JP2011507879A5 - - Google Patents
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- JP2011507879A5 JP2011507879A5 JP2010539763A JP2010539763A JP2011507879A5 JP 2011507879 A5 JP2011507879 A5 JP 2011507879A5 JP 2010539763 A JP2010539763 A JP 2010539763A JP 2010539763 A JP2010539763 A JP 2010539763A JP 2011507879 A5 JP2011507879 A5 JP 2011507879A5
- Authority
- JP
- Japan
- Prior art keywords
- item
- composition
- compound according
- pharmaceutically acceptable
- solvate
- 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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- 150000001875 compounds Chemical class 0.000 claims description 76
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 125000000217 alkyl group Chemical group 0.000 claims description 29
- 239000001257 hydrogen Substances 0.000 claims description 27
- 150000002148 esters Chemical class 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 23
- 239000012453 solvate Substances 0.000 claims description 23
- 229940002612 prodrug Drugs 0.000 claims description 22
- 239000000651 prodrug Substances 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 230000002265 prevention Effects 0.000 claims description 15
- 125000001424 substituent group Chemical group 0.000 claims description 13
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 12
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 11
- 125000003545 alkoxy group Chemical group 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 239000003380 propellant Substances 0.000 claims description 8
- 239000002464 receptor antagonist Substances 0.000 claims description 8
- 229940044551 receptor antagonist Drugs 0.000 claims description 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 7
- 230000001387 anti-histamine Effects 0.000 claims description 6
- 239000000739 antihistaminic agent Substances 0.000 claims description 6
- 208000010668 atopic eczema Diseases 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 239000005557 antagonist Substances 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 4
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims description 4
- 208000006673 asthma Diseases 0.000 claims description 4
- 201000008937 atopic dermatitis Diseases 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 201000009890 sinusitis Diseases 0.000 claims description 4
- 208000017520 skin disease Diseases 0.000 claims description 4
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims description 3
- -1 anti-infectives Substances 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 125000001188 haloalkyl group Chemical group 0.000 claims description 3
- 230000002757 inflammatory effect Effects 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 claims description 2
- 229940078581 Bone resorption inhibitor Drugs 0.000 claims description 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims description 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims description 2
- 108010059108 CD18 Antigens Proteins 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims description 2
- 201000004624 Dermatitis Diseases 0.000 claims description 2
- 206010012434 Dermatitis allergic Diseases 0.000 claims description 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 102000019223 Interleukin-1 receptor Human genes 0.000 claims description 2
- 108050006617 Interleukin-1 receptor Proteins 0.000 claims description 2
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 claims description 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims description 2
- 208000000592 Nasal Polyps Diseases 0.000 claims description 2
- 201000009053 Neurodermatitis Diseases 0.000 claims description 2
- 102100029438 Nitric oxide synthase, inducible Human genes 0.000 claims description 2
- 101710089543 Nitric oxide synthase, inducible Proteins 0.000 claims description 2
- 206010068318 Oropharyngeal discomfort Diseases 0.000 claims description 2
- 208000003251 Pruritus Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 2
- 108010016672 Syk Kinase Chemical class 0.000 claims description 2
- 102000000551 Syk Kinase Human genes 0.000 claims description 2
- 229960005305 adenosine Drugs 0.000 claims description 2
- 239000000048 adrenergic agonist Substances 0.000 claims description 2
- 239000000556 agonist Substances 0.000 claims description 2
- 239000013566 allergen Substances 0.000 claims description 2
- 208000002205 allergic conjunctivitis Diseases 0.000 claims description 2
- 230000000172 allergic effect Effects 0.000 claims description 2
- 201000010105 allergic rhinitis Diseases 0.000 claims description 2
- 239000003242 anti bacterial agent Substances 0.000 claims description 2
- 230000002924 anti-infective effect Effects 0.000 claims description 2
- 239000000043 antiallergic agent Substances 0.000 claims description 2
- 229940088710 antibiotic agent Drugs 0.000 claims description 2
- 229960005475 antiinfective agent Drugs 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 229940121357 antivirals Drugs 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 208000024998 atopic conjunctivitis Diseases 0.000 claims description 2
- 230000001363 autoimmune Effects 0.000 claims description 2
- 210000002449 bone cell Anatomy 0.000 claims description 2
- 239000002617 bone density conservation agent Substances 0.000 claims description 2
- 206010006451 bronchitis Diseases 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 239000000812 cholinergic antagonist Substances 0.000 claims description 2
- 208000007451 chronic bronchitis Diseases 0.000 claims description 2
- 239000006184 cosolvent Substances 0.000 claims description 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 2
- 239000002619 cytotoxin Substances 0.000 claims description 2
- 239000000850 decongestant Substances 0.000 claims description 2
- 229940124581 decongestants Drugs 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003172 expectorant agent Substances 0.000 claims description 2
- 230000003419 expectorant effect Effects 0.000 claims description 2
- 229940066493 expectorants Drugs 0.000 claims description 2
- 230000004761 fibrosis Effects 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 230000004968 inflammatory condition Effects 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 229940043355 kinase inhibitor Drugs 0.000 claims description 2
- 150000002617 leukotrienes Chemical class 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 208000016366 nasal cavity polyp Diseases 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims description 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 2
- 239000000018 receptor agonist Substances 0.000 claims description 2
- 229940044601 receptor agonist Drugs 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 206010039083 rhinitis Diseases 0.000 claims description 2
- 239000004094 surface-active agent Substances 0.000 claims description 2
- 230000000699 topical effect Effects 0.000 claims description 2
- 150000003751 zinc Chemical class 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 18
- 230000006806 disease prevention Effects 0.000 claims 1
- 230000003053 immunization Effects 0.000 claims 1
- 238000002649 immunization Methods 0.000 claims 1
- 239000003199 leukotriene receptor blocking agent Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 9
- 150000002431 hydrogen Chemical class 0.000 description 8
- 208000027866 inflammatory disease Diseases 0.000 description 3
- 208000030533 eye disease Diseases 0.000 description 2
- 0 C*OC(c1ccccc1)OS Chemical compound C*OC(c1ccccc1)OS 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1614407P | 2007-12-21 | 2007-12-21 | |
| PCT/US2008/087301 WO2009085880A2 (en) | 2007-12-21 | 2008-12-18 | C-21 thioethers as glucocorticoid receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011507879A JP2011507879A (ja) | 2011-03-10 |
| JP2011507879A5 true JP2011507879A5 (enExample) | 2012-02-02 |
Family
ID=40513892
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010539763A Pending JP2011507879A (ja) | 2007-12-21 | 2008-12-18 | グルココルチコイド受容体アゴニストとしてのｃ−２１チオエーテル |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20110262368A1 (enExample) |
| EP (1) | EP2235035A2 (enExample) |
