BR112018001535A2 - método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído - Google Patents

método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído

Info

Publication number
BR112018001535A2
BR112018001535A2 BR112018001535A BR112018001535A BR112018001535A2 BR 112018001535 A2 BR112018001535 A2 BR 112018001535A2 BR 112018001535 A BR112018001535 A BR 112018001535A BR 112018001535 A BR112018001535 A BR 112018001535A BR 112018001535 A2 BR112018001535 A2 BR 112018001535A2
Authority
BR
Brazil
Prior art keywords
cyclohexyl
benzimidazol
anilino
acid derivatives
propanoic acid
Prior art date
Application number
BR112018001535A
Other languages
English (en)
Inventor
Schirmer Heiko
Original Assignee
Bayer Pharma 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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of BR112018001535A2 publication Critical patent/BR112018001535A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

"método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído" a presente invenção se refere a um método para preparar derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído da fórmula geral (i) (i) em que r1 representa um átomo de hidrogênio ou r1 representa um grupo selecionado da série de c1-c3-alquila-, c1-c3-alcoxi-, c1-c3-haloalquila- e c1-c3-haloalcoxi-, r2 representa um átomo de hidrogênio ou um grupo c1-c3-alquila, r3 representa um átomo de hidrogênio ou um grupo c1-c3-alquila, r4 representa um grupo ciclohexila, que é opcionalmente substituído de maneira única ou múltipla por um grupo c1-c3-alquila, e r5 representa um átomo de hidrogênio ou um grupo c1-c6-alquila; e, também, intermediários que podem ser utilizados para preparar derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído. a presente invenção também se refere a uma forma cristalina de ácido 3-(2-{[4-(trifluormetoxi)fenil]amino}-1-[(1r,5r)-3,3,5-trimetilciclohexil]-1h-benzimidazol-5-il)propanoico, composições farmacêuticas compreendendo esta forma cristalina e, também, o uso desta forma cristalina para preparar um medicamento para o tratamento de uma doença.
BR112018001535A 2015-07-27 2016-07-25 método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído BR112018001535A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15178413 2015-07-27
PCT/EP2016/067614 WO2017017046A1 (en) 2015-07-27 2016-07-25 Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1h-benzimidazol-5-yl)propanoic acid derivatives

Publications (1)

Publication Number Publication Date
BR112018001535A2 true BR112018001535A2 (pt) 2018-09-18

Family

ID=53758091

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018001535A BR112018001535A2 (pt) 2015-07-27 2016-07-25 método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído

Country Status (18)

Country Link
US (1) US10703727B2 (pt)
EP (1) EP3328838A1 (pt)
JP (1) JP6787998B2 (pt)
KR (1) KR20180030906A (pt)
CN (1) CN107848985B (pt)
AR (1) AR105494A1 (pt)
AU (1) AU2016299329B2 (pt)
BR (1) BR112018001535A2 (pt)
CA (1) CA2993480A1 (pt)
CL (1) CL2018000241A1 (pt)
CO (1) CO2018000795A2 (pt)
HK (1) HK1252848A1 (pt)
IL (1) IL256926A (pt)
MX (1) MX2018001204A (pt)
PE (1) PE20181039A1 (pt)
RU (1) RU2018106948A (pt)
TW (1) TW201718513A (pt)
WO (1) WO2017017046A1 (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP2016009371A0 (en) 2014-02-11 2016-08-31 Bayer Pharma AG Benzimidazol-2-amines as midh1 inhibitors
EP3105210B1 (en) 2014-02-11 2019-01-30 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
US10137110B2 (en) 2014-10-23 2018-11-27 Bayer Pharma Aktiengesellschaft 1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors
CA2988356A1 (en) 2015-06-08 2016-12-15 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
ES2877424T3 (es) 2015-07-07 2021-11-16 Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts 2-Aril- y 2-arilalquil-bencimidazoles como inhibidores de MIDH1
CN108026052B (zh) 2015-07-16 2021-10-08 德国癌症研究公共权益基金会 作为mIDH1抑制剂的5-羟烷基苯并咪唑类
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
TW201708193A (zh) * 2015-07-27 2017-03-01 拜耳製藥公司 突變之異檸檬酸脫氫酶ｉｄｈ１ ｒ１３２ｈ之抑制劑
EP3661559A1 (en) 2017-08-01 2020-06-10 Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts Combination of midh1 inhibitors and dna hypomethylating agents (hma)
EP3816158B1 (en) * 2018-06-26 2023-10-25 KPC Pharmaceuticals, Inc. Benzimidazole derivatives and use thereof as idh1 inhibitors
TWI760017B (zh) * 2019-12-23 2022-04-01 大陸商昆藥集團股份有限公司 一種ｉｄｈ１突變體抑制劑的鹽型、晶型及其製備方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5868851B2 (ja) * 2009-06-23 2016-02-24 ザ・トランスレーショナル・ジェノミクス・リサーチ・インスティチュート ベンズアミド誘導体
AP2016009371A0 (en) 2014-02-11 2016-08-31 Bayer Pharma AG Benzimidazol-2-amines as midh1 inhibitors
EP3105210B1 (en) 2014-02-11 2019-01-30 Bayer Pharma Aktiengesellschaft Benzimidazol-2-amines as midh1 inhibitors
EP3209646B1 (en) 2014-10-23 2020-07-22 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Benzimidazol-2-amines as midh1 inhibitors
US10137110B2 (en) 2014-10-23 2018-11-27 Bayer Pharma Aktiengesellschaft 1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors
CA2988356A1 (en) 2015-06-08 2016-12-15 Bayer Pharma Aktiengesellschaft N-menthylbenzimidazoles as midh1 inhibitors
ES2877424T3 (es) 2015-07-07 2021-11-16 Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts 2-Aril- y 2-arilalquil-bencimidazoles como inhibidores de MIDH1
CN108026052B (zh) 2015-07-16 2021-10-08 德国癌症研究公共权益基金会 作为mIDH1抑制剂的5-羟烷基苯并咪唑类
EP3121166A1 (en) 2015-07-21 2017-01-25 Bayer Pharma Aktiengesellschaft Fused imidazoles as midh1 inhibitors
TW201708193A (zh) 2015-07-27 2017-03-01 拜耳製藥公司 突變之異檸檬酸脫氫酶ｉｄｈ１ ｒ１３２ｈ之抑制劑

