JP2018536685A5 - - Google Patents
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- Publication number
- JP2018536685A5 JP2018536685A5 JP2018529995A JP2018529995A JP2018536685A5 JP 2018536685 A5 JP2018536685 A5 JP 2018536685A5 JP 2018529995 A JP2018529995 A JP 2018529995A JP 2018529995 A JP2018529995 A JP 2018529995A JP 2018536685 A5 JP2018536685 A5 JP 2018536685A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- optionally substituted
- halogen
- substituents
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 98
- 229910052736 halogen Inorganic materials 0.000 claims description 80
- 150000002367 halogens Chemical class 0.000 claims description 80
- 125000001424 substituent group Chemical group 0.000 claims description 58
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 46
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 45
- 229910052757 nitrogen Inorganic materials 0.000 claims description 43
- 150000001875 compounds Chemical class 0.000 claims description 40
- 229910052739 hydrogen Inorganic materials 0.000 claims description 37
- 125000003545 alkoxy group Chemical group 0.000 claims description 35
- 229910052799 carbon Inorganic materials 0.000 claims description 32
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
- 125000001072 heteroaryl group Chemical group 0.000 claims description 27
- 239000001257 hydrogen Substances 0.000 claims description 27
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 25
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 20
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000000304 alkynyl group Chemical group 0.000 claims description 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
- 125000003342 alkenyl group Chemical group 0.000 claims description 12
- 125000004043 oxo group Chemical group O=* 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 10
- 125000002950 monocyclic group Chemical group 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 7
- -1 cyano, hydroxyl Chemical group 0.000 claims description 7
- 229910052731 fluorine Inorganic materials 0.000 claims description 7
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 5
- 229910003849 O-Si Inorganic materials 0.000 claims description 4
- 229910003872 O—Si Inorganic materials 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 3
- 208000006289 Rett Syndrome Diseases 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 208000029560 autism spectrum disease Diseases 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 description 16
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 16
- 125000004122 cyclic group Chemical group 0.000 description 3
- 238000000034 method Methods 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 2
- 235000018936 Vitellaria paradoxa Nutrition 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562265182P | 2015-12-09 | 2015-12-09 | |
| US62/265,182 | 2015-12-09 | ||
| PCT/US2016/065852 WO2017100591A1 (en) | 2015-12-09 | 2016-12-09 | Heteroaromatic nmda receptor modulators and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018536685A JP2018536685A (ja) | 2018-12-13 |
| JP2018536685A5 true JP2018536685A5 (enExample) | 2020-01-23 |
| JP7071917B2 JP7071917B2 (ja) | 2022-05-19 |
Family
ID=57681781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018529995A Active JP7071917B2 (ja) | 2015-12-09 | 2016-12-09 | ヘテロ芳香族ｎｍｄａ受容体モジュレーターおよびその使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US10626122B2 (enExample) |
| EP (1) | EP3386591B1 (enExample) |
| JP (1) | JP7071917B2 (enExample) |
| CY (1) | CY1123359T1 (enExample) |
| DK (1) | DK3386591T3 (enExample) |
