MX339996B - Proceso para la preparacion de derivados de 1-acil-4-fenilsulfonil prolinamida y nuevos intermediarios. - Google Patents

Proceso para la preparacion de derivados de 1-acil-4-fenilsulfonil prolinamida y nuevos intermediarios.

Info

Publication number
MX339996B
MX339996B MX2014005689A MX2014005689A MX339996B MX 339996 B MX339996 B MX 339996B MX 2014005689 A MX2014005689 A MX 2014005689A MX 2014005689 A MX2014005689 A MX 2014005689A MX 339996 B MX339996 B MX 339996B
Authority
MX
Mexico
Prior art keywords
halogen
alkyl
preparation
formula
derivatives
Prior art date
Application number
MX2014005689A
Other languages
English (en)
Other versions
MX2014005689A (es
Inventor
Bartels Bjoern
Bliss Fritz
Cueni Philipp
Pfleger Christophe
Zutter Ulrich
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2014005689A publication Critical patent/MX2014005689A/es
Publication of MX339996B publication Critical patent/MX339996B/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se describe un nuevo proceso para la obtención de derivados de prolina de la fórmula I (ver Fórmula) en la que: R1 se elige entre alquilo C1-7 y entre (ver Fórmula) en el que R4 se elige entre alquilo C1-7, halogenoalquilo C1-7 y fenilo, que está opcionalmente sustituido por halógeno; R2 se elige entre halógeno y halogenoalquilo C1-7 y R3 se elige entre hidrógeno, halógeno, halogenoalquilo C1-7, alcoxi C1-7, halogenoalcoxi C1-7 y entre un anillo heterocíclico de 5 ó 6 miembros que contiene uno o dos átomos de nitrógeno, el anillo está opcionalmente sustituido por alquilo C1-7 o halógeno. Los derivados de prolina de la fórmula I son inhibidores preferentes de la cisteína-proteasa catepsina S y por ello son útiles para tratar enfermedades metabólicas, por ejemplo la diabetes, la aterosclerosis, el aneurismo aórtico abdominal, la enfermedad arterial periférica y la nefropatía diabética.
MX2014005689A 2011-11-11 2012-11-08 Proceso para la preparacion de derivados de 1-acil-4-fenilsulfonil prolinamida y nuevos intermediarios. MX339996B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11188728 2011-11-11
PCT/EP2012/072078 WO2013068434A1 (en) 2011-11-11 2012-11-08 Process for the preparation of 1-acyl-4-phenylsulfonylprolinamide derivatives and new intermediates

Publications (2)

Publication Number Publication Date
MX2014005689A MX2014005689A (es) 2014-08-08
MX339996B true MX339996B (es) 2016-06-21

Family

ID=47143910

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014005689A MX339996B (es) 2011-11-11 2012-11-08 Proceso para la preparacion de derivados de 1-acil-4-fenilsulfonil prolinamida y nuevos intermediarios.

Country Status (22)

Country Link
US (1) US8796471B2 (es)
EP (1) EP2776392B1 (es)
JP (1) JP5852254B2 (es)
KR (1) KR101620769B1 (es)
CN (1) CN103930400B (es)
AR (1) AR088816A1 (es)
AU (1) AU2012334123B2 (es)
BR (1) BR112014011248B1 (es)
CA (1) CA2853877C (es)
DK (1) DK2776392T3 (es)
ES (1) ES2582643T3 (es)
HK (1) HK1194733A1 (es)
HU (1) HUE029182T2 (es)
IL (1) IL232424A (es)
MX (1) MX339996B (es)
MY (1) MY167569A (es)
PL (1) PL2776392T3 (es)
RU (1) RU2615997C2 (es)
SG (1) SG11201402030VA (es)
SI (1) SI2776392T1 (es)
WO (1) WO2013068434A1 (es)
ZA (1) ZA201403152B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103333094B (zh) * 2013-06-19 2015-05-13 广东肇庆星湖生物科技股份有限公司 一种脯氨酸结晶精制的工艺方法
WO2016034602A1 (en) * 2014-09-05 2016-03-10 F. Hoffmann-La Roche Ag Solid forms of (2s,4r)-4-[4-(1-methyl-1h-pyrazol-4-yl)-2-trifluoromethyl-benzenesulfonyl]-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidine-2-carboxylic acid (1-cyano-cyclopropyl)-amide
RS59938B1 (sr) * 2016-02-26 2020-03-31 Hoffmann La Roche Novi derivati pirolidina
MX2019008756A (es) * 2017-01-24 2019-09-11 Astellas Pharma Inc Compuesto de prolinamida sustituida por fenildiflurometilo.
AR114732A1 (es) * 2018-09-18 2020-10-07 Hoffmann La Roche Utilización de un inhibidor de catepsina s contra la formación de anticuerpos antifármaco
EP3725769A1 (en) * 2019-04-17 2020-10-21 Newron Pharmaceuticals S.p.A. Process for the production of substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives
CN111825582B (zh) * 2020-08-12 2022-04-08 江西理工大学 一种以芳基磺酰氯为硫源合成β-硫代羰基化合物的方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6376716B1 (en) * 1998-09-09 2002-04-23 Nippon Finechemical Co., Ltd. Process for the preparation of aromatic sulfur compounds
CN101475517B (zh) * 2009-01-15 2012-08-15 河南大学 一种对称的含二硫键化合物的制备方法
JP5518997B2 (ja) * 2009-04-20 2014-06-11 エフ．ホフマン−ラ ロシュ アーゲー カテプシン阻害薬としてのプロリン誘導体

Also Published As

Publication number Publication date
BR112014011248B1 (pt) 2020-11-17
ES2582643T3 (es) 2016-09-14
WO2013068434A1 (en) 2013-05-16
EP2776392A1 (en) 2014-09-17
JP2014532740A (ja) 2014-12-08
IL232424A0 (en) 2014-06-30
CA2853877A1 (en) 2013-05-16
RU2014122116A (ru) 2015-12-20
NZ623851A (en) 2015-06-26
KR101620769B1 (ko) 2016-05-12
KR20140098123A (ko) 2014-08-07
RU2615997C2 (ru) 2017-04-12
DK2776392T3 (en) 2016-07-04
HUE029182T2 (en) 2017-02-28
US20130123512A1 (en) 2013-05-16
AU2012334123A1 (en) 2014-05-01
MY167569A (en) 2018-09-20
SI2776392T1 (sl) 2016-08-31
SG11201402030VA (en) 2014-06-27
JP5852254B2 (ja) 2016-02-03
IL232424A (en) 2017-01-31
US8796471B2 (en) 2014-08-05
BR112014011248A2 (pt) 2017-05-09
CN103930400B (zh) 2016-04-20
EP2776392B1 (en) 2016-05-18
AU2012334123B2 (en) 2016-12-15
HK1194733A1 (zh) 2014-10-24
AR088816A1 (es) 2014-07-10
PL2776392T3 (pl) 2016-11-30
ZA201403152B (en) 2015-07-29
MX2014005689A (es) 2014-08-08
CN103930400A (zh) 2014-07-16
CA2853877C (en) 2019-10-01

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