RU2011117160A - Хиназолинон, хинолон и родственные аналоги в качестве модуляторов сиртутуина - Google Patents

Хиназолинон, хинолон и родственные аналоги в качестве модуляторов сиртутуина Download PDF

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RU2011117160A
RU2011117160A RU2011117160/04A RU2011117160A RU2011117160A RU 2011117160 A RU2011117160 A RU 2011117160A RU 2011117160/04 A RU2011117160/04 A RU 2011117160/04A RU 2011117160 A RU2011117160 A RU 2011117160A RU 2011117160 A RU2011117160 A RU 2011117160A
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alkyl
substituted
fluoro
compound
optionally substituted
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RU2011117160/04A
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RU2519779C2 (ru
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Чи Б. ВУ (US)
Чи Б. Ву
Кристофер ОУЛМАНН (US)
Кристофер Оулманн
Роберт Б. Перни (US)
Роберт Б. Перни
Брайан УАЙТ (US)
Брайан УАЙТ
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Сертрис Фармасьютикалз Инк. (Us)
Сертрис Фармасьютикалз Инк.
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

1. Соединение, имеющее структуру, описываемую структурной формулой (II): ! ! или его соль, где ! каждый из Z1, Z2 и Z3 независимо выбирают из N и C(R9), где ! не более чем один из Z1, Z2 и Z3 является N; ! каждый R9 независимо выбирают из водорода, галогена, -C≡N, фторзамещенного C1-C2 алкила, -O-(C1-C2) фторзамещенного алкила, -S-(C1-C2) фторзамещенного алкила, C1-C4 алкила, -S-(C1-C4) алкила, C3-C7 циклоалкила, -(C1-C2) алкил-N(R13)(R13), -O-CH2CH(OH)CH2OH, -O-(C1-C3) алкил-N(R13)(R13) и -N(R13)(R13); и ! представляет вторую химическую связь между либо W2 и C(R12), либо W1 и C(R12); ! W1 выбирают из -O-, -NH- или -N=, и ! W2(R14) выбирают из -N(R14)- и -C(R14)=, выбирая так, что ! когда W1 является -O-, один из Z1, Z2 и Z3 является N; ! когда W1 является -O- или -NH-, W2(R14) является -C(R14)= и представляет вторую химическую связь между W2 и C(R12); и ! когда W1 является -N=, W2(R14) является -N(R14)- и представляет вторую химическую связь между W1 и C(R12); ! R11 выбирают из карбоцикла и гетероцикла, где R11 необязательно замещен одним-двумя заместителями, независимо выбранными из галогена, -C≡N, C1-C4 алкила, =O, C3-C7 циклоалкила, фторзамещенного C1-C4 алкила, -O-R13, -S-R13, -(C1-C4 алкил)-N(R13)(R13), -N(R13)(R13), -O-(C1-C4 алкил)-N(R13)(R13), -(C1-C4 алкил)-O-(C1-C4 алкил)-N(R13)(R13), -C(O)-N(R13)(R13) и -(C1-C4 алкил)-C(O)-N(R13)(R13), и когда R11 является фенилом, R11 также необязательно замещен 3,4-метилендиокси, фторзамещенным 3,4-метилендиокси, 3,4-этилендиокси, фторзамещенным 3,4-этилендиокси, O-(насыщенным гетероциклом), фторзамещенным -O-(насыщенным гетероциклом) или C1-C4 алкилзамещенным O-(насыщенным гетероциклом), где ! каждый R13 независимо выбирают из водорода и -C1-C4 алкила; или два R13 вместе с атомом азота, к которому они присоединены, образуют 4-8-членный насыщенный гетероцикл, необязательно включающий один дополнительный гетероатом, �

Claims (18)

1. Соединение, имеющее структуру, описываемую структурной формулой (II):
Figure 00000001
или его соль, где
каждый из Z1, Z2 и Z3 независимо выбирают из N и C(R9), где
