CN102066384B - 作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 - Google Patents
作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 Download PDFInfo
- Publication number
- CN102066384B CN102066384B CN200980123841.9A CN200980123841A CN102066384B CN 102066384 B CN102066384 B CN 102066384B CN 200980123841 A CN200980123841 A CN 200980123841A CN 102066384 B CN102066384 B CN 102066384B
- Authority
- CN
- China
- Prior art keywords
- base
- pyrimidyl
- methyl
- mmol
- phenyl
- 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.)
- Expired - Fee Related
Links
- 0 *NC(*C1(C(CC2)CCN2C1)O)=S Chemical compound *NC(*C1(C(CC2)CCN2C1)O)=S 0.000 description 7
- OMNHZKWWQQBAMJ-UHFFFAOYSA-N Clc1cccc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 Chemical compound Clc1cccc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 OMNHZKWWQQBAMJ-UHFFFAOYSA-N 0.000 description 2
- ITSVVVSRQGZFAZ-UYJHFMRCSA-N Brc1cccc2c1cc(NC1=NC[C@]3(C(C4)C4(CC4)N4C3)O1)nc2 Chemical compound Brc1cccc2c1cc(NC1=NC[C@]3(C(C4)C4(CC4)N4C3)O1)nc2 ITSVVVSRQGZFAZ-UYJHFMRCSA-N 0.000 description 1
- JORBPZWZVPZZKU-SFHVURJKSA-N C(CC1)CC1Oc1cnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)nc1 Chemical compound C(CC1)CC1Oc1cnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)nc1 JORBPZWZVPZZKU-SFHVURJKSA-N 0.000 description 1
- HIZRKONTEWLCNT-INIZCTEOSA-N C/N=C(/Nc(nc1)cc2c1c(Cl)cc(Cl)c2)\O[C@@H]1C(CC2)CCN2C1 Chemical compound C/N=C(/Nc(nc1)cc2c1c(Cl)cc(Cl)c2)\O[C@@H]1C(CC2)CCN2C1 HIZRKONTEWLCNT-INIZCTEOSA-N 0.000 description 1
- NNECDIRQNBQIJA-INIZCTEOSA-N C/N=C(/Nc1cc(cccc2)c2cn1)\O[C@@H]1C(CC2)CCN2C1 Chemical compound C/N=C(/Nc1cc(cccc2)c2cn1)\O[C@@H]1C(CC2)CCN2C1 NNECDIRQNBQIJA-INIZCTEOSA-N 0.000 description 1
- UUKUVVDEABNKOV-NSHDSACASA-N C/N=C(/Nc1ncnc(SC)c1)\O[C@@H]1C(CC2)CCN2C1 Chemical compound C/N=C(/Nc1ncnc(SC)c1)\O[C@@H]1C(CC2)CCN2C1 UUKUVVDEABNKOV-NSHDSACASA-N 0.000 description 1
- PXWGDZJDUOPMGQ-IBGZPJMESA-N C1N=C(Nc(cc2)nnc2-c2ccccc2)O[C@@]11C(CC2)CCN2C1 Chemical compound C1N=C(Nc(cc2)nnc2-c2ccccc2)O[C@@]11C(CC2)CCN2C1 PXWGDZJDUOPMGQ-IBGZPJMESA-N 0.000 description 1
- AVLCTLDGDXTCNZ-FQEVSTJZSA-N C1N=C(Nc2cc(-c3ccccc3)ncc2)O[C@@]11C(CC2)CCN2C1 Chemical compound C1N=C(Nc2cc(-c3ccccc3)ncc2)O[C@@]11C(CC2)CCN2C1 AVLCTLDGDXTCNZ-FQEVSTJZSA-N 0.000 description 1
- FGGUQMSYRSJAII-AWEZNQCLSA-N C1N=C(Nc2ccncc2)O[C@@]11C(CC2)CCN2C1 Chemical compound C1N=C(Nc2ccncc2)O[C@@]11C(CC2)CCN2C1 FGGUQMSYRSJAII-AWEZNQCLSA-N 0.000 description 1
- XNKKRHBZOMRNQS-HNNXBMFYSA-N C1N=C(Nc2nc(nccc3)c3[o]2)O[C@@]11C(CC2)CCN2C1 Chemical compound C1N=C(Nc2nc(nccc3)c3[o]2)O[C@@]11C(CC2)CCN2C1 XNKKRHBZOMRNQS-HNNXBMFYSA-N 0.000 description 1
- NWOGQPOGFKBIMN-UHFFFAOYSA-N C1N=C(Nc2ncccc2)OC11C(CC2)CCN2C1 Chemical compound C1N=C(Nc2ncccc2)OC11C(CC2)CCN2C1 NWOGQPOGFKBIMN-UHFFFAOYSA-N 0.000 description 1
- MTIALXJECNTTKZ-UHFFFAOYSA-N CC(C)(C)C(Nc(nc1Cl)ccc1Cl)=O Chemical compound CC(C)(C)C(Nc(nc1Cl)ccc1Cl)=O MTIALXJECNTTKZ-UHFFFAOYSA-N 0.000 description 1