| ES (1) | ES2821010T3 (enExample) |
| HR (1) | HRP20201522T1 (enExample) |
| HU (1) | HUE051395T2 (enExample) |
| LT (1) | LT3386591T (enExample) |
| PL (1) | PL3386591T3 (enExample) |
| PT (1) | PT3386591T (enExample) |
| RS (1) | RS60834B1 (enExample) |
| SI (1) | SI3386591T1 (enExample) |
| SM (1) | SMT202000534T1 (enExample) |
| WO (1) | WO2017100591A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017100599A1 (en) | 2015-12-09 | 2017-06-15 | Luc Therapeutics | Thienopyrimidinone nmda receptor modulators and uses thereof |
| ES2821010T3 (es) | 2015-12-09 | 2021-04-23 | Cadent Therapeutics Inc | Moduladores heteroaromáticos del receptor NMDA y usos de los mismos |
| AU2017382339B2 (en) | 2016-12-22 | 2024-02-15 | Novartis Ag | NMDA receptor modulators and uses thereof |
| PT3830092T (pt) | 2018-08-03 | 2023-07-25 | Novartis Ag | Moduladores do recetor nmda heteroaromáticos e suas utilizações |
| US11358971B2 (en) * | 2019-07-03 | 2022-06-14 | H. Lundbeck A/S | Prodrugs of modulators of the NMDA receptor |
| IN202011027502A (enExample) * | 2020-06-29 | 2021-12-31 | Council Scient Ind Res | |
| WO2025019109A1 (en) * | 2023-07-17 | 2025-01-23 | Neumora Therapeutics, Inc. | Modulators of nmda receptors and related products and methods |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1067079A (en) | 1976-07-22 | 1979-11-27 | Yamanouchi Pharmaceutical Co. | Nitrogen-containing heterobicyclic compounds |
| FR2549834B1 (fr) | 1983-07-25 | 1985-10-18 | Sanofi Sa | Derives de triazolo-pyrimidine, leur procede de preparation et leur application therapeutique en tant que tonicardiaques |
| US4921854A (en) | 1986-12-30 | 1990-05-01 | Egis Gyogyszergyar | Condensed thiazolopyrimidine, pyrimido-thiazine or thiazepine pyrimidine compounds |
| US5298502A (en) | 1988-12-12 | 1994-03-29 | Fmc Corporation | Method and composition for photodynamic treatment and detection of tumors |
| AU6643694A (en) | 1993-05-21 | 1994-12-20 | Pentapharm Ag | 3-(mercaptoalkyl)- or 3-(alkylthioalkyl)- pyrimidin-2,4(1h, 3h)-diones |
| JP2000513375A (ja) | 1996-06-28 | 2000-10-10 | メルク エンド カンパニー インコーポレーテッド | フィブリノーゲンレセプター拮抗薬プロドラッグ |
| US6339093B1 (en) | 1999-10-08 | 2002-01-15 | Hoffmann-La Roche Inc. | Isoquinoline derivatives |
| WO2002000629A1 (en) | 2000-06-26 | 2002-01-03 | Merck & Co., Inc. | Iminopyrimidine nmda nr2b receptor antagonists |
| US6878743B2 (en) | 2001-09-18 | 2005-04-12 | Sunesis Pharmaceuticals, Inc. | Small molecule inhibitors of caspases |
| AR038118A1 (es) | 2002-01-14 | 2004-12-29 | Upjohn Co | Compuestos derivados de la bencinamida del acido 7-oxo-4,7-dihidrotien[2,3-b[piridin-6-carboxilico 3-sustituido que son utiles como antivirales |
| US7005432B2 (en) | 2002-05-16 | 2006-02-28 | Hoffman-La Roche Inc. | Substituted imidazol-pyridazine derivatives |
| RU2378258C2 (ru) | 2004-07-13 | 2010-01-10 | Ф. Хоффманн-Ля Рош Аг | Производные сульфонамида |
| TW200643015A (en) | 2005-03-11 | 2006-12-16 | Akzo Nobel Nv | 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives |
| US8618115B2 (en) | 2005-10-26 | 2013-12-31 | Bristol-Myers Squibb Company | Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them |
| NZ575426A (en) | 2006-09-11 | 2010-09-30 | Organon Nv | Quinazolinone and isoquinolinone acetamide derivatives useful for the treatment of disorders which are influenced by modulation of the activity of the hpa axis |
| EP2066640B1 (en) * | 2006-09-11 | 2011-09-07 | N.V. Organon | 2-(1-oxo-1h-isoquinolin-2-yl) acetamide derivatives |
| JP5622393B2 (ja) | 2006-12-15 | 2014-11-12 | アブラクシスバイオサイエンス リミテッド ライアビリティー カンパニー | トリアジン誘導体類及びそれらの治療応用 |
| EP1939187A1 (en) | 2006-12-20 | 2008-07-02 | Sanofi-Aventis | Substituted heteroaryl pyridopyrimidone derivatives |
| WO2008097538A1 (en) | 2007-02-08 | 2008-08-14 | Merck & Co., Inc. | Therapeutic agents |
| JP5675341B2 (ja) | 2007-04-18 | 2015-02-25 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオキソキナゾリノン誘導体 |
| WO2008138126A1 (en) | 2007-05-09 | 2008-11-20 | Neuromed Pharmaceuticals Ltd. | Bicyclic pyrimidine derivatives as calcium channel blockers |
| EP2190428A4 (en) | 2007-08-21 | 2012-02-29 | Merck Sharp & Dohme | HETEROCYCLIC COMPOUNDS AS DIPEPTIDYLPEPTIDASE IV HEMMER FOR TREATMENT OR PREVENTION OF DIABETES |
| TW200934497A (en) | 2007-11-13 | 2009-08-16 | Organon Nv | Heterocyclic derivatives |
| AU2009243006B2 (en) | 2008-05-01 | 2013-03-21 | Sirtris Pharmaceuticals, Inc. | Quinolines and related analogs as sirtuin modulators |
| CN102112475A (zh) | 2008-05-29 | 2011-06-29 | 西特里斯药业公司 | 作为沉默调节蛋白调节剂的咪唑并吡啶和相关的类似物 |
| EP2138494A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted alkyl pyrimidin-4-one derivatives |
| BRPI0914006A2 (pt) | 2008-07-03 | 2015-10-27 | Sirtris Pharmaceuticals Inc | benzimidazóis e análogos relacionados como moduladores de sirtuína |
| CN101628913B (zh) | 2008-07-18 | 2013-01-23 | 中国科学院广州生物医药与健康研究院 | 用作雌激素相关受体调节剂的化合物及其应用 |
| CA2738794C (en) | 2008-09-29 | 2016-01-05 | Sirtris Pharmaceuticals, Inc. | Chromenone analogs as sirtuin modulators |
| CA2747419C (en) | 2009-01-12 | 2014-07-08 | Icagen, Inc. | Sulfonamide derivatives |
| WO2010111573A1 (en) | 2009-03-27 | 2010-09-30 | Abbott Laboratories | Compounds as cannabinoid receptor ligands |
| EP2264035A1 (en) | 2009-06-04 | 2010-12-22 | Merz Pharma GmbH & Co. KGaA | Glycine B antagonists |
| TW201116532A (en) | 2009-08-05 | 2011-05-16 | Merz Pharma Gmbh & Co Kgaa | Metabotropic glutamate receptor modulators |
| CN102666540A (zh) * | 2009-10-13 | 2012-09-12 | Msd欧斯股份有限公司 | 用于治疗乙酰胆碱受体相关疾病的稠合吖嗪衍生物 |
| US9290507B2 (en) | 2010-03-26 | 2016-03-22 | Boehringer Ingelheim International Gmbh | B-RAF kinase inhibitors |
| EP2552907B1 (en) | 2010-03-26 | 2014-10-22 | Boehringer Ingelheim International GmbH | Pyridyltriazoles |
| EP2593106A4 (en) | 2010-07-16 | 2014-01-01 | Univ Rockefeller | ORGANIC CONNECTIONS |
| JP2013540145A (ja) | 2010-10-21 | 2013-10-31 | ウニベルシテート デス ザールランデス | コルチゾール依存性疾患の治療用の選択的ｃｙｐ１１ｂ１阻害剤 |
| US20120165330A1 (en) | 2010-12-22 | 2012-06-28 | Sirtris Pharmaceuticals, Inc. | Quinazolinone and related analogs as sirtuin modulators |
| WO2012129562A2 (en) | 2011-03-24 | 2012-09-27 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| WO2012154760A1 (en) | 2011-05-10 | 2012-11-15 | Gilead Sciences, Inc. | Fused heterocyclic compounds as sodium channel modulators |
| WO2013048928A1 (en) | 2011-09-27 | 2013-04-04 | Bristol-Myers Squibb Company | Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors |
| US8946430B2 (en) | 2011-09-30 | 2015-02-03 | Bristol-Myers Squibb Company | Quinolinone carboxamide inhibitors of endothelial lipase |
| US8993557B2 (en) | 2011-09-30 | 2015-03-31 | Bristol-Myers Squibb Company | Pyridinedione carboxamide inhibitors of endothelial lipase |
| CN102336768A (zh) | 2011-10-24 | 2012-02-01 | 中国科学院上海有机化学研究所 | N’-芳亚甲基-2-(4-氧代噻吩[2,3-d]嘧啶-3-基)乙酰腙类化合物、制备方法和用途 |
| MX370976B (es) | 2011-11-11 | 2020-01-10 | Gilead Apollo Llc | Inhibidores de acetil coa carboxilasa (acc) y usos de los mismos. |
| EP3406252B1 (en) | 2012-02-10 | 2020-05-13 | PTC Therapeutics, Inc. | Compounds for treating spinal muscular atrophy |
| WO2014066743A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2014139144A1 (en) | 2013-03-15 | 2014-09-18 | Agios Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
| WO2014179144A1 (en) | 2013-04-29 | 2014-11-06 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic compounds |
| WO2014206343A1 (en) | 2013-06-28 | 2014-12-31 | Beigene, Ltd. | Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors |
| WO2015007453A1 (en) * | 2013-07-15 | 2015-01-22 | Syngenta Participations Ag | Microbiocidal heterobicyclic derivatives |
| TW201609656A (zh) | 2013-09-26 | 2016-03-16 | 美涅莫辛製藥公司 | Ｎｒ２ａ之ｎ-芳基甲基磺醯胺負向調節劑 |
| PT3055315T (pt) | 2013-10-11 | 2018-10-25 | Hoffmann La Roche | Tiazolopirimidonas enquanto moduladores da atividade do recetor nmda |
| WO2015064714A1 (ja) | 2013-10-31 | 2015-05-07 | 国立大学法人東京大学 | オートタキシン阻害活性を有する１－置換イミダゾピリミジノン誘導体 |
| CN103664877A (zh) | 2013-12-25 | 2014-03-26 | 重庆医药工业研究院有限责任公司 | 一种喹啉衍生物、其制备方法和应用 |
| WO2016034703A1 (en) * | 2014-09-05 | 2016-03-10 | AbbVie Deutschland GmbH & Co. KG | Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases |
| WO2016081649A1 (en) | 2014-11-18 | 2016-05-26 | Emory University | Thieno[2,3-d]pyrimidin-4-one derivatives as nmdar modulators and uses related thereto |
| PE20180316A1 (es) | 2015-04-15 | 2018-02-09 | Hoffmann La Roche | Compuestos piridopirimidinona y su uso como moduladores del receptor de nmda |
| KR20180102052A (ko) | 2015-10-16 | 2018-09-14 | 노오쓰웨스턴 유니버시티 | 조현병, 양극성 장애, 인지 손상 및 주요 우울 장애의 치료를 위한 비전형적 항정신병약과 nmda 조절제의 약제학적 병용 |
| ES2821010T3 (es) | 2015-12-09 | 2021-04-23 | Cadent Therapeutics Inc | Moduladores heteroaromáticos del receptor NMDA y usos de los mismos |
| WO2017100599A1 (en) | 2015-12-09 | 2017-06-15 | Luc Therapeutics | Thienopyrimidinone nmda receptor modulators and uses thereof |
| US20170305861A1 (en) | 2016-04-25 | 2017-10-26 | Immunomet Therapeutics, Inc | Heteroaryl compounds comprising nitrogen and use thereof |
| WO2018026371A1 (en) | 2016-08-04 | 2018-02-08 | Sunovion Pharmaceuticals Inc. | Dual nav1.2/5ht2a inhibitors for treating cns disorders |
| AU2017382339B2 (en) | 2016-12-22 | 2024-02-15 | Novartis Ag | NMDA receptor modulators and uses thereof |
| US10633387B2 (en) | 2017-09-27 | 2020-04-28 | Incyte Corporation | Salts of TAM inhibitors |
| US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
| PT3830092T (pt) * | 2018-08-03 | 2023-07-25 | Novartis Ag | Moduladores do recetor nmda heteroaromáticos e suas utilizações |
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2016
- 2016-12-09 ES ES16820103T patent/ES2821010T3/es active Active
- 2016-12-09 SI SI201630931T patent/SI3386591T1/sl unknown
- 2016-12-09 LT LTEP16820103.6T patent/LT3386591T/lt unknown
- 2016-12-09 PL PL16820103.6T patent/PL3386591T3/pl unknown
- 2016-12-09 EP EP16820103.6A patent/EP3386591B1/en active Active
- 2016-12-09 HR HRP20201522TT patent/HRP20201522T1/hr unknown
- 2016-12-09 DK DK16820103.6T patent/DK3386591T3/da active
- 2016-12-09 WO PCT/US2016/065852 patent/WO2017100591A1/en not_active Ceased
- 2016-12-09 SM SM20200534T patent/SMT202000534T1/it unknown
- 2016-12-09 HU HUE16820103A patent/HUE051395T2/hu unknown
- 2016-12-09 RS RS20201142A patent/RS60834B1/sr unknown
- 2016-12-09 PT PT168201036T patent/PT3386591T/pt unknown
- 2016-12-09 JP JP2018529995A patent/JP7071917B2/ja active Active
- 2016-12-09 US US16/060,056 patent/US10626122B2/en active Active
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2020
- 2020-01-31 US US16/779,517 patent/US11236104B2/en active Active
- 2020-09-23 CY CY20201100895T patent/CY1123359T1/el unknown
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2021
- 2021-12-14 US US17/550,435 patent/US12162890B2/en active Active