13 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
ES2975235T3 (es) 2013-02-12 2024-07-04 Buck Inst Res Aging Hidantoínas que modulan el procesamiento de APP mediado por BACE
CN105189469B (zh) * 2013-02-25 2018-09-25 默克专利股份公司 2-氨基-3,4-二氢喹唑啉衍生物及其作为组织蛋白酶d抑制剂的用途
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
US9085576B2 (en) 2013-03-08 2015-07-21 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2968356B1 (en) 2013-03-15 2018-03-07 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiadiazine compounds as bace inhibitors, compositions, and their use
EP2968357B1 (en) 2013-03-15 2018-07-04 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
CN105324372B (zh) * 2013-06-21 2018-03-06 武田药品工业株式会社 作为前动力蛋白受体调节剂的1‑磺酰基哌啶衍生物
US9725468B2 (en) 2013-09-13 2017-08-08 Merck Sharp & Dohme Corp. C5-spiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
CA2934257C (en) 2013-12-17 2022-06-07 Janssen Pharmaceutica Nv Imidazolin-5-one derivative useful as fasn inhibitors for the treatment of cancer
EP3082823B1 (en) 2013-12-18 2020-04-22 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use
EP3083575B1 (en) 2013-12-18 2021-11-03 Merck Sharp & Dohme Corp. C-6 spirocarbocyclic iminothiadiazine dioxides as bace inhibitors, compositions, and their use
AU2015301028B2 (en) 2014-08-08 2019-09-26 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
ES2942308T3 (es) * 2015-04-21 2023-05-31 Allgenesis Biotherapeutics Inc Compuestos y su uso como inhibidores de BACE1
CN105175488A (zh) * 2015-09-07 2015-12-23 西北农林科技大学 一种具有抗老年痴呆症活性的化合物及其制备方法
CN106749033A (zh) * 2015-11-25 2017-05-31 中国人民解放军军事医学科学院毒物药物研究所 乙内酰脲类化合物及其作为β-分泌酶抑制剂的用途
WO2017089453A1 (en) 2015-11-25 2017-06-01 Ucb Biopharma Sprl Iminotetrahydropyrimidinone derivatives as plasmepsin v inhibitors
GB201603104D0 (en) 2016-02-23 2016-04-06 Ucb Biopharma Sprl Therapeutic agents
JP6504106B2 (ja) * 2016-04-21 2019-04-24 三菱電機ビルテクノサービス株式会社 エレベータ装置
CN109641884B (zh) 2016-08-18 2024-01-02 维达克制药有限公司 哌嗪衍生物、其药物组合物及其使用方法
CN107892697B (zh) 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
JOP20180092A1 (ar) 2017-10-13 2019-04-13 Gilead Sciences Inc مثبطات hiv بروتياز
GB201805816D0 (en) 2018-04-06 2018-05-23 Ucb Biopharma Sprl Therapeutic agents
TW202104210A (zh) 2019-04-17 2021-02-01 美商基利科學股份有限公司 Hiv蛋白酶抑制劑
GB201906804D0 (en) 2019-05-14 2019-06-26 Ucb Biopharma Sprl Therapeutic agents
CN114206856A (zh) 2019-08-19 2022-03-18 Ucb生物制药有限责任公司 抗疟疾的六氢嘧啶类似物
GB202010606D0 (en) 2020-07-10 2020-08-26 Ucb Biopharma Sprl Therapeutic agents
CN112010836B (zh) * 2020-09-07 2021-07-09 南通大学 含芳基联吡啶氧基结构的2-取代基咪唑烷衍生物及其制备方法和用途
WO2023152042A1 (en) 2022-02-08 2023-08-17 UCB Biopharma SRL Antimalarial hexahydropyrimidine analogues

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH511863A (de) * 1967-04-13 1971-08-31 Ciba Geigy Ag Verfahren zur Herstellung von 2,4-Benzdiazepinen
DE2448869A1 (de) * 1973-10-19 1975-09-04 Mcneilab Inc 4-oxo-2-imidazolidinylidenharnstoffe, verfahren zu ihrer herstellung und arzneimittel
IL92011A0 (en) * 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
BR9707086A (pt) * 1996-01-26 1999-04-13 Clarence Webster Andrews, Iii. Inibidores de proteinase aspartila
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
US6436989B1 (en) * 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
JP4814427B2 (ja) * 1999-02-12 2011-11-16 バーテックス ファーマシューティカルズ インコーポレイテッド アスパルチルプロテアーゼのインヒビター
WO2000066112A1 (en) * 1999-05-03 2000-11-09 Smithkline Beecham Corporation Cxcr-4 receptor antagonists - thrombopoietin mimetics
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
US7560482B2 (en) 2001-03-15 2009-07-14 The Johns Hopkins University Inhibitors of plasmepsins

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