- VJBULGFITURQHJ-UHFFFAOYSA-N CC(C)(C)OC(Nc1nc(ccc(C(N2CCCC2)=O)c2)c2[s]1)=O Chemical compound CC(C)(C)OC(Nc1nc(ccc(C(N2CCCC2)=O)c2)c2[s]1)=O VJBULGFITURQHJ-UHFFFAOYSA-N 0.000 description 1
- MXDFPKDNQYNZPK-UHFFFAOYSA-N CCOC(Nc([s]c1n2)nc1cnc2Cl)=O Chemical compound CCOC(Nc([s]c1n2)nc1cnc2Cl)=O MXDFPKDNQYNZPK-UHFFFAOYSA-N 0.000 description 1
- DYYIGENAVULQMH-UHFFFAOYSA-N CCOc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 Chemical compound CCOc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 DYYIGENAVULQMH-UHFFFAOYSA-N 0.000 description 1
- QBDRIJRFLYTRHO-ZDUSSCGKSA-N CCc1nnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)[o]1 Chemical compound CCc1nnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)[o]1 QBDRIJRFLYTRHO-ZDUSSCGKSA-N 0.000 description 1
- UQYIJTRKEBHOPX-UHFFFAOYSA-N CN(C)c1ncc2nc(N)[s]c2n1 Chemical compound CN(C)c1ncc2nc(N)[s]c2n1 UQYIJTRKEBHOPX-UHFFFAOYSA-N 0.000 description 1
- QOOQUMTZWQEHTR-UHFFFAOYSA-N COCc1cc(Cl)ncn1 Chemical compound COCc1cc(Cl)ncn1 QOOQUMTZWQEHTR-UHFFFAOYSA-N 0.000 description 1
- ZEEJRACEEDQANN-UHFFFAOYSA-N COCc1ncnc(N)c1 Chemical compound COCc1ncnc(N)c1 ZEEJRACEEDQANN-UHFFFAOYSA-N 0.000 description 1
- YJZQFLXZZGZDKK-UHFFFAOYSA-N COc(cc1)cc(nc2)c1nc2NCc(c(OC)c1)ccc1OC Chemical compound COc(cc1)cc(nc2)c1nc2NCc(c(OC)c1)ccc1OC YJZQFLXZZGZDKK-UHFFFAOYSA-N 0.000 description 1
- OHUNPVCHRGBDHH-AWEZNQCLSA-N COc1cc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)ncn1 Chemical compound COc1cc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)ncn1 OHUNPVCHRGBDHH-AWEZNQCLSA-N 0.000 description 1
- HVISHPMAJALNPD-UHFFFAOYSA-N CSC(SC)=Nc([s]c1n2)nc1ncc2[BrH]C Chemical compound CSC(SC)=Nc([s]c1n2)nc1ncc2[BrH]C HVISHPMAJALNPD-UHFFFAOYSA-N 0.000 description 1
- KZGYCTBSZHPCAQ-UHFFFAOYSA-N CSC(SC)=Nc1nc2cccnc2[s]1 Chemical compound CSC(SC)=Nc1nc2cccnc2[s]1 KZGYCTBSZHPCAQ-UHFFFAOYSA-N 0.000 description 1
- IPBKLPYWVRTALX-UHFFFAOYSA-N CSc1ncc(N)nc1 Chemical compound CSc1ncc(N)nc1 IPBKLPYWVRTALX-UHFFFAOYSA-N 0.000 description 1
- MBJZFTGABOXAIZ-HNNXBMFYSA-N C[C@]1(C(CC2)CCN2C1)O/C(/Nc1nc(ncc(Br)n2)c2[s]1)=N\C Chemical compound C[C@]1(C(CC2)CCN2C1)O/C(/Nc1nc(ncc(Br)n2)c2[s]1)=N\C MBJZFTGABOXAIZ-HNNXBMFYSA-N 0.000 description 1
- PMEUWXPHAUSCND-IBGZPJMESA-N Cc(cc1)cc2c1cnc(NC1=NC[C@]3(C(CC4)CCN4C3)O1)c2 Chemical compound Cc(cc1)cc2c1cnc(NC1=NC[C@]3(C(CC4)CCN4C3)O1)c2 PMEUWXPHAUSCND-IBGZPJMESA-N 0.000 description 1
- PCLVDKIBTLXQTR-INIZCTEOSA-N Cc(nc1OC)nc2c1nc(NC1=NC[C@]3(C(CC4)CCN4C3)O1)[s]2 Chemical compound Cc(nc1OC)nc2c1nc(NC1=NC[C@]3(C(CC4)CCN4C3)O1)[s]2 PCLVDKIBTLXQTR-INIZCTEOSA-N 0.000 description 1
- OZEMQJOXYRKPEG-UHFFFAOYSA-N Cc1c(-c(cc2)ccc2OC)nc(NC2=NCC3(C(CC4)CCN4C3)O2)[s]1 Chemical compound Cc1c(-c(cc2)ccc2OC)nc(NC2=NCC3(C(CC4)CCN4C3)O2)[s]1 OZEMQJOXYRKPEG-UHFFFAOYSA-N 0.000 description 1
- FAVQBTZVFUKSOP-ZDUSSCGKSA-N Cc1c(C)nc(N/C(/O[C@@H]2C(CC3)CCN3C2)=N/C)nc1 Chemical compound Cc1c(C)nc(N/C(/O[C@@H]2C(CC3)CCN3C2)=N/C)nc1 FAVQBTZVFUKSOP-ZDUSSCGKSA-N 0.000 description 1
