JP2016532673A5 - - Google Patents
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- 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 | ||
| CN2014086380 | 2014-09-12 | ||
| CNPCT/CN2014/086380 | 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 (https=) | 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 (https=) |
| EP (1) | EP3055302B1 (https=) |
| JP (2) | JP2016532673A (https=) |
| KR (1) | KR20160064230A (https=) |
| CN (1) | CN105612153B (https=) |
| BR (1) | BR112016002012A2 (https=) |
| CA (1) | CA2917193A1 (https=) |
| DK (1) | DK3055302T3 (https=) |
| ES (1) | ES2713323T3 (https=) |
| HR (1) | HRP20190329T1 (https=) |
| HU (1) | HUE041652T2 (https=) |
| LT (1) | LT3055302T (https=) |
| MX (1) | MX363457B (https=) |
| PL (1) | PL3055302T3 (https=) |
| PT (1) | PT3055302T (https=) |
| RS (1) | RS58376B1 (https=) |
| RU (1) | RU2675792C2 (https=) |
| SG (1) | SG11201609411SA (https=) |
| SI (1) | SI3055302T1 (https=) |
| TR (1) | TR201902249T4 (https=) |
| TW (1) | TWI657076B (https=) |
| WO (1) | WO2015052264A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6700291B2 (ja) * | 2015-02-15 | 2020-05-27 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | １−（ｈｅｔ）アリールスルホニル−（ピロリジン又はピペリジン）−２−カルボキサミド誘導体、及びｔｒｐａ１拮抗薬としてのそれらの使用 |
| 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 |
| WO2017003862A1 (en) * | 2015-07-01 | 2017-01-05 | Pharmakea, Inc. | Lysyl oxidase-like 2 inhibitors and uses thereof |
| MA43978A (fr) * | 2016-02-05 | 2018-12-12 | Ea Pharma Co Ltd | Dérivé de sulfonamide hétérocyclique et médicament le contenant |
| JP2019513700A (ja) | 2016-03-16 | 2019-05-30 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 殺有害生物剤及び植物保護剤としてのｎ−（シアノベンジル）−６−（シクロプロピル−カルボニルアミノ）−４−（フェニル）−ピリジン−２−カルボキサミド誘導体及び関連する化合物 |
| EP3487853B1 (en) * | 2016-07-20 | 2022-06-08 | F. Hoffmann-La Roche AG | Bicyclic proline compounds |
| EP3487849A1 (en) * | 2016-07-20 | 2019-05-29 | H. Hoffnabb-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 |
| HUE056142T2 (hu) | 2017-06-01 | 2022-01-28 | Bristol Myers Squibb Co | Szubsztituált nitrogéntartalmú vegyületek |
| JP2019019124A (ja) * | 2017-07-19 | 2019-02-07 | 日本化薬株式会社 | ピラジン化合物 |
| KR102716244B1 (ko) * | 2017-12-08 | 2024-10-14 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법 |
| TW202000201A (zh) * | 2018-02-20 | 2020-01-01 | 瑞士商赫孚孟拉羅股份公司 | 製備1-芳基磺醯基-吡咯啶-2-甲醯胺瞬時受體電位通道拮抗劑化合物及其結晶型式之方法 |
| 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 |
| TW202542165A (zh) | 2023-12-19 | 2025-11-01 | 瑞士商愛杜西亞製藥有限公司 | 大環食慾素激動劑 |
| 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 |
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| 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 |
| 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 |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| ATE191853T1 (de) | 1992-07-27 | 2000-05-15 | Us Health | Zielgerichte liposome zur blut-hirne schranke |
| 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 |
| US20020065259A1 (en) | 2000-08-30 | 2002-05-30 | Schatzberg Alan F. | 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 |
| AU2002322720B2 (en) | 2001-07-25 | 2008-11-13 | 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 |
| JP4995423B2 (ja) | 2002-12-03 | 2012-08-08 | ブランシェット・ロックフェラー・ニューロサイエンスィズ・インスティテュート | 物質を血液−脳関門を渡って輸送するための人工低密度リポタンパク質キャリア |
| JP2007505142A (ja) | 2003-09-10 | 2007-03-08 | セダーズ−シナイ メディカル センター | 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達 |
| 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 |
-
2014
- 2014-10-09 PL PL14789194T patent/PL3055302T3/pl unknown
- 2014-10-09 TR TR2019/02249T patent/TR201902249T4/tr unknown
- 2014-10-09 CN CN201480053713.2A patent/CN105612153B/zh active Active
- 2014-10-09 KR KR1020167012211A patent/KR20160064230A/ko not_active Withdrawn
- 2014-10-09 EP EP14789194.9A patent/EP3055302B1/en active Active
- 2014-10-09 TW TW103135249A patent/TWI657076B/zh not_active IP Right Cessation
- 2014-10-09 ES ES14789194T patent/ES2713323T3/es active Active
- 2014-10-09 WO PCT/EP2014/071593 patent/WO2015052264A1/en not_active Ceased
- 2014-10-09 HR HRP20190329TT patent/HRP20190329T1/hr unknown
- 2014-10-09 RS RS20190254A patent/RS58376B1/sr unknown
- 2014-10-09 LT LTEP14789194.9T patent/LT3055302T/lt unknown
- 2014-10-09 SI SI201431098T patent/SI3055302T1/sl unknown
- 2014-10-09 DK DK14789194.9T patent/DK3055302T3/en active
- 2014-10-09 SG SG11201609411SA patent/SG11201609411SA/en unknown
- 2014-10-09 BR BR112016002012A patent/BR112016002012A2/pt not_active Application Discontinuation
- 2014-10-09 PT PT14789194T patent/PT3055302T/pt unknown
- 2014-10-09 CA CA2917193A patent/CA2917193A1/en not_active Abandoned
- 2014-10-09 HU HUE14789194A patent/HUE041652T2/hu unknown
- 2014-10-09 JP JP2016522013A patent/JP2016532673A/ja active Pending
- 2014-10-09 MX MX2016002368A patent/MX363457B/es unknown
- 2014-10-09 RU RU2016115868A patent/RU2675792C2/ru not_active IP Right Cessation
-
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
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