JP2011519913A5 - - Google Patents
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- Publication number
- JP2011519913A5 JP2011519913A5 JP2011508035A JP2011508035A JP2011519913A5 JP 2011519913 A5 JP2011519913 A5 JP 2011519913A5 JP 2011508035 A JP2011508035 A JP 2011508035A JP 2011508035 A JP2011508035 A JP 2011508035A JP 2011519913 A5 JP2011519913 A5 JP 2011519913A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- triazaspiro
- thia
- fluorophenyl
- dioxide
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 11
- DIOQZVSQGTUSAI-UHFFFAOYSA-N decane Chemical compound CCCCCCCCCC DIOQZVSQGTUSAI-UHFFFAOYSA-N 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- -1 cyano, amino Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- UZWOFKFOTAZIFO-RBISFHTESA-N (5r,7s)-1-(3-fluorophenyl)-7-methyl-8-[(3-propan-2-yloxyphenyl)methyl]-3-(pyrimidin-2-ylmethyl)-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound CC(C)OC1=CC=CC(CN2[C@H](C[C@]3(N(S(=O)(=O)N(CC=4N=CC=CN=4)C3)C=3C=C(F)C=CC=3)CC2)C)=C1 UZWOFKFOTAZIFO-RBISFHTESA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- ZXOHUCGZHMGSOU-RBISFHTESA-N (5r,7s)-1-(3-fluorophenyl)-3,7-dimethyl-8-[[3-(2-methylphenyl)phenyl]methyl]-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC=2C=C(C=CC=2)C=2C(=CC=CC=2)C)C)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 ZXOHUCGZHMGSOU-RBISFHTESA-N 0.000 claims 1
- KZUCNHLHFYXYIH-OYHNWAKOSA-N (5r,7s)-1-(3-fluorophenyl)-3,7-dimethyl-8-[[3-(trifluoromethyl)-2h-indazol-5-yl]methyl]-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC=2C=C3C(=NNC3=CC=2)C(F)(F)F)C)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 KZUCNHLHFYXYIH-OYHNWAKOSA-N 0.000 claims 1
- FBKPLPCTJVWUBC-AFJIDDCJSA-N (5r,7s)-1-(3-fluorophenyl)-3,7-dimethyl-8-[[3-[(2-methyl-1,3-benzoxazol-6-yl)oxy]phenyl]methyl]-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC=2C=C(OC=3C=C4OC(C)=NC4=CC=3)C=CC=2)C)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 FBKPLPCTJVWUBC-AFJIDDCJSA-N 0.000 claims 1
- CYNJHNQWUQFBEA-FDDCHVKYSA-N (5r,7s)-1-(3-fluorophenyl)-7-methyl-8-[(3-propan-2-yloxyphenyl)methyl]-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound CC(C)OC1=CC=CC(CN2[C@H](C[C@]3(N(S(=O)(=O)NC3)C=3C=C(F)C=CC=3)CC2)C)=C1 CYNJHNQWUQFBEA-FDDCHVKYSA-N 0.000 claims 1
- QSOLHUVFBJBRHK-MUAVYFROSA-N (5r,7s)-1-(3-fluorophenyl)-7-methyl-8-[(3-propan-2-yloxyphenyl)methyl]-3-(pyridin-2-ylmethyl)-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound CC(C)OC1=CC=CC(CN2[C@H](C[C@]3(N(S(=O)(=O)N(CC=4N=CC=CC=4)C3)C=3C=C(F)C=CC=3)CC2)C)=C1 QSOLHUVFBJBRHK-MUAVYFROSA-N 0.000 claims 1
- CPNYKYVZIZDRFM-KDYSTLNUSA-N (5r,7s)-1-(3-fluorophenyl)-7-methyl-8-[(3-propan-2-yloxyphenyl)methyl]-3-pyrimidin-2-yl-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound CC(C)OC1=CC=CC(CN2[C@H](C[C@]3(N(S(=O)(=O)N(C=4N=CC=CN=4)C3)C=3C=C(F)C=CC=3)CC2)C)=C1 CPNYKYVZIZDRFM-KDYSTLNUSA-N 0.000 claims 1
- DWJUVHMOGMDYRQ-RXFWQSSRSA-N (5r,7s)-1-(3-fluorophenyl)-7-methyl-8-[[3-(4-methylpyridin-3-yl)phenyl]methyl]-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC=2C=C(C=CC=2)C=2C(=CC=NC=2)C)C)NS(=O)(=O)N1C1=CC=CC(F)=C1 DWJUVHMOGMDYRQ-RXFWQSSRSA-N 0.000 claims 1
- FUWIMDVZJVRXTN-BXKMTCNYSA-N (5r,7s)-8-[(3-ethyl-2h-indazol-5-yl)methyl]-1-(3-fluorophenyl)-3,7-dimethyl-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@]12CCN([C@H](C2)C)CC2=CC=C3NN=C(C3=C2)CC)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 FUWIMDVZJVRXTN-BXKMTCNYSA-N 0.000 claims 1
- OSYQGIYTQMJNJN-XLNZFTOWSA-N (5r,7s)-8-[[3-[(2r)-butan-2-yl]oxyphenyl]methyl]-1-(3-fluorophenyl)-7-methyl-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound CC[C@@H](C)OC1=CC=CC(CN2[C@H](C[C@]3(N(S(=O)(=O)NC3)C=3C=C(F)C=CC=3)CC2)C)=C1 OSYQGIYTQMJNJN-XLNZFTOWSA-N 0.000 claims 1
- IEUIEHMFISIHRH-GAJHUEQPSA-N (5r,7s)-8-[[4-(cyclobutylmethyl)-1,3-thiazol-5-yl]methyl]-1-(3-fluorophenyl)-3,7-dimethyl-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC2=C(N=CS2)CC2CCC2)C)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 IEUIEHMFISIHRH-GAJHUEQPSA-N 0.000 claims 1
- ZQJULPZFMZOSLA-KSFYIVLOSA-N (5r,7s)-8-[[4-(cyclopropylmethyl)-1,3-thiazol-5-yl]methyl]-1-(3-fluorophenyl)-3,7-dimethyl-2$l^{6}-thia-1,3,8-triazaspiro[4.5]decane 2,2-dioxide Chemical compound C([C@@]12C[C@@H](N(CC2)CC2=C(N=CS2)CC2CC2)C)N(C)S(=O)(=O)N1C1=CC=CC(F)=C1 ZQJULPZFMZOSLA-KSFYIVLOSA-N 0.000 claims 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 239000003693 atypical antipsychotic agent Substances 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 1
- JNODQFNWMXFMEV-UHFFFAOYSA-N latrepirdine Chemical compound C1N(C)CCC2=C1C1=CC(C)=CC=C1N2CCC1=CC=C(C)N=C1 JNODQFNWMXFMEV-UHFFFAOYSA-N 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 1
- 230000000926 neurological effect Effects 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
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5042308P | 2008-05-05 | 2008-05-05 | |
| US61/050,423 | 2008-05-05 | ||
| PCT/IB2009/051815 WO2009136350A1 (en) | 2008-05-05 | 2009-05-04 | Novel class of spiro piperidines for the treatment of neurodegenerative diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011519913A JP2011519913A (ja) | 2011-07-14 |
| JP2011519913A5 true JP2011519913A5 (https=) | 2012-04-26 |
Family
ID=40902870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011508035A Withdrawn JP2011519913A (ja) | 2008-05-05 | 2009-05-04 | 神経変性疾患治療のための新規なクラスのスピロピペリジン |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20110046160A1 (https=) |
| EP (1) | EP2300484B1 (https=) |
| JP (1) | JP2011519913A (https=) |
| KR (1) | KR20110000749A (https=) |
| CN (1) | CN102083841A (https=) |
| AP (1) | AP2010005456A0 (https=) |
| AT (1) | ATE537178T1 (https=) |
| AU (1) | AU2009245322B2 (https=) |
| BR (1) | BRPI0912433A2 (https=) |
| CA (1) | CA2721786A1 (https=) |
| CO (1) | CO6321280A2 (https=) |
| CR (1) | CR11759A (https=) |
| DO (1) | DOP2010000317A (https=) |
| EA (1) | EA201001566A1 (https=) |
| EC (1) | ECSP10010597A (https=) |
| ES (1) | ES2375913T3 (https=) |
| IL (1) | IL208793A0 (https=) |
| MA (1) | MA32290B1 (https=) |
| MX (1) | MX2010012066A (https=) |
| NZ (1) | NZ588589A (https=) |
| SV (1) | SV2010003725A (https=) |
| WO (1) | WO2009136350A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| EP2556076A2 (en) * | 2010-04-09 | 2013-02-13 | Pfizer Inc. | Novel sultam compounds |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| US10752588B2 (en) | 2014-12-19 | 2020-08-25 | The Broad Institute, Inc. | Dopamine D2 receptor ligands |
| WO2016100940A1 (en) | 2014-12-19 | 2016-06-23 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1720873B1 (en) * | 2004-01-08 | 2011-02-23 | F. Hoffmann-La Roche AG | Diaza-spiropiperidine derivatives |
| JP2006044497A (ja) * | 2004-08-05 | 2006-02-16 | Toyota Motor Corp | 車輪情報処理装置 |
| US8114887B2 (en) * | 2004-10-13 | 2012-02-14 | Merck, Sharp & Dohme Corp. | Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| JP2009502786A (ja) * | 2005-07-18 | 2009-01-29 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病を治療するためのスピロピペリジンβ−セクレターゼ阻害剤 |
| US20100298342A1 (en) * | 2006-09-07 | 2010-11-25 | Merck & Co., Inc. | Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease |
| CA2673888A1 (en) * | 2007-01-04 | 2008-07-17 | Merck And Co., Inc. | Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
-
2009
- 2009-05-04 JP JP2011508035A patent/JP2011519913A/ja not_active Withdrawn
- 2009-05-04 WO PCT/IB2009/051815 patent/WO2009136350A1/en not_active Ceased
- 2009-05-04 BR BRPI0912433A patent/BRPI0912433A2/pt not_active Application Discontinuation
- 2009-05-04 AP AP2010005456A patent/AP2010005456A0/xx unknown
- 2009-05-04 US US12/990,739 patent/US20110046160A1/en not_active Abandoned
- 2009-05-04 AU AU2009245322A patent/AU2009245322B2/en not_active Ceased
- 2009-05-04 EA EA201001566A patent/EA201001566A1/ru unknown
- 2009-05-04 ES ES09742523T patent/ES2375913T3/es active Active
- 2009-05-04 CN CN2009801261947A patent/CN102083841A/zh active Pending
- 2009-05-04 EP EP09742523A patent/EP2300484B1/en active Active
- 2009-05-04 KR KR1020107024794A patent/KR20110000749A/ko not_active Ceased
- 2009-05-04 MX MX2010012066A patent/MX2010012066A/es not_active Application Discontinuation
- 2009-05-04 AT AT09742523T patent/ATE537178T1/de active
- 2009-05-04 CA CA2721786A patent/CA2721786A1/en not_active Abandoned
- 2009-05-04 NZ NZ588589A patent/NZ588589A/en not_active IP Right Cessation
-
2010
- 2010-10-18 IL IL208793A patent/IL208793A0/en unknown
- 2010-10-21 DO DO2010000317A patent/DOP2010000317A/es unknown
- 2010-10-26 CR CR11759A patent/CR11759A/es not_active Application Discontinuation
- 2010-11-05 MA MA33328A patent/MA32290B1/fr unknown
- 2010-11-05 SV SV2010003725A patent/SV2010003725A/es not_active Application Discontinuation
- 2010-11-09 EC EC2010010597A patent/ECSP10010597A/es unknown
- 2010-11-11 CO CO10141834A patent/CO6321280A2/es not_active Application Discontinuation
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