- ZZQSEVQIMITDMU-UHFFFAOYSA-N Cc1cc2ncc(N=C=S)nc2cc1 Chemical compound Cc1cc2ncc(N=C=S)nc2cc1 ZZQSEVQIMITDMU-UHFFFAOYSA-N 0.000 description 1
- OXMVTMRZGPMPEJ-UHFFFAOYSA-N Cc1cccc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 Chemical compound Cc1cccc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 OXMVTMRZGPMPEJ-UHFFFAOYSA-N 0.000 description 1
- IELZPOFKHRZRGS-UHFFFAOYSA-N Cc1cnc(N)nc1C Chemical compound Cc1cnc(N)nc1C IELZPOFKHRZRGS-UHFFFAOYSA-N 0.000 description 1
- NYKOHJDWRQIEQZ-UHFFFAOYSA-N Cc1n[o]c(N=C(SC)SC)n1 Chemical compound Cc1n[o]c(N=C(SC)SC)n1 NYKOHJDWRQIEQZ-UHFFFAOYSA-N 0.000 description 1
- UHFZBJIRVAMIPP-LBPRGKRZSA-N Cc1n[s]c(NC2=NC[C@]3(C(CC4)CCN4C3)O2)n1 Chemical compound Cc1n[s]c(NC2=NC[C@]3(C(CC4)CCN4C3)O2)n1 UHFZBJIRVAMIPP-LBPRGKRZSA-N 0.000 description 1
- IWZSFFYAXNHSIT-UHFFFAOYSA-N Cc1nc(OC)c2nc(N=C(SC)SC)[s]c2n1 Chemical compound Cc1nc(OC)c2nc(N=C(SC)SC)[s]c2n1 IWZSFFYAXNHSIT-UHFFFAOYSA-N 0.000 description 1
- LLSDHTXRWBJQEM-LBPRGKRZSA-N Cc1nnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)[o]1 Chemical compound Cc1nnc(NC2=NC[C@]3(C(CC4)CCN4C3)O2)[o]1 LLSDHTXRWBJQEM-LBPRGKRZSA-N 0.000 description 1
- KRNABMMFSKMSJJ-INIZCTEOSA-N Clc(cc1)cc2c1[o]c(NC1=NC[C@]3(C(CC4)CCN4C3)O1)n2 Chemical compound Clc(cc1)cc2c1[o]c(NC1=NC[C@]3(C(CC4)CCN4C3)O1)n2 KRNABMMFSKMSJJ-INIZCTEOSA-N 0.000 description 1
- JFPMKTAXLLHMRR-UHFFFAOYSA-N Clc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 Chemical compound Clc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 JFPMKTAXLLHMRR-UHFFFAOYSA-N 0.000 description 1
- HWDPAJOAZGEWFR-DBRPNBKGSA-N Clc(cc1Cl)cnc1NC1=NC[C@]2(C(C3)C3(CC3)N3C2)O1 Chemical compound Clc(cc1Cl)cnc1NC1=NC[C@]2(C(C3)C3(CC3)N3C2)O1 HWDPAJOAZGEWFR-DBRPNBKGSA-N 0.000 description 1
- KHQUNFNAMOIACW-AWEZNQCLSA-N Clc(ccc(NC1=NC[C@]2(C(CC3)CCN3C2)O1)n1)c1Cl Chemical compound Clc(ccc(NC1=NC[C@]2(C(CC3)CCN3C2)O1)n1)c1Cl KHQUNFNAMOIACW-AWEZNQCLSA-N 0.000 description 1
- LBUXNSKRWJUOKM-AWEZNQCLSA-N Fc1cc(Cl)cnc1NC1=NC[C@]2(C(CC3)CCN3C2)O1 Chemical compound Fc1cc(Cl)cnc1NC1=NC[C@]2(C(CC3)CCN3C2)O1 LBUXNSKRWJUOKM-AWEZNQCLSA-N 0.000 description 1
- VZBQNKTUVDZSCW-UHFFFAOYSA-N Nc1nc(ccc(C(N2CCCC2)=O)c2)c2[s]1 Chemical compound Nc1nc(ccc(C(N2CCCC2)=O)c2)c2[s]1 VZBQNKTUVDZSCW-UHFFFAOYSA-N 0.000 description 1
- OJFPBPCGCSPJIH-UHFFFAOYSA-N O=C(c(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2)N1CCCC1 Chemical compound O=C(c(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2)N1CCCC1 OJFPBPCGCSPJIH-UHFFFAOYSA-N 0.000 description 1
- UDLFPPHYXDHXCU-UHFFFAOYSA-N Oc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 Chemical compound Oc(cc1)cc2c1nc(NC1=NCC3(C(CC4)CCN4C3)O1)[s]2 UDLFPPHYXDHXCU-UHFFFAOYSA-N 0.000 description 1
- MQTXWBGYHOTVHZ-UHFFFAOYSA-N S=C=Nc(nn1)ccc1Br Chemical compound S=C=Nc(nn1)ccc1Br MQTXWBGYHOTVHZ-UHFFFAOYSA-N 0.000 description 1
- VSOBZMWGTWAHSR-UHFFFAOYSA-N S=C=Nc1nc(Br)ccc1 Chemical compound S=C=Nc1nc(Br)ccc1 VSOBZMWGTWAHSR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4721108P | 2008-04-23 | 2008-04-23 | |
