CN107073066B - mTORC1抑制剂 - Google Patents

mTORC1抑制剂 Download PDF

Info

Publication number
CN107073066B
CN107073066B CN201580057417.4A CN201580057417A CN107073066B CN 107073066 B CN107073066 B CN 107073066B CN 201580057417 A CN201580057417 A CN 201580057417A CN 107073066 B CN107073066 B CN 107073066B
Authority
CN
China
Prior art keywords
substituted
unsubstituted
various embodiments
independently
membered
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
CN201580057417.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN107073066A (zh
Inventor
K·邵克特
冈庭正格
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.)
University of California San Diego UCSD
Original Assignee
University of California San Diego UCSD
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.)
Filing date
Publication date
Application filed by University of California San Diego UCSD filed Critical University of California San Diego UCSD
Priority to CN202111002275.5A priority Critical patent/CN113620978A/zh
Publication of CN107073066A publication Critical patent/CN107073066A/zh
Application granted granted Critical
Publication of CN107073066B publication Critical patent/CN107073066B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
CN201580057417.4A 2014-09-11 2015-09-11 mTORC1抑制剂 Active CN107073066B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202111002275.5A CN113620978A (zh) 2014-09-11 2015-09-11 mTORC1抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462049186P 2014-09-11 2014-09-11
US62/049,186 2014-09-11
PCT/US2015/049693 WO2016040806A1 (en) 2014-09-11 2015-09-11 mTORC1 INHIBITORS

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202111002275.5A Division CN113620978A (zh) 2014-09-11 2015-09-11 mTORC1抑制剂

Publications (2)

Publication Number Publication Date
CN107073066A CN107073066A (zh) 2017-08-18
CN107073066B true CN107073066B (zh) 2021-09-17

Family

ID=55459613

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202111002275.5A Pending CN113620978A (zh) 2014-09-11 2015-09-11 mTORC1抑制剂
CN201580057417.4A Active CN107073066B (zh) 2014-09-11 2015-09-11 mTORC1抑制剂

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN202111002275.5A Pending CN113620978A (zh) 2014-09-11 2015-09-11 mTORC1抑制剂

Country Status (7)

