DK3055302T3 - Substituerede heterocykliske sulfonamidforbindelser, der er nyttige som TRPA1-modulatorer - Google Patents

Substituerede heterocykliske sulfonamidforbindelser, der er nyttige som TRPA1-modulatorer Download PDF

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DK3055302T3
DK3055302T3 DK14789194.9T DK14789194T DK3055302T3 DK 3055302 T3 DK3055302 T3 DK 3055302T3 DK 14789194 T DK14789194 T DK 14789194T DK 3055302 T3 DK3055302 T3 DK 3055302T3
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mmol
methyl
trifluoromethyl
fluoro
compound
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DK14789194.9T
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Huifen Chen
Yanyan Chu
Steven Do
Anthony Estrada
Baihua Hu
Aleksandr Kolesnikov
Xingyu Lin
Joseph P Lyssikatos
Daniel Shore
Vishal Verma
Lan Wang
Guosheng Wu
Po-Wai Yuen
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Hoffmann La Roche
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Claims (28)

1. Forbindelse med formlen II: hvor:
(2) A er
B er B2 og R5 er R5b; B2 er en pyridinyl, hvor en hvilken som helst pyridinyl af B2 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt fra halogen, (Ci-Ce)alkyl, -O(Ci-Ce)alkyl, -O(Ci-C6)alkyl-O(Ci-C6)alkyl, (C3-C?)cycloalkyl, (Ci-C6)halogenalkyl, -CN og 6-leddet heteroaryl, hvor en hvilken som helst 6-leddet heteroaryl eventuelt er substitueret med en eller flere (Ci-Ce)alkyl eller (Ci-C6)halogenalkyl; R1 er en phenyl, 5-leddet heteroaryl eller 6-leddet heteroaryl, hvor en hvilken som helst phenyl, 5-leddet heteroaryl eller 6-leddet heteroaryl af R1 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt fra halogen, -CN, (Ci-Ce)alkyl og (C i -C6)halogenalkyl; én R3b-gruppe er halogen, -CN eller (Ci-Ce)alkyl og de øvrige R3b-grupper er uafhængigt valgt fra H, (Ci-Ce)alkyl og (Ci-C6)halogenalkyl; R4 er H, (Ci-Ce)alkyl eller (Ci-C6)halogenalkyl; R5b er
eller et salt deraf.
2. Forbindelse ifølge krav 1, hvor en R3b-gruppe er F og de øvrige R3b-grupper er H.
3. Forbindelse ifølge et hvilket som helst af kravene 1-2, hvor (1) A-gruppen
4. Forbindelse ifølge et hvilket som helst af kravene 1-3, hvor B2 er pyridinyl, hvor en hvilken som helst pyridinyl af B2 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt fra halogen, (Ci-Ce)alkyl, -O(Ci-Ce)alkyl, -O(Ci-C6)alkyl-O(Ci-Ce)alkyl, (Ci-C6)halogenalkyl, -CN og 6-leddet heteroaryl, hvor en hvilken som helst 6-leddet heteroaryl eventuelt er substitueret med en eller flere (Ci-Ce)alkyl eller (C i -C6)halogenalky 1.
5. Forbindelse ifølge et hvilket som helst af kravene 1-4, hvor B2 er:
hvor hver RZ1 er uafhængigt valgt fra H, halogen, (Ci-Ce)alkyl, -O(Ci-Ce)alkyl, -O(Ci-C6)alkyl-O(Ci-C6)alkyl, (C3-C?)cycloalkyl, (Ci-C6)halogenalkyl, -CN og 6-leddet heteroaryl, hvor en hvilken som helst 6-leddet heteroaryl eventuelt er substitueret med (Ci-Ce)alkyl eller (Ci-C6)halogenalkyl.
6. Forbindelse ifølge et hvilket som helst af kravene 1-5, hvor R4 er H.
7. Forbindelse ifølge et hvilket som helst af kravene 1-6, hvor R1 er en phenyl eller thiophenyl, hvor en hvilken som helst phenyl eller thiophenyl i R1 eventuelt er substitueret
med en eller flere grupper, som er uafhængigt valgt fra halogen, -CN, (Ci-Ce)alkyl og (C i -C6)halogenalkyl.
