CN111094299B - 雷帕霉素衍生物 - Google Patents

雷帕霉素衍生物 Download PDF

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Publication number
CN111094299B
CN111094299B CN201880057805.6A CN201880057805A CN111094299B CN 111094299 B CN111094299 B CN 111094299B CN 201880057805 A CN201880057805 A CN 201880057805A CN 111094299 B CN111094299 B CN 111094299B
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pharmaceutically acceptable
acceptable salt
compound
formula
disease
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CN111094299A (zh
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S·波纳齐
M·康诺利
D·J·格拉斯
M·米哈里克
A·W·帕特森
S·罗格
T·沙夫拉卡泽
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Novartis AG
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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 three hetero rings
    • C07D498/18—Bridged systems
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    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/439—Heterocyclic 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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  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
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CN201880057805.6A 2017-09-26 2018-09-25 雷帕霉素衍生物 Active CN111094299B (zh)

Priority Applications (1)

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CN202311329093.8A CN117417351A (zh) 2017-09-26 2018-09-25 雷帕霉素衍生物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762563312P 2017-09-26 2017-09-26
US62/563,312 2017-09-26
PCT/IB2018/057422 WO2019064182A1 (en) 2017-09-26 2018-09-25 RAPAMYCIN DERIVATIVES

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CN111094299B true CN111094299B (zh) 2023-10-31

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CN202311329093.8A Pending CN117417351A (zh) 2017-09-26 2018-09-25 雷帕霉素衍生物

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US (4) US10800793B2 (https=)
EP (2) EP4365179A3 (https=)
JP (2) JP7387590B2 (https=)
KR (2) KR20250054121A (https=)
CN (2) CN111094299B (https=)
AR (1) AR112834A1 (https=)
AU (1) AU2018342784B2 (https=)
BR (1) BR112020005898A2 (https=)
CA (1) CA3078191A1 (https=)
DK (1) DK3687999T3 (https=)
ES (1) ES2973975T3 (https=)
FI (1) FI3687999T3 (https=)
HR (1) HRP20240199T8 (https=)
HU (1) HUE065692T2 (https=)
LT (1) LT3687999T (https=)
MX (2) MX2020007265A (https=)
PL (1) PL3687999T3 (https=)
PT (1) PT3687999T (https=)
RS (1) RS65270B1 (https=)
SI (1) SI3687999T1 (https=)
TW (1) TW201920189A (https=)
UY (1) UY37900A (https=)
WO (1) WO2019064182A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3013783A1 (en) 2016-02-04 2017-08-10 The Johns Hopkins University Rapaglutins, novel inhibitors of glut and use thereof
US10774110B2 (en) 2016-02-04 2020-09-15 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
IL300091A (en) * 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
IL314362A (en) 2018-06-15 2024-09-01 Janssen Pharmaceutica Nv Rapamycin analogs and their uses
MX2021007247A (es) 2018-12-18 2021-07-15 Novartis Ag Derivados de rapamicina.
EP3914245A4 (en) 2019-01-22 2022-08-24 Aeovian Pharmaceuticals, Inc. MTORC-1 MODULATORS AND USES THEREOF
KR102486721B1 (ko) * 2019-08-23 2023-01-10 이화여자대학교 산학협력단 신규 mTOR 억제제 화합물 및 이의 용도
KR102497821B1 (ko) * 2019-08-23 2023-02-08 이화여자대학교 산학협력단 신규 mTOR 억제제 화합물 및 이의 용도
TW202126323A (zh) * 2019-10-01 2021-07-16 約翰斯赫普金斯大學 雷帕弗辛（Ｒａｐａｆｕｃｉｎ）衍生化合物及其使用方法
KR20220128345A (ko) 2019-12-05 2022-09-20 아나쿠리아 테라퓨틱스, 인코포레이티드 라파마이신 유사체 및 이의 용도
DE102020203224A1 (de) 2020-03-12 2021-09-16 Heinrich-Heine-Universität Düsseldorf Inhibition von FKBP1A zur Therapie des Triple-negativen Mammakarzinoms
EP4118431A1 (de) 2020-03-12 2023-01-18 Heinrich-Heine-Universität Düsseldorf Inhibition von fkbp1a zur therapie des triple-negativen mammakarzinoms
WO2021195599A1 (en) * 2020-03-27 2021-09-30 Aeovian Pharmaceuticals, Inc. Mtorc1 modulators and uses thereof
EP4185590A2 (en) * 2020-07-21 2023-05-31 Aeovian Pharmaceuticals, Inc. Mtorc1 modulators and uses thereof
TW202206093A (zh) * 2020-08-12 2022-02-16 中國醫藥大學 Ｓｅｍａ３ｄ拮抗劑用於預防或治療神經退化性疾病以及延長壽命之用途
AU2023275778A1 (en) 2022-05-25 2024-12-12 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor
KR20250169282A (ko) * 2023-04-07 2025-12-02 리제너론 파마슈티칼스 인코포레이티드 선택적 라파마이신 유사체 및 이의 용도
WO2024243449A1 (en) * 2023-05-23 2024-11-28 Tornado Therapeutics, Inc. Rapamycin derivatives and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996041807A1 (en) * 1995-06-09 1996-12-27 Novartis Ag Rapamycin derivatives
CN101389337A (zh) * 2006-02-24 2009-03-18 诺瓦提斯公司 用于治疗神经母细胞瘤的雷帕霉素衍生物
CN104211715A (zh) * 2005-03-11 2014-12-17 巴克年龄研究协会 雷帕霉素的39-去甲氧基衍生物
WO2017044720A1 (en) * 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA737247B (en) 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
US4316885A (en) 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
KR19990022651A (ko) 1995-06-07 1999-03-25 데이비드 엘. 버스테인 생물학적 사건에 대한 라파마이신 기재 조절방법
AU714904C (en) 1995-06-07 2002-08-08 Ariad Pharmaceuticals, Inc. Rapamcycin-based regulation of biological events
GB9606452D0 (en) 1996-03-27 1996-06-05 Sandoz Ltd Organic compounds
JP2002514165A (ja) 1996-07-12 2002-05-14 アリアド・ファーマシューティカルズ・インコーポレイテッド 病原性真菌感染の治療または予防材料および方法
CA2318402A1 (en) 1998-01-15 1999-07-22 Ariad Gene Therapeutics, Inc. Regulation of biological events using multimeric chimeric proteins
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
PL409579A1 (pl) 2001-02-19 2015-03-02 Novartis Ag Leczenie raka
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
GB0601406D0 (en) 2006-01-24 2006-03-08 Novartis Ag Organic Compounds
WO2008022256A2 (en) 2006-08-16 2008-02-21 Blagosklonny Mikhail V Methods and compositions for preventing or treating age-related diseases
GB0911888D0 (en) * 2009-07-08 2009-08-19 Oxford Biodynamics Ltd Method of treating age related disorders
US20150361120A1 (en) * 2010-03-31 2015-12-17 Chengzhi Zhang MACROLIDE INHIBITORS OF mTOR
WO2011133636A1 (en) 2010-04-20 2011-10-27 Cedars-Sinai Medical Center COMBINATION THERAPY WITH CD4 LYMPHOCYTE DEPLETION AND mTOR INHIBITORS
EP2670756B1 (en) 2011-02-04 2017-06-21 Synthon BV Process for making everolimus
EP2675450B1 (en) 2011-02-16 2016-02-10 Novartis AG Combinations of therapeutic agents for use in the treatment of neurodegenerative diseases
CA2856803A1 (en) 2011-11-23 2013-05-30 Intellikine, Llc Enhanced treatment regimens using mtor inhibitors
PH12017500997A1 (en) * 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
SG10201900002QA (en) 2014-01-24 2019-02-27 Dana Farber Cancer Institue Inc Antibody molecules to pd-1 and uses thereof
EP3109250A1 (en) 2015-06-23 2016-12-28 Synbias Pharma AG Method for the synthesis of rapamycin derivatives
CA3061907A1 (en) 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
MX2021007247A (es) 2018-12-18 2021-07-15 Novartis Ag Derivados de rapamicina.
KR20210142689A (ko) 2019-03-26 2021-11-25 노파르티스 아게 이소티아졸리딘 1,1-디옥시드 및 1,4-부탄 술톤 함유 라파마이신 유도체 및 이의 용도

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996041807A1 (en) * 1995-06-09 1996-12-27 Novartis Ag Rapamycin derivatives
CN104211715A (zh) * 2005-03-11 2014-12-17 巴克年龄研究协会 雷帕霉素的39-去甲氧基衍生物
CN101389337A (zh) * 2006-02-24 2009-03-18 诺瓦提斯公司 用于治疗神经母细胞瘤的雷帕霉素衍生物
WO2017044720A1 (en) * 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
雷帕霉素靶蛋白信号通路与靶向雷帕霉素靶蛋白抗肿瘤药物研究进展;林辰初 等;《中国新药杂志》;20131231;第22卷(第14期);第1656-1666页 *

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