JP2004534771A5 - - Google Patents
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- Publication number
- JP2004534771A5 JP2004534771A5 JP2002591441A JP2002591441A JP2004534771A5 JP 2004534771 A5 JP2004534771 A5 JP 2004534771A5 JP 2002591441 A JP2002591441 A JP 2002591441A JP 2002591441 A JP2002591441 A JP 2002591441A JP 2004534771 A5 JP2004534771 A5 JP 2004534771A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- group
- oxide
- alkoxy
- 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
- -1 indazolyl Thienyl Chemical group 0.000 claims 276
- 125000004093 cyano group Chemical group *C#N 0.000 claims 128
- 125000001309 chloro group Chemical group Cl* 0.000 claims 123
- 125000001424 substituent group Chemical group 0.000 claims 109
- 125000000217 alkyl group Chemical group 0.000 claims 91
- 125000003545 alkoxy group Chemical group 0.000 claims 72
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 38
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 38
- 229910052736 halogen Inorganic materials 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 34
- 150000002367 halogens Chemical class 0.000 claims 32
- 229910052717 sulfur Inorganic materials 0.000 claims 32
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 24
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 24
- 125000000753 cycloalkyl group Chemical group 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 125000000304 alkynyl group Chemical class 0.000 claims 21
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 16
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 14
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 14
- 125000000335 thiazolyl group Chemical group 0.000 claims 14
- 125000002883 imidazolyl group Chemical group 0.000 claims 13
- 125000002971 oxazolyl group Chemical group 0.000 claims 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims 12
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000004600 benzothiopyranyl group Chemical group S1C(C=CC2=C1C=CC=C2)* 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 11
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 11
- 125000001041 indolyl group Chemical group 0.000 claims 11
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 11
- 125000000842 isoxazolyl group Chemical group 0.000 claims 11
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 10
- RCCPEORTSYDPMB-UHFFFAOYSA-N hydroxy benzenecarboximidothioate Chemical compound OSC(=N)C1=CC=CC=C1 RCCPEORTSYDPMB-UHFFFAOYSA-N 0.000 claims 10
- 125000002757 morpholinyl group Chemical group 0.000 claims 10
- 125000004193 piperazinyl group Chemical group 0.000 claims 10
- 125000003386 piperidinyl group Chemical group 0.000 claims 10
- 125000004076 pyridyl group Chemical group 0.000 claims 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 10
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 10
- 125000000168 pyrrolyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 8
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 8
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 8
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 8
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 8
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 8
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 8
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 8
- 125000004617 chromonyl group Chemical group O1C(=CC(C2=CC=CC=C12)=O)* 0.000 claims 8
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 8
- 125000000332 coumarinyl group Chemical group O1C(=O)C(=CC2=CC=CC=C12)* 0.000 claims 8
- 125000005992 dihydrobenzisothiazinyl group Chemical group 0.000 claims 8
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000005990 isobenzothienyl group Chemical group 0.000 claims 8
- 125000003151 isocoumarinyl group Chemical group C1(=O)OC(=CC2=CC=CC=C12)* 0.000 claims 8
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 8
- 125000005956 isoquinolyl group Chemical group 0.000 claims 8
- 125000001786 isothiazolyl group Chemical group 0.000 claims 8
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 8
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 8
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 8
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 8
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 8
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 8
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 8
- 125000003373 pyrazinyl group Chemical group 0.000 claims 8
- 125000002098 pyridazinyl group Chemical group 0.000 claims 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 8
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 8
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 8
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 8
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 8
- 125000003831 tetrazolyl group Chemical group 0.000 claims 8
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 8
- 125000004306 triazinyl group Chemical group 0.000 claims 8
- 125000001425 triazolyl group Chemical group 0.000 claims 8
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 8
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 6
- 125000004935 benzoxazolinyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 6
- 125000005993 dihydrobenzisoxazinyl group Chemical group 0.000 claims 6
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 6
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 claims 6
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims 6
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims 6
- 125000004655 dihydropyridinyl group Chemical group N1(CC=CC=C1)* 0.000 claims 6
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims 6
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 6
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 6
- 125000005995 isobenzotetrahydrothienyl group Chemical group 0.000 claims 6
- 125000004620 quinolinyl-N-oxide group Chemical group 0.000 claims 6
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 6
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 6
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 6
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 5
- 206010012289 Dementia Diseases 0.000 claims 5
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000005046 dihydronaphthyl group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 3
- 208000027061 mild cognitive impairment Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 3
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 2
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000006288 3,5-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(C([H])=C1F)C([H])([H])* 0.000 claims 2
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052740 iodine Inorganic materials 0.000 claims 2
- 125000005994 isobenzotetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 0 C*C(C(CN(C)*(C)C(*)=O)O)NC(C1=C*(I)=CC(*)C=C1)=* Chemical compound C*C(C(CN(C)*(C)C(*)=O)O)NC(C1=C*(I)=CC(*)C=C1)=* 0.000 description 3
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29285601P | 2001-05-22 | 2001-05-22 | |
| US30135501P | 2001-06-27 | 2001-06-27 | |
| US36060102P | 2002-03-01 | 2002-03-01 | |
| PCT/US2002/016199 WO2002094768A2 (en) | 2001-05-22 | 2002-05-22 | Aza hydroxylated ethyl amine compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004534771A JP2004534771A (ja) | 2004-11-18 |
| JP2004534771A5 true JP2004534771A5 (https=) | 2006-01-05 |
Family
ID=27404155
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002591441A Pending JP2004534771A (ja) | 2001-05-22 | 2002-05-22 | アザヒドロキシル化エチルアミン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US6960664B2 (https=) |
| EP (1) | EP1392645A2 (https=) |
| JP (1) | JP2004534771A (https=) |
| BR (1) | BR0209985A (https=) |
| CA (1) | CA2448084A1 (https=) |
| MX (1) | MXPA03010733A (https=) |
| WO (1) | WO2002094768A2 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004502664A (ja) * | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病処置用化合物 |
| CA2497979A1 (en) * | 2002-09-06 | 2004-03-18 | Elan Pharmaceuticals, Inc. | 1, 3-diamino-2-hydroxypropane prodrug derivatives |
| PL377777A1 (pl) * | 2002-12-11 | 2006-02-20 | Pharmacia & Upjohn Company Llc | Leczenie chorób połączeniami agonistów receptora alfa 7-nikotynowego i innych związków |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| ES2378669T3 (es) * | 2003-12-11 | 2012-04-16 | Abbott Laboratories | Compuestos inhibidores de proteasa de VIH |
| NZ562314A (en) | 2005-04-08 | 2010-02-26 | Comentis Inc | Compounds which inhibit beta-secretase activity and methods of use thereof |
| AR110922A1 (es) | 2017-02-06 | 2019-05-15 | Gilead Sciences Inc | Compuestos inhibidores del vih |
| TWI829205B (zh) | 2018-07-30 | 2024-01-11 | 美商基利科學股份有限公司 | 抗hiv化合物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA93002392A (es) * | 1992-03-11 | 2005-02-04 | Narhex Ltd | Derivados amino de hidrocarburos-oxo e hidroxi-substituidos. |
| ES2177816T3 (es) * | 1995-11-21 | 2002-12-16 | Novartis Ag | Derivados de azahexano como isosteros de sustrato de aspartato proteasas retroviricas. |
| US6087383A (en) * | 1998-01-20 | 2000-07-11 | Bristol-Myers Squibb Company | Bisulfate salt of HIV protease inhibitor |
| JP2004502664A (ja) * | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病処置用化合物 |
-
2002
- 2002-05-22 JP JP2002591441A patent/JP2004534771A/ja active Pending
- 2002-05-22 MX MXPA03010733A patent/MXPA03010733A/es not_active Application Discontinuation
- 2002-05-22 BR BR0209985-3A patent/BR0209985A/pt not_active IP Right Cessation
- 2002-05-22 EP EP02739333A patent/EP1392645A2/en not_active Withdrawn
- 2002-05-22 US US10/152,601 patent/US6960664B2/en not_active Expired - Fee Related
- 2002-05-22 WO PCT/US2002/016199 patent/WO2002094768A2/en not_active Ceased
- 2002-05-22 CA CA002448084A patent/CA2448084A1/en not_active Abandoned
-
2005
- 2005-11-01 US US11/264,738 patent/US20060069264A1/en not_active Abandoned
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