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
Links
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000003342 alkenyl 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 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
- 125000001424 substituent group Chemical group 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 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
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-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
- 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
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-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
- 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
- 125000004093 cyano group Chemical group *C#N 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
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method 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
- 150000003839 salts Chemical class 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 (enExample) | 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)
| Country | Link |
|---|---|
| US (1) | US8394807B2 (enExample) |
| EP (1) | EP2376083A4 (enExample) |
| JP (1) | JP2012509352A (enExample) |
| CA (1) | CA2744425A1 (enExample) |
| WO (1) | WO2010059953A1 (enExample) |
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 |
| CN101394852A (zh) | 2005-06-14 | 2009-03-25 | 先灵公司 | 作为蛋白酶抑制剂的化合物的制备和用途 |
| SG162790A1 (en) | 2005-06-14 | 2010-07-29 | Schering Corp | Aspartyl protease inhibitors |
| PE20080155A1 (es) | 2006-06-12 | 2008-03-10 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
| CN101868457B (zh) | 2007-09-24 | 2013-02-13 | 科门蒂斯公司 | 作为β-分泌酶抑制剂用于治疗的(3-羟基-4-氨基-丁-2-基)-3-(2-噻唑-2-基-吡咯烷-1-羰基)苯甲酰胺衍生物和相关化合物 |
| US8541427B2 (en) | 2008-04-22 | 2013-09-24 | Merck, Sharp & Dohme, Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| JP2012505241A (ja) | 2008-10-10 | 2012-03-01 | パーデュー・リサーチ・ファウンデーション | アルツハイマー病の治療用組成物 |
| HK1255074A1 (zh) | 2015-07-01 | 2019-08-02 | Crinetics Pharmaceuticals, Inc. | 生长抑素调节剂及其用途 |
| 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 |
| WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN 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 |
| GEP20074171B (en) | 2001-11-08 | 2007-07-25 | Elan Pharm 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 |
| CA2529994A1 (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 |
| JP2008534541A (ja) | 2005-03-30 | 2008-08-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換１，２−エチレンジアミン、前記化合物を含む薬物、それらの使用及びそれらの製造方法 |
| PT1966198E (pt) | 2005-10-25 | 2011-05-13 | Janssen Pharmaceutica Nv | Derivados de 2-amino-3,4-di-hidro-pirido[3,4-d]pirimidina ?teis como inibidores de beta-secretase (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 WO PCT/US2009/065358 patent/WO2010059953A1/en not_active Ceased
- 2009-11-20 CA CA2744425A patent/CA2744425A1/en not_active Abandoned
- 2009-11-20 US US13/130,508 patent/US8394807B2/en not_active Expired - Fee Related
- 2009-11-20 EP EP09828297A patent/EP2376083A4/en not_active Withdrawn