JP2017526724A5 - - Google Patents
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- Publication number
- JP2017526724A5 JP2017526724A5 JP2017514306A JP2017514306A JP2017526724A5 JP 2017526724 A5 JP2017526724 A5 JP 2017526724A5 JP 2017514306 A JP2017514306 A JP 2017514306A JP 2017514306 A JP2017514306 A JP 2017514306A JP 2017526724 A5 JP2017526724 A5 JP 2017526724A5
- Authority
- JP
- Japan
- Prior art keywords
- chemical entity
- formula
- fluoro
- cyclopropyl
- optionally substituted
- 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
- 150000005829 chemical entities Chemical class 0.000 claims description 47
- 125000001153 fluoro group Chemical group F* 0.000 claims description 16
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 208000035475 disorder Diseases 0.000 claims description 8
- 102000034527 Retinoid X Receptors Human genes 0.000 claims description 6
- 108010038912 Retinoid X Receptors Proteins 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 230000008485 antagonism Effects 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 208000016285 Movement disease Diseases 0.000 claims description 2
- 208000002193 Pain Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 201000009032 substance abuse Diseases 0.000 claims description 2
- 231100000736 substance abuse Toxicity 0.000 claims description 2
- 208000011117 substance-related disease Diseases 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 description 7
- 238000000034 method Methods 0.000 description 4
- 208000037765 diseases and disorders Diseases 0.000 description 3
- 0 *c1c(*)c(*)c(*)c(C(CN(CC2)CCC2N(c2ncnc3c2cc[n]3)N)(F)F)c1 Chemical compound *c1c(*)c(*)c(*)c(C(CN(CC2)CCC2N(c2ncnc3c2cc[n]3)N)(F)F)c1 0.000 description 2
- 239000002464 receptor antagonist Substances 0.000 description 2
- 229940044551 receptor antagonist Drugs 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462050692P | 2014-09-15 | 2014-09-15 | |
| US62/050,692 | 2014-09-15 | ||
| PCT/US2015/050267 WO2016044323A1 (en) | 2014-09-15 | 2015-09-15 | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017526724A JP2017526724A (ja) | 2017-09-14 |
| JP2017526724A5 true JP2017526724A5 (enExample) | 2018-10-25 |
| JP6612331B2 JP6612331B2 (ja) | 2019-11-27 |
Family
ID=54293326
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514306A Active JP6612331B2 (ja) | 2014-09-15 | 2015-09-15 | Ｎｒ２ｂ ｎｍｄａ受容体アンタゴニストとしてのピロロピリミジン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9567341B2 (enExample) |
| EP (1) | EP3194403B1 (enExample) |
| JP (1) | JP6612331B2 (enExample) |
| KR (1) | KR102569031B1 (enExample) |
| CN (1) | CN106715435B (enExample) |
| AU (1) | AU2015317886A1 (enExample) |
| CA (1) | CA2957898C (enExample) |
| DK (1) | DK3194403T3 (enExample) |
| ES (1) | ES2723436T3 (enExample) |
| IL (1) | IL251027A0 (enExample) |
| MX (1) | MX2017002775A (enExample) |
| RU (1) | RU2017107558A (enExample) |
| SG (1) | SG11201701853YA (enExample) |
| WO (1) | WO2016044323A1 (enExample) |
| ZA (1) | ZA201701069B (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股（開曼）有限公司 | 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| MX380424B (es) | 2015-06-01 | 2025-03-12 | Rugen Holdings Cayman Ltd | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
| US10487055B2 (en) | 2016-06-01 | 2019-11-26 | Rhode Island Board Of Education | Diindole compounds useful in treatment of nervous system disorders |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| ES2897050T3 (es) * | 2017-12-08 | 2022-02-28 | Boehringer Ingelheim Int | Derivados de imidazopiridina y el uso de los mismos como medicamento |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
| CN117185897A (zh) * | 2023-08-31 | 2023-12-08 | 上海泰坦科技股份有限公司 | 一种二氟甲基卤苯的合成方法 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ296236B6 (cs) | 1995-08-11 | 2006-02-15 | Pfizer Inc. | Trihydrát methansulfonátu (1S,2S)-1-(4-hydroxyfenyl)-2-(4-hydroxy-4-fenylpiperidin-1-yl)-1-propanolu, farmaceutický prostredek a farmaceutická kombinace s jeho obsahem |
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| HU227197B1 (en) | 2000-10-24 | 2010-10-28 | Richter Gedeon Nyrt | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