не более чем один из Z1, Z2 и Z3 является N;
каждый R9 независимо выбирают из водорода, галогена, -C≡N, фторзамещенного C1-C2 алкила, -O-(C1-C2) фторзамещенного алкила, -S-(C1-C2) фторзамещенного алкила, C1-C4 алкила, -S-(C1-C4) алкила, C3-C7 циклоалкила, -(C1-C2) алкил-N(R13)(R13), -O-CH2CH(OH)CH2OH, -O-(C1-C3) алкил-N(R13)(R13) и -N(R13)(R13); и
Figure 00000002
представляет вторую химическую связь между либо W2 и C(R12), либо W1 и C(R12);
W1 выбирают из -O-, -NH- или -N=, и
W2(R14) выбирают из -N(R14)- и -C(R14)=, выбирая так, что
когда W1 является -O-, один из Z1, Z2 и Z3 является N;
когда W1 является -O- или -NH-, W2(R14) является -C(R14)= и
Figure 00000002
представляет вторую химическую связь между W2 и C(R12); и
когда W1 является -N=, W2(R14) является -N(R14)- и
Figure 00000002
представляет вторую химическую связь между W1 и C(R12);
R11 выбирают из карбоцикла и гетероцикла, где R11 необязательно замещен одним-двумя заместителями, независимо выбранными из галогена, -C≡N, C1-C4 алкила, =O, C3-C7 циклоалкила, фторзамещенного C1-C4 алкила, -O-R13, -S-R13, -(C1-C4 алкил)-N(R13)(R13), -N(R13)(R13), -O-(C1-C4 алкил)-N(R13)(R13), -(C1-C4 алкил)-O-(C1-C4 алкил)-N(R13)(R13), -C(O)-N(R13)(R13) и -(C1-C4 алкил)-C(O)-N(R13)(R13), и когда R11 является фенилом, R11 также необязательно замещен 3,4-метилендиокси, фторзамещенным 3,4-метилендиокси, 3,4-этилендиокси, фторзамещенным 3,4-этилендиокси, O-(насыщенным гетероциклом), фторзамещенным -O-(насыщенным гетероциклом) или C1-C4 алкилзамещенным O-(насыщенным гетероциклом), где
каждый R13 независимо выбирают из водорода и -C1-C4 алкила; или два R13 вместе с атомом азота, к которому они присоединены, образуют 4-8-членный насыщенный гетероцикл, необязательно включающий один дополнительный гетероатом, выбранный из NH, S, S(=O), S(=O)2 и O, где
когда R13 является алкилом, алкил необязательно замещен одним или более заместителями, выбранными из -OH, фтора, -NH2, -NH(C1-C4 алкила), -N(C1-C4 алкила)2, -NH(CH2CH2OCH3) и -N(CH2CH2OCH3)2, и
когда два R13 вместе с атомом азота, к которому они присоединены, образуют 4-8-членный насыщенный гетероцикл, насыщенный гетероцикл необязательно замещен на любом углеродном атоме -OH, -C1-C4 алкилом, фтором, -NH2, -NH(C1-C4 алкилом), -N(C1-C4 алкилом)2, -NH(CH2CH2OCH3) или -N(CH2CH2OCH3)2, и необязательно замещен на любом способном к замещению атоме азота -C1-C4 алкилом, фторзамещенным C1-C4 алкилом или -(CH2)2-O-CH3;
R12 выбирают из карбоцикла и гетероцикла, не являющегося тетразолилом, где R12 необязательно замещен одним или более заместителями, независимо выбранными из галогена, -C=N, C1-C4 алкила, C3-C7 циклоалкила, C1-C2 фторзамещенного алкила, -O-R13, -S-R13, -S(O)-R13, -S(O)2-R13, -(C1-C4 алкил)-N(R13)(R13), -N(R13)(R13), -O-(C1-C4 алкил)-N(R13)(R13), -(C1-C4 алкил)-O-(C1-C4 алкил)-N(R13)(R13), -C(O)-N(R13)(R13), -(C1-C4 алкил)-C(O)-N(R13)(R13), -O-фенила, фенила и второго гетероцикла, и когда R12 является фенилом, R12 также необязательно замещен 3,4-метилендиокси, фторзамещенным 3,4-метилендиокси, 3,4-этилендиокси или фторзамещенным 3,4-этилендиокси или -O-(насыщенным гетероциклом), где любой фенил, второй гетероцикл или часть из насыщенного гетероцикла в заместителе в R12 необязательно замещены галогеном; -C≡N; C1-C4 алкилом, фторзамещенным C1-C2 алкилом, -O-(C1-C2) фторзамещенным алкилом, -O-(C1-C4) алкилом, -S-(C1-C4) алкилом, -S-(C1-C2) фторзамещенным алкилом, -NH-(C1-C4) алкилом и -N-(C1-C4) алкилом;