| US61/047,211 | 2008-04-23 | ||
| US12/423,299 US7863291B2 (en) | 2008-04-23 | 2009-04-14 | Quinuclidine compounds as alpha-7 nicotinic acetylcholine receptor ligands |
| US12/423,299 | 2009-04-14 | ||
| PCT/US2009/041076 WO2009131926A1 (en) | 2008-04-23 | 2009-04-20 | Quinuclidine compounds as alpha-7 nicotinic acetylcholine receptor ligands |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102066384A CN102066384A (zh) | 2011-05-18 |
| CN102066384B true CN102066384B (zh) | 2014-07-30 |
Family
ID=41215599
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980123841.9A Expired - Fee Related CN102066384B (zh) | 2008-04-23 | 2009-04-20 | 作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7863291B2 (https=) |
| EP (1) | EP2271650B1 (https=) |
| JP (1) | JP5389905B2 (https=) |
| KR (1) | KR20110015565A (https=) |
| CN (1) | CN102066384B (https=) |
| AR (1) | AR071215A1 (https=) |
| AU (1) | AU2009239575B2 (https=) |
| BR (1) | BRPI0911542A2 (https=) |
| CA (1) | CA2722325A1 (https=) |
| CL (1) | CL2009000975A1 (https=) |
| CO (1) | CO6300941A2 (https=) |
| CY (1) | CY1117045T1 (https=) |
| DK (1) | DK2271650T3 (https=) |
| EA (1) | EA017628B1 (https=) |
| ES (1) | ES2553753T3 (https=) |
| HR (1) | HRP20151111T1 (https=) |
| HU (1) | HUE028302T2 (https=) |
| IL (1) | IL208673A (https=) |
| MX (1) | MX2010011374A (https=) |
| NZ (1) | NZ588649A (https=) |
| PE (1) | PE20091977A1 (https=) |
| PL (1) | PL2271650T3 (https=) |
| PT (1) | PT2271650E (https=) |
| SI (1) | SI2271650T1 (https=) |
| TW (1) | TWI431007B (https=) |
| WO (1) | WO2009131926A1 (https=) |
| ZA (1) | ZA201007527B (https=) |
Families Citing this family (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8309577B2 (en) * | 2008-04-23 | 2012-11-13 | Bristol-Myers Squibb Company | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands |
| ES2398684T3 (es) | 2008-04-23 | 2013-03-21 | Gilead Sciences, Inc. | Análogos de carbanucleósido para el tratamiento antiviral |
| JP5693452B2 (ja) * | 2008-08-04 | 2015-04-01 | シーエイチディーアイ ファウンデーション,インコーポレーテッド | 特定のキヌレニン−3−モノオキシゲナーゼインヒビター、医薬組成物およびそれらの使用方法 |
| TWI453207B (zh) * | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶,其組合物及使用其之治療方法 |
| TWI483950B (zh) | 2009-09-21 | 2015-05-11 | Gilead Sciences Inc | 用於製備1’-取代碳核苷類似物之方法及中間物 |
| US8278320B2 (en) | 2009-10-28 | 2012-10-02 | Bristol-Myers Squibb Company | Azabicyclo[2.2.1]heptane compounds as alpha-7 nicotinic acetylcholine receptor ligands |
| US8507516B2 (en) | 2009-10-28 | 2013-08-13 | Bristol-Myers Squibb Company | Azabicyclic compounds as alpha-7 nicotinic acetylcholine receptor ligands |
| MX2012004560A (es) * | 2009-10-29 | 2012-05-08 | Bristol Myers Squibb Co | Compuestos de quinuclidina como ligandos del receptor de acetilcolina nicotinico alfa-7. |
| CN102834400B (zh) * | 2010-01-14 | 2015-06-10 | 赛诺菲 | 2,5-取代的*唑并嘧啶衍生物 |
| CN103025744A (zh) * | 2010-04-30 | 2013-04-03 | 百时美施贵宝公司 | 作为α-7烟碱乙酰胆碱受体配体前药的氮杂二环胺N-氧化物化合物 |
