HRP20100714T1 - Derivati 5-(benz-(z)-iliden)-tiazolidin-4-ona kao imunosupresivna sredstva - Google Patents
Derivati 5-(benz-(z)-iliden)-tiazolidin-4-ona kao imunosupresivna sredstva Download PDFInfo
- Publication number
- HRP20100714T1 HRP20100714T1 HR20100714T HRP20100714T HRP20100714T1 HR P20100714 T1 HRP20100714 T1 HR P20100714T1 HR 20100714 T HR20100714 T HR 20100714T HR P20100714 T HRP20100714 T HR P20100714T HR P20100714 T1 HRP20100714 T1 HR P20100714T1
- Authority
- HR
- Croatia
- Prior art keywords
- thiazolidin
- benz
- ylidene
- hydroxy
- ethoxy
- Prior art date
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- 229960003444 immunosuppressant agent Drugs 0.000 title 1
- 239000003018 immunosuppressive agent Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 43
- NOLHRFLIXVQPSZ-UHFFFAOYSA-N 1,3-thiazolidin-4-one Chemical class O=C1CSCN1 NOLHRFLIXVQPSZ-UHFFFAOYSA-N 0.000 claims abstract 24
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 24
- 239000001257 hydrogen Substances 0.000 claims abstract 24
- -1 5,6,7,8-tetrahydronaphth-1-yl Chemical group 0.000 claims abstract 16
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 15
- 229910052736 halogen Inorganic materials 0.000 claims abstract 15
- 150000002367 halogens Chemical class 0.000 claims abstract 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 10
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 9
- 125000003282 alkyl amino group Chemical group 0.000 claims abstract 9
- 239000000203 mixture Substances 0.000 claims abstract 9
- 150000002431 hydrogen Chemical group 0.000 claims abstract 7
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims abstract 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 3
- 230000000877 morphologic effect Effects 0.000 claims abstract 2
- 239000002904 solvent Chemical class 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 210000000987 immune system Anatomy 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 1
- 239000000463 material Substances 0.000 claims 1
- XOJVVFBFDXDTEG-UHFFFAOYSA-N pristane Chemical compound CC(C)CCCC(C)CCCC(C)CCCC(C)C XOJVVFBFDXDTEG-UHFFFAOYSA-N 0.000 claims 1
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- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0313072 | 2003-11-21 | ||
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| EP2295418A1 (en) | 2003-11-21 | 2011-03-16 | Actelion Pharmaceuticals Ltd. | 5-(benz-(z)-ylidene)-thiazolidin-4-one derivatives as immunosuppressant agents |
| WO2005082901A1 (en) * | 2004-02-25 | 2005-09-09 | Smithkline Beecham Corporation | Novel chemical compounds |
| JP2008509931A (ja) | 2004-08-13 | 2008-04-03 | プレーシス ファーマスーティカルズ インコーポレイテッド | スフィンゴシン−１−ホスフェート（ｓ１ｐ）レセプター活性を調節するための方法および組成物 |
| EP1959958A4 (en) * | 2005-11-14 | 2010-07-14 | Univ Southern California | INTEGRIN-BINDING SMALL MOLECULES |
| JP4182986B2 (ja) * | 2006-04-19 | 2008-11-19 | トヨタ自動車株式会社 | 半導体装置とその製造方法 |
| CN103087004A (zh) | 2006-11-23 | 2013-05-08 | 埃科特莱茵药品有限公司 | 一种制备2-亚氨基-四氢噻唑-4-酮衍生物的新方法 |
| US8912340B2 (en) | 2006-11-23 | 2014-12-16 | Actelion Pharmaceuticals Ltd. | Process for the preparation of 2-imino-thiazolidin-4-one derivatives |
| KR101718639B1 (ko) * | 2008-03-17 | 2017-03-21 | 액테리온 파마슈티칼 리미티드 | 선별적 ｓ1ｐ₁ 수용체 작동약에 대한 투약 섭생 |
| GB0819182D0 (en) * | 2008-10-20 | 2008-11-26 | Actelion Pharmaceuticals Ltd | Crystalline forms |
| US8747844B2 (en) | 2010-07-30 | 2014-06-10 | Saint Louis University | Methods of treating pain |
| CA2895172C (en) * | 2012-08-17 | 2020-08-18 | Actelion Pharmaceuticals Ltd | Process for the preparation of|(2z,5z)-5-(3-chloro-4-((r)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-|(o-tolyl)thiazolidin-4-one and intermediate used in said process |
| US9629834B2 (en) | 2013-04-26 | 2017-04-25 | Kyoto University | Medicinal composition for inhibiting formation and/or enlargement of cerebral aneurysm or shrinking same |
| EP2862574A1 (en) | 2013-10-15 | 2015-04-22 | Sanofi | {4-[5-(3-chloro-phenoxy)-oxazolo[5,4 d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid for use in the prevention or treatment of acute kidney injury |
| EP2952188A1 (en) * | 2014-06-03 | 2015-12-09 | Universität Bern | Thiazolidinones as cellular anandamide uptake inhibitors and their use in the treatment of psychiatric or neurological disorders and inflammation, in particular neuroinflammation |