R14 выбирают из водорода, C1-C4 алкила, C1-C4 фторзамещенного алкила, C1-C4 алкил-N(R13)(R13), C1-C4 алкил-C(O)-N(R13)(R13), C1-C4 алкил-O-R13 и C1-C4 алкил-NR13-C(O)R13; и
X1 выбирают из -NH-C(=O)-†, -C(=O)-NH-†, -NH-C(=S)-†, -C(=S)-NH-†, -NH-S(=O)-†, -S(=O)-NH-†, -S(=O)2-NH-†, -NH-S(=O)2-†, -NH-S(O)2-NR15-†, -NR15-S(O)2-NH-†, -NH-C(=O)O-†, -0C(=O)NH-†, -NH-C(=O)NR15-†, -NR15-C(=O)NH-†, -NH-NR15-†, -NR15-NH-†, -O-NH-†, -NH-O-†, -NH-CR15R16-†, -CR15R16-NH-†, -NH-C(=NR15)-†, -C(=NR15)-NH-†, -C(=O)-NH-CR15R16-†, -CR15R16-NH-C(O)-†, -NH-C(=S)-CR15R16-†, -CR15R16-C(=S)-NH-†, -NH-S(O)-CR15R16-†, -CR15R16-S(O)-NH-†, -NH-S(O)2-CR15R16-†, -CR15R16-S(O)2-NH-†, -NH-C(=O)-O-CR15R16-†, -CR15R16-O-C(=O)-NH-†, -NH-C(=O)-NR15-CR15R16-†, -NH-C(=O)-CR15R16-† и -CR15R16-NH-C(=O)-O-†, где
† обозначает место, в котором X1 соединен с R11; и
каждый R15 и R16 независимо выбирают из водорода, C1-C4 алкила, -CF3 и (C1-C3 алкил)-CF3.
2. Соединение по п.1, где соединение имеет структуру, представленную структурной формулой:
Figure 00000003
3. Соединение по п.1, где X1 выбирают из -NH-C(O)-† и -C(O)-NH-†.
4. Соединение по п.1, где R11 выбирают из
Figure 00000004
где R11 необязательно замещен одним-двумя заместителями, независимо выбранными из галогена, C1-C4 алкила, -(C1-C4 алкил)-N(R13)(R13), =О, -N(R13)(R13) и -O-R13.
5. Соединение по п.4, где R11 выбирают из
Figure 00000005
Figure 00000006
Figure 00000007
6. Соединение по п.5, где R11 выбирают из
Figure 00000008
+
Figure 00000009
Figure 00000010
7. Соединение п.1, где R12 выбирают из
Figure 00000011
где R12 необязательно замещен одной или более группами, независимо выбранными из галогена, C1-C4 алкила, -(C1-C4 алкил)-N(R13)(R13), C1-C2 фторзамещенного алкила, -O-R13, -SO2-R13, -N(R13)(R13) и -O-(C1-C4 алкил)-N(R13)(R13).
8. Соединение по п.7, где R12 выбирают из
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
9. Соединение по п.8, где R12 выбирают из
Figure 00000016
Figure 00000017
10. Соединение по п.1, где W2(R14) является -N(R14)- и R14 выбирают из водорода и -(C1-C4) алкила.
11. Соединение по п.1, где W2(R14) является -C(R14)- и R14 является водородом.
12. Соединение по п.1, где соединение выбирают из любого одного из соединений
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
и
Figure 00000039
13. Соединение по п.12, где соединение выбирают из любого одного из соединений
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
и
Figure 00000052
14. Соединение по п.1, где соединение выбирают из любого одного из соединений
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
и
Figure 00000067
15. Соединение по п.14, где соединение выбирают из любого одного из соединений
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
и
Figure 00000077
16. Апирогенная фармацевтическая композиция, включающая фармацевтически приемлемый носитель или разбавитель и соединение по любому из пп.1-15, или его фармацевтически приемлемую соль.