Country Link
US (5) US10117945B2 (cg-RX-API-DMAC7.html)
EP (1) EP3193902A4 (cg-RX-API-DMAC7.html)
JP (3) JP6692798B2 (cg-RX-API-DMAC7.html)
CN (2) CN113620978A (cg-RX-API-DMAC7.html)
CA (1) CA2960992C (cg-RX-API-DMAC7.html)
MX (2) MX2017001981A (cg-RX-API-DMAC7.html)
WO (1) WO2016040806A1 (cg-RX-API-DMAC7.html)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113620978A (zh) * 2014-09-11 2021-11-09 加利福尼亚大学董事会 mTORC1抑制剂
WO2016094307A1 (en) 2014-12-08 2016-06-16 The Research Foundation For The State University Of New York Anti-fungals targeting the synthesis of fungal shingolipids
WO2017044720A1 (en) * 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
SG11201909924VA (en) * 2017-05-02 2019-11-28 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors
WO2018232298A1 (en) 2017-06-16 2018-12-20 The Research Foundation For The State University Of New York Anti-fungals compounds targeting the synthesis of fungal sphingolipids
EP3656859A4 (en) * 2017-07-20 2021-04-14 Curigin Co.,Ltd. NUCLEIC ACID SIMULTANEOUSLY INHIBITING THE EXPRESSION OF THE AR GENE AND THE MTOR GENE
WO2019178536A1 (en) * 2018-03-16 2019-09-19 The Regents Of The University Of California Mtor inhibitors and uses thereof
FI3788049T3 (fi) * 2018-05-01 2023-05-30 Revolution Medicines Inc C40-, c28- ja c-32-liittyneitä rapamysiinianalogeja mtor-estäjinä
SG11202010560QA (en) 2018-05-01 2020-11-27 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
CN108676882B (zh) * 2018-05-30 2022-02-22 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) NOP14基因及其蛋白作为肿瘤对mTOR抑制剂敏感性的标志物的应用
EA202092692A1 (ru) 2018-06-15 2021-04-21 Навитор Фармасьютикалз, Инк. Аналоги рапамицина и их применения
JP7061236B2 (ja) * 2019-01-22 2022-04-27 エオビアン ファーマシューティカルズ, インコーポレイテッド Mtorcモジュレーターおよびその使用
WO2020163598A1 (en) * 2019-02-07 2020-08-13 The Regents Of The University Of California Immunophilin-dependent inhibitors and uses thereof
US20230063768A1 (en) * 2019-02-07 2023-03-02 The Regents Of The University Of California Immunophilin binding agents and uses thereof
CN110152004B (zh) * 2019-07-08 2021-09-03 天津医科大学 甘氨酸在制备药物递送增强剂及细胞移植试剂方面的用途
CN115209897A (zh) 2019-12-05 2022-10-18 安纳库利亚治疗公司 雷帕霉素类似物及其用途
KR102805250B1 (ko) 2020-03-27 2025-05-08 에오비안 파마슈티컬스, 인크. Mtorc1 조절제 및 이의 용도
KR20230042600A (ko) 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
WO2022020522A2 (en) * 2020-07-21 2022-01-27 Aeovian Pharmaceuticals, Inc. Mtorc1 modulators and uses thereof
CN114507236A (zh) * 2022-02-28 2022-05-17 山东中医药大学 mTOR蛋白降解靶向嵌合体及其制备方法和应用
AU2023275778A1 (en) 2022-05-25 2024-12-12 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor
CN119462690A (zh) * 2024-11-08 2025-02-18 西安交通大学 一类基于自噬-溶酶体途径的选择性mTORC1降解剂及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102740851A (zh) * 2009-10-12 2012-10-17 霍夫曼-拉罗奇有限公司 Pi3k抑制剂和mek抑制剂的组合
CN103703174A (zh) * 2011-05-04 2014-04-02 因特利凯有限责任公司 联合药物组合物及其用途
CN103796655A (zh) * 2011-05-06 2014-05-14 加利福尼亚大学董事会 多囊性疾病的治疗

Family Cites Families (98)

