JP2016532673A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016532673A5 JP2016532673A5 JP2016522013A JP2016522013A JP2016532673A5 JP 2016532673 A5 JP2016532673 A5 JP 2016532673A5 JP 2016522013 A JP2016522013 A JP 2016522013A JP 2016522013 A JP2016522013 A JP 2016522013A JP 2016532673 A5 JP2016532673 A5 JP 2016532673A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- compound
- substituted
- phenyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 77
- -1 substituted Chemical group 0.000 claims description 43
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 126
- 229910052736 halogen Inorganic materials 0.000 claims 65
- 150000002367 halogens Chemical class 0.000 claims 58
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 54
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 49
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 38
- 125000004093 cyano group Chemical group *C#N 0.000 claims 37
- 125000004076 pyridyl group Chemical group 0.000 claims 32
- 125000001072 heteroaryl group Chemical group 0.000 claims 30
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 28
- 125000003226 pyrazolyl group Chemical group 0.000 claims 22
- 125000003373 pyrazinyl group Chemical group 0.000 claims 20
- 125000002098 pyridazinyl group Chemical group 0.000 claims 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000003386 piperidinyl group Chemical group 0.000 claims 13
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000001425 triazolyl group Chemical group 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 8
- 125000000335 thiazolyl group Chemical group 0.000 claims 8
- 125000001544 thienyl group Chemical group 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 7
- 101000764872 Homo sapiens Transient receptor potential cation channel subfamily A member 1 Proteins 0.000 claims 6
- 208000027601 Inner ear disease Diseases 0.000 claims 6
- 208000002193 Pain Diseases 0.000 claims 6
- 208000003251 Pruritus Diseases 0.000 claims 6
- 102100026186 Transient receptor potential cation channel subfamily A member 1 Human genes 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 206010011224 Cough Diseases 0.000 claims 3
- 206010021143 Hypoxia Diseases 0.000 claims 3
- 206010021639 Incontinence Diseases 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 206010037660 Pyrexia Diseases 0.000 claims 3
- 208000026723 Urinary tract disease Diseases 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 230000017531 blood circulation Effects 0.000 claims 3
- 230000001079 digestive effect Effects 0.000 claims 3
- 230000004064 dysfunction Effects 0.000 claims 3
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 230000007954 hypoxia Effects 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 208000023504 respiratory system disease Diseases 0.000 claims 3
- 230000028016 temperature homeostasis Effects 0.000 claims 3
- 208000014001 urinary system disease Diseases 0.000 claims 3
- 241000031711 Cytophagaceae Species 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 **(C1)C(*)(*)C[C@]1N Chemical compound **(C1)C(*)(*)C[C@]1N 0.000 description 9
- GDOPTJXRTPNYNR-UHFFFAOYSA-N CC1CCCC1 Chemical compound CC1CCCC1 GDOPTJXRTPNYNR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361890127P | 2013-10-11 | 2013-10-11 | |
| US61/890,127 | 2013-10-11 | ||
| CNPCT/CN2014/086380 | 2014-09-12 | ||
| CN2014086380 | 2014-09-12 | ||
| PCT/EP2014/071593 WO2015052264A1 (en) | 2013-10-11 | 2014-10-09 | Substituted heterocyclic sulfonamide compounds useful as trpa1 modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018231696A Division JP6735330B2 (ja) | 2013-10-11 | 2018-12-11 | Ｔｒｐａ１調節因子として有用な置換複素環式スルホンアミド化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016532673A JP2016532673A (ja) | 2016-10-20 |
| JP2016532673A5 true JP2016532673A5 (enExample) | 2017-11-16 |
Family
ID=51794850
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016522013A Pending JP2016532673A (ja) | 2013-10-11 | 2014-10-09 | Ｔｒｐａ１調節因子として有用な置換複素環式スルホンアミド化合物 |
| JP2018231696A Active JP6735330B2 (ja) | 2013-10-11 | 2018-12-11 | Ｔｒｐａ１調節因子として有用な置換複素環式スルホンアミド化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018231696A Active JP6735330B2 (ja) | 2013-10-11 | 2018-12-11 | Ｔｒｐａ１調節因子として有用な置換複素環式スルホンアミド化合物 |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US20160221945A1 (enExample) |
| EP (1) | EP3055302B1 (enExample) |
| JP (2) | JP2016532673A (enExample) |
| KR (1) | KR20160064230A (enExample) |
| CN (1) | CN105612153B (enExample) |
| BR (1) | BR112016002012A2 (enExample) |
| CA (1) | CA2917193A1 (enExample) |
| DK (1) | DK3055302T3 (enExample) |
| ES (1) | ES2713323T3 (enExample) |
| HR (1) | HRP20190329T1 (enExample) |
| HU (1) | HUE041652T2 (enExample) |
| LT (1) | LT3055302T (enExample) |
| MX (1) | MX363457B (enExample) |
| PL (1) | PL3055302T3 (enExample) |
| PT (1) | PT3055302T (enExample) |
| RS (1) | RS58376B1 (enExample) |
| RU (1) | RU2675792C2 (enExample) |