17. Способ лечения субъекта, страдающего от или подверженного резистентности к инсулину, метаболическому синдрому, диабету или его осложнениям, включающий введение субъекту, если это ему необходимо, композиции по п.16.
18. Способ повышения чувствительности к инсулину у субъекта, включающий введение субъекту, если это ему необходимо, композиции по п.16.
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Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG190603A1 (en) 2008-05-01 2013-06-28 Sirtris Pharmaceuticals Inc Quinolines and related analogs as sirtuin modulators
EP2315763B1 (en) * 2008-07-03 2016-06-01 Glaxosmithkline LLC Benzimidazoles and related analogs as sirtuin modulators
EP2342188B1 (en) 2008-09-29 2014-07-30 GlaxoSmithKline LLC Chromenone analogs as sirtuin modulators
AU2010221417A1 (en) * 2009-03-02 2011-09-22 Sirtris Pharmaceuticals, Inc. 8-substituted quinolines and related analogs as sirtuin modulators
EP2493888B1 (en) 2009-10-29 2016-04-06 GlaxoSmithKline LLC Bicyclic pyridines and analogs as sirtuin modulators
CA2844670A1 (en) 2011-08-12 2013-02-21 Salk Institute For Biological Studies Neuroprotective polyphenol analogs
WO2013025484A1 (en) * 2011-08-12 2013-02-21 Lapchak Paul A Polyphenol analogs to treat ischemia
CN105796546B (zh) * 2011-10-18 2020-03-03 株式会社爱茉莉太平洋 包含丁香脂素的sirt1活化剂
CN103086965A (zh) * 2012-12-24 2013-05-08 金华职业技术学院 烟酸对乙酰氨基苯酯化合物及其合成方法
CA2912683A1 (en) 2013-05-13 2014-11-20 Glaxosmithkline Llc Substituted bridged urea analogs as sirtuin modulators
US9624211B2 (en) * 2013-07-18 2017-04-18 Board Of Regents, The University Of Texas System Anti-cancer compounds
US10172915B2 (en) 2013-10-20 2019-01-08 Duke University Methods and compositions for activation of sirtuins with Annexin A1 peptides
WO2015186068A1 (en) 2014-06-02 2015-12-10 Glaxosmithkline Intellectual Property (No.2) Limited Preparation and use of crystalline beta-d-nicotinamide riboside
AU2015270090A1 (en) 2014-06-06 2016-12-22 Glaxosmithkline Intellectual Property (No.2) Limited Nicotinamide riboside analogs and pharmaceutical compositions and uses thereof
EP3191459A1 (en) 2014-09-05 2017-07-19 AbbVie Deutschland GmbH & Co. KG Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases
US10457662B2 (en) 2015-05-20 2019-10-29 The Regents Of The University Of Michigan Substituted amides for treating and preventing cancer
WO2017003723A1 (en) 2015-07-01 2017-01-05 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
JP7071917B2 (ja) 2015-12-09 2022-05-19 カデント セラピューティクス，インコーポレーテッド ヘテロ芳香族ｎｍｄａ受容体モジュレーターおよびその使用
EP4006038A1 (en) 2015-12-09 2022-06-01 Cadent Therapeutics, Inc. Thienopyrimidinone nmda receptor modulators and uses thereof
RU2612875C1 (ru) * 2015-12-14 2017-03-13 Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) Средство для ингибирования фермента тирозил-днк-фосфодиэстеразы 1 человека
EP3426242A4 (en) * 2016-03-11 2020-03-18 H. Lee Moffitt Cancer Center And Research Institute, Inc. ICARITINE AND ICARITINE DERIVATIVES
JP7332472B2 (ja) 2016-12-22 2023-08-23 ノバルティス アーゲー Ｎｍｄａ受容体モジュレーターおよびその使用
CN106977500A (zh) * 2017-04-17 2017-07-25 牡丹江医学院 一种用于治疗脑梗塞的药物及其制备方法
US11028068B2 (en) 2017-07-25 2021-06-08 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
CN112513047B (zh) 2018-08-03 2023-10-20 诺华股份有限公司 芳香杂环nmda受体调节剂及其用途
