TWI739783B - 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 - Google Patents
作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 Download PDFInfo
- Publication number
- TWI739783B TWI739783B TW105143703A TW105143703A TWI739783B TW I739783 B TWI739783 B TW I739783B TW 105143703 A TW105143703 A TW 105143703A TW 105143703 A TW105143703 A TW 105143703A TW I739783 B TWI739783 B TW I739783B
- Authority
- TW
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- Prior art keywords
- alkyl
- group
- het
- substituted
- heterocyclic group
- Prior art date
Links
- 0 *[C@@](CCO*)CC1(*)c2cc(-c3nc(*=*=I)ncc3*)cc(C#N)c2N(*)C1 Chemical compound *[C@@](CCO*)CC1(*)c2cc(-c3nc(*=*=I)ncc3*)cc(C#N)c2N(*)C1 0.000 description 7
- QQHCZIGCKZYIJK-UHFFFAOYSA-N CC(C)(C)OC(N(CC(C)(C)c1cc(-c2ccnc(Nc(cc(c(C(O)=O)c3)Cl)c3OC)n2)c2)c1c2C#N)=O Chemical compound CC(C)(C)OC(N(CC(C)(C)c1cc(-c2ccnc(Nc(cc(c(C(O)=O)c3)Cl)c3OC)n2)c2)c1c2C#N)=O QQHCZIGCKZYIJK-UHFFFAOYSA-N 0.000 description 1
- SLTBEMKENUGZDJ-UHFFFAOYSA-N CC(C)(C)OC(N(CC1(C)C)c2c1cc(B1OC(C)(C)C(C)(C)O1)cc2C#N)=O Chemical compound CC(C)(C)OC(N(CC1(C)C)c2c1cc(B1OC(C)(C)C(C)(C)O1)cc2C#N)=O SLTBEMKENUGZDJ-UHFFFAOYSA-N 0.000 description 1
- ZMZLWAWOJPOEOI-JGCGQSQUSA-N CC(C)(C)[Si](C)(C)OC[C@]1(C)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(F)c4)c4OC4CC4)n3)cc(C#N)c2NC1 Chemical compound CC(C)(C)[Si](C)(C)OC[C@]1(C)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(F)c4)c4OC4CC4)n3)cc(C#N)c2NC1 ZMZLWAWOJPOEOI-JGCGQSQUSA-N 0.000 description 1
- SQDXMSPXVYLVFO-JGCGQSQUSA-N CC(C)(C)[Si](C)(C)OC[C@]1(C)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(OC4CC4)c4)c4F)n3)cc(C#N)c2NC1 Chemical compound CC(C)(C)[Si](C)(C)OC[C@]1(C)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(OC4CC4)c4)c4F)n3)cc(C#N)c2NC1 SQDXMSPXVYLVFO-JGCGQSQUSA-N 0.000 description 1
- BAIUUICQTSVWSL-UHFFFAOYSA-N CC(C)COC(OC(c1cc(NC(C)=O)c(C)cc1)=O)=O Chemical compound CC(C)COC(OC(c1cc(NC(C)=O)c(C)cc1)=O)=O BAIUUICQTSVWSL-UHFFFAOYSA-N 0.000 description 1
- BLDOZYVSDJRZKH-UHFFFAOYSA-N CC(C)N(CC1)CCN1C(Cc(ccc(Cl)c1)c1N)=O Chemical compound CC(C)N(CC1)CCN1C(Cc(ccc(Cl)c1)c1N)=O BLDOZYVSDJRZKH-UHFFFAOYSA-N 0.000 description 1
- ZHXITFMUFDDONY-UHFFFAOYSA-N CC1(CO)c2cc(-c3ccnc(Nc4c(C)ccc(C#N)c4)n3)cc(C#N)c2NC1 Chemical compound CC1(CO)c2cc(-c3ccnc(Nc4c(C)ccc(C#N)c4)n3)cc(C#N)c2NC1 ZHXITFMUFDDONY-UHFFFAOYSA-N 0.000 description 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N CN1CCNCC1 Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- XNBLEAGPKPYTCT-UHFFFAOYSA-N CNC(c(ccc(F)c1)c1F)=O Chemical compound CNC(c(ccc(F)c1)c1F)=O XNBLEAGPKPYTCT-UHFFFAOYSA-N 0.000 description 1
- VCVQUCAIJKTZQU-UHFFFAOYSA-N COC(c(cc(c([N+]([O-])=O)c1)OC)c1Cl)=O Chemical compound COC(c(cc(c([N+]([O-])=O)c1)OC)c1Cl)=O VCVQUCAIJKTZQU-UHFFFAOYSA-N 0.000 description 1
- LUISPVNHVFUFES-UHFFFAOYSA-N COC(c(cc(cc1)[N+]([O-])=O)c1C1=CCOCC1)OC Chemical compound COC(c(cc(cc1)[N+]([O-])=O)c1C1=CCOCC1)OC LUISPVNHVFUFES-UHFFFAOYSA-N 0.000 description 1
- WVPMJFDSKVTEIQ-UHFFFAOYSA-N COc(c([N+]([O-])=O)c1)cc(CO)c1Cl Chemical compound COc(c([N+]([O-])=O)c1)cc(CO)c1Cl WVPMJFDSKVTEIQ-UHFFFAOYSA-N 0.000 description 1