* 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
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US5023264A (en) 1990-07-16 1991-06-11 American Home Products Corporation Rapamycin oximes
US5023263A (en) 1990-08-09 1991-06-11 American Home Products Corporation 42-oxorapamycin
US5130307A (en) 1990-09-28 1992-07-14 American Home Products Corporation Aminoesters of rapamycin
US5221670A (en) 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
DE69212850T2 (de) 1991-01-15 1997-03-06 Alcon Lab Inc Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen
GB9103430D0 (en) 1991-02-19 1991-04-03 Smithkline Beecham Plc Novel compound
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5162333A (en) 1991-09-11 1992-11-10 American Home Products Corporation Aminodiesters of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
US5177203A (en) 1992-03-05 1993-01-05 American Home Products Corporation Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5411967A (en) 1992-10-13 1995-05-02 American Home Products Corporation Carbamates of rapamycin
US5480989A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5480988A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5489680A (en) 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5262423A (en) 1992-10-29 1993-11-16 American Home Products Corporation Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5260300A (en) 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
US5252579A (en) 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
US5504091A (en) 1993-04-23 1996-04-02 American Home Products Corporation Biotin esters of rapamycin
US5391730A (en) 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5378836A (en) 1993-10-08 1995-01-03 American Home Products Corporation Rapamycin oximes and hydrazones
US5373014A (en) 1993-10-08 1994-12-13 American Home Products Corporation Rapamycin oximes
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5385910A (en) 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
US5385909A (en) 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
US5385908A (en) 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
CN1046944C (zh) 1993-12-17 1999-12-01 山道士有限公司 雷怕霉素类衍生物
US5389639A (en) 1993-12-29 1995-02-14 American Home Products Company Amino alkanoic esters of rapamycin
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5463048A (en) 1994-06-14 1995-10-31 American Home Products Corporation Rapamycin amidino carbamates
US5491231A (en) 1994-11-28 1996-02-13 American Home Products Corporation Hindered N-oxide esters of rapamycin
US5563145A (en) 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US5985890A (en) 1995-06-09 1999-11-16 Novartis Ag Rapamycin derivatives
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
PL330814A1 (en) 1996-06-20 1999-06-07 Regents Board Of Compounds for and methods of delivering pharmaceutical preparations and their application
EP1212331B1 (en) 1999-08-24 2004-04-21 Ariad Gene Therapeutics, Inc. 28-epirapalogs
US6277983B1 (en) 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Jnk阻害剤
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
US7220755B2 (en) 2003-11-12 2007-05-22 Biosensors International Group, Ltd. 42-O-alkoxyalkyl rapamycin derivatives and compositions comprising same
ES2315745T3 (es) 2004-03-01 2009-04-01 Terumo Kabushiki Kaisha Procedimiento para la fabricacion de derivados o-alquilados de rapamicina.
AU2005238386A1 (en) 2004-04-30 2005-11-10 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof as an MMP-13 inhibitor
CN100516195C (zh) 2004-07-19 2009-07-22 汕头市双骏生物科技有限公司 一种新的菌株及应用该菌株生产紫杉醇的方法
WO2006068760A2 (en) 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
GB0504994D0 (en) 2005-03-11 2005-04-20 Biotica Tech Ltd Novel compounds
US7642059B2 (en) 2005-09-07 2010-01-05 Roche Diagnostics Operations, Inc. Single receptor assays for immunosuppressive drugs
US20080032960A1 (en) 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists
US20090274739A1 (en) * 2006-04-13 2009-11-05 The Trustees Of Columbia University In The City Of New York Methods and compositions for treating neointimal hyperplasia
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
US20090287133A1 (en) 2006-06-06 2009-11-19 Lagreca Sr Alfred J Disposable or Reclosable Wound or Skin Condition Dressing and Treatment System
EP2298772A1 (en) 2006-10-18 2011-03-23 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
JP5456321B2 (ja) 2006-11-27 2014-03-26 テルモ株式会社 O−アルキル化ラパマイシン誘導体の製造方法およびo−アルキル化ラパマイシン誘導体
JP2010523566A (ja) * 2007-04-05 2010-07-15 ワイス エルエルシー ワートマニン−ラパマイシンコンジュゲートおよびその使用
US20090074831A1 (en) 2007-09-18 2009-03-19 Robert Falotico LOCAL VASCULAR DELIVERY OF mTOR INHIBITORS IN COMBINATION WITH PEROXISOME PROLIFERATORS-ACTIVATED RECEPTOR STIMULATORS
WO2009046436A1 (en) * 2007-10-04 2009-04-09 Memorial Sloan-Kettering Cancer Center Methods for inhibiting senescence of epithelial cells
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
MX2010007418A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
US20110098241A1 (en) 2008-04-14 2011-04-28 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
TW200948361A (en) 2008-05-26 2009-12-01 Chunghwa Chemical Synthesis & Biotech Co Ltd Method for synthesizing Biolimus A9 and the like and method for improving stability of the same
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン, エルエルシー キナーゼインヒビターおよび使用方法
US20100055145A1 (en) 2008-08-29 2010-03-04 Biosensors International Group Stent coatings for reducing late stent thrombosis
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン, エルエルシー 複素環キナーゼ阻害剤
US8697709B2 (en) 2008-10-16 2014-04-15 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
WO2010059593A1 (en) 2008-11-18 2010-05-27 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
ES2709108T3 (es) 2009-08-17 2019-04-15 Intellikine Llc Compuestos heterocíclicos y usos de los mismos
WO2011047384A2 (en) 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
WO2011146882A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
WO2012024558A2 (en) * 2010-08-20 2012-02-23 The University Of North Carolina At Chapel Hill Light mediated regulation of protein dimerization
CA2818225C (en) 2010-11-19 2016-10-25 Biocon Limited Processes for preparation of everolimus and intermediates thereof
WO2012103959A1 (en) 2011-02-04 2012-08-09 Synthon Bv Process for making everolimus
CN106619647A (zh) 2011-02-23 2017-05-10 因特利凯有限责任公司 激酶抑制剂的组合及其用途
CN118078979A (zh) * 2011-04-29 2024-05-28 西莱克塔生物科技公司 用于降低针对治疗性蛋白的免疫应答的致耐受性合成纳米载体
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
CN113620978A (zh) * 2014-09-11 2021-11-09 加利福尼亚大学董事会 mTORC1抑制剂
SG11201909924VA (en) * 2017-05-02 2019-11-28 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102740851A (zh) * 2009-10-12 2012-10-17 霍夫曼-拉罗奇有限公司 Pi3k抑制剂和mek抑制剂的组合
CN103703174A (zh) * 2011-05-04 2014-04-02 因特利凯有限责任公司 联合药物组合物及其用途
CN103796655A (zh) * 2011-05-06 2014-05-14 加利福尼亚大学董事会 多囊性疾病的治疗