8. Forbindelse ifølge et hvilket som helst af kravene 1-7, hvor R1 er en phenyl eller thiophenyl, hvor en hvilken som helst phenyl eller thiophenyl af R1 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt fra halogen og -CN.
9. Forbindelse ifølge et hvilket som helst af kravene 1-8, hvor R1 er en phenyl eller thiophenyl, hvor en hvilken som helst phenyl eller thiophenyl i R1 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt fra fluor, chlor og -CN.
10. Forbindelse ifølge et hvilket som helst af kravene 1-9, hvor R1 er 4-fluorphenyl, 3-fluorphenyl, 4-cyanophenyl, 2-chlorthiophen-5-yl, 3,4-difluorphenyl eller 3-fluorpyridin-5-yl.
11. Forbindelse ifølge krav 1, der er:
12. Forbindelse ifølge krav 1, der er:
eller eller et salt deraf.
13. Forbindelse ifølge krav 1, hvor (1) A-gruppen
14. Forbindelse ifølge krav 1, hvor (1) A-gruppen
15. Forbindelse ifølge krav 1, hvor (1) A-gruppen
16. Forbindelse ifølge krav 1, hvor (1) A-gruppen
17. Forbindelse ifølge krav 1, hvor (1) A-gruppen
18. Forbindelse ifølge krav 1, hvor (1) A-gruppen
19. Forbindelse ifølge krav 1, hvor (1) A-gruppen
20. Forbindelse ifølge krav 1, hvor (1) A-gruppen
21. Forbindelse ifølge krav 1, hvor (1) A-gruppen
22. Forbindelse ifølge et hvilket som helst af kravene 13-21, hvor: R1 er en phenyl eller thiophenyl, hvor en hvilken som helst phenyl eller thiophenyl af R1 eventuelt er substitueret med en eller flere grupper, som er uafhængigt valgt ffa fluor, chlor og -CN; og R4 er H.
23. Farmaceutisk sammensætning, der omfatter en forbindelse med formlen II som beskrevet i et hvilket som helst af kravene 1-22 eller et farmaceutisk acceptabelt salt deraf og en farmaceutisk acceptabel bærer, diluent eller excipiens.
24. Forbindelse med formlen II som beskrevet i et hvilket som helst af kravene 1-22 eller et farmaceutisk acceptabelt salt deraf til anvendelse i medicinsk behandling.
25. Forbindelse med formlen II som beskrevet i et hvilket som helst af kravene 1-22 eller et farmaceutisk acceptabelt salt deraf til anvendelse i behandling eller forebyggelse af en luftvejslidelse.
26. Forbindelse med formlen II som beskrevet i et hvilket som helst af kravene 1-22 eller et farmaceutisk acceptabelt salt deraf til anvendelse i modulering af TRPA1-aktivitet.
27. Forbindelse med formlen II som beskrevet i et hvilket som helst af kravene 1-22 eller et farmaceutisk acceptabelt salt deraf til anvendelse i behandling eller forebyggelse af en sygdom eller lidelse, der medieres af TRPA1-aktivitet.
28. Forbindelse til anvendelse ifølge krav 27, hvor sygdommen eller lidelsen er smerte, kløe, en inflammatorisk lidelse, en lidelse i det indre øre, feber eller en anden forstyrrelse af varmereguleringen, trakeobronkial eller diafragmal funktionssvigt, en mave-
tarm- eller urinvejslidelse, kronisk obstruktiv lungesygdom, inkontinens eller en lidelse forbundet med reduceret blodstrømning til centralnervesystemet eller CNS-hypoxi, især smerte, artrit, kløe, hoste, astma, inflammatorisk tarmsygdom eller en lidelse i det indre øre.
DK14789194.9T 2013-10-11 2014-10-09 Substituerede heterocykliske sulfonamidforbindelser, der er nyttige som TRPA1-modulatorer DK3055302T3 (da)

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EA033497B1 (ru) * 2015-02-15 2019-10-31 Hoffmann La Roche 1-(тиофенил или фенил)сульфонил-(пирролидин)-2-карбоксамидные производные и их применение в качестве антагонистов trpa1
US9981944B2 (en) 2015-02-20 2018-05-29 Rigel Pharmaceuticals, Inc GDF-8 inhibitors
WO2017003862A1 (en) * 2015-07-01 2017-01-05 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
DK3412664T3 (da) * 2016-02-05 2022-06-07 Ea Pharma Co Ltd Heterocyklisk sulfonamidderivat og medicin indeholdende samme
CN109071444A (zh) 2016-03-16 2018-12-21 拜耳作物科学股份公司 作为农药和植物保护剂的n-(氰苄基)-6-(环丙基-羰基氨基)-4-(苯基)-吡啶-2-羧酰胺衍生物及相关化合物
EP3487853B1 (en) * 2016-07-20 2022-06-08 F. Hoffmann-La Roche AG Bicyclic proline compounds
WO2018015411A1 (en) * 2016-07-20 2018-01-25 F. Hoffmann-La Roche Ag Sulfonylcycloalkyl carboxamide compounds as trpa1 modulators
WO2018029288A1 (en) * 2016-08-12 2018-02-15 F. Hoffmann-La Roche Ag Sulfonyl pyridyl trp inhibitors
WO2018222795A1 (en) 2017-06-01 2018-12-06 Bristol-Myers Squibb Company Substituted nitrogen containing compounds
JP2019019124A (ja) * 2017-07-19 2019-02-07 日本化薬株式会社 ピラジン化合物
AR114585A1 (es) * 2018-02-20 2020-09-23 Hoffmann La Roche Proceso para preparar compuestos antagonistas de canales potenciales transitorios del receptor de 1-arilsulfonil-pirrolidin-2-carboxamida y formas cristalinas de los mismos
KR102006157B1 (ko) 2018-03-22 2019-08-01 (주)에스더블유엠 자율주행 차량의 주행 유도선 제공 방법 및 장치
KR102006158B1 (ko) 2018-03-27 2019-08-01 (주)에스더블유엠 차량 주행유도 장치 및 방법
KR102068473B1 (ko) 2018-03-30 2020-02-11 (주)에스더블유엠 차량 시뮬레이션 방법 및 장치
KR20210140742A (ko) 2019-03-28 2021-11-23 스미토모 겐키 가부시키가이샤 쇼벨 및 시공시스템
CN111116456B (zh) * 2019-12-26 2022-01-28 南通华祥医药科技有限公司 一种4,4-二氟哌啶盐酸盐的制备方法
FR3114235A1 (fr) 2020-09-18 2022-03-25 Université Grenoble Alpes Inhibition du canal trpa1 astrocytaire comme nouvelle cible therapeutique neuroprotectrice dans les phases prodromales de la maladie d’alzheimer
CN112624966B (zh) * 2020-12-25 2022-12-23 杭州澳赛诺生物科技有限公司 一种2-氨甲基-4-甲基-5-吡啶羧酸的合成方法
IT202100015098A1 (it) 2021-06-09 2022-12-09 Flonext S R L Composto antagonista del canale trpa1 per uso in patologie degenerative della retina

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
AU677216B2 (en) 1992-07-27 1997-04-17 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Targeting of liposomes to the blood-brain barrier
GB9826174D0 (en) * 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
AU2001286930A1 (en) 2000-08-30 2002-03-13 The Board Of Trustees Of The Leland Stanford Junior University Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
EP1554572B1 (en) 2001-07-25 2009-10-14 Raptor Pharmaceutical Inc. Compositions and methods for modulating blood-brain barrier transport
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
CA2791165C (en) 2002-12-03 2015-02-24 Blanchette Rockefeller Neurosciences Institute A conjugate comprising cholesterol linked to tetracycline
WO2005025511A2 (en) 2003-09-10 2005-03-24 Cedars-Sinai Medical Center Potassium channel mediated delivery of agents through the blood-brain barrier
JP2009096764A (ja) * 2007-10-17 2009-05-07 Japan Tobacco Inc ピペリジン化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用
WO2010141805A1 (en) * 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of trpa1
JP2013028537A (ja) * 2009-11-11 2013-02-07 Dainippon Sumitomo Pharma Co Ltd Ｎ−ベンジルアミド誘導体およびそれを含有する医薬組成物
EP2520566A1 (en) * 2011-05-06 2012-11-07 Orion Corporation New Pharmaceutical Compounds
WO2013108857A1 (ja) * 2012-01-17 2013-07-25 味の素株式会社 複素環アミド誘導体及びそれを含有する医薬
RU2603770C2 (ru) * 2014-11-28 2016-11-27 Федеральное государственное автономное образовательное учреждение высшего образования "Белгородский государственный национальный исследовательский университет" (НИУ "БелГУ") Замещенные пиразинопиримидиноны как блокаторы trpa1 каналов, фармацевтическая композиция, способы их получения и применения

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