| HRP20220490T8 (hr) * | 2014-05-28 | 2022-06-10 | Universität Bern | Spojevi tiazolidinona i njihova upotreba u liječenju psihijatrijskih ili neuroloških poremećaja i inflamacije, posebno neuroinflamacije |
| US10300048B2 (en) * | 2014-05-28 | 2019-05-28 | Universitat Bern | Thiazolidinones as cellular anandamide uptake inhibitors and their use in the treatment of psychiatric or neurological disorders and inflammation, in particular neuroinflammation |
| KR20200013086A (ko) | 2014-12-11 | 2020-02-05 | 액테리온 파마슈티칼 리미티드 | 선택적 s1p1 수용체 효능제에 대한 투약 섭생 |
| MA41139A (fr) | 2014-12-11 | 2017-10-17 | Actelion Pharmaceuticals Ltd | Combinaison pharmaceutique comportant un agoniste sélectif du récepteur sip1 |
| US10111841B2 (en) | 2015-06-19 | 2018-10-30 | University Of South Florida | Stabilization of alcohol intoxication-induced cardiovascular instability |
| MX2018007887A (es) | 2015-12-25 | 2019-02-20 | Crystal Pharmatech Co Ltd | Formas cristalinas de modulador selectivo del receptor s1p1 y método de preparación del mismo. |
| JOP20190207A1 (ar) * | 2017-03-14 | 2019-09-10 | Actelion Pharmaceuticals Ltd | تركيبة صيدلانية تشتمل على بونيسيمود |
| WO2019060147A1 (en) * | 2017-09-19 | 2019-03-28 | Teva Pharmaceuticals Usa, Inc. | NEW CRYSTALLINE POLYMORPHE FROM PONESIMOD |
| TWI647229B (zh) * | 2017-11-14 | 2019-01-11 | 國立暨南國際大學 | Method for synthesizing 3,4-hydroisoquinoline thiazolidine |
| US11013723B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms of a thiazolidinone compound, compositions and methods of use thereof |
| US11014897B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms comprising a thiazolidinone compound, compositions and methods of use thereof |
| US11014940B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Thiazolidinone and oxazolidinone compounds and formulations |
| US11186556B1 (en) | 2018-10-16 | 2021-11-30 | Celgene Corporation | Salts of a thiazolidinone compound, solid forms, compositions and methods of use thereof |
| JP2023501217A (ja) | 2019-10-31 | 2023-01-18 | イドーシア ファーマシューティカルズ リミテッド | Ｃｘｃｒ７アンタゴニストのｓ１ｐ１受容体調節剤との合剤 |
| WO2021157682A1 (ja) | 2020-02-06 | 2021-08-12 | 田辺三菱製薬株式会社 | 筋痛性脳脊髄炎／慢性疲労症候群治療剤 |
| WO2023022896A1 (en) | 2021-08-17 | 2023-02-23 | Teva Czech Industries S.R.O | Polymorphs of ponesimod |
| EP4212156A1 (en) | 2022-01-13 | 2023-07-19 | Abivax | Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a s1p receptor modulator |
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| US3077402A (en) | 1954-12-06 | 1963-02-12 | Polaroid Corp | Photographic color processes, products, and compositions |
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| OA03835A (fr) | 1970-07-17 | 1971-12-24 | Rhone Poulenc Sa | Nouveaux dérivés de la thiazolidine, leur préparation et les compositions qui les contiennent. |
| US5362733A (en) | 1990-04-27 | 1994-11-08 | Orion-Yhtyma Oy | Pharmacologically active catechol derivatives |
| TW221689B (el) | 1991-08-27 | 1994-03-11 | Otsuka Pharma Co Ltd | |
| AU669427B2 (en) | 1993-02-26 | 1996-06-06 | Otsuka Pharmaceutical Co., Ltd. | Thiazole or imidazole derivatives as maillard reaction inhibbitors |
| KR960022486A (ko) | 1994-12-29 | 1996-07-18 | 김준웅 | 신규 티아졸리딘-4-온 유도체 |
| US6353006B1 (en) | 1999-01-14 | 2002-03-05 | Bayer Corporation | Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents |
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| US20050019825A9 (en) * | 2002-03-15 | 2005-01-27 | Qing Dong | Common ligand mimics: pseudothiohydantoins |
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| EP2295418A1 (en) | 2003-11-21 | 2011-03-16 | Actelion Pharmaceuticals Ltd. | 5-(benz-(z)-ylidene)-thiazolidin-4-one derivatives as immunosuppressant agents |
| USRE43833E1 (en) | 2003-11-21 | 2012-11-27 | Actelion Pharmaceuticals Ltd. | Thiazolidin-4-one derivatives |
| WO2005082901A1 (en) | 2004-02-25 | 2005-09-09 | Smithkline Beecham Corporation | Novel chemical compounds |
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| US8912340B2 (en) | 2006-11-23 | 2014-12-16 | Actelion Pharmaceuticals Ltd. | Process for the preparation of 2-imino-thiazolidin-4-one derivatives |
| CN103087004A (zh) | 2006-11-23 | 2013-05-08 | 埃科特莱茵药品有限公司 | 一种制备2-亚氨基-四氢噻唑-4-酮衍生物的新方法 |
| KR101718639B1 (ko) | 2008-03-17 | 2017-03-21 | 액테리온 파마슈티칼 리미티드 | 선별적 ｓ1ｐ₁ 수용체 작동약에 대한 투약 섭생 |
| GB0819182D0 (en) | 2008-10-20 | 2008-11-26 | Actelion Pharmaceuticals Ltd | Crystalline forms |
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