CR20220316A (es) 2019-12-06 2022-10-07 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio
CN113135884B (zh) * 2020-01-20 2023-03-10 西华大学 一种异色烯类化合物及其制备方法和用途
AR121719A1 (es) 2020-04-03 2022-06-29 Petra Pharma Corp Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades
CR20230517A (es) 2021-05-03 2023-11-28 Petra Pharma Corp Inhibidores alostéricos de cromenona del fosfoinosítido 3-quinasa (pi3k) para el tratamiento de enfermedades
TWI829179B (zh) 2021-05-27 2024-01-11 美商佩特拉製藥公司 用於治療疾病之磷酸肌醇3-激酶(pi3k)異位色烯酮抑制劑
CN117794920A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N-(羟烷基(杂)芳基)四氢呋喃甲酰胺作为钠通道调节剂
CN113549044B (zh) * 2021-07-23 2024-01-23 中国药科大学 8-氮杂环取代色酮类衍生物及其制备方法与制药用途
CN113620887B (zh) * 2021-09-14 2023-07-04 西华大学 一类sirt5蛋白抑制剂及其用途
WO2023078252A1 (en) 2021-11-02 2023-05-11 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
WO2024026424A1 (en) * 2022-07-27 2024-02-01 Black Diamond Therapeutics, Inc. Quinazolinone derivatives as and related uses
WO2024099437A1 (en) * 2022-11-11 2024-05-16 Fochon Biosciences, Ltd. Compounds as protein kinase inhibitors

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1108698B (de) 1959-09-03 1961-06-15 Hoechst Ag Verfahren zur Herstellung von 2-(2'-Aminoaryl)-4, 5-arylen-1, 2, 3-triazolen
JPS58225083A (ja) 1982-06-23 1983-12-27 Nippon Shinyaku Co Ltd メチルフラボン誘導体
EP0108986A1 (en) * 1982-11-02 1984-05-23 Hokuriku Pharmaceutical Co.,Ltd N-substituted flavone-8-carboxamides
JPS6064976A (ja) * 1983-09-19 1985-04-13 Hokuriku Seiyaku Co Ltd Ν−置換フラボン−８−カルボキサミド誘導体，及びその製造方法
US4727064A (en) 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
JPS60246384A (ja) * 1984-05-21 1985-12-06 Hokuriku Seiyaku Co Ltd クロモン−８−カルポキサミド誘導体
CA1261835A (en) 1984-08-20 1989-09-26 Masaaki Toda (fused) benz(thio)amides
IL85554A0 (en) 1987-03-02 1988-08-31 Takeda Chemical Industries Ltd Chromone derivatives
US5116954A (en) 1988-04-06 1992-05-26 Lipha, Lyonnaise Industrielle Pharmaceutique Pharmaceutically useful flavonoic compounds containing at least one substituent on the benzopyranone ring moiety
MA21528A1 (fr) * 1988-04-06 1989-12-31 Lipha Composants substituants du flavonoide, leurs sels, leurs manufactures et produits contenant ces matieres .
HUT58310A (en) * 1988-12-21 1992-02-28 Upjohn Co Anti-atherosclerotic and anti-thrombotic 1-benzopyran-4-one- and 2-amino-1,3-benzoxazin-4-one derivatives, process for producing them and pharmaceutical compositions containing them
US5703075A (en) * 1988-12-21 1997-12-30 Pharmacia & Upjohn Company Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
RU2066322C1 (ru) * 1991-06-28 1996-09-10 Киевский Государственный Университет Им.Т.Г.Шевченко 3-(4-метил-2-тиазолил)-6-пропил-7-(1-метил-1-этоксикарбонил)метоксихромон, обладающий гипогликемическим, гиполипидемическим действием и аналептическим действием
IT1254469B (it) * 1992-02-25 1995-09-25 Recordati Chem Pharm Derivati benzopiranici e benzotiopiranici
EP0558245A1 (en) * 1992-02-25 1993-09-01 RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY Heterobicyclic compounds as antagogists of alpha-1 adrenergic and SHT1A receptors
DE69310367T2 (de) * 1992-07-10 1997-08-14 Glaxo Lab Sa Anilide-derivate
GB9410207D0 (en) 1994-05-21 1994-07-06 Smithkline Beecham Plc Process
WO1996031206A2 (en) * 1995-04-07 1996-10-10 Warner-Lambert Company Flavones and coumarins as agents for the treatment of atherosclerosis
