MX368101B - 12-epi-pleuromutilinas. - Google Patents

12-epi-pleuromutilinas.

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Publication number
MX368101B
MX368101B MX2016008781A MX2016008781A MX368101B MX 368101 B MX368101 B MX 368101B MX 2016008781 A MX2016008781 A MX 2016008781A MX 2016008781 A MX2016008781 A MX 2016008781A MX 368101 B MX368101 B MX 368101B
Authority
MX
Mexico
Prior art keywords
ring
epi
mutilin
stereochemistry
substituents
Prior art date
Application number
MX2016008781A
Other languages
English (en)
Other versions
MX2016008781A (es
Inventor
Thirring Klaus
Heilmayer Werner
Riedl Rosemarie
Kollmann Hermann
IVEZIC-SCHOENFELD Zrinka
Wicha Wolfgang
Paukner Susanne
Strickmann Dirk
Original Assignee
Nabriva Therapeutics 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 Nabriva Therapeutics Ag filed Critical Nabriva Therapeutics Ag
Publication of MX2016008781A publication Critical patent/MX2016008781A/es
Publication of MX368101B publication Critical patent/MX368101B/es

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    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
    • C07C323/63—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/52—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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    • A61K31/495—Heterocyclic 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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Abstract

La presente invención se refiere a un compuesto seleccionado de 14-O- [((alquil, cicloalquil, heterocicloalquil, heteoroaril- o aril) -sulfanil) -acetil] -12-epi-mutilinas, o 14-O- [((alquilo, cicloalquilo, heterocicloalquilo, heteoroaril- o aril) -oxi) -acetil] -12-epi-mutilinas, en donde la 12-epi-mutilina se caracteriza porque el anillo de mutilina en la posición 12 es sustituido por dos sustituyentes, el primer sustituyente en la posición 12 del anillo de mutilina es un grupo metilo, grupo metilo el cual tiene la estereoquímica inversa en comparación con la estereoquímica del grupo metilo en la posición 12 del anillo de pleuromutilina de origen natural, el segundo sustituyente en la posición 12 del anillo de mutilina es un grupo hidrocarburo que comprende por lo menos un átomo de nitrógeno y todos los otros sustituyentes del anillo de mutilina tienen la misma estereoquímica en comparación con la estereoquímica de los sustituyentes en las posiciones correspondientes en el anillo de pleuromutilina de origen natural; opcionalmente en la forma de una sal y/o solvato, en donde la pleuromutilina de origen natural tiene la fórmula PLEU, un proceso para la preparación de estos compuestos y su uso como composiciones farmacéuticas.
MX2016008781A 2014-01-22 2015-01-21 12-epi-pleuromutilinas. MX368101B (es)

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CN107235971B (zh) * 2017-07-31 2019-11-12 重庆华邦胜凯制药有限公司 一种制备瑞他莫林的新方法
CN109666009B (zh) * 2018-11-02 2023-02-03 华南农业大学 一种以2-氨基苯巯醇为连接基团截短侧耳素衍生物制备方法和用途
WO2020210158A1 (en) * 2019-04-06 2020-10-15 The Board Of Trustees Of The University Of Illinois Compounds that induce ferroptic cell death
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TW202204337A (zh) 2020-04-17 2022-02-01 奧地利商納畢瓦治療有限責任公司 截短側耳素類之醫療用途
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CN116199690B (zh) * 2023-04-28 2023-07-07 西华大学 嘌呤类截短侧耳素衍生物、立体异构体或药学上可接受的盐及其用途和药物组合物

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