JP2012505241A5 - - Google Patents
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- Publication number
- JP2012505241A5 JP2012505241A5 JP2011531201A JP2011531201A JP2012505241A5 JP 2012505241 A5 JP2012505241 A5 JP 2012505241A5 JP 2011531201 A JP2011531201 A JP 2011531201A JP 2011531201 A JP2011531201 A JP 2011531201A JP 2012505241 A5 JP2012505241 A5 JP 2012505241A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- aryl
- alkyl
- arylalkyl
- alkylene
- 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- Withdrawn
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- 150000001875 compounds Chemical class 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004404 heteroalkyl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 2
- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- CIISBYKBBMFLEZ-UHFFFAOYSA-N 1,2-oxazolidine Chemical compound C1CNOC1 CIISBYKBBMFLEZ-UHFFFAOYSA-N 0.000 claims 1
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 101100277337 Arabidopsis thaliana DDM1 gene Proteins 0.000 claims 1
- WYNCHZVNFNFDNH-UHFFFAOYSA-N Oxazolidine Chemical compound C1COCN1 WYNCHZVNFNFDNH-UHFFFAOYSA-N 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000005237 alkyleneamino group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 101150113676 chr1 gene Proteins 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- IWELDVXSEVIIGI-UHFFFAOYSA-N piperazin-2-one Chemical compound O=C1CNCCN1 IWELDVXSEVIIGI-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000005531 substituted alkyleneoxy group Chemical group 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 0 CCCCC(C(*)C(*)*(*)**)N* Chemical compound CCCCC(C(*)C(*)*(*)**)N* 0.000 description 6
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10443408P | 2008-10-10 | 2008-10-10 | |
| US61/104,434 | 2008-10-10 | ||
| US17562409P | 2009-05-05 | 2009-05-05 | |
| US61/175,624 | 2009-05-05 | ||
| PCT/US2009/060132 WO2010042796A1 (en) | 2008-10-10 | 2009-10-09 | Compounds for treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012505241A JP2012505241A (ja) | 2012-03-01 |
| JP2012505241A5 true JP2012505241A5 (https=) | 2012-11-22 |
Family
ID=42100967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011531201A Withdrawn JP2012505241A (ja) | 2008-10-10 | 2009-10-09 | アルツハイマー病の治療用組成物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8703947B2 (https=) |
| EP (1) | EP2349308A4 (https=) |
| JP (1) | JP2012505241A (https=) |
| CA (1) | CA2740107A1 (https=) |
| WO (1) | WO2010042796A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5055432B2 (ja) | 2007-09-24 | 2012-10-24 | コメンティス，インコーポレーテッド | 治療のためのβ−セクレターゼ阻害剤としての（３−ヒドロキシ−４−アミノブタン−２−イル）−３−（２−チアゾール−２−イル−ピロリジン−１−カルボニル）ベンズアミド誘導体及び関連する化合物 |
| US20120214802A1 (en) * | 2009-03-25 | 2012-08-23 | Bilcer Geoffrey M | Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof |
| WO2013148130A1 (en) * | 2012-03-29 | 2013-10-03 | Oklahoma Medical Research Foundation | Inhibition of memapsin 1 cleavage in the treatment of diabetes |
| US10085969B1 (en) * | 2016-02-12 | 2018-10-02 | University Of South Florida | Sortilin binding compounds, formulations, and uses thereof |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (34)
| 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 |
| JP3421720B2 (ja) * | 1992-11-17 | 2003-06-30 | シチズン時計株式会社 | 角速度検出回路 |
| 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 |
| AU2002360508A1 (en) | 2001-12-06 | 2003-06-23 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamines |
| ATE443043T1 (de) | 2002-11-12 | 2009-10-15 | Merck & Co Inc | Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer |
| JP2007516207A (ja) | 2003-06-30 | 2007-06-21 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療のためのＮ−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤 |
| WO2005016876A2 (en) * | 2003-08-08 | 2005-02-24 | Schering Corporation | Cyclic amine bace-1 inhibitors having a benzamide substituent |
| 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 |
| NZ562314A (en) | 2005-04-08 | 2010-02-26 | Comentis Inc | Compounds which inhibit beta-secretase activity and methods of use thereof |
| TW200804290A (en) | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| CA2629317A1 (en) | 2005-11-16 | 2007-05-24 | Merck & Co., Inc. | Imidazolidinone compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| US7902218B2 (en) | 2006-12-12 | 2011-03-08 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinolines as β-secretase inhibitors |
| EP2349244A4 (en) | 2008-10-10 | 2012-09-19 | Comentis Inc | BICYCLIC COMPOUNDS FOR INHIBITING BETA SEKRETASE ACTIVITY AND METHOD OF USE THEREOF |
| US8394807B2 (en) | 2008-11-20 | 2013-03-12 | Purdue Research Foundation | Quinazoline inhibitors of BACE 1 and methods of using |
| US8859590B2 (en) | 2008-12-05 | 2014-10-14 | Purdue Research Foundation | Inhibitors of BACE1 and methods for treating Alzheimer's disease |
-
2009
- 2009-10-09 CA CA2740107A patent/CA2740107A1/en not_active Abandoned
- 2009-10-09 EP EP09819930A patent/EP2349308A4/en not_active Withdrawn
- 2009-10-09 US US13/123,157 patent/US8703947B2/en not_active Expired - Fee Related
- 2009-10-09 WO PCT/US2009/060132 patent/WO2010042796A1/en not_active Ceased
- 2009-10-09 JP JP2011531201A patent/JP2012505241A/ja not_active Withdrawn
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