US6080757A (en) * 1996-06-06 2000-06-27 Pfizer Inc Antibiotic quinolones and derivatives
US6187779B1 (en) 1998-11-20 2001-02-13 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to 2,8-disubstituted quinazoline derivatives
NZ520300A (en) 2000-01-24 2004-05-28 Kinacia Pty Ltd Morpholino-substituted pyridopyrimidine, quinolone and benzopyranone derivatives that inhibit the enzyme phosphoinositide (PI) 3-kinase
BR0113358A (pt) * 2000-08-21 2003-07-01 Astrazeneca Ab Derivado de quinazolina ou de um seu sal farmaceuticamente aceitável, processo para a sua preparação, composição farmacêutica, e, uso do derivado ou de um seu sal farmaceuticamente aceitável
JP4646626B2 (ja) * 2002-08-16 2011-03-09 アストラゼネカ アクチボラグ ホスホイノシチド３−キナーゼβの阻害
US20060025337A1 (en) * 2003-07-01 2006-02-02 President And Fellows Of Harvard College Sirtuin related therapeutics and diagnostics for neurodegenerative diseases
JP2007530417A (ja) 2003-07-01 2007-11-01 プレジデント・アンド・フェロウズ・オブ・ハーバード・カレッジ 細胞及び生物の寿命及びストレス応答を操作するための組成物
JP2007527418A (ja) 2003-12-29 2007-09-27 プレジデント・アンド・フェロウズ・オブ・ハーバード・カレッジ 肥満及びインシュリン耐性障害を治療又は防止するための組成物
FR2869615B1 (fr) * 2004-05-03 2007-11-16 Merck Sante Soc Par Actions Si Derives de l'acide butanoique, procedes pour leur preparation, compositions pharmaceutiques les contenant et leurs applications therapeutiques
US20080090863A1 (en) * 2004-09-30 2008-04-17 Taisho Pharmaceutical Co., Ltd. Pyridine Derivatives and Their Use as Medicaments for Treating Diseases Related to Mch Receptor
WO2006094246A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-arylmethyl benzamide sirtuin modulators
WO2006094210A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Tetrahydroquinoxalinone sirtuin modulators
WO2006094248A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Aryl-substituted cyclic sirtuin modulators
WO2006094233A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N,n'-dicyclic isothiourea sirtuin modulators
WO2006094236A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-phenyl benzamide derivatives as sirtuin modulators
ATE544071T1 (de) 2005-03-03 2012-02-15 Sirtris Pharmaceuticals Inc Fluoreszenzpolarisationstests für die acetyltransferase-deacetylase-aktivität
US20070014833A1 (en) 2005-03-30 2007-01-18 Sirtris Pharmaceuticals, Inc. Treatment of eye disorders with sirtuin modulators
US20060229265A1 (en) 2005-03-30 2006-10-12 Sirtris Pharmaceuticals, Inc. Nicotinamide riboside and analogues thereof
CA2609549A1 (en) 2005-05-25 2006-11-30 Sirtris Pharmaceuticals, Inc. Treatment of eye disorders with sirtuin modulators
JP2009500357A (ja) 2005-07-07 2009-01-08 サートリス ファーマシューティカルズ， インコーポレイテッド 肥満、インスリン抵抗性障害およびミトコンドリア関連障害を処置または予防するための方法および関連する組成物
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
WO2007019417A1 (en) 2005-08-04 2007-02-15 Sirtris Pharmaceuticals, Inc. Oxazolopyridine derivatives as sirtuin modulators
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
CA2631713A1 (en) 2005-12-02 2007-09-13 Sirtris Pharmaceuticals, Inc. Modulators of cdc2-like kinases (clks) and methods of use thereof
US8304206B2 (en) 2005-12-02 2012-11-06 Sirtris Pharmaceuticals, Inc. Mass spectrometry assays for identifying compounds that activate deacetylases
US20080021063A1 (en) 2006-07-18 2008-01-24 Kazantsev Aleksey G Compositions and methods for modulating sirtuin activity
