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

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P25/16—Anti-Parkinson drugs
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    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
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    • A61P27/06—Antiglaucoma agents or miotics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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)

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US201762563312P 2017-09-26 2017-09-26

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AR112834A1 true AR112834A1 (es) 2019-12-18

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US (3) US10800793B2 (es)
EP (1) EP3687999B1 (es)
JP (2) JP7387590B2 (es)
KR (1) KR20200059219A (es)
CN (2) CN117417351A (es)
AR (1) AR112834A1 (es)
AU (1) AU2018342784B2 (es)
BR (1) BR112020005898A2 (es)
CA (1) CA3078191A1 (es)
DK (1) DK3687999T3 (es)
FI (1) FI3687999T3 (es)
LT (1) LT3687999T (es)
MX (2) MX2020007265A (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)

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RU2020112056A3 (es) 2022-02-18
US10800793B2 (en) 2020-10-13
EP3687999A1 (en) 2020-08-05
JP7387590B2 (ja) 2023-11-28
UY37900A (es) 2019-04-30
US20220242878A1 (en) 2022-08-04
KR20200059219A (ko) 2020-05-28
AU2018342784A1 (en) 2020-02-06
RU2020112056A (ru) 2021-10-28
WO2019064182A1 (en) 2019-04-04
US20200392159A1 (en) 2020-12-17
TW201920189A (zh) 2019-06-01
LT3687999T (lt) 2024-02-26
JP2023106500A (ja) 2023-08-01
CA3078191A1 (en) 2019-04-04
SI3687999T1 (sl) 2024-03-29
JP2020535134A (ja) 2020-12-03
CN111094299B (zh) 2023-10-31
PT3687999T (pt) 2024-02-12
RS65270B1 (sr) 2024-03-29
EP3687999B1 (en) 2024-01-03
CN117417351A (zh) 2024-01-19
US20190092788A1 (en) 2019-03-28
CN111094299A (zh) 2020-05-01
FI3687999T3 (fi) 2024-02-14
BR112020005898A2 (pt) 2020-11-17
AU2018342784B2 (en) 2021-01-28
DK3687999T3 (da) 2024-02-12
MX2023001876A (es) 2023-03-10
MX2020007265A (es) 2020-09-18

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