JP2011516499A5 - - Google Patents
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- Publication number
- JP2011516499A5 JP2011516499A5 JP2011503235A JP2011503235A JP2011516499A5 JP 2011516499 A5 JP2011516499 A5 JP 2011516499A5 JP 2011503235 A JP2011503235 A JP 2011503235A JP 2011503235 A JP2011503235 A JP 2011503235A JP 2011516499 A5 JP2011516499 A5 JP 2011516499A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- hydroxy
- alkoxy
- different
- same
- 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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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 52
- 125000005843 halogen group Chemical group 0.000 claims 39
- 125000003545 alkoxy group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- -1 1-naphthalenyl Chemical group 0.000 claims 12
- 125000001246 bromo group Chemical group Br* 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 claims 3
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 claims 3
- 230000002159 abnormal effect Effects 0.000 claims 3
- 125000006850 spacer group Chemical group 0.000 claims 3
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 2
- YSCNMFDFYJUPEF-OWOJBTEDSA-N 4,4'-diisothiocyano-trans-stilbene-2,2'-disulfonic acid Chemical compound OS(=O)(=O)C1=CC(N=C=S)=CC=C1\C=C\C1=CC=C(N=C=S)C=C1S(O)(=O)=O YSCNMFDFYJUPEF-OWOJBTEDSA-N 0.000 claims 2
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 0.000 claims 2
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000037427 ion transport Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 229920002873 Polyethylenimine Polymers 0.000 claims 1
- 150000001335 aliphatic alkanes Chemical class 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 239000000412 dendrimer Substances 0.000 claims 1
- 229920000736 dendritic polymer Polymers 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 125000005059 halophenyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 210000002011 intestinal secretion Anatomy 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 201000009881 secretory diarrhea Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 0 CCCC(CC(*)C(O)=C1*)=C1O Chemical compound CCCC(CC(*)C(O)=C1*)=C1O 0.000 description 3
- HGJKSKDZSVEQSK-UHFFFAOYSA-N CC(C(CC(NN)=O)N)O Chemical compound CC(C(CC(NN)=O)N)O HGJKSKDZSVEQSK-UHFFFAOYSA-N 0.000 description 1
- SSMYAZCJPHHEQV-UHFFFAOYSA-N CC1C=CC(Cl)=CC1 Chemical compound CC1C=CC(Cl)=CC1 SSMYAZCJPHHEQV-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4265108P | 2008-04-04 | 2008-04-04 | |
| US61/042,651 | 2008-04-04 | ||
| PCT/US2009/039566 WO2009146144A2 (en) | 2008-04-04 | 2009-04-03 | Divalent hydrazide compound conjugates for inhibiting cystic fibrosis transmembrane conductance regulator |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011516499A JP2011516499A (ja) | 2011-05-26 |
| JP2011516499A5 true JP2011516499A5 (cg-RX-API-DMAC10.html) | 2012-05-31 |
Family
ID=41133847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011503235A Pending JP2011516499A (ja) | 2008-04-04 | 2009-04-03 | 嚢胞性線維症膜コンダクタンス制御因子を阻害するための二価ヒドラジド化合物コンジュゲート |
Country Status (10)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0509282A (pt) * | 2004-03-30 | 2007-09-18 | Univ California | compostos contendo hidrazida inibidores de cftr e seus usos |
| US8552067B2 (en) * | 2006-12-22 | 2013-10-08 | The Regents Of The University Of California | Macromolecular conjugates of cystic fibrosis transmembrane conductance regulator protein inhibitors and uses therefor |
| EP2142498A2 (en) * | 2007-04-02 | 2010-01-13 | Institute for Oneworld Health | Cftr inhibitor compounds and uses thereof |
| JP2011517674A (ja) * | 2008-03-25 | 2011-06-16 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 嚢胞性線維症膜コンダクタンス制御因子の水溶性小分子阻害剤 |
| US8236838B2 (en) * | 2008-04-21 | 2012-08-07 | Institute For Oneworld Health | Compounds, compositions and methods comprising isoxazole derivatives |
| EP2278879B1 (en) | 2008-04-21 | 2016-06-15 | PATH Drug Solutions | Compounds, compositions and methods comprising oxadiazole derivatives |
| WO2009131952A1 (en) * | 2008-04-21 | 2009-10-29 | Institute For Oneworld Health | Compounds, compositions and methods comprising thiazole derivatives |
| US20090264481A1 (en) * | 2008-04-21 | 2009-10-22 | Institute For Oneworld Health | Compounds, Compositions and Methods Comprising Oxadiazole Derivatives |
| WO2009131958A2 (en) * | 2008-04-21 | 2009-10-29 | Institute For Oneworld Health | Compounds, compositions and methods comprising triazine derivatives |
| US20090270398A1 (en) * | 2008-04-21 | 2009-10-29 | Institute For Oneworld Health | Compounds, Compositions and Methods Comprising Pyridazine Derivatives |
| WO2009131956A1 (en) * | 2008-04-21 | 2009-10-29 | Institute For Oneworld Health | Compounds, compositions and methods comprising triazole derivatives |
| JP2012503005A (ja) * | 2008-09-19 | 2012-02-02 | インスティテュート フォア ワンワールド ヘルス | イミダゾール誘導体およびトリアゾール誘導体を含む、化合物、組成物ならびに方法。 |
| US8511216B2 (en) * | 2009-03-30 | 2013-08-20 | Kanzaki Kokyukoki Mfg. Co., Ltd. | Hydraulic actuator unit |
| US8343976B2 (en) * | 2009-04-20 | 2013-01-01 | Institute For Oneworld Health | Compounds, compositions and methods comprising pyrazole derivatives |
| EP2464354B1 (en) | 2009-08-10 | 2015-04-01 | The Regents of The University of California | Pyrimido-pyrrolo-quinoxalinedione inhibitors of cystic fibrosis transmembrane conductance regulator protein and uses therefor |
| USRE48842E1 (en) | 2011-05-27 | 2021-12-07 | The Regents Of The University Of California | Pyrimido-pyrrolo-oxazine-dione compound inhibitors of the cystic fibrosis transmembrane conductance regulator protein and uses therefor |
| JPWO2019088270A1 (ja) * | 2017-11-02 | 2020-12-03 | 宇部興産株式会社 | 蛋白分解酵素の双頭型阻害剤 |
| KR20220046544A (ko) | 2019-06-12 | 2022-04-14 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 답즙산 설사를 치료하는 방법 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE103902T1 (de) * | 1982-05-07 | 1994-04-15 | Ciba Geigy Ag | Verwendung von chinolinderivaten zum schuetzen von kulturpflanzen. |
| US6331555B1 (en) * | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
| ES2161594B1 (es) * | 1998-12-17 | 2003-04-01 | Servier Lab | Nuevos derivados de la hidrazida, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen. |
| US7235573B2 (en) * | 2002-09-30 | 2007-06-26 | The Regents Of The University Of California | Methods of treating secretory diarrhea using cystic fibrosis transmembrane conductance regulator protein inhibitors |
| US20050023974A1 (en) | 2003-08-01 | 2005-02-03 | Universal Display Corporation | Protected organic electronic devices and methods for making the same |
| BRPI0509282A (pt) * | 2004-03-30 | 2007-09-18 | Univ California | compostos contendo hidrazida inibidores de cftr e seus usos |
| US8552067B2 (en) * | 2006-12-22 | 2013-10-08 | The Regents Of The University Of California | Macromolecular conjugates of cystic fibrosis transmembrane conductance regulator protein inhibitors and uses therefor |
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2009
- 2009-04-03 EP EP09755506A patent/EP2288592A2/en not_active Withdrawn
- 2009-04-03 CA CA2718676A patent/CA2718676A1/en not_active Abandoned
- 2009-04-03 WO PCT/US2009/039566 patent/WO2009146144A2/en not_active Ceased
- 2009-04-03 US US12/418,147 patent/US20090253799A1/en not_active Abandoned
- 2009-04-03 AU AU2009251519A patent/AU2009251519A1/en not_active Abandoned
- 2009-04-03 BR BRPI0910416A patent/BRPI0910416A2/pt not_active IP Right Cessation
- 2009-04-03 JP JP2011503235A patent/JP2011516499A/ja active Pending
- 2009-04-03 KR KR1020107024636A patent/KR20110004413A/ko not_active Withdrawn
- 2009-04-03 MX MX2010010783A patent/MX2010010783A/es not_active Application Discontinuation
- 2009-04-06 TW TW098111395A patent/TW200946129A/zh unknown