WO2008027379A2 (en) 2006-08-29 2008-03-06 Sirtris Pharmaceuticals, Inc. Indicators of sirtuin activity and methods of use thereof
US20080249103A1 (en) 2006-11-15 2008-10-09 Sirtris Pharmaceuticals, Inc. Sirtuin polymorphisms and methods of use thereof
WO2008073451A2 (en) 2006-12-11 2008-06-19 Sirtris Pharmaceuticals, Inc. Benzoimidazole derivatives as sirtuin (sir) modulating compounds
WO2008100423A1 (en) 2007-02-09 2008-08-21 Sirtris Pharmaceuticals, Inc. Gut microsomal triglyceride transport protein inhibitors
WO2008100376A2 (en) 2007-02-15 2008-08-21 Sirtris Pharmaceuticals, Inc. Truncation variants of sirt1 and methods of use thereof
AU2008229385A1 (en) 2007-03-19 2008-09-25 Sirtris Pharmaceuticals, Inc. Biomarkers of sirtuin activity and methods of use thereof
TW200918542A (en) 2007-06-20 2009-05-01 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
TW200916472A (en) 2007-06-20 2009-04-16 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
CA2704336A1 (en) 2007-11-01 2009-05-07 Sirtris Pharmaceuticals, Inc. Amide derivatives as sirtuin modulators
US20110009381A1 (en) 2007-11-08 2011-01-13 Sirtis Pharmaceuticals, Inc. Solubilized thiazolopyridines
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
WO2009085226A2 (en) 2007-12-21 2009-07-09 Sirtris Pharmaceuticals, Inc. Inhibitors of cdc2-like kinases (clks) and methods of use thereof
US20110009496A1 (en) 2008-01-08 2011-01-13 Sirtris Pharmaceuticas, Inc. Resveratrol formulations
SG190603A1 (en) * 2008-05-01 2013-06-28 Sirtris Pharmaceuticals Inc Quinolines and related analogs as sirtuin modulators
WO2009140562A1 (en) 2008-05-15 2009-11-19 Sirtris Pharmaceuticals, Inc. Sirt1 polymorphic variants and methods of use thereof
KR20110019385A (ko) 2008-05-29 2011-02-25 서트리스 파마슈티컬즈, 인코포레이티드 시르투인 조절제로서의 이미다조피리딘 및 관련 유사체
EP2315763B1 (en) 2008-07-03 2016-06-01 Glaxosmithkline LLC Benzimidazoles and related analogs as sirtuin modulators
AU2009282076A1 (en) 2008-08-12 2010-02-18 Sirtris Pharmaceuticals, Inc. Benzoxazoles, benzthiazoles and related analogs as sirtuin modulators
EP2342188B1 (en) 2008-09-29 2014-07-30 GlaxoSmithKline LLC Chromenone analogs as sirtuin modulators
US20110263564A1 (en) 2008-10-29 2011-10-27 Sirtris Pharmaceuticals, Inc. Pyridine, bicyclic pyridine and related analogs as sirtuin modulators
BRPI0922180A2 (pt) 2008-12-08 2015-12-29 Sirtris Pharmaceuticals Inc insoindolinona e análogos correlatos como moduladores de sirtuína
US20130190309A1 (en) 2008-12-16 2013-07-25 Chi B. Vu Phthalazinone and related analogs as sirtuin modulators
EA021424B1 (ru) 2008-12-19 2015-06-30 Сертрис Фармасьютикалз, Инк. Тиазолопиридиновые соединения, регулирующие сиртуин
WO2010088574A1 (en) 2009-01-30 2010-08-05 Sirtris Pharmaceuticals, Inc. Azabenzimidazoles and related analogs as sirtuin modulators
AU2010221417A1 (en) 2009-03-02 2011-09-22 Sirtris Pharmaceuticals, Inc. 8-substituted quinolines and related analogs as sirtuin modulators
EP2493888B1 (en) 2009-10-29 2016-04-06 GlaxoSmithKline LLC Bicyclic pyridines and analogs as sirtuin modulators
WO2011116176A1 (en) 2010-03-17 2011-09-22 Sirtris Pharmaceuticals Inc. 3-substitued imidazo (4, 5-b) pyridines and analogs as sirtuin modulators

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US20150148343A1 (en) 2015-05-28
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