| WO2012002577A1 (ja) | 2010-06-30 | 2012-01-05 | 富士フイルム株式会社 | 新規なニコチンアミド誘導体またはその塩 |
| KR101995598B1 (ko) | 2010-07-19 | 2019-07-02 | 길리애드 사이언시즈, 인코포레이티드 | 부분입체 이성질성으로 순수한 포스포라미데이트 전구약물의 제조 방법 |
| BR122020020745B8 (pt) | 2010-07-22 | 2023-10-31 | Gilead Sciences Inc | Composto antiviral para o tratamento de infecções por paramyxoviridae e composição farmacêutica que o compreende |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| MX2014000648A (es) | 2011-07-19 | 2014-09-25 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y sus usos. |
| SI2750677T1 (sl) | 2011-08-30 | 2017-10-30 | Chdi Foundation, Inc. | Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe |
| RS54936B1 (sr) | 2011-10-14 | 2016-11-30 | Ambit Biosciences Corp | Heterociklična jedinjenja i njihova upotreba kao modulatora receptora tirozin kinaza tipa iii |
| AR090037A1 (es) | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| WO2013177024A1 (en) | 2012-05-24 | 2013-11-28 | Bristol-Myers Squibb Company | QUINUCLIDINE, 1-AZABICYCLO[2.2.1]HEPTANE, 1-AZABICYCLO [3.2.1]OCTANE, and 1-AZABICYCLO[3.2.2]NONANE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| RS58768B1 (sr) | 2013-03-14 | 2019-06-28 | Merck Patent Gmbh | Inhibitori glikozidaze |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| EP3102576B8 (en) | 2014-02-03 | 2019-06-19 | Vitae Pharmaceuticals, LLC | Dihydropyrrolopyridine inhibitors of ror-gamma |
| JP5714745B2 (ja) * | 2014-04-28 | 2015-05-07 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | α7ニコチン性アセチルコリン受容体リガンドとしてのキヌクリジン化合物 |
| CN106715421A (zh) | 2014-07-17 | 2017-05-24 | Chdi基金会股份有限公司 | 用于治疗hiv相关病症的方法和组合物 |
| KR102043337B1 (ko) | 2014-08-28 | 2019-11-11 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| PT3207043T (pt) | 2014-10-14 | 2019-03-25 | Vitae Pharmaceuticals Llc | Inibidores de di-hidropirrolopiridina de ror-gama |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| TWI767201B (zh) | 2014-10-29 | 2022-06-11 | 美商基利科學股份有限公司 | 絲狀病毒科病毒感染之治療 |
| US10174052B2 (en) | 2014-11-04 | 2019-01-08 | Bristol-Myers Squibb Company | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| WO2017024018A1 (en) | 2015-08-05 | 2017-02-09 | Vitae Pharmaceuticals, Inc. | Modulators of ror-gamma |
| SI3349758T1 (sl) | 2015-09-16 | 2022-08-31 | Gilead Sciences, Inc. | Postopki za zdravljenje okužb z virusom arenaviridae |
| US11008340B2 (en) | 2015-11-20 | 2021-05-18 | Vitae Pharmaceuticals, Llc | Modulators of ROR-gamma |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
| US11261183B2 (en) | 2016-02-25 | 2022-03-01 | Asceneuron Sa | Sulfoximine glycosidase inhibitors |
| CA3014572C (en) | 2016-02-25 | 2023-10-03 | Asceneuron S.A. | Acid addition salts of piperazine derivatives |
| KR20180132629A (ko) | 2016-02-25 | 2018-12-12 | 아셰뉴론 에스아 | 글리코시다제 저해제 |
| AU2017222964B2 (en) | 2016-02-25 | 2020-01-02 | Asceneuron S. A. | Glycosidase inhibitors |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US10682368B2 (en) | 2017-03-14 | 2020-06-16 | Gilead Sciences, Inc. | Methods of treating feline coronavirus infections |
