JP2010502736A5 - - Google Patents
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- JP2010502736A5 JP2010502736A5 JP2009527579A JP2009527579A JP2010502736A5 JP 2010502736 A5 JP2010502736 A5 JP 2010502736A5 JP 2009527579 A JP2009527579 A JP 2009527579A JP 2009527579 A JP2009527579 A JP 2009527579A JP 2010502736 A5 JP2010502736 A5 JP 2010502736A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical agent
- agent according
- disease
- ace2
- moiety
- 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
- 239000008177 pharmaceutical agent Substances 0.000 claims 32
- 102000053723 Angiotensin-converting enzyme 2 Human genes 0.000 claims 11
- 108090000975 Angiotensin-converting enzyme 2 Proteins 0.000 claims 11
- 239000003112 inhibitor Substances 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 208000011231 Crohn disease Diseases 0.000 claims 5
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 claims 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims 3
- 206010016717 Fistula Diseases 0.000 claims 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 229960004909 aminosalicylic acid Drugs 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 239000003246 corticosteroid Substances 0.000 claims 3
- 229960001334 corticosteroids Drugs 0.000 claims 3
- 230000003890 fistula Effects 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000003018 immunosuppressive agent Substances 0.000 claims 3
- 239000012071 phase Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- NTCCRGGIJNDEAB-IRXDYDNUSA-N MLN-4760 Chemical group CC(C)C[C@@H](C(O)=O)N[C@H](C(O)=O)CC1=CN=CN1CC1=CC(Cl)=CC(Cl)=C1 NTCCRGGIJNDEAB-IRXDYDNUSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 230000003110 anti-inflammatory effect Effects 0.000 claims 2
- 238000002648 combination therapy Methods 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims 2
- 229940124589 immunosuppressive drug Drugs 0.000 claims 2
- -1 methylenedioxyphenyl Chemical group 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims 1
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 1
- 108010036949 Cyclosporine Proteins 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- UETNIIAIRMUTSM-UHFFFAOYSA-N Jacareubin Natural products CC1(C)OC2=CC3Oc4c(O)c(O)ccc4C(=O)C3C(=C2C=C1)O UETNIIAIRMUTSM-UHFFFAOYSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 claims 1
- 208000037273 Pathologic Processes Diseases 0.000 claims 1
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 claims 1
- 229960002170 azathioprine Drugs 0.000 claims 1
- 229960004168 balsalazide Drugs 0.000 claims 1
- IPOKCKJONYRRHP-FMQUCBEESA-N balsalazide Chemical compound C1=CC(C(=O)NCCC(=O)O)=CC=C1\N=N\C1=CC=C(O)C(C(O)=O)=C1 IPOKCKJONYRRHP-FMQUCBEESA-N 0.000 claims 1
- 229950000210 beclometasone dipropionate Drugs 0.000 claims 1
- 229940092705 beclomethasone Drugs 0.000 claims 1
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 claims 1
- 229960004436 budesonide Drugs 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000023652 chronic gastritis Diseases 0.000 claims 1
- 229960001265 ciclosporin Drugs 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229930182912 cyclosporin Natural products 0.000 claims 1
- 229960003957 dexamethasone Drugs 0.000 claims 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229960002714 fluticasone Drugs 0.000 claims 1
- MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229960000890 hydrocortisone Drugs 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 239000012073 inactive phase Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229960000598 infliximab Drugs 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 1
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- KBOPZPXVLCULAV-UHFFFAOYSA-N mesalamine Chemical compound NC1=CC=C(O)C(C(O)=O)=C1 KBOPZPXVLCULAV-UHFFFAOYSA-N 0.000 claims 1
- 229960004963 mesalazine Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 229960004584 methylprednisolone Drugs 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229960004110 olsalazine Drugs 0.000 claims 1
- QQBDLJCYGRGAKP-FOCLMDBBSA-N olsalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=C(C(O)=CC=2)C(O)=O)=C1 QQBDLJCYGRGAKP-FOCLMDBBSA-N 0.000 claims 1
- 230000009054 pathological process Effects 0.000 claims 1
- 229960005205 prednisolone Drugs 0.000 claims 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims 1
- 229960004618 prednisone Drugs 0.000 claims 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229960001940 sulfasalazine Drugs 0.000 claims 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 claims 1
- NCEXYHBECQHGNR-UHFFFAOYSA-N sulfasalazine Natural products C1=C(O)C(C(=O)O)=CC(N=NC=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-UHFFFAOYSA-N 0.000 claims 1
