JP2012521429A5 - - Google Patents
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- JP2012521429A5 JP2012521429A5 JP2012502098A JP2012502098A JP2012521429A5 JP 2012521429 A5 JP2012521429 A5 JP 2012521429A5 JP 2012502098 A JP2012502098 A JP 2012502098A JP 2012502098 A JP2012502098 A JP 2012502098A JP 2012521429 A5 JP2012521429 A5 JP 2012521429A5
- Authority
- JP
- Japan
- Prior art keywords
- chry
- alkyl
- optionally substituted
- heterocyclyl
- aryl
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 46
- 125000000623 heterocyclic group Chemical group 0.000 claims 26
- 125000003118 aryl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000004076 pyridyl group Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000003226 pyrazolyl group Chemical group 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 7
- 125000003373 pyrazinyl group Chemical group 0.000 claims 7
- 125000001425 triazolyl group Chemical group 0.000 claims 7
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000001041 indolyl group Chemical group 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 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 claims 3
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- -1 (CH 2 ) n CF 3 Chemical group 0.000 claims 2
- 102000012289 Corticotropin-Releasing Hormone Human genes 0.000 claims 2
- 108010022152 Corticotropin-Releasing Hormone Proteins 0.000 claims 2
- 239000000055 Corticotropin-Releasing Hormone Substances 0.000 claims 2
- 101000600903 Homo sapiens Substance-P receptor Proteins 0.000 claims 2
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 claims 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 102100037346 Substance-P receptor Human genes 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000002899 monoamine oxidase inhibitor Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 claims 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims 2
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 1
- 229940121991 Serotonin and norepinephrine reuptake inhibitor Drugs 0.000 claims 1
- 229940089973 Sodium channel antagonist Drugs 0.000 claims 1
- 229940123445 Tricyclic antidepressant Drugs 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 239000000674 adrenergic antagonist Substances 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 102000004305 alpha Adrenergic Receptors Human genes 0.000 claims 1
- 108090000861 alpha Adrenergic Receptors Proteins 0.000 claims 1
- 230000001430 anti-depressive effect Effects 0.000 claims 1
- 239000000935 antidepressant agent Substances 0.000 claims 1
- 229940005513 antidepressants Drugs 0.000 claims 1
- 229940049706 benzodiazepine Drugs 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 229940111134 coxibs Drugs 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 229910052744 lithium Inorganic materials 0.000 claims 1
- 229960001078 lithium Drugs 0.000 claims 1
- 229940072228 neurontin Drugs 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 claims 1
- 229960002748 norepinephrine Drugs 0.000 claims 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 claims 1
- 229940127221 norepinephrine reuptake inhibitor Drugs 0.000 claims 1
- 239000003402 opiate agonist Substances 0.000 claims 1
- 239000003401 opiate antagonist Substances 0.000 claims 1
- 239000004031 partial agonist Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 1
- 229960001233 pregabalin Drugs 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 230000002441 reversible effect Effects 0.000 claims 1
- 239000003195 sodium channel blocking agent Substances 0.000 claims 1
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 claims 1
- 229940102566 valproate Drugs 0.000 claims 1
- 0 *N(*)C(c1ccc2[n](*)nc(*=C)c2c1)O Chemical compound *N(*)C(c1ccc2[n](*)nc(*=C)c2c1)O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21077809P | 2009-03-23 | 2009-03-23 | |
| US61/210,778 | 2009-03-23 | ||
| PCT/US2010/027303 WO2010111060A1 (en) | 2009-03-23 | 2010-03-15 | P2x3, receptor antagonists for treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012521429A JP2012521429A (ja) | 2012-09-13 |
| JP2012521429A5 true JP2012521429A5 (enExample) | 2013-05-02 |
Family
ID=42781387
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012502098A Pending JP2012521429A (ja) | 2009-03-23 | 2010-03-15 | 疼痛治療用のｐ２ｘ３受容体アンタゴニスト |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8569512B2 (enExample) |
| EP (1) | EP2411001B1 (enExample) |
| JP (1) | JP2012521429A (enExample) |
| AU (1) | AU2010229144B2 (enExample) |
| CA (1) | CA2755768A1 (enExample) |
| ES (1) | ES2660892T3 (enExample) |
| WO (1) | WO2010111060A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102430072B1 (ko) | 2013-12-16 | 2022-08-10 | 에이비에스 디벨롭먼트 원 인코포레이티드 | P2x3 및/또는 p2x2/3 화합물 및 방법 |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8946439B2 (en) | 2008-02-29 | 2015-02-03 | Evotec Ag | Amide compounds, compositions and uses thereof |
| US20110237578A1 (en) | 2008-09-18 | 2011-09-29 | Zhi-Liang Wei | Amide compounds, compositions and uses thereof |
| EP2210891A1 (en) * | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
| CA2761921A1 (en) * | 2009-06-22 | 2010-12-29 | F. Hoffmann-La Roche Ag | Indole, indazole and benzimidazole arylamides |
| BR112012002854B1 (pt) | 2009-08-10 | 2020-02-18 | Samumed, Llc | Composto ou sal farmaceuticamente aceitável, composição farmacêutica e uso dos mesmos |
| WO2011084486A1 (en) | 2009-12-21 | 2011-07-14 | Epitherix, Llc | 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| EP2673728B1 (en) | 2011-02-08 | 2018-09-12 | dacadoo ag | System, method and apparatus for the remote analysis of chemical compound microarrays |
| AU2012308570B2 (en) | 2011-09-14 | 2016-11-10 | Samumed, Llc | Indazole-3-carboxamides and their use as Wnt/b-catenin signaling pathway inhibitors |
| WO2013072693A1 (en) * | 2011-11-15 | 2013-05-23 | Xention Limited | Thieno [2, 3 - c] pyrazoles for use as potassium channel inhibitors |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| RU2689141C2 (ru) | 2012-05-04 | 2019-05-24 | СЭМЬЮМЕД, ЭлЭлСи | 1н-пиразоло[3,4-b]пиридины и их терапевтические применения |
| CN105120862A (zh) | 2013-01-08 | 2015-12-02 | 萨穆梅德有限公司 | Wnt信号途径的3-(苯并咪唑-2-基)-吲唑抑制剂及其治疗应用 |
| WO2014127256A1 (en) * | 2013-02-18 | 2014-08-21 | The Trustees Of Columbia University In The City Of New York | Kappa opioid receptor selective compounds |
| EP2905282A1 (en) | 2014-02-05 | 2015-08-12 | AXXAM S.p.A. | Substituted thiazole or oxazole as P2X7 receptor antagonists |
| EP3188731B1 (en) | 2014-09-05 | 2019-04-03 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016036633A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| EP3188730B1 (en) | 2014-09-05 | 2019-05-01 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| EP3954685B1 (en) | 2014-12-29 | 2025-08-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Small molecule inhibitors of lactate dehydrogenase and methods of use thereof |
| KR101663277B1 (ko) * | 2015-03-30 | 2016-10-06 | 주식회사 녹십자 | TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물 |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023996A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US10519169B2 (en) | 2015-08-03 | 2019-12-31 | Samumed, Llc | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10226448B2 (en) | 2015-08-03 | 2019-03-12 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof |
| WO2017023986A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017023989A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017024010A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10188634B2 (en) | 2015-08-03 | 2019-01-29 | Samumed, Llc | 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017023984A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10285982B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10329309B2 (en) | 2015-08-03 | 2019-06-25 | Samumed, Llc | 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017023972A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023975A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10226453B2 (en) | 2015-08-03 | 2019-03-12 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10231956B2 (en) | 2015-08-03 | 2019-03-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10166218B2 (en) | 2015-08-03 | 2019-01-01 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| WO2017028314A1 (en) * | 2015-08-20 | 2017-02-23 | Changzhou Jiekai Pharmatech Co., Ltd. | Pyrazolo fused heterocyclic compounds as erk inhibitors |
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| AR108325A1 (es) | 2016-04-27 | 2018-08-08 | Samumed Llc | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas |
| SG11201810683VA (en) | 2016-06-01 | 2018-12-28 | Samumed Llc | Process for preparing n-(5-(3-(7-(3-fluorophenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide |
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| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
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| CN112574180B (zh) * | 2020-12-30 | 2021-10-15 | 浙江工业大学 | N-2-嘧啶基-3-氟吲哚类化合物及其制备方法与应用 |
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-
2010
- 2010-03-15 ES ES10756588.9T patent/ES2660892T3/es active Active
- 2010-03-15 WO PCT/US2010/027303 patent/WO2010111060A1/en not_active Ceased
- 2010-03-15 CA CA2755768A patent/CA2755768A1/en not_active Abandoned
- 2010-03-15 EP EP10756588.9A patent/EP2411001B1/en active Active
- 2010-03-15 JP JP2012502098A patent/JP2012521429A/ja active Pending
- 2010-03-15 AU AU2010229144A patent/AU2010229144B2/en not_active Ceased
- 2010-03-15 US US13/258,943 patent/US8569512B2/en active Active
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102430072B1 (ko) | 2013-12-16 | 2022-08-10 | 에이비에스 디벨롭먼트 원 인코포레이티드 | P2x3 및/또는 p2x2/3 화합물 및 방법 |
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