[go: up one dir, main page]

AR112834A1 - Derivados de rapamicina - Google Patents

Derivados de rapamicina

Info

Publication number
AR112834A1
AR112834A1 ARP180102741A ARP180102741A AR112834A1 AR 112834 A1 AR112834 A1 AR 112834A1 AR P180102741 A ARP180102741 A AR P180102741A AR P180102741 A ARP180102741 A AR P180102741A AR 112834 A1 AR112834 A1 AR 112834A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
alkyl
hydrogen
group
compounds
Prior art date
Application number
ARP180102741A
Other languages
English (en)
Inventor
Tea Shavlakadze
Silvio Roggo
Andrew W Patterson
Manuel Mihalic
David Jonathan Glass
Michael Connolly
Simone Bonazzi
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR112834A1 publication Critical patent/AR112834A1/es

Links

Classifications

    • 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
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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
    • C07D491/18Bridged 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)

Abstract

La divulgación se refiere a compuestos y sales farmacéuticamente aceptables, y composiciones de los mismos. También se proporcionan métodos para preparar los compuestos y métodos que implican los compuestos o composiciones para tratar trastornos y enfermedades descritos en este documento. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: R¹ se selecciona a partir del grupo que consta de hidroxilo, o un compuesto del grupo de fórmulas (2); y R² se selecciona del grupo que consiste en los compuestos del grupo de fórmulas (3) en donde m es 0, 1, 2 ó 3; n es 1, 2 ó 3; o es 1, 2, 3, 4, 5 ó 6; p es 1, 2, 3, 4 ó 5; q es 1, 2, 3, 4 ó 5, en donde la suma de p y q es 2, 3, 4, 5 ó 6; r es 2, 3 ó 4; s es 2, 3 ó 4, en donde la suma de r y s es 4, 5 ó 6; X es O, S, NR⁶ o SO₂; R³ es hidrógeno, alquilo C₁₋₄, hidroxialquilo C₁₋₈, cicloalquilo C₃₋₈alquilo C₀₋₆ o fenilalquilo C₀₋₆; R⁴ es hidrógeno; R⁵ es hidrógeno, hidroxi o ciano; o R⁴ y R⁵ juntos forman =O; y R⁶ es hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₈alquilo C₀₋₆, fenilalquilo C₀₋₆, alquilo C₁₋₆-CO-, cicloalquilo C₃₋₈alquilo C₀₋₆-CO-, alquilo C₁₋₆-SO₂- o cicloalquilo C₃₋₈alquilo C₀₋₆-SO₂-.
ARP180102741A 2017-09-26 2018-09-24 Derivados de rapamicina AR112834A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201762563312P 2017-09-26 2017-09-26

Publications (1)

Publication Number Publication Date
AR112834A1 true AR112834A1 (es) 2019-12-18

Family

ID=63857991

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180102741A AR112834A1 (es) 2017-09-26 2018-09-24 Derivados de rapamicina

Country Status (23)

Country Link
US (4) US10800793B2 (es)
EP (2) EP3687999B1 (es)
JP (2) JP7387590B2 (es)
KR (2) KR102794731B1 (es)
CN (2) CN111094299B (es)
AR (1) AR112834A1 (es)
AU (1) AU2018342784B2 (es)
BR (1) BR112020005898A2 (es)
CA (1) CA3078191A1 (es)
DK (1) DK3687999T3 (es)
ES (1) ES2973975T3 (es)
FI (1) FI3687999T3 (es)
HR (1) HRP20240199T8 (es)
HU (1) HUE065692T2 (es)
LT (1) LT3687999T (es)
MX (2) MX2020007265A (es)
PL (1) PL3687999T3 (es)
PT (1) PT3687999T (es)
RS (1) RS65270B1 (es)
SI (1) SI3687999T1 (es)
TW (1) TW201920189A (es)
UY (1) UY37900A (es)
WO (1) WO2019064182A1 (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
CA3013650A1 (en) 2016-02-04 2017-08-10 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
CN108697729B (zh) 2016-02-04 2023-05-09 约翰霍普金斯大学 新型GLUT抑制剂rapaglutin及其用途
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
LT3813946T (lt) 2018-06-15 2024-07-10 Janssen Pharmaceutica Nv Rapamicino analogai ir jų panaudojimas
BR112021011325A2 (pt) 2018-12-18 2021-11-16 Novartis Ag Derivados de rapamicina
KR102705165B1 (ko) 2019-01-22 2024-09-11 에오비안 파마슈티컬스, 인크. Mtorc 조절제 및 이의 용도
WO2020194209A1 (en) * 2019-03-26 2020-10-01 Novartis Ag Isothiazolidine 1,1-dioxide and 1,4-butan sultone containing rapamycin derivatives and uses thereof
KR102497821B1 (ko) * 2019-08-23 2023-02-08 이화여자대학교 산학협력단 신규 mTOR 억제제 화합물 및 이의 용도
KR102486721B1 (ko) * 2019-08-23 2023-01-10 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
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
DE102020203224A1 (de) 2020-03-12 2021-09-16 Heinrich-Heine-Universität Düsseldorf Inhibition von FKBP1A zur Therapie des Triple-negativen Mammakarzinoms
US20230133761A1 (en) 2020-03-12 2023-05-04 Heinrich-Heine-Universität Düsseldorf Inhibition of fkbp1a for the treatment of triple-negative mammary carcinoma
KR102805250B1 (ko) * 2020-03-27 2025-05-08 에오비안 파마슈티컬스, 인크. Mtorc1 조절제 및 이의 용도
CN116322677B (zh) * 2020-07-21 2025-09-23 艾奥维安制药公司 Mtorc1调节剂及其用途
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
JP2025522296A (ja) 2022-05-25 2025-07-15 レヴォリューション・メディスンズ,インコーポレイテッド mTOR阻害剤によりがんを処置する方法
CN121127477A (zh) * 2023-04-07 2025-12-12 瑞泽恩制药公司 选择性雷帕霉素类似物及其用途
WO2024243449A1 (en) * 2023-05-23 2024-11-28 Tornado Therapeutics, Inc. Rapamycin derivatives and uses thereof

Family Cites Families (38)

* 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
ATE404663T1 (de) 1995-06-07 2008-08-15 Ariad Gene Therapeutics Inc Auf rapamycin basierende regulation biologischer vorgänge
WO1996041865A1 (en) 1995-06-07 1996-12-27 Ariad Gene Therapeutics, Inc. Rapamcycin-based regulation of biological events
CZ292233B6 (cs) * 1995-06-09 2003-08-13 Novartis Ag Deriváty rapamycinu a jejich použití jako léčiv
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
EP1363627A2 (en) 2001-02-19 2003-11-26 Novartis AG Treatment of solid tumours with rapamycin derivatives
EP1478648B1 (en) 2002-02-01 2014-04-30 ARIAD Pharmaceuticals, Inc. Phosphorus-containing compounds and uses thereof
GB0504994D0 (en) * 2005-03-11 2005-04-20 Biotica Tech Ltd Novel compounds
GB0601406D0 (en) 2006-01-24 2006-03-08 Novartis Ag Organic Compounds
US20090023768A1 (en) * 2006-02-24 2009-01-22 Novartis Ag Rapamycin derivatives for treating neuroblastoma
US20100081681A1 (en) 2006-08-16 2010-04-01 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
WO2011123524A2 (en) * 2010-03-31 2011-10-06 Auspex Pharmaceutical, Inc. Macrolide inhibitors of mtor
US8906374B2 (en) 2010-04-20 2014-12-09 Cedars-Sinai Medical Center Combination therapy with CD4 lymphocyte depletion and mTOR inhibitors
EP2670758B1 (en) 2011-02-04 2022-09-28 Synthon BV Process for making trisubstituted silyloxyethyl triflates
WO2012110953A1 (en) 2011-02-16 2012-08-23 Novartis Ag Combinations of therapeutic agents for use in the treatment of neurodegenerative diseases
JP6130391B2 (ja) 2011-11-23 2017-05-17 インテリカイン, エルエルシー Mtor阻害剤を使用する強化された治療レジメン
PH12017500997A1 (en) * 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
EP3109250A1 (en) 2015-06-23 2016-12-28 Synbias Pharma AG Method for the synthesis of rapamycin derivatives
US10683308B2 (en) * 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
KR20200012876A (ko) 2017-05-02 2020-02-05 레볼루션 메디슨즈, 인크. mTOR 억제제로서의 파라마이신 유사체
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
BR112021011325A2 (pt) 2018-12-18 2021-11-16 Novartis Ag Derivados de rapamicina
WO2020194209A1 (en) 2019-03-26 2020-10-01 Novartis Ag Isothiazolidine 1,1-dioxide and 1,4-butan sultone containing rapamycin derivatives and uses thereof

Also Published As

Publication number Publication date
US10800793B2 (en) 2020-10-13
HUE065692T2 (hu) 2024-06-28
JP7387590B2 (ja) 2023-11-28
HRP20240199T1 (hr) 2024-04-26
ES2973975T3 (es) 2024-06-25
US20200392159A1 (en) 2020-12-17
LT3687999T (lt) 2024-02-26
RU2020112056A (ru) 2021-10-28
KR102794731B1 (ko) 2025-04-14
CN117417351A (zh) 2024-01-19
RS65270B1 (sr) 2024-03-29
BR112020005898A2 (pt) 2020-11-17
HRP20240199T8 (hr) 2024-09-27
TW201920189A (zh) 2019-06-01
WO2019064182A1 (en) 2019-04-04
PL3687999T3 (pl) 2024-05-06
EP3687999A1 (en) 2020-08-05
FI3687999T3 (fi) 2024-02-14
MX2023001876A (es) 2023-03-10
JP7699626B2 (ja) 2025-06-27
EP3687999B1 (en) 2024-01-03
KR20250054121A (ko) 2025-04-22
JP2023106500A (ja) 2023-08-01
US12091424B2 (en) 2024-09-17
RU2020112056A3 (es) 2022-02-18
US20190092788A1 (en) 2019-03-28
US20250223297A1 (en) 2025-07-10
MX2020007265A (es) 2020-09-18
CN111094299A (zh) 2020-05-01
UY37900A (es) 2019-04-30
CN111094299B (zh) 2023-10-31
EP4365179A3 (en) 2024-07-10
AU2018342784A1 (en) 2020-02-06
PT3687999T (pt) 2024-02-12
KR20200059219A (ko) 2020-05-28
JP2020535134A (ja) 2020-12-03
DK3687999T3 (da) 2024-02-12
US20220242878A1 (en) 2022-08-04
AU2018342784B2 (en) 2021-01-28
EP4365179A2 (en) 2024-05-08
CA3078191A1 (en) 2019-04-04
SI3687999T1 (sl) 2024-03-29

Similar Documents

Publication Publication Date Title
AR112834A1 (es) Derivados de rapamicina
AR120109A1 (es) Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores
AR121044A1 (es) Inhibidores de egfr
AR099177A1 (es) Determinadas (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1
AR100033A1 (es) Compuestos y composiciones para inhibir la actividad de shp2
AR108812A1 (es) Proceso para preparar un derivado de piridona policíclica sustituida y cristal del mismo
AR116283A1 (es) Inhibidores del sarcómero cardíaco
AR102361A1 (es) Compuestos de metil-quinolina útiles para inhibir la sintasa-1 de prostaglandina microsomal e2
AR109349A1 (es) Compuestos y usos
AR090945A1 (es) Moduladores de la via del complemento y usos de los mismos
AR114793A1 (es) Moduladores de enzimas modificadoras de metilo, composiciones y usos de los mismos
AR119728A1 (es) Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2
AR108710A1 (es) Compuestos modulares de fxr (nr1h4)
AR103828A1 (es) INHIBIDORES DEL FACTOR TRANSFORMADOR DEL CRECIMIENTO b
AR069798A1 (es) Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa.
AR101815A1 (es) Compuestos y composiciones como inhibidores de quinasa
AR109709A1 (es) Inhibidores de la fosfatidilinositol 3-quinasa
AR095430A1 (es) Compuestos de pirimidina y piridina y su uso como inhibidores de la actividad de fgfr
AR099914A1 (es) Derivados de indol y de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR098522A1 (es) Compuesto de triazolo-piridina
AR094790A1 (es) Derivados sustituidos del ácido bisfenil butanóico fosfónico como inhibidores de la nep
AR123078A1 (es) Medicamentos antiplaquetarios y usos de estos
AR094272A1 (es) Compuestos de diona ciclica activos como herbicidas, o derivados de los mismos, sustituidos por un fenilo que tiene un sustituyente que contiene alquinilo
AR097894A1 (es) Inhibidores terapéuticos de cdk8 o uso de los mismos
AR104512A1 (es) Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap)

Legal Events

Date Code Title Description
FB Suspension of granting procedure