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Target of Rapamycin Signaling in Leukemia and Lymphoma;Collin Vu等;《Clinical Cancer Research》;20100908;第16卷(第22期);5374-5380 *

Also Published As

Publication number Publication date
WO2016040806A1 (en) 2016-03-17
US20250099597A1 (en) 2025-03-27
US20240066134A1 (en) 2024-02-29
US20170246305A1 (en) 2017-08-31
CA2960992A1 (en) 2016-03-17
CN113620978A (zh) 2021-11-09
JP6692798B2 (ja) 2020-05-13
US11452780B2 (en) 2022-09-27
US20210052735A1 (en) 2021-02-25
JP2020125320A (ja) 2020-08-20
US10646577B2 (en) 2020-05-12
EP3193902A4 (en) 2018-03-28
MX2017001981A (es) 2017-12-12
JP2017531624A (ja) 2017-10-26
CN107073066A (zh) 2017-08-18
JP7057798B2 (ja) 2022-04-20
US12097262B2 (en) 2024-09-24
US10117945B2 (en) 2018-11-06
EP3193902A1 (en) 2017-07-26
CA2960992C (en) 2024-04-09
US20190091340A1 (en) 2019-03-28
MX2022013114A (es) 2022-11-14
JP2022091995A (ja) 2022-06-21

Similar Documents

Publication Publication Date Title
CN107073066B (zh) mTORC1抑制剂
KR102236605B1 (ko) 피리도피리미딘온 cdk2/4/6 억제제
JP6980649B2 (ja) イソキノリノン誘導体の固体形態、それを製造する方法、それを含む組成物、及びそれを使用する方法
US20230339902A1 (en) Tricyclic ligands for degradation of ikzf2 or ikzf4
CA3154073A1 (en) Isoindolinone and indazole compounds for the degradation of egfr
CA3194351A1 (en) Tricyclic compounds to degrade neosubstrates for medical therapy
CN113620958A (zh) 用于治疗PI3K-γ介导的障碍的杂环化合物
CN107995911A (zh) 苯并氧氮杂*噁唑烷酮化合物及其使用方法
CN117881683A (zh) PI3Kα抑制剂及其使用方法
JPWO2008001886A1 (ja) オーロラ(Aurora)阻害剤
JP2024521791A (ja) 脳又はcnsへの癌転移を治療するためのegfrデグレーダー
KR20240112283A (ko) Pi3k-알파 저해제 그리고 이의 제조 방법 및 사용 방법
HK1242971B (zh) Mtorc1抑制剂
HK1242971A1 (zh) Mtorc1抑制劑
EP4648766A1 (en) Pi3k inhibitors and methods of making and using the same
WO2025240847A1 (en) Ras inhibitors
CN117440813A (zh) 治疗脑或cns的癌转移的egfr降解剂
CN117720516A (zh) 选择性brd9降解剂的有利晶型形式
HK1254517B (zh) 苯并氧氮杂䓬恶唑烷酮化合物及其使用方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1242971

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant