JP2016512536A5 - - Google Patents
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- JP2016512536A5 JP2016512536A5 JP2016501497A JP2016501497A JP2016512536A5 JP 2016512536 A5 JP2016512536 A5 JP 2016512536A5 JP 2016501497 A JP2016501497 A JP 2016501497A JP 2016501497 A JP2016501497 A JP 2016501497A JP 2016512536 A5 JP2016512536 A5 JP 2016512536A5
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- Japan
- Prior art keywords
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- halogen
- alkoxy
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 120
- 125000000217 alkyl group Chemical group 0.000 claims description 46
- 125000003545 alkoxy group Chemical group 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 32
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 30
- 125000004076 pyridyl group Chemical group 0.000 claims description 30
- 150000002367 halogens Chemical class 0.000 claims description 27
- -1 imidazothiazolyl Chemical group 0.000 claims description 27
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 25
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 25
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 19
- 125000002971 oxazolyl group Chemical group 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 125000001544 thienyl group Chemical group 0.000 claims description 16
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 15
- 125000001425 triazolyl group Chemical group 0.000 claims description 15
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 14
- 208000035475 disorder Diseases 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 11
- 125000002757 morpholinyl group Chemical group 0.000 claims description 11
- 125000004193 piperazinyl group Chemical group 0.000 claims description 11
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 208000019116 sleep disease Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 7
- 208000020685 sleep-wake disease Diseases 0.000 claims description 7
- 125000000335 thiazolyl group Chemical group 0.000 claims description 7
- 206010013654 Drug abuse Diseases 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 6
- 208000010877 cognitive disease Diseases 0.000 claims description 6
- 208000019906 panic disease Diseases 0.000 claims description 6
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 6
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 6
- 208000011117 substance-related disease Diseases 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 206010002383 Angina Pectoris Diseases 0.000 claims description 5
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 5
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 206010033307 Overweight Diseases 0.000 claims description 5
- 208000001871 Tachycardia Diseases 0.000 claims description 5
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 5
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims description 5
- 230000006794 tachycardia Effects 0.000 claims description 5
- 208000019022 Mood disease Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 125000005599 alkyl carboxylate group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 201000001119 neuropathy Diseases 0.000 claims description 4
- 230000007823 neuropathy Effects 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 4
- 125000004385 trihaloalkyl group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 208000006820 Arthralgia Diseases 0.000 claims description 3
- 208000008035 Back Pain Diseases 0.000 claims description 3
- 206010007556 Cardiac failure acute Diseases 0.000 claims description 3
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims description 3
- 206010012218 Delirium Diseases 0.000 claims description 3
- 206010012289 Dementia Diseases 0.000 claims description 3
- 206010012735 Diarrhoea Diseases 0.000 claims description 3
- 208000000059 Dyspnea Diseases 0.000 claims description 3
- 206010013975 Dyspnoeas Diseases 0.000 claims description 3
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 3
- 206010022489 Insulin Resistance Diseases 0.000 claims description 3
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 208000005793 Restless legs syndrome Diseases 0.000 claims description 3
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 3
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 3
- 208000016620 Tourette disease Diseases 0.000 claims description 3
- 208000025865 Ulcer Diseases 0.000 claims description 3
- 239000000654 additive Substances 0.000 claims description 3
- 230000000996 additive effect Effects 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 201000001883 cholelithiasis Diseases 0.000 claims description 3
- 125000002541 furyl group Chemical group 0.000 claims description 3
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 3
- 125000005945 imidazopyridyl group Chemical group 0.000 claims description 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 3
- 208000000509 infertility Diseases 0.000 claims description 3
- 230000036512 infertility Effects 0.000 claims description 3
- 231100000535 infertility Toxicity 0.000 claims description 3
- 206010022437 insomnia Diseases 0.000 claims description 3
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 3
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 3
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims description 3
- 201000008482 osteoarthritis Diseases 0.000 claims description 3
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 3
- 208000013220 shortness of breath Diseases 0.000 claims description 3
- 201000002859 sleep apnea Diseases 0.000 claims description 3
- 231100000397 ulcer Toxicity 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims 8
- 125000004429 atom Chemical group 0.000 claims 3
- 230000000155 isotopic effect Effects 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
- 206010002329 Aneurysm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000022249 Sleep-Wake Transition disease Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000022925 sleep disturbance Diseases 0.000 claims 1
- 210000003462 vein Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 description 8
- 108050000742 Orexin Receptor Proteins 0.000 description 4
- 102000008834 Orexin receptor Human genes 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 230000001404 mediated effect Effects 0.000 description 4
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 4
- 125000004438 haloalkoxy group Chemical group 0.000 description 3
- 125000006384 methylpyridyl group Chemical group 0.000 description 3
- 208000020925 Bipolar disease Diseases 0.000 description 2
- 208000001640 Fibromyalgia Diseases 0.000 description 2
- 206010026749 Mania Diseases 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- 206010046996 Varicose vein Diseases 0.000 description 2
- 208000028683 bipolar I disease Diseases 0.000 description 2
- 208000004296 neuralgia Diseases 0.000 description 2
- 208000021722 neuropathic pain Diseases 0.000 description 2
- 235000020825 overweight Nutrition 0.000 description 2
- 201000000980 schizophrenia Diseases 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 208000027185 varicose disease Diseases 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
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361780428P | 2013-03-13 | 2013-03-13 | |
| US61/780,428 | 2013-03-13 | ||
| PCT/US2014/024322 WO2014159591A1 (en) | 2013-03-13 | 2014-03-12 | Substituted 7-azabicycles and their use as orexin receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016512536A JP2016512536A (ja) | 2016-04-28 |
| JP2016512536A5 true JP2016512536A5 (enExample) | 2017-04-13 |
| JP6337082B2 JP6337082B2 (ja) | 2018-06-06 |
Family
ID=50483527
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501497A Active JP6337082B2 (ja) | 2013-03-13 | 2014-03-12 | 置換した７−アザビシクル及びオレキシン受容体調節因子としてのそれらの使用 |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US9637496B2 (enExample) |
| EP (1) | EP2970313B1 (enExample) |
| JP (1) | JP6337082B2 (enExample) |
| KR (1) | KR102209432B1 (enExample) |
| CN (1) | CN105209468B (enExample) |
| AR (1) | AR095424A1 (enExample) |
| AU (2) | AU2014240388B2 (enExample) |
| BR (1) | BR112015022058A2 (enExample) |
| CA (1) | CA2905012C (enExample) |
| CL (1) | CL2015002616A1 (enExample) |
| CR (1) | CR20150434A (enExample) |
| EA (1) | EA028386B1 (enExample) |
| ES (1) | ES2659222T3 (enExample) |
| IL (1) | IL240929B (enExample) |
| MX (1) | MX360791B (enExample) |
| NI (1) | NI201500129A (enExample) |
| PE (1) | PE20151668A1 (enExample) |
| PH (1) | PH12015502030A1 (enExample) |
| SG (1) | SG11201507431UA (enExample) |
| TW (1) | TW201444849A (enExample) |
| UA (1) | UA116132C2 (enExample) |
| UY (1) | UY35408A (enExample) |
| WO (1) | WO2014159591A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| MX384432B (es) | 2014-06-27 | 2025-03-14 | Asc Eng Solutions Llc | Abrazadera ajustable y cubo para soporte de manguera flexible. |
| GB201415569D0 (en) | 2014-09-03 | 2014-10-15 | C4X Discovery Ltd | Therapeutic Compounds |
| BR112017004742B1 (pt) * | 2014-09-11 | 2022-11-29 | Janssen Pharmaceutica Nv | 2-azabiciclos substituídos e seu uso como moduladores de receptor de orexina |
| 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 |
| US10040795B2 (en) * | 2015-09-04 | 2018-08-07 | Janssen Pharmaceutica Nv | Therapeutic compounds for pain and synthesis thereof |
| GB201601703D0 (en) * | 2016-01-29 | 2016-03-16 | C4X Discovery Ltd | Therapeutic compounds |
| CA3059394C (en) * | 2017-05-03 | 2023-09-12 | Idorsia Pharmaceuticals Ltd | Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives |
| IL300063B2 (en) * | 2017-08-03 | 2024-02-01 | Takeda Pharmaceuticals Co | Methanesulfonamide and its use for the prevention or treatment of narcolepsy |
| CN107573294A (zh) * | 2017-09-19 | 2018-01-12 | 四川大学 | 5‑甲基‑2‑(2h‑1,2,3‑三唑‑2‑基)苯甲酸的合成方法 |
| GB201906914D0 (en) | 2019-05-16 | 2019-07-03 | Ucl Business Plc | Substituted naphtahlene diimdes and their use |
| EP3972588A4 (en) * | 2019-06-04 | 2023-05-31 | Hager Biosciences, LLC | IMIDAZOL DERIVATIVES, COMPOSITIONS AND METHODS AS OREXIN ANTAGONISTS |
| CA3174409A1 (en) * | 2020-04-17 | 2021-10-21 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Solid pharmaceutical preparation, preparation method therefor and use thereof |
| PE20231103A1 (es) * | 2020-07-17 | 2023-07-19 | Eisai Randd Man Co Ltd | Compuestos de piperidina sustituida y su uso |
| JP7591592B2 (ja) * | 2022-01-14 | 2024-11-28 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 置換ピペリジン化合物を含有する医薬 |
| KR20240134870A (ko) * | 2022-01-14 | 2024-09-10 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 치환된 피페리딘 화합물의 결정, 치환된 피페리딘 화합물의 염, 및 이의 결정 |
| ES3038762A1 (es) * | 2024-04-12 | 2025-10-14 | Moehs Iberica Sl | Procedimiento de síntesis de ácido 5-metoxi-2-(2H-1,2,3-triazol-2yl)benzoico, sal sódica de dicho ácido como intermedio de síntesis y uso del ácido o de su sal en la preparación de daridorexant y ciertos intermedios en la síntesis del mismo |
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| 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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| US8030495B2 (en) * | 2007-05-23 | 2011-10-04 | Coleman Paul J | Cyclopropyl pyrrolidine orexin receptor antagonists |
| CN101801956B (zh) | 2007-07-17 | 2013-11-20 | 百时美施贵宝公司 | 用于调节gpr119 g蛋白偶联受体的方法及所选化合物 |
| BRPI0821141A2 (pt) | 2007-12-21 | 2015-06-16 | Hoffmann La Roche | Derivados de heteroarila como antagonistas do receptor de orexina |
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| DE102009015516A1 (de) | 2009-04-02 | 2010-10-07 | Mediri Gmbh | Verfahren und Vorrichtung zur Ermittlung von T2 und T2* mittels Magnet- Resonanz-Tomographie |
| AR076024A1 (es) | 2009-04-03 | 2011-05-11 | Schering Corp | Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos |
| EA201171293A1 (ru) | 2009-04-24 | 2012-05-30 | Глэксо Груп Лимитед | 3-азабицикло[4.1.0]гептаны, применяемые в качестве антагонистов орексина |
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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 |
-
2014
- 2014-03-11 TW TW103108292A patent/TW201444849A/zh unknown
- 2014-03-12 AU AU2014240388A patent/AU2014240388B2/en active Active
- 2014-03-12 CA CA2905012A patent/CA2905012C/en active Active
- 2014-03-12 JP JP2016501497A patent/JP6337082B2/ja active Active
- 2014-03-12 ES ES14717297.7T patent/ES2659222T3/es active Active
- 2014-03-12 US US14/774,554 patent/US9637496B2/en active Active
- 2014-03-12 SG SG11201507431UA patent/SG11201507431UA/en unknown
- 2014-03-12 UA UAA201510021A patent/UA116132C2/uk unknown
- 2014-03-12 KR KR1020157028726A patent/KR102209432B1/ko active Active
- 2014-03-12 WO PCT/US2014/024322 patent/WO2014159591A1/en not_active Ceased
- 2014-03-12 CN CN201480027442.3A patent/CN105209468B/zh active Active
- 2014-03-12 EA EA201591675A patent/EA028386B1/ru not_active IP Right Cessation
- 2014-03-12 BR BR112015022058A patent/BR112015022058A2/pt not_active IP Right Cessation
- 2014-03-12 PE PE2015001941A patent/PE20151668A1/es not_active Application Discontinuation
- 2014-03-12 EP EP14717297.7A patent/EP2970313B1/en active Active
- 2014-03-12 MX MX2015011816A patent/MX360791B/es active IP Right Grant
- 2014-03-12 US US14/206,764 patent/US9062078B2/en active Active
- 2014-03-13 AR ARP140100968A patent/AR095424A1/es unknown
- 2014-03-13 UY UY0001035408A patent/UY35408A/es unknown
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2015
- 2015-05-21 US US14/718,327 patent/US9475819B2/en active Active
- 2015-08-24 CR CR20150434A patent/CR20150434A/es unknown
- 2015-08-31 IL IL240929A patent/IL240929B/en active IP Right Grant
- 2015-09-10 PH PH12015502030A patent/PH12015502030A1/en unknown
- 2015-09-10 NI NI201500129A patent/NI201500129A/es unknown
- 2015-09-11 CL CL2015002616A patent/CL2015002616A1/es unknown
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2016
- 2016-09-12 US US15/262,882 patent/US9695183B2/en active Active
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2018
- 2018-10-24 AU AU2018253525A patent/AU2018253525A1/en not_active Abandoned
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