| JP (1) | JP2011507879A (enExample) |
| CN (1) | CN102099368A (enExample) |
| AR (1) | AR070040A1 (enExample) |
| CA (1) | CA2710240A1 (enExample) |
| CL (1) | CL2008003802A1 (enExample) |
| MX (1) | MX2010007024A (enExample) |
| PE (1) | PE20091215A1 (enExample) |
| TW (1) | TW200940070A (enExample) |
| WO (1) | WO2009085880A2 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101970452A (zh) * | 2007-12-21 | 2011-02-09 | 先灵公司 | C20-c21取代的糖皮质激素受体激动剂 |
| UY32520A (es) | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| CN103694306B (zh) * | 2014-01-07 | 2016-03-23 | 成都医路康医学技术服务有限公司 | 一种布地奈德s异构体制备r异构体的方法 |
| RS62040B1 (sr) | 2016-06-02 | 2021-07-30 | Abbvie Inc | Agonist receptora glukokortikoida i njegovi imunokonjugati |
| CA3042428A1 (en) * | 2016-11-08 | 2018-05-17 | Regeneron Pharmaceuticals, Inc. | Steroids and protein-conjugates thereof |
| KR20250008984A (ko) | 2017-05-18 | 2025-01-16 | 리제너론 파마슈티칼스 인코포레이티드 | 사이클로덱스트린 단백질 약물 접합체 |
| CA3247730A1 (en) | 2017-11-07 | 2025-10-30 | Regeneron Pharmaceuticals, Inc. | Hydrophilic linkers for antibody drug conjugates |
| EP3658192B1 (en) | 2017-12-01 | 2021-04-28 | AbbVie Inc. | Glucocorticoid receptor agonist and immunoconjugates thereof |
| MA50259A1 (fr) | 2018-01-08 | 2021-07-29 | Regeneron Pharma | Stéroïdes et leurs conjugués-anticorps |
| WO2019217591A1 (en) | 2018-05-09 | 2019-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-msr1 antibodies and methods of use thereof |
| EP3868368A1 (en) * | 2020-02-21 | 2021-08-25 | Dompe' Farmaceutici S.P.A. | Cxcl8 (interleukin-8) activity inhibitor and corticosteroid combination and pharmaceutical composition and use thereof |
| EP4635969A4 (en) * | 2022-12-16 | 2026-06-10 | Tianjin Pharmaceutical Biotechnology Co Ltd | NEW GLUCOCORTICOID, ITS PREPARATION PROCESS AND ITS USE |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2231374B1 (enExample) * | 1973-05-30 | 1976-10-22 | Jouveinal Sa | |
| FR2510582B1 (fr) * | 1981-07-30 | 1986-05-30 | Sipsy | Steroides esterifies en la position 17 et thio-esterifies en la position 21, leur procede de preparation et leur application comme medicament |
| FR2551069B1 (fr) * | 1983-08-26 | 1986-07-25 | Jouveinal Sa | 17-oxo-21-thioesters d'hydrocortisone, leur preparation et leurs applications comme medicament |
| US5223493A (en) * | 1984-12-28 | 1993-06-29 | Alcon Laboratories, Inc. | Anti-inflammatory compounds for ophthalmic use |
| US4861765A (en) * | 1985-06-26 | 1989-08-29 | Jouveinal | 21-alkyl-, cycloalkyl- or aryl-substituted thio steroids and pharmaceutical compositions containing them |
| US5420120A (en) * | 1993-12-17 | 1995-05-30 | Alcon Laboratories, Inc. | Anti-inflammatory glucocorticoid compounds for topical ophthalmic use |
| WO1997024367A1 (en) * | 1995-12-29 | 1997-07-10 | Glaxo Group Limited | 21-(2-oxo-tetrahydrofuran)-thio pregnane derivatives, a process for their production and pharmaceutical compositions containing them |
| AU2006259604A1 (en) * | 2005-06-14 | 2006-12-28 | Gilead Sciences, Inc. | Substituted phenylphosphates as mutual prodrugs of steroids and beta -agonists for the treatment of pulmonary inflammation and bronchoconstriction |
| CN101970452A (zh) * | 2007-12-21 | 2011-02-09 | 先灵公司 | C20-c21取代的糖皮质激素受体激动剂 |
-
2008
- 2008-12-18 US US12/736,064 patent/US20110262368A1/en not_active Abandoned
- 2008-12-18 CA CA2710240A patent/CA2710240A1/en not_active Abandoned
- 2008-12-18 CN CN2008801273009A patent/CN102099368A/zh active Pending
- 2008-12-18 AR ARP080105526A patent/AR070040A1/es not_active Application Discontinuation
- 2008-12-18 MX MX2010007024A patent/MX2010007024A/es not_active Application Discontinuation
- 2008-12-18 EP EP08866275A patent/EP2235035A2/en not_active Withdrawn
- 2008-12-18 WO PCT/US2008/087301 patent/WO2009085880A2/en not_active Ceased
- 2008-12-18 PE PE2008002135A patent/PE20091215A1/es not_active Application Discontinuation
- 2008-12-18 JP JP2010539763A patent/JP2011507879A/ja active Pending
- 2008-12-18 TW TW097149503A patent/TW200940070A/zh unknown
- 2008-12-18 CL CL2008003802A patent/CL2008003802A1/es unknown
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