| SG (1) | SG11201609411SA (enExample) |
| SI (1) | SI3055302T1 (enExample) |
| TR (1) | TR201902249T4 (enExample) |
| TW (1) | TWI657076B (enExample) |
| WO (1) | WO2015052264A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3256463B1 (en) * | 2015-02-15 | 2019-10-09 | F. Hoffmann-La Roche AG | 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists |
| JP6800158B2 (ja) | 2015-02-20 | 2020-12-16 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｇｄｆ−８阻害剤 |
| US20180186755A1 (en) * | 2015-07-01 | 2018-07-05 | Pharmakea, Inc. | Lysyl oxidase-like 2 inhibitors and uses thereof |
| ES2911416T3 (es) * | 2016-02-05 | 2022-05-19 | Ea Pharma Co Ltd | Derivados heterocíclicos de sulfonamida y medicamentos que los contienen |
| WO2017157885A1 (de) | 2016-03-16 | 2017-09-21 | Bayer Cropscience Aktiengesellschaft | N-(cyanbenzyl)-6-(cyclopropylcarbonylamino)-4-(phenyl)-pyridin-2-carboxamid-derivate und verwandte verbindungen als pestizide pflanzenschutzmittel |
| CN109476628B (zh) * | 2016-07-20 | 2022-01-11 | 豪夫迈·罗氏有限公司 | 作为trpa1调节剂的磺酰基环烷基酰胺化合物 |
| JP7043483B2 (ja) * | 2016-07-20 | 2022-03-29 | エフ．ホフマン－ラ ロシュ アーゲー | 二環式プロリン化合物 |
| EP3497093B1 (en) * | 2016-08-12 | 2021-09-15 | F. Hoffmann-La Roche AG | Sulfonyl pyridyl trp inhibitors |
| TWI791527B (zh) | 2017-06-01 | 2023-02-11 | 美商必治妥美雅史谷比公司 | 經取代之含氮化合物 |
| JP2019019124A (ja) * | 2017-07-19 | 2019-02-07 | 日本化薬株式会社 | ピラジン化合物 |
| US11465985B2 (en) * | 2017-12-08 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| WO2019164778A1 (en) * | 2018-02-20 | 2019-08-29 | Genentech, Inc. | Process for preparing 1-arylsulfonyl-pyrrolidine-2-carboxamide transient receptor potential channel antagonist compounds and crystalline forms thereof |
| 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 |
| CN117468520A (zh) | 2019-03-28 | 2024-01-30 | 住友建机株式会社 | 挖土机及施工系统 |
| 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 |
| CN116478076A (zh) * | 2023-04-26 | 2023-07-25 | 南京优氟医药科技有限公司 | 一种(2s,4s)-1-叔丁氧羰基-2-(二氟甲基)-4-羟基吡咯烷的制备方法 |
| WO2025132542A1 (en) | 2023-12-19 | 2025-06-26 | Idorsia Pharmaceuticals Ltd | Macrocyclic orexin agonists |
| WO2025259779A1 (en) * | 2024-06-12 | 2025-12-18 | Insmed Incorporated | Uses of certain carboxamides as dpp1 inhibitors |
| CN119019440A (zh) * | 2024-10-24 | 2024-11-26 | 浙江雅辰药物科技股份有限公司 | 一种6-环丙基吡啶-3-硼酸频那醇酯的制备方法 |
Family Cites Families (24)
| 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 |
| WO1994002178A1 (en) | 1992-07-27 | 1994-02-03 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | 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 |
| WO2002017930A2 (en) | 2000-08-30 | 2002-03-07 | 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 |
| WO2003009815A2 (en) | 2001-07-25 | 2003-02-06 | Biomarin 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 |
| EP1663239A4 (en) | 2003-09-10 | 2008-07-23 | Cedars Sinai Medical Center | KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY 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 |
| JP6182072B2 (ja) * | 2012-01-17 | 2017-08-16 | Ｅａファーマ株式会社 | 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 |
-
2014
- 2014-10-09 JP JP2016522013A patent/JP2016532673A/ja active Pending
- 2014-10-09 TR TR2019/02249T patent/TR201902249T4/tr unknown
- 2014-10-09 EP EP14789194.9A patent/EP3055302B1/en active Active
- 2014-10-09 PT PT14789194T patent/PT3055302T/pt unknown
- 2014-10-09 SG SG11201609411SA patent/SG11201609411SA/en unknown
- 2014-10-09 DK DK14789194.9T patent/DK3055302T3/en active
- 2014-10-09 PL PL14789194T patent/PL3055302T3/pl unknown
- 2014-10-09 KR KR1020167012211A patent/KR20160064230A/ko not_active Withdrawn
- 2014-10-09 WO PCT/EP2014/071593 patent/WO2015052264A1/en not_active Ceased
- 2014-10-09 RU RU2016115868A patent/RU2675792C2/ru not_active IP Right Cessation
- 2014-10-09 ES ES14789194T patent/ES2713323T3/es active Active
- 2014-10-09 BR BR112016002012A patent/BR112016002012A2/pt not_active Application Discontinuation
- 2014-10-09 RS RS20190254A patent/RS58376B1/sr unknown
- 2014-10-09 SI SI201431098T patent/SI3055302T1/sl unknown
- 2014-10-09 CA CA2917193A patent/CA2917193A1/en not_active Abandoned
- 2014-10-09 TW TW103135249A patent/TWI657076B/zh not_active IP Right Cessation
- 2014-10-09 CN CN201480053713.2A patent/CN105612153B/zh active Active
- 2014-10-09 MX MX2016002368A patent/MX363457B/es unknown
- 2014-10-09 HR HRP20190329TT patent/HRP20190329T1/hr unknown
- 2014-10-09 HU HUE14789194A patent/HUE041652T2/hu unknown
- 2014-10-09 LT LTEP14789194.9T patent/LT3055302T/lt unknown
-
2016
- 2016-04-11 US US15/095,467 patent/US20160221945A1/en not_active Abandoned
-
2017
- 2017-12-21 US US15/851,322 patent/US20180118680A1/en not_active Abandoned
-
2018
- 2018-06-06 US US16/001,770 patent/US20180282272A1/en not_active Abandoned
- 2018-12-11 JP JP2018231696A patent/JP6735330B2/ja active Active
-
2019
- 2019-10-18 US US16/657,102 patent/US11236046B2/en active Active