JP2012513990A5 - - Google Patents
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- Publication number
- JP2012513990A5 JP2012513990A5 JP2011543458A JP2011543458A JP2012513990A5 JP 2012513990 A5 JP2012513990 A5 JP 2012513990A5 JP 2011543458 A JP2011543458 A JP 2011543458A JP 2011543458 A JP2011543458 A JP 2011543458A JP 2012513990 A5 JP2012513990 A5 JP 2012513990A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocyclyl
- heteroaryl
- aryl
- alkoxy
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 74
- 125000000623 heterocyclic group Chemical group 0.000 claims 62
- 125000003118 aryl group Chemical group 0.000 claims 44
- 125000001072 heteroaryl group Chemical group 0.000 claims 44
- 125000003545 alkoxy group Chemical group 0.000 claims 36
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 23
- -1 COOR1a Chemical group 0.000 claims 22
- 125000005842 heteroatom Chemical group 0.000 claims 17
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000004104 aryloxy group Chemical group 0.000 claims 12
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 12
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 12
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000004430 oxygen atom Chemical group O* 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- PNNCWTXUWKENPE-UHFFFAOYSA-N [N].NC(N)=O Chemical compound [N].NC(N)=O PNNCWTXUWKENPE-UHFFFAOYSA-N 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- PRULMJKVHATYQP-UHFFFAOYSA-N 4-(quinolin-2-ylmethyl)piperazine-1-carbaldehyde Chemical group C1CN(C=O)CCN1CC1=CC=C(C=CC=C2)C2=N1 PRULMJKVHATYQP-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 101000918494 Homo sapiens Fatty-acid amide hydrolase 1 Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000007201 Myocardial reperfusion injury Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 231100000354 acute hepatitis Toxicity 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 235000021229 appetite regulation Nutrition 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229930003827 cannabinoid Natural products 0.000 claims 1
- 239000003557 cannabinoid Substances 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000005796 circulatory shock Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 229960003920 cocaine Drugs 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229940127240 opiate Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000003368 psychostimulant agent Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 231100000419 toxicity Toxicity 0.000 claims 1
- 230000001988 toxicity Effects 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
- 0 *c1c(*)nc(*)[n]1C(N(*)*)=O Chemical compound *c1c(*)nc(*)[n]1C(N(*)*)=O 0.000 description 17
- BDVYXMRYPRBKMG-UHFFFAOYSA-N CN(C1CCOCC1)C([n]1cnc(-c2c[n+]([U-])ccc2)c1)=O Chemical compound CN(C1CCOCC1)C([n]1cnc(-c2c[n+]([U-])ccc2)c1)=O BDVYXMRYPRBKMG-UHFFFAOYSA-N 0.000 description 2
- HSLOZRQCLQVPAH-UHFFFAOYSA-N CN(C1CCCCC1)C([n]1cnc(-c2cc[n+](C)cc2)c1)=O Chemical compound CN(C1CCCCC1)C([n]1cnc(-c2cc[n+](C)cc2)c1)=O HSLOZRQCLQVPAH-UHFFFAOYSA-N 0.000 description 1
- OUOUTIJTFIDAHJ-UHFFFAOYSA-N CN(C1CCOCC1)C([n]1cnc(-c2cnccc2)c1)=O Chemical compound CN(C1CCOCC1)C([n]1cnc(-c2cnccc2)c1)=O OUOUTIJTFIDAHJ-UHFFFAOYSA-N 0.000 description 1
- XUEBIYRDHFIJGD-UHFFFAOYSA-N COc(cc(cc1)-c(nc2)c[n]2C(NC2CCCC2)=O)c1F Chemical compound COc(cc(cc1)-c(nc2)c[n]2C(NC2CCCC2)=O)c1F XUEBIYRDHFIJGD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14064008P | 2008-12-24 | 2008-12-24 | |
| US61/140,640 | 2008-12-24 | ||
| US15928109P | 2009-03-11 | 2009-03-11 | |
| US61/159,281 | 2009-03-11 | ||
| US17471209P | 2009-05-01 | 2009-05-01 | |
| US61/174,712 | 2009-05-01 | ||
| US22116609P | 2009-06-29 | 2009-06-29 | |
| US61/221,166 | 2009-06-29 | ||
| US24247209P | 2009-09-15 | 2009-09-15 | |
| US61/242,472 | 2009-09-15 | ||
| PCT/PT2009/000080 WO2010074588A2 (en) | 2008-12-24 | 2009-12-23 | Pharmaceutical compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014237957A Division JP2015071622A (ja) | 2008-12-24 | 2014-11-25 | 医薬品 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012513990A JP2012513990A (ja) | 2012-06-21 |
| JP2012513990A5 true JP2012513990A5 (https=) | 2013-02-14 |
| JP5657566B2 JP5657566B2 (ja) | 2015-01-21 |
Family
ID=42288334
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011543458A Expired - Fee Related JP5657566B2 (ja) | 2008-12-24 | 2009-12-23 | 医薬品 |
| JP2014237957A Pending JP2015071622A (ja) | 2008-12-24 | 2014-11-25 | 医薬品 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014237957A Pending JP2015071622A (ja) | 2008-12-24 | 2014-11-25 | 医薬品 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9353082B2 (https=) |
| EP (1) | EP2382012A2 (https=) |
| JP (2) | JP5657566B2 (https=) |
| KR (1) | KR101715190B1 (https=) |
| CN (2) | CN102333568B (https=) |
| AR (1) | AR075111A1 (https=) |
| AU (1) | AU2009330821B2 (https=) |
| BR (2) | BRPI0923819B1 (https=) |
| CA (1) | CA2747784C (https=) |
| IL (1) | IL213747A (https=) |
| MX (1) | MX342128B (https=) |
| NZ (1) | NZ593418A (https=) |
| RU (1) | RU2553451C2 (https=) |
| SG (1) | SG172301A1 (https=) |
| TW (1) | TWI469979B (https=) |
| WO (1) | WO2010074588A2 (https=) |
| ZA (1) | ZA201104336B (https=) |
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| WO2010056309A2 (en) | 2008-11-14 | 2010-05-20 | The Scripps Research Institute | Methods and compositions related to targeting monoacylglycerol lipase |
| KR101763656B1 (ko) | 2009-06-29 | 2017-08-01 | 인사이트 홀딩스 코포레이션 | Ｐｉ3ｋ 저해물질로서의 피리미디논 |
| WO2011058766A1 (en) * | 2009-11-16 | 2011-05-19 | Raqualia Pharma Inc. | Aryl carboxamide derivatives as ttx-s blockers |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| WO2011085216A2 (en) | 2010-01-08 | 2011-07-14 | Ironwood Pharmaceuticals, Inc. | Use of faah inhibitors for treating parkinson's disease and restless legs syndrome |
| US20130224151A1 (en) | 2010-03-31 | 2013-08-29 | United States Of America | Use of FAAH Inhibitors for Treating Abdominal, Visceral and Pelvic Pain |
| EP2558463A1 (en) | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| JP5996532B2 (ja) * | 2010-07-15 | 2016-09-21 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 有害生物防除剤としての新規複素環式化合物 |
| BR112013001721A2 (pt) * | 2010-07-29 | 2016-05-31 | Bial Portela & Ca Sa | processo de síntese de compostos de ureia substituída |
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| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| CA2830958A1 (en) | 2011-04-06 | 2012-10-11 | The Scripps Research Institute | N1- and n2-carbamoyl-1,2,3-triazole serine hydrolase inhibitors and methods |
| JP6094578B2 (ja) * | 2011-06-09 | 2017-03-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 代謝性障害の治療のためのｇｐｒ１１９モジュレーターとしての置換ピペリジン |
| PT3513793T (pt) | 2011-09-02 | 2021-05-10 | Incyte Holdings Corp | Heterociclilaminas como inibidores de pi3k |
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| WO2014017936A2 (en) * | 2012-07-24 | 2014-01-30 | Bial- Portela & Ca, S.A. | Urea compounds and their use as enzyme inhibitors |
| JP2015528013A (ja) * | 2012-07-27 | 2015-09-24 | ビアル−ポルテラ エ コンパニア，ソシエダッド アノニマ | 置換ウレア化合物の合成方法 |
| AU2014293731B2 (en) | 2013-07-24 | 2018-03-08 | Bial - Portela & Ca, S.A. | Imidazolecarboxamides and their use as FAAH inhibitors |
| RU2016105158A (ru) | 2013-08-01 | 2017-09-06 | БИАЛ - ПОРТЕЛА ЭНД Ка, С.А. | Соединения мочевины и их применение в качестве ингибиторов гидролазы амидов жирных кислот |
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| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| BR112017003918B1 (pt) | 2014-08-29 | 2022-05-03 | Fmc Corporation | Composto, composições e mistura herbicida e método para o controle do crescimento da vegetação |
| CN104292172B (zh) * | 2014-09-12 | 2016-08-17 | 浙江理工大学 | 一种苯并三氮唑类衍生物及其制备方法 |
| SG10201907576SA (en) | 2015-02-27 | 2019-09-27 | Incyte Corp | Salts of pi3k inhibitor and processes for their preparation |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
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| DK3548033T3 (da) | 2016-11-28 | 2024-07-15 | Praxis Prec Medicines Inc | Forbindelser og deres fremgangsmåde til anvendelse |
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| US20250145598A1 (en) * | 2021-08-18 | 2025-05-08 | The Regents Of The University Of California | Acid ceramidase inhibitors and uses thereof |
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2009
- 2009-12-23 MX MX2011006643A patent/MX342128B/es active IP Right Grant
- 2009-12-23 TW TW98144476A patent/TWI469979B/zh not_active IP Right Cessation
- 2009-12-23 CN CN200980157449.6A patent/CN102333568B/zh not_active Expired - Fee Related
- 2009-12-23 AU AU2009330821A patent/AU2009330821B2/en not_active Ceased
- 2009-12-23 BR BRPI0923819-0A patent/BRPI0923819B1/pt not_active IP Right Cessation
- 2009-12-23 BR BR122013027950A patent/BR122013027950A2/pt not_active Application Discontinuation
- 2009-12-23 KR KR1020117017329A patent/KR101715190B1/ko not_active Expired - Fee Related
- 2009-12-23 US US13/141,205 patent/US9353082B2/en not_active Expired - Fee Related
- 2009-12-23 WO PCT/PT2009/000080 patent/WO2010074588A2/en not_active Ceased
- 2009-12-23 SG SG2011045465A patent/SG172301A1/en unknown
- 2009-12-23 JP JP2011543458A patent/JP5657566B2/ja not_active Expired - Fee Related
- 2009-12-23 RU RU2011129416/04A patent/RU2553451C2/ru active
- 2009-12-23 EP EP09801307A patent/EP2382012A2/en not_active Withdrawn
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- 2009-12-23 NZ NZ593418A patent/NZ593418A/xx not_active IP Right Cessation
- 2009-12-23 CN CN201510829064.7A patent/CN105399731A/zh active Pending
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