JP2016512535A5 - - Google Patents
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- JP2016512535A5 JP2016512535A5 JP2016501487A JP2016501487A JP2016512535A5 JP 2016512535 A5 JP2016512535 A5 JP 2016512535A5 JP 2016501487 A JP2016501487 A JP 2016501487A JP 2016501487 A JP2016501487 A JP 2016501487A JP 2016512535 A5 JP2016512535 A5 JP 2016512535A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- halo
- alkyl
- disorder
- pyrimidinyl
- 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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- 150000001875 compounds Chemical class 0.000 claims description 63
- 125000000217 alkyl group Chemical group 0.000 claims description 35
- 125000005843 halogen group Chemical group 0.000 claims description 35
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 24
- 125000004076 pyridyl group Chemical group 0.000 claims description 21
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
- 125000001425 triazolyl group Chemical group 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
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 14
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 13
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 13
- 125000002971 oxazolyl group Chemical group 0.000 claims description 13
- 125000000335 thiazolyl group Chemical group 0.000 claims description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- -1 2 -cyclopropyl Chemical group 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims description 6
- 208000019116 sleep disease Diseases 0.000 claims description 6
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 4
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 4
- 208000010877 cognitive disease Diseases 0.000 claims description 4
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims description 4
- 208000019906 panic disease Diseases 0.000 claims description 4
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 208000011117 substance-related disease Diseases 0.000 claims description 4
- 125000004385 trihaloalkyl group Chemical group 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 206010002383 Angina Pectoris Diseases 0.000 claims description 3
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims description 3
- 206010013654 Drug abuse Diseases 0.000 claims description 3
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 208000012902 Nervous system disease Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 206010033307 Overweight Diseases 0.000 claims description 3
- 208000001871 Tachycardia Diseases 0.000 claims description 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 230000006794 tachycardia Effects 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000006820 Arthralgia Diseases 0.000 claims description 2
- 208000008035 Back Pain Diseases 0.000 claims description 2
- 206010007556 Cardiac failure acute Diseases 0.000 claims description 2
- 206010012218 Delirium Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 206010012735 Diarrhoea Diseases 0.000 claims description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims description 2
- 208000008930 Low Back Pain Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000005793 Restless legs syndrome Diseases 0.000 claims description 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 2
- 208000016620 Tourette disease Diseases 0.000 claims description 2
- 208000025865 Ulcer Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 208000008784 apnea Diseases 0.000 claims description 2
- 206010003119 arrhythmia Diseases 0.000 claims description 2
- 230000006793 arrhythmia Effects 0.000 claims description 2
- 201000001883 cholelithiasis Diseases 0.000 claims description 2
- 208000001130 gallstones Diseases 0.000 claims description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 2
- 208000000509 infertility Diseases 0.000 claims description 2
- 230000036512 infertility Effects 0.000 claims description 2
- 231100000535 infertility Toxicity 0.000 claims description 2
- 206010022437 insomnia Diseases 0.000 claims description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 2
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000002859 sleep apnea Diseases 0.000 claims description 2
- 231100000397 ulcer Toxicity 0.000 claims description 2
- 210000003462 vein Anatomy 0.000 claims description 2
- 230000000155 isotopic effect Effects 0.000 claims 3
- 208000020685 sleep-wake disease Diseases 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000022249 Sleep-Wake Transition disease Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 208000022925 sleep disturbance Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 3
- 108050000742 Orexin Receptor Proteins 0.000 description 2
- 102000008834 Orexin receptor Human genes 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 235000020825 overweight Nutrition 0.000 description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 208000001640 Fibromyalgia Diseases 0.000 description 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 description 1
- 206010026749 Mania Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 208000028683 bipolar I disease Diseases 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 208000021722 neuropathic pain Diseases 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 201000009032 substance abuse Diseases 0.000 description 1
- 231100000736 substance abuse Toxicity 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361780378P | 2013-03-13 | 2013-03-13 | |
| US61/780,378 | 2013-03-13 | ||
| PCT/US2014/024293 WO2014165070A1 (en) | 2013-03-13 | 2014-03-12 | Substituted 2-azabicycles and their use as orexin receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016512535A JP2016512535A (ja) | 2016-04-28 |
| JP2016512535A5 true JP2016512535A5 (enExample) | 2017-04-13 |
| JP6275815B2 JP6275815B2 (ja) | 2018-02-07 |
Family
ID=50487148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501487A Active JP6275815B2 (ja) | 2013-03-13 | 2014-03-12 | 置換２−アザ二環式化合物及びオレキシン受容体調節因子としてのその使用 |
Country Status (38)
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2778484C (en) | 2009-10-23 | 2018-07-31 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| CA2784807C (en) | 2009-12-29 | 2021-12-14 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US9382239B2 (en) | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| KR101920472B1 (ko) | 2014-03-06 | 2019-02-08 | 상하이 하이옌 파마슈티컬 테크놀로지 컴퍼니, 리미티드 | 오렉신 수용체 길항제로서의 피페리딘 유도체 |
| BR112017004742B1 (pt) * | 2014-09-11 | 2022-11-29 | Janssen Pharmaceutica Nv | 2-azabiciclos substituídos e seu uso como moduladores de receptor de orexina |
| US9938276B2 (en) * | 2014-12-19 | 2018-04-10 | Merck Sharp & Dohme Corp. | 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists |
| EP3236959B1 (en) | 2014-12-23 | 2025-09-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10196383B2 (en) | 2015-07-17 | 2019-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| CN107709318B (zh) | 2015-08-14 | 2020-09-25 | 上海海雁医药科技有限公司 | 食欲素受体拮抗剂受体化合物的制备方法及其中间体和晶型 |
| CA2996978A1 (en) | 2015-09-09 | 2017-03-16 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| EP3380475A4 (en) | 2015-11-23 | 2019-07-03 | Sunshine Lake Pharma Co., Ltd. | OCTAHYDROPYRROLO [3,4-C |
| MX2018010852A (es) | 2016-03-10 | 2019-02-07 | Janssen Pharmaceutica Nv | Metodos para tratar la depresion con antagonistas del receptor de orexina-2. |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| PT3730487T (pt) | 2016-06-13 | 2022-07-22 | Gilead Sciences Inc | Derivados de azetidina como moduladores de fxr (nr1h4) |
| CA3041563C (en) | 2016-11-22 | 2023-10-31 | Dana-Farber Cancer Institute, Inc. | Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12) |
| PL4122464T3 (pl) | 2017-03-28 | 2024-09-16 | Gilead Sciences, Inc. | Kombinacje terapeutyczne do leczenia chorób wątroby |
| CN111315734B (zh) | 2017-09-01 | 2024-03-08 | 克罗诺斯治疗有限公司 | 作为食欲素受体拮抗剂的经取代的2-氮杂双环[3.1.1]庚烷和2-氮杂双环[3.2.1]辛烷衍生物 |
| GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
| CA3099763A1 (en) | 2018-06-25 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| WO2020123925A1 (en) * | 2018-12-14 | 2020-06-18 | Dana-Farber Cancer Institute, Inc. | Pyrazolopyridine inhibitors of c-jun-n-terminal kinases and uses thereof |
| US12281126B2 (en) | 2018-12-28 | 2025-04-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| EP3911647B1 (en) | 2019-01-15 | 2023-12-13 | Gilead Sciences, Inc. | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
| AU2020225225B2 (en) | 2019-02-19 | 2022-12-22 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
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| US3674793A (en) | 1967-03-29 | 1972-07-04 | Sterling Drug Inc | 6-hydroxy-2-azabicyclo(2.2.2)octan-3-ones and 2-azabicyclo(2.2.2.)octane-3,6-diones |
| US6505492B2 (en) | 2001-04-11 | 2003-01-14 | Bethlehem Steel Corporation | Method and apparatus for forming deep-drawn articles |
| EP1396488A1 (en) | 2001-05-23 | 2004-03-10 | Mitsubishi Pharma Corporation | Fused heterocyclic compound and medicinal use thereof |
| EP1594852A1 (en) | 2003-02-07 | 2005-11-16 | Ranbaxy Laboratories, Ltd. | Oxazolidinone derivatives as antimicrobials |
| MXPA05008108A (es) | 2003-02-21 | 2005-09-21 | Pharmacia & Upjohn Co Llc | Exo-(2r)(+))-2-amino-7-azabiciclo[2.2.1]heptan-7-carboxilato de terc-butilo, compuestos intermedios y procedimiento para prepararlos y aislarlos. |
| RU2008129622A (ru) | 2005-12-20 | 2010-01-27 | Новартис АГ (CH) | Производные никотиновой кислоты в качестве модуляторов метаботропных глутаматных рецепторов |
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| EA201171293A1 (ru) | 2009-04-24 | 2012-05-30 | Глэксо Груп Лимитед | 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина |
| JP5848251B2 (ja) | 2009-10-23 | 2016-01-27 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節因子としての縮合複素環式化合物 |
| CA2778484C (en) | 2009-10-23 | 2018-07-31 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
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| US8697691B2 (en) | 2009-12-21 | 2014-04-15 | Vanderbilt University | Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective M1 agonists and methods of making and using same |
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| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
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| JP6297582B2 (ja) | 2012-11-16 | 2018-03-20 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ヒトホスファチジルイノシトール３−キナーゼデルタのプリン阻害剤 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| WO2015119998A1 (en) | 2014-02-06 | 2015-08-13 | Abbvie, Inc. | 6-heteroaryloxy- and 6-aryloxy-quinoline-2-carboxamides and uses thereof |
| BR112017004742B1 (pt) | 2014-09-11 | 2022-11-29 | Janssen Pharmaceutica Nv | 2-azabiciclos substituídos e seu uso como moduladores de receptor de orexina |
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2014
- 2014-03-11 TW TW103108293A patent/TWI621618B/zh active
- 2014-03-12 PT PT147175764T patent/PT2970314T/pt unknown
- 2014-03-12 JO JOP/2014/0092A patent/JOP20140092B1/ar active
- 2014-03-12 LT LTEP14717576.4T patent/LT2970314T/lt unknown
- 2014-03-12 ES ES17206491T patent/ES2760564T3/es active Active
- 2014-03-12 RS RS20180158A patent/RS56875B1/sr unknown
- 2014-03-12 HR HRP20180303TT patent/HRP20180303T1/hr unknown
- 2014-03-12 ES ES19193122T patent/ES2950032T3/es active Active
- 2014-03-12 EP EP14717576.4A patent/EP2970314B1/en active Active
- 2014-03-12 PT PT172064917T patent/PT3363438T/pt unknown
- 2014-03-12 US US14/774,555 patent/US9611277B2/en active Active
- 2014-03-12 HU HUE19193122A patent/HUE063608T2/hu unknown
- 2014-03-12 DK DK17206491T patent/DK3363438T3/da active
- 2014-03-12 UA UAA201509932A patent/UA118669C2/uk unknown
- 2014-03-12 EP EP23176328.5A patent/EP4272824A3/en not_active Withdrawn
- 2014-03-12 SI SI201431351T patent/SI3363438T1/sl unknown
- 2014-03-12 EP EP17206491.7A patent/EP3363438B1/en active Active
- 2014-03-12 PE PE2015001954A patent/PE20151599A1/es active IP Right Grant
- 2014-03-12 ME MEP-2018-46A patent/ME03011B/me unknown
- 2014-03-12 SG SG11201507415QA patent/SG11201507415QA/en unknown
- 2014-03-12 SM SM20180056T patent/SMT201800056T1/it unknown
- 2014-03-12 JP JP2016501487A patent/JP6275815B2/ja active Active
- 2014-03-12 MX MX2015011815A patent/MX361529B/es active IP Right Grant
- 2014-03-12 CN CN201810842686.7A patent/CN108864093A/zh active Pending
- 2014-03-12 AU AU2014248680A patent/AU2014248680B2/en active Active
- 2014-03-12 SI SI201430542T patent/SI2970314T1/en unknown
- 2014-03-12 SM SM20190655T patent/SMT201900655T1/it unknown
- 2014-03-12 MX MX2018015165A patent/MX368466B/es unknown
- 2014-03-12 ME MEP-2019-314A patent/ME03572B/me unknown
- 2014-03-12 EP EP19193122.9A patent/EP3622956B9/en active Active
- 2014-03-12 SM SM20230223T patent/SMT202300223T1/it unknown
- 2014-03-12 DK DK14717576.4T patent/DK2970314T3/en active
- 2014-03-12 PL PL17206491T patent/PL3363438T3/pl unknown
- 2014-03-12 RS RS20230703A patent/RS64551B9/sr unknown
- 2014-03-12 CR CR20210523A patent/CR20210523A/es unknown
- 2014-03-12 WO PCT/US2014/024293 patent/WO2014165070A1/en not_active Ceased
- 2014-03-12 LT LT17206491T patent/LT3363438T/lt unknown
- 2014-03-12 PL PL19193122.9T patent/PL3622956T3/pl unknown
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