| RU2019133646A (ru) | 2017-03-30 | 2021-04-30 | Ф. Хоффманн-Ля Рош Аг | Изохинолины в качестве ингибиторов hpk1 |
| CN110709386B (zh) | 2017-03-30 | 2022-06-07 | 凯瑞康宁生物工程(武汉)有限公司 | 双环杂芳基衍生物及其制备与用途 |
| AU2018262501B2 (en) | 2017-05-01 | 2020-12-10 | Gilead Sciences, Inc. | Crystalline forms of (S) 2 ethylbutyl 2 (((S) (((2R,3S,4R,5R) 5 (4 aminopyrrolo[2,1-f] [1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2 yl)methoxy)(phenoxy) phosphoryl)amino)propanoate |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2019014247A1 (en) | 2017-07-11 | 2019-01-17 | Gilead Sciences, Inc. | COMPOSITIONS COMPRISING POLYMERASE RNA INHIBITOR AND CYCLODEXTRIN FOR THE TREATMENT OF VIRAL INFECTIONS |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| JP2020528904A (ja) | 2017-07-24 | 2020-10-01 | ヴァイティー ファーマシューティカルズ,エルエルシー | RORγの阻害剤 |
| US11213525B2 (en) | 2017-08-24 | 2022-01-04 | Asceneuron Sa | Linear glycosidase inhibitors |
| CN107868039A (zh) * | 2017-11-27 | 2018-04-03 | 中国药科大学 | 一种贝曲沙班中间体n-(5-氯-2-吡啶基)-2-[(4-氰基苯甲酰基)氨基]-5-甲氧基苯甲酰胺的制备方法 |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| CN112601584A (zh) | 2018-07-24 | 2021-04-02 | 豪夫迈·罗氏有限公司 | 异喹啉化合物及其用途 |
| WO2020039029A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Spiro compounds as glycosidase inhibitors |
| JP7407171B2 (ja) | 2018-08-22 | 2023-12-28 | エースニューロン・ソシエテ・アノニム | グリコシダーゼ阻害剤として有用なピペラジン誘導体のコハク酸付加塩及びフマル酸付加塩 |
| WO2020039027A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Pyrrolidine glycosidase inhibitors |
| WO2020039028A1 (en) | 2018-08-22 | 2020-02-27 | Asceneuron S. A. | Tetrahydro-benzoazepine glycosidase inhibitors |
| TW202024053A (zh) | 2018-10-02 | 2020-07-01 | 美商建南德克公司 | 異喹啉化合物及其用途 |
| US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3146459A1 (en) | 2019-08-30 | 2021-03-04 | Sumitomo Dainippon Pharma Co., Ltd. | 2-aminoquinazolinone derivative |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11660307B2 (en) | 2020-01-27 | 2023-05-30 | Gilead Sciences, Inc. | Methods for treating SARS CoV-2 infections |
| JP7554841B2 (ja) | 2020-03-12 | 2024-09-20 | ギリアード サイエンシーズ, インコーポレイテッド | 1’-シアノヌクレオシドを調製する方法 |
| WO2021207049A1 (en) | 2020-04-06 | 2021-10-14 | Gilead Sciences, Inc. | Inhalation formulations of 1'-cyano substituted carbanucleoside analogs |
| CA3179226A1 (en) | 2020-05-29 | 2021-12-02 | Tomas Cihlar | Remdesivir treatment methods |
| AU2021296841B2 (en) | 2020-06-24 | 2025-01-23 | Gilead Sciences, Inc. | 1'-cyano nucleoside analogs and uses thereof |
| SI4204421T1 (sl) | 2020-08-27 | 2024-07-31 | Gilead Sciences, Inc., | Spojine in postopki za zdravljenje virusnih okužb |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| IL315102A (en) | 2022-03-02 | 2024-10-01 | Gilead Sciences Inc | COMPOSITIONS AND METHODS FOR THE TREATMENT OF VIRAL INFECTIONS |
