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
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- 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
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- 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
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- 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 |
| HUE025528T2 (en) | 2008-04-23 | 2016-05-30 | Gilead Sciences Inc | 1'-substituted carba-nucleoside analogs for antiviral treatment |
| 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 |
| MX2012003126A (es) | 2009-09-21 | 2012-06-19 | Gilead Sciences Inc | Procesos e intermedios para la preparacion de analogos de 1'-carbonucleosidos sustituidos. |
| 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 |
| WO2011056573A1 (en) | 2009-10-28 | 2011-05-12 | Bristol-Myers Squibb Company | Azabicyclic compounds as alpha-7 nicotinic acetylcholine receptor ligands |
| CN102791718B (zh) * | 2009-10-29 | 2015-11-25 | 百时美施贵宝公司 | 作为α-7烟碱乙酰胆碱受体配体的奎宁环化合物 |
| MX2012007837A (es) | 2010-01-14 | 2012-07-30 | Sanofi Sa | Derivados de oxazolopirimidina 2, 5 - sustituidos. |
| 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 |
| ES2689103T3 (es) | 2010-06-30 | 2018-11-08 | Fujifilm Corporation | Nuevo derivado de nicotinamida o sal del mismo |
| AU2011282241B2 (en) | 2010-07-19 | 2015-07-30 | Gilead Sciences, Inc. | Methods for the preparation of diasteromerically pure phosphoramidate prodrugs |
| ES2524356T3 (es) | 2010-07-22 | 2014-12-05 | Gilead Sciences, Inc. | Métodos y compuestos para tratar infecciones provocadas por virus Paramyxoviridae |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| AR088218A1 (es) | 2011-07-19 | 2014-05-21 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos utiles como inhibidores de pi3k |
| SI2750677T1 (sl) | 2011-08-30 | 2017-10-30 | Chdi Foundation, Inc. | Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe |
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