- 229960001967 tacrolimus Drugs 0.000 claims 1
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims 1
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82507506P | 2006-09-08 | 2006-09-08 | |
| US82780706P | 2006-10-02 | 2006-10-02 | |
| PCT/US2007/077857 WO2008031014A1 (en) | 2006-09-08 | 2007-09-07 | Method for reducing or alleviating inflammation in the digestive tract |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010502736A JP2010502736A (ja) | 2010-01-28 |
| JP2010502736A5 true JP2010502736A5 (enExample) | 2010-10-14 |
Family
ID=38670723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009527579A Pending JP2010502736A (ja) | 2006-09-08 | 2007-09-07 | 消化管の炎症を低減または軽減するための方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20080234345A1 (enExample) |
| EP (1) | EP2059234B1 (enExample) |
| JP (1) | JP2010502736A (enExample) |
| CN (1) | CN101568331A (enExample) |
| AT (1) | ATE531362T1 (enExample) |
| AU (1) | AU2007292247A1 (enExample) |
| CA (1) | CA2662535A1 (enExample) |
| DK (1) | DK2059234T3 (enExample) |
| ES (1) | ES2376493T3 (enExample) |
| IL (1) | IL197362A0 (enExample) |
| WO (1) | WO2008031014A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2095819A1 (en) * | 2008-02-28 | 2009-09-02 | Maastricht University | N-benzyl imidazole derivatives and their use as aldosterone synthase inhibitors |
| WO2009114516A1 (en) * | 2008-03-10 | 2009-09-17 | Ore Pharmaceuticals Inc. | Therapy for disorders of the proximal digestive tract |
| WO2010093804A1 (en) * | 2009-02-12 | 2010-08-19 | Ore Pharmaceuticals, Inc. | Ace2 inhibitors for reducing gastrointestinal adverse effects of cytotoxic agents |
| WO2011108638A1 (ja) * | 2010-03-04 | 2011-09-09 | 大日本住友製薬株式会社 | 炎症性腸疾患用薬剤 |
| KR101713453B1 (ko) | 2010-03-12 | 2017-03-07 | 오메로스 코포레이션 | Pde10 억제제 및 관련 조성물 및 방법 |
| NZ716494A (en) | 2014-04-28 | 2017-07-28 | Omeros Corp | Processes and intermediates for the preparation of a pde10 inhibitor |
| NZ630803A (en) | 2014-04-28 | 2016-03-31 | Omeros Corp | Optically active pde10 inhibitor |
| MA41271A (fr) * | 2014-12-26 | 2017-10-31 | Celgene Alpine Invest Company Ii Llc | Méthodes d'utilisation d'oligonucléotides antisens ciblant smad7 |
| KR20170139074A (ko) | 2015-04-24 | 2017-12-18 | 오메로스 코포레이션 | Pde10 억제제 및 관련 조성물 및 방법 |
| WO2017079678A1 (en) | 2015-11-04 | 2017-05-11 | Omeros Corporation | Solid state forms of a pde10 inhibitor |
| GB202116266D0 (en) * | 2021-11-11 | 2021-12-29 | Bicycletx Ltd | Novel use |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6194556B1 (en) * | 1997-12-11 | 2001-02-27 | Millennium Pharmaceuticals, Inc. | Angiotensin converting enzyme homolog and therapeutic and diagnostic uses therfor |
| US6632830B1 (en) * | 1999-04-30 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | ACE-2 inhibiting compounds and methods of use thereof |
| US7045532B2 (en) | 1999-04-30 | 2006-05-16 | Millennium Pharmaceuticals, Inc. | ACE-2 modulating compounds and methods of use thereof |
| US6900033B2 (en) * | 2001-06-04 | 2005-05-31 | Human Genome Sciences, Inc. | Methods and compositions for modulating ACE-2 activity |
| GB0203061D0 (en) | 2002-02-08 | 2002-03-27 | Novartis Ag | Organic compounds |
| AU2003299196A1 (en) * | 2002-09-24 | 2004-04-23 | Combinatorx, Incorporated | Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines |
| TW200509958A (en) * | 2003-02-14 | 2005-03-16 | Combinatorx Inc | Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines |
| US20050203168A1 (en) * | 2004-03-11 | 2005-09-15 | The Regents Of The University Of Michigan | Angiotensin converting enzyme inhibitor use for treatment and prevention of gastrointestinal disorders |
| WO2008031013A1 (en) * | 2006-09-08 | 2008-03-13 | Gene Logic Inc. | Method for treating inflammatory diseases of the digestive tract |
-
2007
- 2007-09-07 CN CNA2007800394181A patent/CN101568331A/zh active Pending
- 2007-09-07 JP JP2009527579A patent/JP2010502736A/ja active Pending
- 2007-09-07 AU AU2007292247A patent/AU2007292247A1/en not_active Abandoned
- 2007-09-07 US US11/851,694 patent/US20080234345A1/en not_active Abandoned
- 2007-09-07 EP EP07814746A patent/EP2059234B1/en not_active Not-in-force
- 2007-09-07 DK DK07814746.9T patent/DK2059234T3/da active
- 2007-09-07 AT AT07814746T patent/ATE531362T1/de active
- 2007-09-07 ES ES07814746T patent/ES2376493T3/es active Active
- 2007-09-07 CA CA002662535A patent/CA2662535A1/en not_active Abandoned
- 2007-09-07 WO PCT/US2007/077857 patent/WO2008031014A1/en not_active Ceased
-
2009
- 2009-03-03 IL IL197362A patent/IL197362A0/en unknown
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