| US12357577B1 (en) | 2024-02-02 | 2025-07-15 | Gilead Sciences, Inc. | Pharmaceutical formulations and uses thereof |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0337547A1 (en) * | 1988-04-11 | 1989-10-18 | Merck Sharp & Dohme Ltd. | Spirocyclic compounds incorporating five-membered rings with two heteroatoms |
| EP0452101A2 (en) * | 1990-04-10 | 1991-10-16 | Israel Institute For Biological Research | Spiro bridged and unbridged heterocyclic compounds |
| WO1996006098A1 (en) * | 1994-08-24 | 1996-02-29 | Astra Aktiebolag | Spiro-azabicyclic compounds useful in therapy |
| CN1129942A (zh) * | 1993-07-20 | 1996-08-28 | 以色列国有生物学研究所 | 作用于胆碱能系统的具有毒蕈碱拮抗性的氮杂螺环化合物 |
| WO2005005435A1 (en) * | 2003-07-08 | 2005-01-20 | Astrazeneca Ab | Spiro ′1-azabicyclo ′2.2.2!octan-3,5′-oxazolidin -2′-one! derivatives with affinity to the alpha7 nicotinic acetylcholine receptor |
| CN1662506A (zh) * | 2002-05-03 | 2005-08-31 | 以色列生物研究所 | 治疗中枢和周围神经系统疾病的方法和组合物及其有用的新化合物 |
| WO2006065209A1 (en) * | 2004-12-15 | 2006-06-22 | Astrazeneca Ab | Nicotinic acetylcholine receptor ligands |
| US20070004715A1 (en) * | 2005-06-30 | 2007-01-04 | Yifang Huang | Novel spiro-quinuclidinyl derivatives for the treatment of central nervous system disorders |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5053412A (en) | 1990-04-10 | 1991-10-01 | Israel Institute For Biological Research | Spiro nitrogen-bridged heterocyclic compounds |
| ITMI20061279A1 (it) | 2006-06-30 | 2008-01-01 | Consiglio Nazionale Ricerche | Agonisti nicotinici selettivi per il sottotipo recettoriale alfa7,procedimento per la loro preparazione e relative composizioni farmaceutiche |
| US8309577B2 (en) * | 2008-04-23 | 2012-11-13 | Bristol-Myers Squibb Company | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands |
-
2009
- 2009-04-14 US US12/423,299 patent/US7863291B2/en active Active
- 2009-04-20 EA EA201001696A patent/EA017628B1/ru not_active IP Right Cessation
- 2009-04-20 KR KR1020107026057A patent/KR20110015565A/ko not_active Ceased
- 2009-04-20 DK DK09733949.3T patent/DK2271650T3/en active
- 2009-04-20 PT PT97339493T patent/PT2271650E/pt unknown
- 2009-04-20 HR HRP20151111TT patent/HRP20151111T1/hr unknown
- 2009-04-20 BR BRPI0911542A patent/BRPI0911542A2/pt not_active IP Right Cessation
- 2009-04-20 ES ES09733949.3T patent/ES2553753T3/es active Active
- 2009-04-20 PL PL09733949T patent/PL2271650T3/pl unknown
- 2009-04-20 CN CN200980123841.9A patent/CN102066384B/zh not_active Expired - Fee Related
- 2009-04-20 EP EP09733949.3A patent/EP2271650B1/en active Active
- 2009-04-20 NZ NZ588649A patent/NZ588649A/en unknown
- 2009-04-20 SI SI200931324T patent/SI2271650T1/sl unknown
- 2009-04-20 AU AU2009239575A patent/AU2009239575B2/en not_active Ceased
- 2009-04-20 WO PCT/US2009/041076 patent/WO2009131926A1/en not_active Ceased
- 2009-04-20 HU HUE09733949A patent/HUE028302T2/en unknown
- 2009-04-20 JP JP2011506374A patent/JP5389905B2/ja not_active Expired - Fee Related
- 2009-04-20 CA CA2722325A patent/CA2722325A1/en not_active Abandoned
- 2009-04-20 MX MX2010011374A patent/MX2010011374A/es active IP Right Grant
- 2009-04-23 AR ARP090101442A patent/AR071215A1/es unknown
- 2009-04-23 CL CL2009000975A patent/CL2009000975A1/es unknown
- 2009-04-23 PE PE2009000562A patent/PE20091977A1/es not_active Application Discontinuation
- 2009-04-23 TW TW098113525A patent/TWI431007B/zh not_active IP Right Cessation
-
2010
- 2010-10-12 IL IL208673A patent/IL208673A/en not_active IP Right Cessation
- 2010-10-21 ZA ZA2010/07527A patent/ZA201007527B/en unknown
- 2010-10-22 CO CO10131169A patent/CO6300941A2/es active IP Right Grant
-
2015
- 2015-12-14 CY CY20151101139T patent/CY1117045T1/el unknown
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0337547A1 (en) * | 1988-04-11 | 1989-10-18 | Merck Sharp & Dohme Ltd. | Spirocyclic compounds incorporating five-membered rings with two heteroatoms |
| EP0452101A2 (en) * | 1990-04-10 | 1991-10-16 | Israel Institute For Biological Research | Spiro bridged and unbridged heterocyclic compounds |
| CN1129942A (zh) * | 1993-07-20 | 1996-08-28 | 以色列国有生物学研究所 | 作用于胆碱能系统的具有毒蕈碱拮抗性的氮杂螺环化合物 |
| WO1996006098A1 (en) * | 1994-08-24 | 1996-02-29 | Astra Aktiebolag | Spiro-azabicyclic compounds useful in therapy |
| CN1662506A (zh) * | 2002-05-03 | 2005-08-31 | 以色列生物研究所 | 治疗中枢和周围神经系统疾病的方法和组合物及其有用的新化合物 |
| WO2005005435A1 (en) * | 2003-07-08 | 2005-01-20 | Astrazeneca Ab | Spiro ′1-azabicyclo ′2.2.2!octan-3,5′-oxazolidin -2′-one! derivatives with affinity to the alpha7 nicotinic acetylcholine receptor |
| WO2006065209A1 (en) * | 2004-12-15 | 2006-06-22 | Astrazeneca Ab | Nicotinic acetylcholine receptor ligands |
| US20070004715A1 (en) * | 2005-06-30 | 2007-01-04 | Yifang Huang | Novel spiro-quinuclidinyl derivatives for the treatment of central nervous system disorders |
Non-Patent Citations (2)
| Title |
|---|
| (R)-3′-(3-Methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5′-oxazolidin]-2′-one, a Novel and Potent 7 Nicotinic Acetylcholine Receptor Partial Agonist Displays Cognitive Enhancing Properties;Ryo Tatsumi等;《J. Med. Chem》;20060616;第49卷;第4374-4383页 * |
| Novel 5-HT3 Antagonists: Indol-3-ylspiro(azabicycloalkane-3,5"(4"~)-oxazoles;C. J. Swain等;《J. Med. Chem》;19921231;第35卷;第1019-1031页 * |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102066384B (zh) | 作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 | |
| US8309577B2 (en) | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands | |
| CN105814054B (zh) | 作为tnf活性调节剂的稠合咪唑和吡唑衍生物 | |
| CN107873031B (zh) | 作为tnf活性调节剂的苯并噁嗪酮衍生物及其类似物 | |
| CN105814048A (zh) | 作为tnf活性调节剂的稠合三环苯并咪唑衍生物 | |
| CN102791718B (zh) | 作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 | |
| EP2864331B1 (en) | Positive allosteric modulators of mglur2 | |
| CN102686596A (zh) | 作为α-7烟碱乙酰胆碱受体配体的氮杂二环[2.2.1]庚烷化合物 | |
| JP5714745B2 (ja) | α7ニコチン性アセチルコリン受容体リガンドとしてのキヌクリジン化合物 | |
| HK40038625A (en) | Pyrazine compounds and uses thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20140730 Termination date: 20180420 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |