CN102395562A - 新的p2x7r拮抗剂及其用途 - Google Patents
新的p2x7r拮抗剂及其用途 Download PDFInfo
- Publication number
- CN102395562A CN102395562A CN2010800166929A CN201080016692A CN102395562A CN 102395562 A CN102395562 A CN 102395562A CN 2010800166929 A CN2010800166929 A CN 2010800166929A CN 201080016692 A CN201080016692 A CN 201080016692A CN 102395562 A CN102395562 A CN 102395562A
- Authority
- CN
- China
- Prior art keywords
- indol
- chloro
- bromo
- hydroxypropyl
- cycloheptylacetamide
- 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.)
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- 0 *CC(c1c[n]c2ccccc12)=NO Chemical compound *CC(c1c[n]c2ccccc12)=NO 0.000 description 2
- IUYJIHUNZJXWLV-UHFFFAOYSA-N CC(C[n]1c2cccc(Br)c2c(NC(CC2CCCCC2)=O)c1)O Chemical compound CC(C[n]1c2cccc(Br)c2c(NC(CC2CCCCC2)=O)c1)O IUYJIHUNZJXWLV-UHFFFAOYSA-N 0.000 description 1
- SFONSAAWBCIDER-UHFFFAOYSA-N CC(C[n]1c2cccc(Cl)c2c(NC(CCC2CCCCCC2)=O)c1)O Chemical compound CC(C[n]1c2cccc(Cl)c2c(NC(CCC2CCCCCC2)=O)c1)O SFONSAAWBCIDER-UHFFFAOYSA-N 0.000 description 1
- NYDOQLJTXSWCJK-UHFFFAOYSA-N CC(C[n]1c2nccc(Cl)c2c(NC(CC2CCCCCC2)=O)c1)O Chemical compound CC(C[n]1c2nccc(Cl)c2c(NC(CC2CCCCCC2)=O)c1)O NYDOQLJTXSWCJK-UHFFFAOYSA-N 0.000 description 1
- MYGYHZJROGQMBC-UHFFFAOYSA-N C[n]1c2cccc(Br)c2c(NC(CCC2CCCCCC2)=O)c1 Chemical compound C[n]1c2cccc(Br)c2c(NC(CCC2CCCCCC2)=O)c1 MYGYHZJROGQMBC-UHFFFAOYSA-N 0.000 description 1
- YEKWPKSJTPUULO-UHFFFAOYSA-N NCC(C[n]1c2cccc(Br)c2c(NC(CC2CCCCC2)=O)c1)O Chemical compound NCC(C[n]1c2cccc(Br)c2c(NC(CC2CCCCC2)=O)c1)O YEKWPKSJTPUULO-UHFFFAOYSA-N 0.000 description 1
- CHOANFGJVZEOFH-UHFFFAOYSA-N OCC(CO)[n]1c2cccc(Br)c2c(NC(CC2CCCCCC2)=O)c1 Chemical compound OCC(CO)[n]1c2cccc(Br)c2c(NC(CC2CCCCCC2)=O)c1 CHOANFGJVZEOFH-UHFFFAOYSA-N 0.000 description 1
- HIIVSNPXBZCNEN-UHFFFAOYSA-N OCC(CO)[n]1c2cccc(Cl)c2c(NC(CC2CCCCC2)=O)c1 Chemical compound OCC(CO)[n]1c2cccc(Cl)c2c(NC(CC2CCCCC2)=O)c1 HIIVSNPXBZCNEN-UHFFFAOYSA-N 0.000 description 1
- CVXARHQUPAZUEY-UHFFFAOYSA-N OCC(CO)[n]1c2cccc(Cl)c2c(NC(CCC2CCCCC2)=O)c1 Chemical compound OCC(CO)[n]1c2cccc(Cl)c2c(NC(CCC2CCCCC2)=O)c1 CVXARHQUPAZUEY-UHFFFAOYSA-N 0.000 description 1
- DVTXIRRZDXMDPE-UHFFFAOYSA-N OCC(CO)[n]1c2cccc(Cl)c2c(NC(CCC2CCCCCC2)=O)c1 Chemical compound OCC(CO)[n]1c2cccc(Cl)c2c(NC(CCC2CCCCCC2)=O)c1 DVTXIRRZDXMDPE-UHFFFAOYSA-N 0.000 description 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
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09005324.0 | 2009-04-14 | ||
| EP09005324 | 2009-04-14 | ||
| PCT/EP2010/053097 WO2010118921A1 (en) | 2009-04-14 | 2010-03-11 | Novel p2x7r antagonists and their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102395562A true CN102395562A (zh) | 2012-03-28 |
Family
ID=42167925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800166929A Pending CN102395562A (zh) | 2009-04-14 | 2010-03-11 | 新的p2x7r拮抗剂及其用途 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7919503B2 (enExample) |
| EP (1) | EP2243772B1 (enExample) |
| JP (1) | JP2012523440A (enExample) |
| KR (1) | KR20120006547A (enExample) |
| CN (1) | CN102395562A (enExample) |
| AT (1) | ATE541832T1 (enExample) |
| AU (1) | AU2010237302A1 (enExample) |
| BR (1) | BRPI1014902A2 (enExample) |
| CA (1) | CA2758474A1 (enExample) |
| CY (1) | CY1112758T1 (enExample) |
| DK (1) | DK2243772T3 (enExample) |
| EA (1) | EA201101479A1 (enExample) |
| ES (1) | ES2380908T3 (enExample) |
| HR (1) | HRP20120271T1 (enExample) |
| IL (1) | IL215444A0 (enExample) |
| MX (1) | MX2011010810A (enExample) |
| PL (1) | PL2243772T3 (enExample) |
| PT (1) | PT2243772E (enExample) |
| SG (1) | SG175232A1 (enExample) |
| SI (1) | SI2243772T1 (enExample) |
| SM (1) | SMT201200017B (enExample) |
| WO (1) | WO2010118921A1 (enExample) |
| ZA (1) | ZA201108305B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8815892B2 (en) | 2008-03-25 | 2014-08-26 | Affectis Pharmaceuticals Ag | P2X7R antagonists and their use |
| NZ587799A (en) * | 2008-03-25 | 2012-06-29 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| MX2012013075A (es) * | 2010-05-14 | 2012-12-17 | Affectis Pharmaceuticals Ag | Metodos novedosos para preparacion de antagonistas p2x7r. |
| WO2012110190A1 (en) | 2011-02-17 | 2012-08-23 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| EP2701719A4 (en) * | 2011-04-28 | 2015-04-22 | Claire Mitchell | METHOD FOR TREATING MACULAR OBGENATION BY MODULATION OF P2Y12 OR P2X7 RECEPTORS |
| WO2012163792A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| WO2012163456A1 (en) | 2011-05-27 | 2012-12-06 | Affectis Pharmaceuticals Ag | Novel p2x7r antagonists and their use |
| RU2014106611A (ru) * | 2011-07-22 | 2015-08-27 | Актелион Фармасьютиклз Лтд | Производные гетероциклических амидов в качестве антагонистов р2х7 рецептора |
| WO2013082565A1 (en) * | 2011-12-02 | 2013-06-06 | Michael Kaleko | Therapies for disorders of the cornea and conjunctiva |
| NZ628910A (en) * | 2012-01-20 | 2016-02-26 | Actelion Pharmaceuticals Ltd | Heterocyclic amide derivatives as p2x7 receptor antagonists |
| PL2931717T3 (pl) | 2012-12-12 | 2017-05-31 | Actelion Pharmaceuticals Ltd. | Pochodne indolokarboksyamidu jako antagoniści receptora p2x7 |
| AR094053A1 (es) | 2012-12-18 | 2015-07-08 | Actelion Pharmaceuticals Ltd | Derivados de indol carboxamida como antagonistas del receptor p2x₇ |
| EP2956457B1 (en) | 2013-01-22 | 2016-11-23 | Actelion Pharmaceuticals Ltd | Heterocyclic amide derivatives as p2x7 receptor antagonists |
| ES2616114T3 (es) | 2013-01-22 | 2017-06-09 | Actelion Pharmaceuticals Ltd. | Derivados de amida heterocíclica como antagonistas del receptor P2X7 |
| WO2014182601A1 (en) | 2013-05-08 | 2014-11-13 | Children's Medical Center Corporation | A method of preventing and treating type 1 diabetes, allograft rejection and lung fibrosis (by targeting the atp/p2x7r axis) |
| TW202043198A (zh) * | 2019-01-17 | 2020-12-01 | 美商Ifm Due有限公司 | 用於治療與sting活性相關之病況的化合物及組合物 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3705175A (en) * | 1969-04-01 | 1972-12-05 | Egyt Gyogyszervegyeszeti Gyar | Indazole-3-carboxylic amides |
| CN1742004A (zh) * | 2003-02-18 | 2006-03-01 | 方济各安吉利克化学联合股份有限公司 | 具有止痛活性的吲唑酰胺类 |
| WO2009023623A1 (en) * | 2007-08-10 | 2009-02-19 | H, Lundbeck A/S | Heteroaryl amide analogues |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA981532B (en) | 1997-02-26 | 1999-08-24 | Glaxo Group Ltd | Reverse hydroxamate derivatives as matrix metalloprotease inhibitors, metalloprotease inhibitors, and TNF alpha inhibitors. |
| ZA988967B (en) | 1997-10-03 | 2000-04-03 | Du Pont Pharm Co | Lactam metalloprotease inhibitors. |
| SE9704544D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Pharma Prod | Novel compounds |
| SE9704546D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Pharma Prod | Novel compounds |
| SE9704545D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Pharma Prod | Novel compounds |
| EP1087937A1 (en) | 1998-06-17 | 2001-04-04 | Du Pont Pharmaceuticals Company | Cyclic hydroxamic acids as metalloproteinase inhibitors |
| US6239151B1 (en) | 1998-06-26 | 2001-05-29 | Hoffmann-La Roche Inc. | Compounds as inhibitor of tumor necrosis factor alpha release |
| UA59453C2 (uk) | 1998-08-12 | 2003-09-15 | Пфайзер Продактс Інк. | Похідні гідроксипіпеколат гідроксамової кислоти як інгібітори матричних металопротеїназ |
| US20040122011A1 (en) | 1998-12-23 | 2004-06-24 | Pharmacia Corporation | Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy |
| US6225311B1 (en) | 1999-01-27 | 2001-05-01 | American Cyanamid Company | Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors |
| WO2000061569A1 (en) | 1999-04-09 | 2000-10-19 | Astrazeneca Ab | Adamantane derivatives |
| SE9901875D0 (sv) | 1999-05-25 | 1999-05-25 | Astra Pharma Prod | Novel compounds |
| SE9904505D0 (sv) | 1999-12-09 | 1999-12-09 | Astra Pharma Prod | Novel compounds |
| TWI258462B (en) | 1999-12-17 | 2006-07-21 | Astrazeneca Ab | Adamantane derivative compounds, process for preparing the same and pharmaceutical composition comprising the same |
| SE9904652D0 (sv) | 1999-12-17 | 1999-12-17 | Astra Pharma Prod | Novel Compounds |
| SE9904738D0 (sv) | 1999-12-22 | 1999-12-22 | Astra Pharma Prod | Novel compounds |
| GB0013737D0 (en) | 2000-06-07 | 2000-07-26 | Astrazeneca Ab | Novel compounds |
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- 2010-03-11 CN CN2010800166929A patent/CN102395562A/zh active Pending
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- 2010-03-11 WO PCT/EP2010/053097 patent/WO2010118921A1/en not_active Ceased
- 2010-03-11 DK DK10156190.0T patent/DK2243772T3/da active
- 2010-03-11 AU AU2010237302A patent/AU2010237302A1/en not_active Abandoned
- 2010-03-11 PL PL10156190T patent/PL2243772T3/pl unknown
- 2010-03-11 SI SI201030020T patent/SI2243772T1/sl unknown
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- 2010-03-11 EP EP10156190A patent/EP2243772B1/en not_active Not-in-force
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- 2010-03-11 JP JP2012505103A patent/JP2012523440A/ja active Pending
- 2010-03-11 CA CA2758474A patent/CA2758474A1/en not_active Abandoned
- 2010-03-11 EA EA201101479A patent/EA201101479A1/ru unknown
- 2010-03-11 MX MX2011010810A patent/MX2011010810A/es active IP Right Grant
- 2010-04-12 US US12/758,557 patent/US7919503B2/en not_active Expired - Fee Related
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- 2011-09-27 IL IL215444A patent/IL215444A0/en unknown
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2012
- 2012-03-27 HR HR20120271T patent/HRP20120271T1/hr unknown
- 2012-04-04 CY CY20121100340T patent/CY1112758T1/el unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| EP2243772B1 (en) | 2012-01-18 |
| JP2012523440A (ja) | 2012-10-04 |
| BRPI1014902A2 (pt) | 2016-04-19 |
| AU2010237302A1 (en) | 2011-12-01 |
| ES2380908T3 (es) | 2012-05-21 |
| PL2243772T3 (pl) | 2012-05-31 |
| CA2758474A1 (en) | 2010-10-21 |
| CY1112758T1 (el) | 2016-02-10 |
| EP2243772A1 (en) | 2010-10-27 |
| ATE541832T1 (de) | 2012-02-15 |
| US20100267762A1 (en) | 2010-10-21 |
| MX2011010810A (es) | 2012-01-12 |
| US20110212992A1 (en) | 2011-09-01 |
| EA201101479A1 (ru) | 2012-05-30 |
| SMT201200017B (it) | 2012-07-10 |
| US7919503B2 (en) | 2011-04-05 |
| SG175232A1 (en) | 2011-12-29 |
| WO2010118921A1 (en) | 2010-10-21 |
| KR20120006547A (ko) | 2012-01-18 |
| DK2243772T3 (da) | 2012-02-13 |
| HRP20120271T1 (hr) | 2012-04-30 |
| PT2243772E (pt) | 2012-03-28 |
| SI2243772T1 (sl) | 2012-05-31 |
| US8268861B2 (en) | 2012-09-18 |
| IL215444A0 (en) | 2011-12-29 |
| ZA201108305B (en) | 2012-08-29 |
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