| EA005974B1 (ru) * | 2001-02-23 | 2005-08-25 | Мерк Энд Ко., Инк. | N-замещенные неарильные гетероциклические антагонисты nmda/nr2b |
| CA2527093C (en) | 2003-06-04 | 2009-10-20 | Merck & Co., Inc. | 3-fluoro-piperidines as nmda/nr2b antagonists |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| US7452893B2 (en) * | 2003-08-15 | 2008-11-18 | Merck & Co., Inc. | 4-cycloakylaminopyrazolo pyrimidine NMDA/NR2B antagonists |
| WO2005102390A2 (en) | 2004-04-22 | 2005-11-03 | Pfizer Japan, Inc. | Combinations comprising alpha-2-delta ligands and nmda receptor antagonists |
| CN1993363A (zh) | 2004-08-03 | 2007-07-04 | 默克公司 | 1,3－二取代的杂芳基nmda/nr2b拮抗剂 |
| JP2008525486A (ja) | 2004-12-22 | 2008-07-17 | メルク エンド カムパニー インコーポレーテッド | 置換ピペリジンの製造方法 |
| WO2006113471A2 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| CA2614907C (en) * | 2005-07-29 | 2012-02-28 | Pfizer Products Inc. | Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis |
| WO2007061868A2 (en) | 2005-11-17 | 2007-05-31 | Trustees Of Tufts College | Treatment of stereotypic, self-injurious and compulsive behaviors using specific serotonin reuptake inhibitors and antagonists of nmda receptors |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| RU2009128693A (ru) | 2006-12-27 | 2011-02-10 | Санофи-Авентис (Fr) | Замещенные производные изохинолина и изохинолинона |
| WO2010015637A1 (en) | 2008-08-06 | 2010-02-11 | Novartis Ag | New antiviral modified nucleosides |
| EP2519241A2 (en) | 2009-12-28 | 2012-11-07 | Afraxis, Inc. | Methods for treating autism |
| CA2794808C (en) | 2010-04-16 | 2019-08-20 | Ac Immune S.A. | Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
| EP2580213A4 (en) | 2010-06-09 | 2013-12-25 | Afraxis Holdings Inc | 8- (HETEROARYLMETHYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF CNS DISORDERS |
| EP2582374A4 (en) | 2010-06-16 | 2014-03-19 | Afraxis Holdings Inc | METHOD FOR TREATING NERVOUS ELEMENTS |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| US20140005188A1 (en) | 2011-03-11 | 2014-01-02 | Glaxo Group Limited | Pyrido[3,4-b]pyrazine derivatives as syk inhibitors |
| DK2713722T3 (en) | 2011-05-31 | 2017-07-03 | Celgene Int Ii Sarl | Newly known GLP-1 receptor stabilizers and modulators |
| AU2013251079B2 (en) | 2012-04-20 | 2017-03-23 | Ucb Pharma S.A. | Methods for treating Parkinson's disease |
| PE20151436A1 (es) | 2013-01-29 | 2015-10-10 | Naurex Inc | Moduladores de receptores nmda de espiro-lactama y sus usos |
| MX2016014581A (es) | 2014-05-06 | 2018-02-16 | Univ Northwestern | Composiciones de compuestos que modulan nmdar. |
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股（開曼）有限公司 | 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| WO2016049048A1 (en) | 2014-09-22 | 2016-03-31 | Rugen Holdings (Cayman) Limited | Treatment of anxiety disorders and autism spectrum disorders |
| WO2016100349A2 (en) | 2014-12-16 | 2016-06-23 | Rugen Holdings (Cayman) Limited | Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| MX380424B (es) | 2015-06-01 | 2025-03-12 | Rugen Holdings Cayman Ltd | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
-
2015
- 2015-09-15 WO PCT/US2015/050267 patent/WO2016044323A1/en not_active Ceased
- 2015-09-15 US US14/855,010 patent/US9567341B2/en active Active
- 2015-09-15 JP JP2017514306A patent/JP6612331B2/ja active Active
- 2015-09-15 MX MX2017002775A patent/MX2017002775A/es unknown
- 2015-09-15 KR KR1020177010056A patent/KR102569031B1/ko active Active
- 2015-09-15 SG SG11201701853YA patent/SG11201701853YA/en unknown
- 2015-09-15 EP EP15779059.3A patent/EP3194403B1/en active Active
- 2015-09-15 CN CN201580049617.5A patent/CN106715435B/zh active Active
- 2015-09-15 CA CA2957898A patent/CA2957898C/en active Active
- 2015-09-15 AU AU2015317886A patent/AU2015317886A1/en not_active Abandoned
- 2015-09-15 DK DK15779059.3T patent/DK3194403T3/en active
- 2015-09-15 ES ES15779059T patent/ES2723436T3/es active Active
- 2015-09-15 RU RU2017107558A patent/RU2017107558A/ru not_active Application Discontinuation
-
2017
- 2017-02-09 US US15/428,321 patent/US9968610B2/en active Active
- 2017-02-13 ZA ZA2017/01069A patent/ZA201701069B/en unknown
- 2017-03-08 IL IL251027A patent/IL251027A0/en unknown
-
2018
- 2018-04-24 US US15/961,553 patent/US10420768B2/en active Active