JP2012509352A5 - - Google Patents
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- Publication number
- JP2012509352A5 JP2012509352A5 JP2011537659A JP2011537659A JP2012509352A5 JP 2012509352 A5 JP2012509352 A5 JP 2012509352A5 JP 2011537659 A JP2011537659 A JP 2011537659A JP 2011537659 A JP2011537659 A JP 2011537659A JP 2012509352 A5 JP2012509352 A5 JP 2012509352A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- optionally substituted
- alkylene
- alkyl
- heteroaryl
- 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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- 150000001875 compounds Chemical class 0.000 claims 15
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 150000001408 amides Chemical class 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- -1 carbamoyloxy, amino Chemical group 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 206010001897 Alzheimer's disease Diseases 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 1
- 125000004948 alkyl aryl alkyl group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000005135 aryl sulfinyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N furane Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11643808P | 2008-11-20 | 2008-11-20 | |
| US61/116,438 | 2008-11-20 | ||
| US17563009P | 2009-05-05 | 2009-05-05 | |
| US61/175,630 | 2009-05-05 | ||
| PCT/US2009/065358 WO2010059953A1 (en) | 2008-11-20 | 2009-11-20 | Quinazoline inhibitors of bace 1 and methods of using |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012509352A JP2012509352A (ja) | 2012-04-19 |
| JP2012509352A5 true JP2012509352A5 (US07794700-20100914-C00152.png) | 2013-01-17 |
Family
ID=42198516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011537659A Pending JP2012509352A (ja) | 2008-11-20 | 2009-11-20 | Ｂａｃｅ１のキナゾリン阻害剤および使用方法 |
Country Status (5)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP4896972B2 (ja) | 2005-06-14 | 2012-03-14 | シェーリング コーポレイション | 複素環式アスパルチルプロテアーゼ阻害剤、その調製及び使用 |
| KR20080029965A (ko) | 2005-06-14 | 2008-04-03 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
| US8168641B2 (en) | 2006-06-12 | 2012-05-01 | Schering Corporation | Aspartyl protease inhibitors |
| US8299267B2 (en) | 2007-09-24 | 2012-10-30 | Comentis, Inc. | (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating |
| AU2009239536C1 (en) | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| US8703947B2 (en) | 2008-10-10 | 2014-04-22 | Purdue Research Foundation | Compounds for treatment of Alzheimer's disease |
| WO2017003724A1 (en) | 2015-07-01 | 2017-01-05 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| CN106824269B (zh) * | 2017-03-07 | 2019-05-17 | 马鞍山市泰博化工科技有限公司 | 一种吡唑[5，4-b]-γ-吡喃衍生物及其制备方法和制备用催化剂 |
| US11028068B2 (en) | 2017-07-25 | 2021-06-08 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) * | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) * | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3630200A (en) * | 1969-06-09 | 1971-12-28 | Alza Corp | Ocular insert |
| US3847770A (en) * | 1972-04-10 | 1974-11-12 | Continental Can Co | Photopolymerizable compositions prepared from beta hydroxy esters and polyitaconates |
| US3916899A (en) * | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) * | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US4769027A (en) * | 1984-08-15 | 1988-09-06 | Burroughs Wellcome Co. | Delivery system |
| US4687610A (en) * | 1986-04-30 | 1987-08-18 | E. I. Du Pont De Neumours And Company | Low crystallinity polyester yarn produced at ultra high spinning speeds |
| US5073543A (en) * | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| IT1229203B (it) * | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| US5120548A (en) * | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) * | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5627165A (en) * | 1990-06-13 | 1997-05-06 | Drug Innovation & Design, Inc. | Phosphorous prodrugs and therapeutic delivery systems using same |
| US5580578A (en) * | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| US5591767A (en) * | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| US5354566A (en) * | 1993-06-02 | 1994-10-11 | Kraft General Foods, Inc. | Preparation of yeast-leavened dough crusts |
| IT1270594B (it) * | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| AU2002359376B2 (en) * | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| EP1562897B1 (en) * | 2002-11-12 | 2009-09-16 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease |
| WO2005004802A2 (en) * | 2003-06-30 | 2005-01-20 | Merck & Co., Inc. | N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
| US7585885B2 (en) * | 2004-04-22 | 2009-09-08 | Eli Lilly And Company | Pyrrolidine derivatives useful as BACE inhibitors |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US7745470B2 (en) * | 2005-03-10 | 2010-06-29 | Bristol-Myers Squibb Company | Isophthalates as beta-secretase inhibitors |
| WO2006103038A1 (en) | 2005-03-30 | 2006-10-05 | Boehringer Ingelheim International Gmbh | Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture |
| PL1966198T3 (pl) | 2005-10-25 | 2011-07-29 | Janssen Pharmaceutica Nv | Pochodne 2-amino-3,4-dihydropirydo[3,4-d]pirymidyny do zastosowania jako inhibitory beta-sekretazy (BACE) |
| TW200804290A (en) * | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
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2009
- 2009-11-20 JP JP2011537659A patent/JP2012509352A/ja active Pending
- 2009-11-20 CA CA2744425A patent/CA2744425A1/en not_active Abandoned
- 2009-11-20 EP EP09828297A patent/EP2376083A4/en not_active Withdrawn
- 2009-11-20 WO PCT/US2009/065358 patent/WO2010059953A1/en active Application Filing
- 2009-11-20 US US13/130,508 patent/US8394807B2/en active Active
