BR112014011248A2 - processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários - Google Patents

processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários

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Publication number
BR112014011248A2
BR112014011248A2 BR112014011248A BR112014011248A BR112014011248A2 BR 112014011248 A2 BR112014011248 A2 BR 112014011248A2 BR 112014011248 A BR112014011248 A BR 112014011248A BR 112014011248 A BR112014011248 A BR 112014011248A BR 112014011248 A2 BR112014011248 A2 BR 112014011248A2
Authority
BR
Brazil
Prior art keywords
halogen
alkyl
derivatives
formula
phenylsulfonylprolinamide
Prior art date
Application number
BR112014011248A
Other languages
English (en)
Other versions
BR112014011248B1 (pt
Inventor
Bartels Bjoern
Pfleger Christophe
Bliss Fritz
Cueni Philipp
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 BR112014011248A2 publication Critical patent/BR112014011248A2/pt
Publication of BR112014011248B1 publication Critical patent/BR112014011248B1/pt

Links

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
    • 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
    • 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
    • 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
    • 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

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

resumo processo para preparação de derivados de 1-acil- fenilsulfonilprolinamida e novos intermediários novo processo para a preparação de derivados de prolina da fórmula i: r1nonhocnsoor2r3i em que, r1 é selecionado de alquila c1-7 ou da fórmula ii: r4 em que r4 é selecionado de alquila c1-7, halogênio-alquila c1-7 ou de fenila que é opcionalmente substituída por halogênio; r2 é selecionado de halogênio ou halogênio-alquila c1-7; e r3 é selecionado de hidrogênio, halogênio, halogênio-alquila c1-7, alcóxi c1-7, halogênio- alcóxi c1-7 ou de um anel heterocíclico de 5 ou 6 elementos contendo um ou dois átomos de nitrogênio, o anel que é opcionalmente substituído por alquila c1-7 ou halogênio sendo descrito. os derivados de prolina da fórmula i são inibidores preferidos de cisteína protease catepsina s e são, portanto, úteis para tratamento de doenças metabólicas, tais como, diabetes, aterosclerose, aneurisma aórtico abdominal, doença arterial periférica e nefropatia diabética.
BR112014011248-7A 2011-11-11 2012-11-08 processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários BR112014011248B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11188728.7 2011-11-11
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
BR112014011248A2 true BR112014011248A2 (pt) 2017-05-09
BR112014011248B1 BR112014011248B1 (pt) 2020-11-17

Family

ID=47143910

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014011248-7A BR112014011248B1 (pt) 2011-11-11 2012-11-08 processo para preparação de derivados de 1-acil-fenilsulfonilprolinamida e novos intermediários

Country Status (22)

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

Families Citing this family (6)

* 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
EP3419970B1 (en) 2016-02-26 2020-01-01 H. Hoffnabb-La Roche Ag Novel pyrrolidine derivatives
JP7001068B2 (ja) * 2017-01-24 2022-01-19 アステラス製薬株式会社 フェニルジフルオロメチル置換プロリンアミド化合物
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
WO2000014060A1 (fr) * 1998-09-09 2000-03-16 Nippon Finechemical Co., Ltd. Procede de preparation de composes sulfures aromatiques
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
WO2010121918A1 (en) 2009-04-20 2010-10-28 F. Hoffmann-La Roche Ag Proline derivatives as cathepsin inhibitors

Also Published As

Publication number Publication date
IL232424A0 (en) 2014-06-30
US8796471B2 (en) 2014-08-05
EP2776392A1 (en) 2014-09-17
SG11201402030VA (en) 2014-06-27
KR101620769B1 (ko) 2016-05-12
JP5852254B2 (ja) 2016-02-03
KR20140098123A (ko) 2014-08-07
CA2853877C (en) 2019-10-01
BR112014011248B1 (pt) 2020-11-17
ES2582643T3 (es) 2016-09-14
RU2014122116A (ru) 2015-12-20
AU2012334123A1 (en) 2014-05-01
PL2776392T3 (pl) 2016-11-30
EP2776392B1 (en) 2016-05-18
MY167569A (en) 2018-09-20
HUE029182T2 (en) 2017-02-28
JP2014532740A (ja) 2014-12-08
CN103930400B (zh) 2016-04-20
WO2013068434A1 (en) 2013-05-16
AU2012334123B2 (en) 2016-12-15
DK2776392T3 (en) 2016-07-04
CN103930400A (zh) 2014-07-16
NZ623851A (en) 2015-06-26
MX2014005689A (es) 2014-08-08
AR088816A1 (es) 2014-07-10
MX339996B (es) 2016-06-21
HK1194733A1 (zh) 2014-10-24
IL232424A (en) 2017-01-31
SI2776392T1 (sl) 2016-08-31
RU2615997C2 (ru) 2017-04-12
CA2853877A1 (en) 2013-05-16
ZA201403152B (en) 2015-07-29
US20130123512A1 (en) 2013-05-16

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 08/11/2012, OBSERVADAS AS CONDICOES LEGAIS.