SI3166925T1 - Izoindolinski derivati za uporabo pri zdravljenju virusne infekcije - Google Patents
Izoindolinski derivati za uporabo pri zdravljenju virusne infekcije Download PDFInfo
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- SI3166925T1 SI3166925T1 SI201530238T SI201530238T SI3166925T1 SI 3166925 T1 SI3166925 T1 SI 3166925T1 SI 201530238 T SI201530238 T SI 201530238T SI 201530238 T SI201530238 T SI 201530238T SI 3166925 T1 SI3166925 T1 SI 3166925T1
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- compound
- alkyl
- viral infection
- phenyl
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- 208000036142 Viral infection Diseases 0.000 title claims abstract 7
- 230000009385 viral infection Effects 0.000 title claims abstract 7
- GWVMLCQWXVFZCN-UHFFFAOYSA-N isoindoline Chemical class C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 19
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 229910052796 boron Inorganic materials 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000004474 heteroalkylene group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 230000001177 retroviral effect Effects 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract 1
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Claims (16)
- ·· * - Izoindolinski derivati za uporabo pri zdravljenju virusne infekcije Patentni zahtevki L Spojina s formulo I: kjer:R1 je Ci_6alkil; R2 je C5_i4aril, C3_7cikloalkil, C3.7cikloalkenil, C2-9heterocikel ali C2-9heteroaril, kjer je vsaka skupina R2 po izbiri substituirana z 1-4 substituenti, izbranimi izmed halo, Ci^alkila, Ci^hetereoalkila ali C^alkilena ali Ci.6heteroalkilena, kjer sta Ci^alkilen ali Ci.6heteroalkilen vezana na sosednje atome ogljika na C5_i4arilu, C3_7cikloalkilu, C3.7cikloalkemlu, C3.9heterociklu ali C5.9heteroarilu, da se tvori kondenziran obroč; L je vez, -CH2(CO)-, -C^alkilen-, -S02-, -C(0>, -C(S>, -C(NH)-, -C(0)NH-, -C(0)NHCH2-, -C(0)N-, -C(0)0CH2-, -C(0)0-, -C(0)C(0)-, -S02-NH- ali -CH2C(0)-; R3 je H, CN, C|_6alkil, C5.i4aril, CH2C5.i4aril, CH2C3.7cikloalkil, C3.7cikloalkil, C3.7spirocikloalkil, C3.7cikloalkenil, C2.9heterocikel ali C2_9heteroaril, kjer je vsaka skupina R3 po izbiri substituirana z 1-4 substituenti, izbranimi izmed halo, Ci^alkila, premoščenega C2.8heterocikla, C3.7cikloalkila, Ci.3fluoroalkila, -OCj.6alkila, -C(0)R4, -C(0)NR4, -C(0)NHR4, C5.i4arila, C^hetereoalkila, -Β(ΟΗ)2, C2_9heterocikla, Ci^heteroarila, -C(0)OCi_6alkila, ali sta dva substituenta, ki sta vezana na sosednje atome, lahko vezana skupaj, da se tvori kondenziran obroč in je ta kondenziran obroč po izbiri lahko substituiran z R4; R4 je CN, halo, -OCi.6alkil, Cj^alkil, C3.7cikloalkil, C2-9heterocikel ali C5_i4aril; in kjer vsak heterocikel, heteroaril, heteroalkil in heteroalkilen obsega 1-3 heteroatome, izbrane izmed S, N, B ali O.
- 2. Spojina po zahtevku 1, kjer je R1 t-butil.
- 3. Spojina po katerem koli od zahtevkov 1-2, kjer je R2 po izbiri substituiran fenil.
- 4. Spojina po zahtevku 3, kjer je R2 fenil, substituiran z 1-4 substituenti, izbranimi izmed fluora, metila, -CH2CH2CH2O-, kjer je -CH2CH2CH2O- vezan na sosednje atome ogljika na fenilu, da se tvori bicikličen obroč, ali -NHCH2CH2O-, kjer je NHCH2CH2O- vezan na sosednje atome ogljika na fenilu, da se tvori bicikličen obroč.
- 5. Spojina po katerem koli od zahtevkov 1-4, kjer je R3 C^aUdl, fenil, naftil, ciklopentil, cikloheksil, piridil ali tetrahidropiranil, od katerih je vsak po izbiri substituiran z 1-3 substituenti, izbranimi izmed halogena, Ci^alkila, -OC^alkila, Ci_3fluoroalkila ali fenila.
- 6. Spojina po katerem koli od zahtevkov 1-5, kjer je stereokemija na ogljiku, na katerega je vezan OR1, prikazana spodaj :
- 7. Spojina po zahtevku 1, kjer je spojina:
- 8. Spojina po zahtevku 1, kjer je spojina:
- 9. Spojina po zahtevku 1, kjer je spojina:
- 10. Farmacevtsko sprejemljiva sol spojine po katerem koli od zahtevkov 1-9.
