JP2016512534A5 - - Google Patents
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- Publication number
- JP2016512534A5 JP2016512534A5 JP2016501463A JP2016501463A JP2016512534A5 JP 2016512534 A5 JP2016512534 A5 JP 2016512534A5 JP 2016501463 A JP2016501463 A JP 2016501463A JP 2016501463 A JP2016501463 A JP 2016501463A JP 2016512534 A5 JP2016512534 A5 JP 2016512534A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- halo
- pyrimidinyl
- disorder
- 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 82
- 125000000217 alkyl group Chemical group 0.000 claims description 61
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 33
- 125000001424 substituent group Chemical group 0.000 claims description 26
- 125000001425 triazolyl group Chemical group 0.000 claims description 22
- 125000002971 oxazolyl group Chemical group 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 19
- 125000004385 trihaloalkyl group Chemical group 0.000 claims description 15
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 12
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 11
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 10
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 10
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 10
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 6
- 208000019116 sleep disease Diseases 0.000 claims description 6
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 5
- 206010013654 Drug abuse Diseases 0.000 claims description 4
- 208000019022 Mood 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
- 208000011117 substance-related disease Diseases 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 206010002383 Angina Pectoris Diseases 0.000 claims description 3
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 3
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 3
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims description 3
- 206010020772 Hypertension 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
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 3
- 230000001149 cognitive effect Effects 0.000 claims description 3
- 230000007812 deficiency Effects 0.000 claims description 3
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims description 3
- -1 methyl-oxadiazolyl Chemical group 0.000 claims description 3
- 201000001119 neuropathy Diseases 0.000 claims description 3
- 230000007823 neuropathy Effects 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 208000033808 peripheral neuropathy Diseases 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
- 208000000059 Dyspnea Diseases 0.000 claims description 2
- 206010013975 Dyspnoeas Diseases 0.000 claims description 2
- 201000004311 Gilles de la Tourette syndrome 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
- 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
- 206010003119 arrhythmia Diseases 0.000 claims description 2
- 230000006793 arrhythmia Effects 0.000 claims description 2
- 229910052794 bromium Inorganic materials 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 201000001883 cholelithiasis Diseases 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 208000001130 gallstones Diseases 0.000 claims description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000013220 shortness of breath Diseases 0.000 claims description 2
- 201000002859 sleep apnea Diseases 0.000 claims description 2
- 231100000397 ulcer Toxicity 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 20
- 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
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 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
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 208000022925 sleep disturbance Diseases 0.000 claims 1
- 210000003462 vein Anatomy 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 21
- 238000000034 method Methods 0.000 description 3
- 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 2
- 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
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 208000001640 Fibromyalgia Diseases 0.000 description 1
- 206010026749 Mania Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 206010046996 Varicose vein Diseases 0.000 description 1
- 208000028683 bipolar I disease Diseases 0.000 description 1
- 125000006389 halopyrimidinyl group Chemical group 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
- 208000011580 syndromic disease Diseases 0.000 description 1
- 208000027185 varicose disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361780302P | 2013-03-13 | 2013-03-13 | |
| US61/780,302 | 2013-03-13 | ||
| PCT/US2014/024284 WO2014165065A1 (en) | 2013-03-13 | 2014-03-12 | Substituted piperidine compounds and their use as orexin receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016512534A JP2016512534A (ja) | 2016-04-28 |
| JP2016512534A5 true JP2016512534A5 (OSRAM) | 2017-04-13 |
| JP6275814B2 JP6275814B2 (ja) | 2018-02-07 |
Family
ID=50842314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501463A Active JP6275814B2 (ja) | 2013-03-13 | 2014-03-12 | 置換ピペリジン化合物及びこれらのオレキシン受容体調節因子としての使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US9115117B2 (OSRAM) |
| EP (1) | EP2970207B1 (OSRAM) |
| JP (1) | JP6275814B2 (OSRAM) |
| CN (1) | CN105228995B (OSRAM) |
| AR (1) | AR095422A1 (OSRAM) |
| AU (2) | AU2014248763B2 (OSRAM) |
| TW (1) | TW201444821A (OSRAM) |
| UY (1) | UY35410A (OSRAM) |
| WO (1) | WO2014165065A1 (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2519517B1 (en) | 2009-12-29 | 2015-03-25 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| WO2016095204A1 (en) | 2014-12-19 | 2016-06-23 | Merck Sharp & Dohme Corp. | Pyrrolidine orexin receptor antagonists |
| WO2016105528A2 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| US10196383B2 (en) | 2015-07-17 | 2019-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| AU2016360245B2 (en) | 2015-11-23 | 2020-07-09 | Sunshine Lake Pharma Co., Ltd. | Octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof |
| GB201601703D0 (en) * | 2016-01-29 | 2016-03-16 | C4X Discovery Ltd | Therapeutic compounds |
| US10899734B2 (en) * | 2016-06-23 | 2021-01-26 | St. Jude Children's Research Hospital, Inc. | Small molecule modulators of pantothenate kinases |
| CN106045902A (zh) * | 2016-06-30 | 2016-10-26 | 苏州健雄职业技术学院 | 一种3‑溴‑6‑甲基‑2‑吡啶甲醛的制备方法 |
| JP7258748B2 (ja) | 2016-11-22 | 2023-04-17 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ１２（ｃｄｋ１２）の阻害剤およびその使用 |
| RS62357B1 (sr) | 2017-05-03 | 2021-10-29 | Idorsia Pharmaceuticals Ltd | Dobijanje derivata 2-([1,2,3]triazol-2-il)-benzojeve kiseline |
| IL275658B2 (en) | 2017-12-27 | 2024-04-01 | St Jude Childrens Res Hospital Inc | Small molecule modulators of pantothenate kinases |
| EP3731859B1 (en) | 2017-12-27 | 2025-08-20 | St. Jude Children's Research Hospital, Inc. | Pyridazine compounds for use to treat disorders associated with castor |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| CA3124422A1 (en) | 2018-12-28 | 2020-07-02 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| WO2020198526A2 (en) | 2019-03-27 | 2020-10-01 | St. Jude Children's Research Hospital | Small molecule modulators of pank |
| WO2024148210A1 (en) * | 2023-01-05 | 2024-07-11 | Allianthera (Suzhou) Biopharmaceutical Co., Ltd. | Cyclin-dependent kinase 12 modulators and therapeutic uses thereof |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2003202753A1 (en) | 2003-02-07 | 2004-08-30 | Ranbaxy Laboratories Limited | Oxazolidinone derivatives as antimicrobials |
| JP2006518367A (ja) | 2003-02-21 | 2006-08-10 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | エキソ−（ｔ−ブチル２Ｒ（＋））−２−アミノ−７−アザビシクロ［２．２．１］ヘプタン−７−カルボキシレート、中間体、およびそれらを製造および単離する方法 |
| AR058554A1 (es) | 2005-12-20 | 2008-02-13 | Novartis Ag | Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5. |
| AU2007296964B2 (en) | 2006-09-11 | 2012-05-31 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutanate receptors |
| DE602007012142D1 (en) | 2006-12-01 | 2011-03-03 | Actelion Pharmaceuticals Ltd | 3-heteroaryl (amino bzw. amido)-1- (biphenyl bzw. phenylthiazolyl) carbonylpiperdinderivate als orexinrezeptor-inhibitoren |
| CL2007003827A1 (es) | 2006-12-28 | 2008-09-26 | Actelion Pharmaceuticals Ltd | Compuestos derivados de n-(2-aza-biciclo(3.1.0)hex-3-ilmetil)amida; y su uso para prevenir o tratar la depresion, neurosis, esquizofrenia, ansiedad, adicciones, epilepsia, dolor, enfermedades cardiacas, entre otras. |
| AU2008260647A1 (en) | 2007-05-23 | 2008-12-11 | Merck Sharp & Dohme Corp. | Cyclopropyl pyrrolidine orexin receptor antagonists |
| JP5318867B2 (ja) | 2007-07-17 | 2013-10-16 | ブリストル−マイヤーズ スクイブ カンパニー | ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト |
| BRPI0821141A2 (pt) * | 2007-12-21 | 2015-06-16 | Hoffmann La Roche | Derivados de heteroarila como antagonistas do receptor de orexina |
| ATE555107T1 (de) | 2008-02-21 | 2012-05-15 | Actelion Pharmaceuticals Ltd | 2-aza-bicyclo-ä2,2,1-üheptan-derivate |
| KR20100135962A (ko) * | 2008-04-30 | 2010-12-27 | 액테리온 파마슈티칼 리미티드 | 피페리딘 및 피롤리딘 화합물 |
| JP2011528365A (ja) | 2008-07-16 | 2011-11-17 | シェーリング コーポレイション | Ｇｐｒ１１９モジュレーターとしての二環式ヘテロ環誘導体およびそれらの使用方法 |
| CA2740190A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| EP2349269A4 (en) | 2008-10-21 | 2012-04-25 | Merck Sharp & Dohme | 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS |
| EP2370426A1 (en) | 2008-12-02 | 2011-10-05 | Glaxo Group Limited | N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and uses thereof |
| 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 |
| SI2491038T1 (sl) | 2009-10-23 | 2016-08-31 | Janssen Pharmaceutica N.V. | Disubstituirani oktahil-dropirolo(3,4-c)piroli kot modulatorji oreksinskega receptorja |
| 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 |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| WO2011053688A1 (en) | 2009-10-29 | 2011-05-05 | Schering Corporation | Bridged bicyclic piperidine derivatives and methods of use thereof |
| US9301929B2 (en) | 2009-11-24 | 2016-04-05 | Merck Sharp & Dohme Corp. | Substituted biaryl derivatives and methods of use thereof |
| AU2010332010A1 (en) | 2009-12-14 | 2012-08-02 | Inspire Pharmaceuticals, Inc. | Bridged bicyclic Rho kinase inhibitor compounds, composition and use |
| 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 |
| UY33227A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de la cdk4/6 |
| US20130096141A1 (en) | 2010-06-18 | 2013-04-18 | Bernard R. Neustadt | Bicyclic heterocycle derivatives and methods of use thereof |
| WO2012089606A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists |
| WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| EP2911675A4 (en) * | 2012-10-23 | 2016-06-01 | Merck Sharp & Dohme | 2-PYRIDYLOXY-3-SUBSTITUTED 4-NITRIL-OREXINE RECEPTOR ANTAGONISTS |
| CA2891009A1 (en) | 2012-11-16 | 2014-05-22 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| 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 |
| MX2016010056A (es) | 2014-02-06 | 2016-11-15 | Abbvie Inc | 6-heteroariloxi o 6-ariloxi-quinolina-2-carboxamidas y metodos de uso. |
-
2014
- 2014-03-11 TW TW103108298A patent/TW201444821A/zh unknown
- 2014-03-12 CN CN201480027361.3A patent/CN105228995B/zh active Active
- 2014-03-12 AU AU2014248763A patent/AU2014248763B2/en active Active
- 2014-03-12 US US14/206,662 patent/US9115117B2/en active Active
- 2014-03-12 WO PCT/US2014/024284 patent/WO2014165065A1/en not_active Ceased
- 2014-03-12 JP JP2016501463A patent/JP6275814B2/ja active Active
- 2014-03-12 EP EP14727268.6A patent/EP2970207B1/en active Active
- 2014-03-12 US US14/774,529 patent/US9611251B2/en active Active
- 2014-03-13 UY UY0001035410A patent/UY35410A/es unknown
- 2014-03-13 AR ARP140100966A patent/AR095422A1/es unknown
-
2018
- 2018-09-12 AU AU2018229449A patent/AU2018229449A1/en not_active Abandoned
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