Also Published As

Publication number Publication date
AU2016299329B2 (en) 2020-08-13
JP2018527328A (ja) 2018-09-20
PE20181039A1 (es) 2018-07-03
RU2018106948A (ru) 2019-08-27
EP3328838A1 (en) 2018-06-06
MX2018001204A (es) 2018-04-24
KR20180030906A (ko) 2018-03-26
CO2018000795A2 (es) 2018-05-10
IL256926A (en) 2018-03-29
US10703727B2 (en) 2020-07-07
US20180222871A1 (en) 2018-08-09
HK1252848A1 (zh) 2019-06-06
CA2993480A1 (en) 2017-02-02
CL2018000241A1 (es) 2018-07-13
TW201718513A (zh) 2017-06-01
WO2017017046A1 (en) 2017-02-02
AR105494A1 (es) 2017-10-11
CN107848985B (zh) 2021-09-03
AU2016299329A1 (en) 2018-02-01
JP6787998B2 (ja) 2020-11-18
CN107848985A (zh) 2018-03-27

Similar Documents

Publication Publication Date Title
BR112018001535A2 (pt) método para preparação de derivados de ácido 3-(2-anilino-1-ciclohexil-1h-benzimidazol-5-il)propanoico substituído
PH12019550050A1 (en) Isoxazole analogs as fxr agonists and methods of use thereof
PH12017500828A1 (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
PH12017501586A1 (en) Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EA201992128A1 (ru) Конденсированные имидазопиперидиновые ингибиторы jak
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
CU20190045A7 (es) Compuestos derivados de 1,2,4-triazolonas 2,4,5-trisustituidas que son inhibidores de la dihidroorotato deshidrogenasa (dhodh) útiles para el tratamiento o prevención de trastornos hiperproliferativos e inflamatorios
PH12017500914A1 (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
BR112017003658A2 (pt) composto, mistura, métodos para tratamento de uma doença e para inibição de uma glicosidase, e, composição farmacêutica.
CR20160478A (es) Composición de control de enfermedades de plantas y método para controlar enfermedades de plantas mediante su aplicación
EA201890086A1 (ru) 1,4-замещенные производные пиперидина
TN2015000429A1 (en) 3-acetylamino-1-(phenyl-heteroaryl-aminocarbonyl or phenyl-heteroaryl-carbonylamino)benzene derivatives for the treatment of hyperproliferative disorders
BR112015024530A2 (pt) composto, métodos para tratamentos de distúrbios e de doenças e para profilaxia de distúrbios, composição farmacêutica, e, uso de um composto
BR112015028452A2 (pt) agonistas do receptor somastatina subtipo 4 (sstr4)
BR112018001534A2 (pt) inibidor de isocitrato desidrogenase idh1 r132h mutante
EA201391486A1 (ru) Способы и композиции для лечения болезни паркинсона
NZ726638A (en) Phosphatidylinositol 3-kinase inhibitors
WO2014145887A8 (en) Benzimidazole derivatives and uses thereof
NZ721645A (en) Compounds for use as gpr120 agonists
BR112017004173A2 (pt) composto, composição farmacêutica, e, método para tratar uma doença ou condição patológica.
MX2016008665A (es) Derivado basado en 1,2-naftoquinona y metodo de preparacion del mismo.
BR112019003320A2 (pt) compostos de heteroaril carboxamida como inibidores de ripk2
BR112017000132A2 (pt) composto, composição farmacêutica e método de tratamento ou prevenção de uma doença responsiva à inibição da atividade de pi3k
EA201791432A1 (ru) Композиции на основе пролекарства монометилфумарата
MX2020004842A (es) Compuestos heterociclicos antiinfecciosos y sus usos.

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]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements