JP2015506355A5 - - Google Patents
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- Publication number
- JP2015506355A5 JP2015506355A5 JP2014549480A JP2014549480A JP2015506355A5 JP 2015506355 A5 JP2015506355 A5 JP 2015506355A5 JP 2014549480 A JP2014549480 A JP 2014549480A JP 2014549480 A JP2014549480 A JP 2014549480A JP 2015506355 A5 JP2015506355 A5 JP 2015506355A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- heterocyclyl
- substituted
- carbocyclyl
- 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.)
- Granted
Links
- 125000000623 heterocyclic group Chemical group 0.000 claims description 44
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 29
- 125000001424 substituent group Chemical group 0.000 claims description 28
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 18
- 229910052799 carbon Inorganic materials 0.000 claims description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims description 8
- -1 aryl-C 1-3 -alkyl Chemical group 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000005549 heteroarylene group Chemical group 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims 1
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims 1
- 108010018763 Biotin carboxylase Proteins 0.000 claims 1
- ZSLZBFCDCINBPY-ZSJPKINUSA-N acetyl-CoA Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSC(=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 ZSLZBFCDCINBPY-ZSJPKINUSA-N 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 0 *C(N(*)I[Al]C(C1)CN1[Al])=O Chemical compound *C(N(*)I[Al]C(C1)CN1[Al])=O 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000012159 carrier gas Substances 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11196170 | 2011-12-30 | ||
| EP11196170.2 | 2011-12-30 | ||
| PCT/EP2012/077027 WO2013098375A1 (en) | 2011-12-30 | 2012-12-28 | New azetidine derivatives, pharmaceutical compositions and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015506355A JP2015506355A (ja) | 2015-03-02 |
| JP2015506355A5 true JP2015506355A5 (enExample) | 2016-02-25 |
| JP6130399B2 JP6130399B2 (ja) | 2017-05-17 |
Family
ID=47553036
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014549480A Active JP6130399B2 (ja) | 2011-12-30 | 2012-12-28 | 新規アゼチジン誘導体、医薬組成物およびそれらの使用 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8623860B2 (enExample) |
| EP (1) | EP2797884B1 (enExample) |
| JP (1) | JP6130399B2 (enExample) |
| KR (1) | KR20140115307A (enExample) |
| CN (1) | CN104093705A (enExample) |
| AU (1) | AU2012360797A1 (enExample) |
| BR (1) | BR112014015845A8 (enExample) |
| CA (1) | CA2861013A1 (enExample) |
| EA (1) | EA201400771A1 (enExample) |
| IL (1) | IL232914A0 (enExample) |
| MX (1) | MX2014007897A (enExample) |
| PH (1) | PH12014501514A1 (enExample) |
| WO (1) | WO2013098375A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112013028886A2 (pt) | 2011-05-10 | 2016-08-09 | Gilead Sciences Inc | compostos heterocíclicos fundidos como moduladores dde canal de sódio |
| NO3175985T3 (enExample) | 2011-07-01 | 2018-04-28 | ||
| TW201837023A (zh) | 2011-07-01 | 2018-10-16 | 美商基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| WO2014061693A1 (ja) * | 2012-10-17 | 2014-04-24 | 塩野義製薬株式会社 | 新規非芳香族炭素環又は非芳香族複素環誘導体 |
| CN105530940A (zh) | 2013-09-12 | 2016-04-27 | 辉瑞大药厂 | 乙酰辅酶a羧化酶抑制剂用于治疗寻常痤疮的用途 |
| CN103483273B (zh) * | 2013-09-12 | 2015-11-25 | 浙江工业大学 | 6-甲基-5-氟-2,4-嘧啶二胺类化合物及其制备与应用 |
| JPWO2015056782A1 (ja) | 2013-10-17 | 2017-03-09 | 塩野義製薬株式会社 | 新規アルキレン誘導体 |
| CA2942386A1 (en) | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| WO2015138934A1 (en) | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US10174014B2 (en) | 2014-06-19 | 2019-01-08 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
| US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US10738011B2 (en) | 2014-12-23 | 2020-08-11 | Proteostasis Therapeutics, Inc. | Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| CA2971835A1 (en) | 2014-12-23 | 2016-06-30 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| EP3325474A1 (en) | 2015-07-24 | 2018-05-30 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| KR20250136942A (ko) | 2015-10-06 | 2025-09-16 | 프로테오스타시스 테라퓨틱스, 인크. | Cftr 조절용 화합물, 조성물, 및 방법 |
| SG11201808682XA (en) | 2016-04-07 | 2018-11-29 | Proteostasis Therapeutics Inc | Silicone atoms containing ivacaftor analogues |
| CA3028966A1 (en) | 2016-06-21 | 2017-12-28 | Proteostasis Therapeutics, Inc. | Substituted phenyl-isoxazole-carboxamide compounds and use thereof for increasing cftr activity |
| CN110776504B (zh) * | 2019-11-29 | 2021-07-30 | 扬州工业职业技术学院 | 一种苯异噁唑乙氧基环丁胺衍生物及其制备方法与应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ534582A (en) | 2002-02-27 | 2006-03-31 | Pfizer Prod Inc | ACC inhibitors |
| DE102005055726A1 (de) | 2005-11-23 | 2007-08-30 | Sanofi-Aventis Deutschland Gmbh | Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| AU2006331882A1 (en) | 2005-12-21 | 2007-07-05 | Schering Corporation | Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists |
| CA2654792A1 (en) * | 2006-06-12 | 2007-12-21 | Merck Frosst Canada Ltd. | Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| WO2010043052A1 (en) | 2008-10-17 | 2010-04-22 | Merck Frosst Canada Ltd. | Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| WO2010127212A1 (en) | 2009-04-30 | 2010-11-04 | Forest Laboratories Holdings Limited | Inhibitors of acetyl-coa carboxylase |
| NZ603777A (en) | 2010-04-27 | 2013-08-30 | Takeda Pharmaceutical | Bicyclic compound derivatives and their use as acc inhibitors. |
| SG185515A1 (en) * | 2010-05-13 | 2012-12-28 | Amgen Inc | Nitrogen heterocyclic compounds useful as pde10 inhibitors |
-
2012
- 2012-12-14 US US13/714,525 patent/US8623860B2/en active Active
- 2012-12-28 WO PCT/EP2012/077027 patent/WO2013098375A1/en not_active Ceased
- 2012-12-28 CN CN201280068972.3A patent/CN104093705A/zh active Pending
- 2012-12-28 BR BR112014015845A patent/BR112014015845A8/pt not_active Application Discontinuation
- 2012-12-28 CA CA2861013A patent/CA2861013A1/en not_active Abandoned
- 2012-12-28 AU AU2012360797A patent/AU2012360797A1/en not_active Abandoned
- 2012-12-28 EA EA201400771A patent/EA201400771A1/ru unknown
- 2012-12-28 MX MX2014007897A patent/MX2014007897A/es unknown
- 2012-12-28 EP EP12813379.0A patent/EP2797884B1/en active Active
- 2012-12-28 JP JP2014549480A patent/JP6130399B2/ja active Active
- 2012-12-28 KR KR1020147018007A patent/KR20140115307A/ko not_active Withdrawn
-
2014
- 2014-06-02 IL IL232914A patent/IL232914A0/en unknown
- 2014-06-30 PH PH12014501514A patent/PH12014501514A1/en unknown
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