- 11. Farmacevtski sestavek, ki obsega spojino ali sol po katerem koli od zahtevkov Ι-ΙΟ.
- 12. Farmacevtski sestavek po zahtevku 11 za uporabo pri zdravljenju virusne infekcije pri pacientu, posredovane vsaj delno z virusom retrovirusne družine virusov.
- 13. Farmacevtski sestavek za uporabo po zahtevku 12, kjer je virusna infekcija posredovana z virusom HIV.
- 14. Spojina ali sol, kot je definirana v katerem koli od zahtevkov 1-10, za uporabo v medicinski terapiji.
- 15. Spojina ali sol, kot je definirana v katerem koli od zahtevkov 1-10, za uporabo pri zdravljenju virusne infekcije pri človeku.
- 16. Uporaba spojine ali soli, kot je definirana v katerem koli od zahtevkov 1-10, pri izdelavi zdravila za uporabo pri zdravljenju virusne infekcije pri človeku.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462021844P | 2014-07-08 | 2014-07-08 | |
| US201462064615P | 2014-10-16 | 2014-10-16 | |
| US201562134616P | 2015-03-18 | 2015-03-18 | |
| EP15742106.6A EP3166925B1 (en) | 2014-07-08 | 2015-07-06 | Isoindoline derivatives for use in the treatment of a viral infection |
| PCT/IB2015/055095 WO2016005878A1 (en) | 2014-07-08 | 2015-07-06 | Isoindoline derivatives for use in the treatment of a viral infection |
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| SI3166925T1 true SI3166925T1 (sl) | 2018-06-29 |
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| SI201530238T SI3166925T1 (sl) | 2014-07-08 | 2015-07-06 | Izoindolinski derivati za uporabo pri zdravljenju virusne infekcije |
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| KR (1) | KR20170024115A (sl) |
| CN (1) | CN106795141A (sl) |
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| BR (1) | BR112017000246A2 (sl) |
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| HR (1) | HRP20180639T1 (sl) |
| HU (1) | HUE037884T2 (sl) |
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| MA (1) | MA40221A (sl) |
| ME (1) | ME03066B (sl) |
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| PE (1) | PE20170440A1 (sl) |
| PH (1) | PH12016502559A1 (sl) |
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| PT (1) | PT3166925T (sl) |
| RS (1) | RS57108B1 (sl) |
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| SI (1) | SI3166925T1 (sl) |
| SM (1) | SMT201800276T1 (sl) |
| TR (1) | TR201807217T4 (sl) |
| TW (1) | TW201617331A (sl) |
| UY (1) | UY36204A (sl) |
| WO (1) | WO2016005878A1 (sl) |
| ZA (1) | ZA201608554B (sl) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6579549B2 (ja) | 2014-05-16 | 2019-09-25 | 塩野義製薬株式会社 | Hiv複製阻害作用を有する3環性複素環誘導体 |
| CA2987384A1 (en) | 2015-05-29 | 2016-12-08 | Shionogi & Co., Ltd. | Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity |
| TW201720798A (zh) * | 2015-09-17 | 2017-06-16 | Viiv醫療保健英國有限公司 | 苯并氮呯衍生物 |
| WO2017093937A1 (en) * | 2015-12-04 | 2017-06-08 | Viiv Healthcare Uk Limited | Isoindoline derivatives |
| WO2017093930A1 (en) * | 2015-12-04 | 2017-06-08 | Viiv Healthcare Uk Limited | Isoindoline derivatives |
| JP2018536000A (ja) * | 2015-12-04 | 2018-12-06 | ヴィーブ ヘルスケア ユーケー リミテッド | イソインドリン誘導体 |
| GB201604647D0 (en) | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| JP6936820B2 (ja) * | 2016-06-30 | 2021-09-22 | ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド | ヒト免疫不全ウイルス複製の阻害剤としてのアザデカリン誘導体 |
| WO2018020357A1 (en) | 2016-07-25 | 2018-02-01 | Viiv Healthcare Uk Limited | Indoline derivatives |
| WO2018051250A1 (en) | 2016-09-14 | 2018-03-22 | Viiv Healthcare Company | Combination comprising tenofovir alafenamide, bictegravir and 3tc |
| US20230382831A1 (en) * | 2020-10-12 | 2023-11-30 | Basf Se | Process for the preparation of alpha-alkyl-2-(trifluoromethyl)-benzyl alcohols |
| TW202432557A (zh) * | 2022-10-28 | 2024-08-16 | 大陸商紐歐申醫藥(上海)有限公司 | 一種含氮雜環化合物、其藥學上可接受的鹽及其製備方法與應用 |
| WO2025089372A1 (ja) * | 2023-10-26 | 2025-05-01 | 国立研究開発法人理化学研究所 | イソインドリン誘導体 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7405237B2 (en) * | 2004-07-28 | 2008-07-29 | Celgene Corporation | Isoindoline compounds and methods of their use |
| DE102007028521A1 (de) | 2007-06-21 | 2008-12-24 | Merck Patent Gmbh | Indazolamidderivate |
| DE102007041116A1 (de) | 2007-08-30 | 2009-03-05 | Merck Patent Gmbh | 1,3-Dihydro-isoindolderivate |
| GB0908394D0 (en) | 2009-05-15 | 2009-06-24 | Univ Leuven Kath | Novel viral replication inhibitors |
| US8338441B2 (en) | 2009-05-15 | 2012-12-25 | Gilead Sciences, Inc. | Inhibitors of human immunodeficiency virus replication |
| US8609653B2 (en) * | 2011-07-15 | 2013-12-17 | Glaxosmithkline Llc | Azaindole compounds and methods for treating HIV |
| CN102491932A (zh) * | 2011-12-26 | 2012-06-13 | 天津科技大学 | 一种3-吲哚啉酮类衍生物及其制备方法及其应用 |
| WO2013103738A1 (en) * | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | Napthalene acetic acid derivatives against hiv infection |
| US9006235B2 (en) | 2012-03-06 | 2015-04-14 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EP3070081B1 (en) * | 2012-04-20 | 2018-02-28 | Gilead Sciences, Inc. | Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection |
| AU2013288369B2 (en) * | 2012-07-12 | 2018-03-29 | Viiv Healthcare Uk Limited | Compounds and methods for treating HIV |
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2015
- 2015-07-06 RS RS20180469A patent/RS57108B1/sr unknown
- 2015-07-06 SI SI201530238T patent/SI3166925T1/sl unknown
- 2015-07-06 WO PCT/IB2015/055095 patent/WO2016005878A1/en not_active Ceased
- 2015-07-06 PT PT157421066T patent/PT3166925T/pt unknown
- 2015-07-06 MX MX2017000312A patent/MX2017000312A/es unknown
- 2015-07-06 US US15/314,549 patent/US10112899B2/en not_active Expired - Fee Related
- 2015-07-06 PL PL15742106T patent/PL3166925T3/pl unknown
- 2015-07-06 SM SM20180276T patent/SMT201800276T1/it unknown
- 2015-07-06 TR TR2018/07217T patent/TR201807217T4/tr unknown
- 2015-07-06 SG SG11201610746SA patent/SG11201610746SA/en unknown
- 2015-07-06 PE PE2017000008A patent/PE20170440A1/es not_active Application Discontinuation
- 2015-07-06 AU AU2015287334A patent/AU2015287334B2/en not_active Ceased
- 2015-07-06 CR CR20170005A patent/CR20170005A/es unknown
- 2015-07-06 EP EP15742106.6A patent/EP3166925B1/en active Active
- 2015-07-06 TW TW104121895A patent/TW201617331A/zh unknown
- 2015-07-06 LT LTEP15742106.6T patent/LT3166925T/lt unknown
- 2015-07-06 DK DK15742106.6T patent/DK3166925T3/en active
- 2015-07-06 CN CN201580048182.2A patent/CN106795141A/zh active Pending
- 2015-07-06 ES ES15742106.6T patent/ES2667793T3/es active Active
- 2015-07-06 KR KR1020177003445A patent/KR20170024115A/ko not_active Withdrawn
- 2015-07-06 HK HK17104954.7A patent/HK1231466A1/zh unknown
- 2015-07-06 UY UY0001036204A patent/UY36204A/es not_active Application Discontinuation
- 2015-07-06 JP JP2017500900A patent/JP2017521428A/ja active Pending
- 2015-07-06 ME MEP-2018-109A patent/ME03066B/me unknown
- 2015-07-06 HU HUE15742106A patent/HUE037884T2/hu unknown
- 2015-07-06 EA EA201692358A patent/EA030204B8/ru not_active IP Right Cessation
- 2015-07-06 RU RU2016150326A patent/RU2016150326A/ru not_active Application Discontinuation
- 2015-07-06 CA CA2954603A patent/CA2954603A1/en not_active Abandoned
- 2015-07-06 MA MA040221A patent/MA40221A/fr unknown
- 2015-07-06 HR HRP20180639TT patent/HRP20180639T1/hr unknown
- 2015-07-06 BR BR112017000246A patent/BR112017000246A2/pt not_active IP Right Cessation
-
2016
- 2016-12-12 ZA ZA2016/08554A patent/ZA201608554B/en unknown
- 2016-12-12 IL IL249520A patent/IL249520A0/en unknown
- 2016-12-21 PH PH12016502559A patent/PH12016502559A1/en unknown
- 2016-12-28 DO DO2016000336A patent/DOP2016000336A/es unknown
-
2017
- 2017-01-04 CL CL2017000014A patent/CL2017000014A1/es unknown
-
2018
- 2018-05-23 CY CY181100550T patent/CY1120607T1/el unknown
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