- LEEIHBRGOFAAKY-UHFFFAOYSA-N COc(cc(cc1)C(NC2CCOCC2)=O)c1[N+]([O-])=O Chemical compound COc(cc(cc1)C(NC2CCOCC2)=O)c1[N+]([O-])=O LEEIHBRGOFAAKY-UHFFFAOYSA-N 0.000 description 1
- DRDOUUATQDCECH-UHFFFAOYSA-N CS(c(cc1)cc(C#CC2CC2)c1[N+]([O-])=O)(=O)=O Chemical compound CS(c(cc1)cc(C#CC2CC2)c1[N+]([O-])=O)(=O)=O DRDOUUATQDCECH-UHFFFAOYSA-N 0.000 description 1
- ZHXITFMUFDDONY-HSZRJFAPSA-N C[C@@]1(CO)c(cc(cc2C#N)-c3ccnc(Nc4cc(C#N)ccc4C)n3)c2NC1 Chemical compound C[C@@]1(CO)c(cc(cc2C#N)-c3ccnc(Nc4cc(C#N)ccc4C)n3)c2NC1 ZHXITFMUFDDONY-HSZRJFAPSA-N 0.000 description 1
- RUAYESDPZPQWKG-XMMPIXPASA-N C[C@@]1(CO)c2cc(-c3ccnc(Nc(c(C)c4)cc(C(NC)=O)c4F)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(CO)c2cc(-c3ccnc(Nc(c(C)c4)cc(C(NC)=O)c4F)n3)cc(C#N)c2NC1 RUAYESDPZPQWKG-XMMPIXPASA-N 0.000 description 1
- WPMMAADCSGORHR-AREMUKBSSA-N C[C@@]1(CO)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(F)c4)c4OC4CC4)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(CO)c2cc(-c3ccnc(Nc(cc(C(NC)=O)c(F)c4)c4OC4CC4)n3)cc(C#N)c2NC1 WPMMAADCSGORHR-AREMUKBSSA-N 0.000 description 1
- IGIVJMJBNABMTD-HHHXNRCGSA-N C[C@@]1(CO)c2cc(-c3ccnc(Nc(cc4C(NCC5COC5)=O)c(C)cc4F)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(CO)c2cc(-c3ccnc(Nc(cc4C(NCC5COC5)=O)c(C)cc4F)n3)cc(C#N)c2NC1 IGIVJMJBNABMTD-HHHXNRCGSA-N 0.000 description 1
- KTKIDNLSWOEHAZ-AREMUKBSSA-N C[C@@]1(CO)c2cc(-c3ccnc(Nc4c(CCCCN)ccc(C#N)c4)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(CO)c2cc(-c3ccnc(Nc4c(CCCCN)ccc(C#N)c4)n3)cc(C#N)c2NC1 KTKIDNLSWOEHAZ-AREMUKBSSA-N 0.000 description 1
- UHQFQXCDWMDXTR-XMMPIXPASA-N C[C@@]1(CO)c2cc(-c3ccnc(Nc4cc(C#N)cc(C(O)=O)c4C)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(CO)c2cc(-c3ccnc(Nc4cc(C#N)cc(C(O)=O)c4C)n3)cc(C#N)c2NC1 UHQFQXCDWMDXTR-XMMPIXPASA-N 0.000 description 1
- ZEJZWWAPHPFXAK-RUZDIDTESA-N C[C@@]1(COC(C)=O)c2cc(-c3ccnc(Nc4cc(C#N)ccc4C)n3)cc(C#N)c2NC1 Chemical compound C[C@@]1(COC(C)=O)c2cc(-c3ccnc(Nc4cc(C#N)ccc4C)n3)cc(C#N)c2NC1 ZEJZWWAPHPFXAK-RUZDIDTESA-N 0.000 description 1
- IQPLGOCGOCXUPI-UHFFFAOYSA-N Cc(c(C1=CCNCC1)c1)cc([N+]([O-])=O)c1OC Chemical compound Cc(c(C1=CCNCC1)c1)cc([N+]([O-])=O)c1OC IQPLGOCGOCXUPI-UHFFFAOYSA-N 0.000 description 1
- AXXXTPRFYAKSGZ-UHFFFAOYSA-N Cc(c([N+]([O-])=O)c1)cc(-c2c[n](C)nc2)c1C#N Chemical compound Cc(c([N+]([O-])=O)c1)cc(-c2c[n](C)nc2)c1C#N AXXXTPRFYAKSGZ-UHFFFAOYSA-N 0.000 description 1
- UBAWHHHAAFFKGE-UHFFFAOYSA-N Cc(c([N+]([O-])=O)c1)cc(F)c1C(O)=O Chemical compound Cc(c([N+]([O-])=O)c1)cc(F)c1C(O)=O UBAWHHHAAFFKGE-UHFFFAOYSA-N 0.000 description 1
- MBNOTYINXNBURZ-UHFFFAOYSA-N Cc(c([N+]([O-])=O)cc(Cl)c1)c1C(N1CCN(C)CC1)=O Chemical compound Cc(c([N+]([O-])=O)cc(Cl)c1)c1C(N1CCN(C)CC1)=O MBNOTYINXNBURZ-UHFFFAOYSA-N 0.000 description 1
- WLWGJMFTWWHOOR-UHFFFAOYSA-N Cc(cc(C1CN(C)CCC1)c(C#N)c1)c1N Chemical compound Cc(cc(C1CN(C)CCC1)c(C#N)c1)c1N WLWGJMFTWWHOOR-UHFFFAOYSA-N 0.000 description 1
- WRXKWGJLBYHGKE-UHFFFAOYSA-N Cc1cc(F)c(CO)cc1[N+]([O-])=O Chemical compound Cc1cc(F)c(CO)cc1[N+]([O-])=O WRXKWGJLBYHGKE-UHFFFAOYSA-N 0.000 description 1
- MPYNYOFTORDKNG-UHFFFAOYSA-N Cc1cc([N+]([O-])=O)c(CN2CCOCC2)cc1 Chemical compound Cc1cc([N+]([O-])=O)c(CN2CCOCC2)cc1 MPYNYOFTORDKNG-UHFFFAOYSA-N 0.000 description 1
- BFELLSYKJYHQOF-UHFFFAOYSA-N N#Cc1cc([N+]([O-])=O)c(CN2CCOCC2)cc1 Chemical compound N#Cc1cc([N+]([O-])=O)c(CN2CCOCC2)cc1 BFELLSYKJYHQOF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/535—Organo-phosphoranes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16152416 | 2016-01-22 | ||
| EP16152416.0 | 2016-01-22 | ||
| EP16159651.5 | 2016-03-10 | ||
| EP16159651 | 2016-03-10 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201728577A TW201728577A (zh) | 2017-08-16 |
| TWI739783B true TWI739783B (zh) | 2021-09-21 |
Family
ID=57868252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW105143703A TWI739783B (zh) | 2016-01-22 | 2017-01-20 | 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US11180487B2 (OSRAM) |
| EP (1) | EP3405196B1 (OSRAM) |
| JP (1) | JP6910359B2 (OSRAM) |
| KR (1) | KR102784966B1 (OSRAM) |
| CN (1) | CN108697710B (OSRAM) |
| AU (1) | AU2017209935B2 (OSRAM) |
| BR (1) | BR112018014675B1 (OSRAM) |
| CA (1) | CA3011880A1 (OSRAM) |
| DK (1) | DK3405196T3 (OSRAM) |
| ES (1) | ES2775449T3 (OSRAM) |
| HR (1) | HRP20200133T1 (OSRAM) |
| HU (1) | HUE047684T2 (OSRAM) |
| IL (1) | IL260500B (OSRAM) |
| LT (1) | LT3405196T (OSRAM) |
| MX (1) | MX2018008974A (OSRAM) |
| PH (1) | PH12018501567A1 (OSRAM) |
| SI (1) | SI3405196T1 (OSRAM) |
| TW (1) | TWI739783B (OSRAM) |
| WO (1) | WO2017125530A1 (OSRAM) |
| ZA (1) | ZA201804688B (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI3405196T1 (sl) | 2016-01-22 | 2020-03-31 | Janssen Pharmaceutica Nv | Novi substituirani derivati cianoindolina kot inhibitorji NIK |
| KR102720461B1 (ko) | 2016-01-22 | 2024-10-21 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체 |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| CA3027416A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| WO2018019204A1 (zh) * | 2016-07-26 | 2018-02-01 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| BR112020006294A2 (pt) * | 2017-09-30 | 2020-10-06 | Shanghai Haihe Pharmaceutical Co., Ltd. | composto com atividade inibidora da erk quinase e seu uso |
| TW202045008A (zh) | 2019-02-01 | 2020-12-16 | 印度商皮埃企業有限公司 | 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途 |
| BR112021019508A2 (pt) * | 2019-04-02 | 2022-02-01 | Hinova Pharmaceuticals Inc | Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4 |
| RS66105B1 (sr) | 2019-05-31 | 2024-11-29 | Janssen Pharmaceutica Nv | Inhibitori malih molekula nf-kb koji indukuju kinazu |
| WO2021242505A1 (en) | 2020-05-08 | 2021-12-02 | Halia Therapeutics, Inc. | Inhibitors of nek7 kinase |
| US20240285599A1 (en) * | 2021-08-23 | 2024-08-29 | Osaka University | Mature-Hepatocyte Transdifferentiation Suppressing Composition |
| WO2024059200A1 (en) | 2022-09-14 | 2024-03-21 | Halia Therapeutics, Inc. | Nek7 inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2386218A1 (en) | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
| CA2400447C (en) | 2000-02-17 | 2008-04-22 | Amgen Inc. | Kinase inhibitors |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| ES2292753T4 (es) * | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
| HUP0402352A2 (hu) | 2001-06-19 | 2005-02-28 | Bristol-Myers Squibb Co. | Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| WO2003030909A1 (en) * | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| NZ589843A (en) | 2008-06-27 | 2012-12-21 | Avila Therapeutics Inc | Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors |
| CN108752280A (zh) | 2009-08-17 | 2018-11-06 | 纪念斯隆-凯特琳癌症中心 | 热休克蛋白结合化合物、组合物以及其制备和使用方法 |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| KR101764952B1 (ko) | 2010-07-29 | 2017-08-03 | 리겔 파마슈티칼스, 인크. | Ampk-활성화 헤테로시클릭 화합물 및 그의 사용 방법 |
| CA2832919A1 (en) | 2011-04-12 | 2012-10-18 | Ryan C. Holcomb | Compounds, compositions, and therapeutic uses thereof |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| JP6524094B2 (ja) | 2013-08-30 | 2019-06-05 | ピーティーシー セラピューティクス, インコーポレイテッド | 置換ピリミジンBmi−1阻害剤 |
| TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 |
| TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
| WO2015154038A1 (en) | 2014-04-04 | 2015-10-08 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| KR20170030474A (ko) | 2014-05-22 | 2017-03-17 | 더 유니버시티 오브 시드니 | 오메가―3 유사체 |
| WO2016022645A1 (en) | 2014-08-06 | 2016-02-11 | Merck Sharp & Dohme Corp. | Heterocyclic cgrp receptor antagonists |
| JP6499282B2 (ja) | 2014-09-26 | 2019-04-10 | ギリアード サイエンシーズ, インコーポレイテッド | Tank結合キナーゼ阻害剤化合物として有用なアミノトリアジン誘導体 |
| CN106928216A (zh) | 2015-12-31 | 2017-07-07 | 中国科学院上海药物研究所 | 具有erk激酶抑制活性的化合物、其制备方法和用途 |
| SI3405196T1 (sl) | 2016-01-22 | 2020-03-31 | Janssen Pharmaceutica Nv | Novi substituirani derivati cianoindolina kot inhibitorji NIK |
| KR102720461B1 (ko) | 2016-01-22 | 2024-10-21 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체 |
| CN114539284A (zh) | 2016-03-16 | 2022-05-27 | 库拉肿瘤学公司 | 经取代的menin-mll抑制剂及使用方法 |
| CA3027416A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
-
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- 2017-01-20 WO PCT/EP2017/051150 patent/WO2017125530A1/en not_active Ceased
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
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| BR112018014675A2 (pt) | 2018-12-11 |
| CN108697710A (zh) | 2018-10-23 |
| JP6910359B2 (ja) | 2021-07-28 |
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| HUE047684T2 (hu) | 2020-05-28 |
| AU2017209935A1 (en) | 2018-08-09 |
| EP3405196A1 (en) | 2018-11-28 |
| ZA201804688B (en) | 2022-03-30 |
| HRP20200133T1 (hr) | 2020-05-15 |
| PH12018501567A1 (en) | 2019-01-28 |
| SI3405196T1 (sl) | 2020-03-31 |
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| IL260500B (en) | 2021-01-31 |
| KR20180100441A (ko) | 2018-09-10 |
| LT3405196T (lt) | 2020-02-25 |
| US20210087182A1 (en) | 2021-03-25 |
| KR102784966B1 (ko) | 2025-03-20 |
| ES2775449T3 (es) | 2020-07-27 |
| BR112018014675B1 (pt) | 2023-12-19 |
| AU2017209935B2 (en) | 2021-04-01 |
| TW201728577A (zh) | 2017-08-16 |
| EP3405196B1 (en) | 2019-12-04 |
| US11180487B2 (en) | 2021-11-23 |
| CA3011880A1 (en) | 2017-07-27 |
| WO2017125530A1 (en) | 2017-07-27 |
| CN108697710B (zh) | 2022-02-18 |
| JP2019504067A (ja) | 2019-02-14 |
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