CN105008346B - 作为磷酸二酯酶10（pde-10）抑制剂的嘧啶衍生物 - Google Patents
作为磷酸二酯酶10（pde-10）抑制剂的嘧啶衍生物 Download PDFInfo
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- CN105008346B CN105008346B CN201480006098.XA CN201480006098A CN105008346B CN 105008346 B CN105008346 B CN 105008346B CN 201480006098 A CN201480006098 A CN 201480006098A CN 105008346 B CN105008346 B CN 105008346B
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- Prior art keywords
- bromo
- pyrimidine
- diamine
- pyrazol
- prop
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- 0 CC(C)c1cc(*)nc(SC)n1 Chemical compound CC(C)c1cc(*)nc(SC)n1 0.000 description 3
Classifications
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
-
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ESP201330082 | 2013-01-24 | ||
| ES201330082A ES2480341B1 (es) | 2013-01-24 | 2013-01-24 | Nuevos derivados de pirimidina como inhibidores de la fosfodiesterasa 10 (PDE-10) |
| PCT/EP2014/051290 WO2014114695A1 (en) | 2013-01-24 | 2014-01-23 | New pyrimidine derivatives as phosphodiesterase 10 inhibitors (pde-10) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105008346A CN105008346A (zh) | 2015-10-28 |
| CN105008346B true CN105008346B (zh) | 2018-11-13 |
Family
ID=50071592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480006098.XA Active CN105008346B (zh) | 2013-01-24 | 2014-01-23 | 作为磷酸二酯酶10（pde-10）抑制剂的嘧啶衍生物 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9447095B2 (https=) |
| EP (1) | EP2948443B1 (https=) |
| JP (1) | JP6254194B2 (https=) |
| KR (1) | KR101869144B1 (https=) |
| CN (1) | CN105008346B (https=) |
| AU (1) | AU2014209950B2 (https=) |
| BR (1) | BR112015017678B1 (https=) |
| CA (1) | CA2897260C (https=) |
| CY (1) | CY1118552T1 (https=) |
| DK (1) | DK2948443T3 (https=) |
| EA (1) | EA026330B1 (https=) |
| ES (2) | ES2480341B1 (https=) |
| HR (1) | HRP20161495T1 (https=) |
| HU (1) | HUE031831T2 (https=) |
| LT (1) | LT2948443T (https=) |
| ME (1) | ME02551B (https=) |
| MX (1) | MX361160B (https=) |
| PL (1) | PL2948443T3 (https=) |
| PT (1) | PT2948443T (https=) |
| RS (1) | RS55449B1 (https=) |
| SI (1) | SI2948443T1 (https=) |
| SM (1) | SMT201600428B (https=) |
| WO (1) | WO2014114695A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017133657A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Pyridine and pyrimidine derivatives and their use in treatment, amelioration or prevention of influenza |
| CN107286146B (zh) * | 2017-07-05 | 2020-07-31 | 上海肇钰医药科技有限公司 | 作为腺苷a2a受体拮抗剂的4-氨基嘧啶衍生物及其用途 |
| CN116836162B (zh) * | 2023-05-24 | 2025-09-05 | 南方医科大学 | 吡唑[4,3-c]吡啶类化合物或其药学上可接受的盐及其应用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011119518A1 (en) * | 2010-03-25 | 2011-09-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| CN102892761A (zh) * | 2010-03-31 | 2013-01-23 | 帕罗生物制药有限公司 | 4-氨基嘧啶衍生物和它们作为腺苷a2a 受体拮抗剂 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008110891A2 (en) * | 2007-03-09 | 2008-09-18 | Orchid Research Laboratories Limited, | New heterocyclic compounds |
| CN105125547A (zh) | 2009-05-07 | 2015-12-09 | 费瑞姆医药有限公司 | 苯氧基甲基杂环化合物 |
| EP2434885B1 (en) | 2009-05-27 | 2014-03-26 | Merck Sharp & Dohme Corp. | Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors |
| JP6007102B2 (ja) | 2009-06-24 | 2016-10-12 | コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． | 画像情報に基づいた構造の輪郭の決定 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| KR101713453B1 (ko) | 2010-03-12 | 2017-03-07 | 오메로스 코포레이션 | Pde10 억제제 및 관련 조성물 및 방법 |
| US8969349B2 (en) | 2010-05-26 | 2015-03-03 | Sunovion Pharmaceuticals Inc. | Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors |
| US8592423B2 (en) | 2011-06-21 | 2013-11-26 | Bristol-Myers Squibb Company | Inhibitors of PDE10 |
| AU2012318874A1 (en) * | 2011-10-06 | 2014-05-15 | Merck Sharp & Dohme Corp. | 1,3-substituted azetidine PDE10 inhibitors |
-
2013
- 2013-01-24 ES ES201330082A patent/ES2480341B1/es not_active Expired - Fee Related
-
2014
- 2014-01-23 HU HUE14703553A patent/HUE031831T2/en unknown
- 2014-01-23 HR HRP20161495TT patent/HRP20161495T1/hr unknown
- 2014-01-23 CN CN201480006098.XA patent/CN105008346B/zh active Active
- 2014-01-23 PT PT147035539T patent/PT2948443T/pt unknown
- 2014-01-23 DK DK14703553.9T patent/DK2948443T3/en active
- 2014-01-23 CA CA2897260A patent/CA2897260C/en active Active
- 2014-01-23 BR BR112015017678-0A patent/BR112015017678B1/pt active IP Right Grant
- 2014-01-23 EA EA201591369A patent/EA026330B1/ru not_active IP Right Cessation
- 2014-01-23 JP JP2015554139A patent/JP6254194B2/ja active Active
- 2014-01-23 WO PCT/EP2014/051290 patent/WO2014114695A1/en not_active Ceased
- 2014-01-23 KR KR1020157022767A patent/KR101869144B1/ko active Active
- 2014-01-23 ME MEP-2016-254A patent/ME02551B/me unknown
- 2014-01-23 SI SI201430093A patent/SI2948443T1/sl unknown
- 2014-01-23 ES ES14703553.9T patent/ES2611170T3/es active Active
- 2014-01-23 PL PL14703553T patent/PL2948443T3/pl unknown
- 2014-01-23 RS RS20160971A patent/RS55449B1/sr unknown
- 2014-01-23 EP EP14703553.9A patent/EP2948443B1/en active Active
- 2014-01-23 MX MX2015009627A patent/MX361160B/es active IP Right Grant
- 2014-01-23 LT LTEP14703553.9T patent/LT2948443T/lt unknown
- 2014-01-23 AU AU2014209950A patent/AU2014209950B2/en active Active
- 2014-01-24 US US14/762,655 patent/US9447095B2/en active Active
-
2016
- 2016-11-23 SM SM201600428T patent/SMT201600428B/it unknown
- 2016-11-23 CY CY20161101206T patent/CY1118552T1/el unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011119518A1 (en) * | 2010-03-25 | 2011-09-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| CN102892761A (zh) * | 2010-03-31 | 2013-01-23 | 帕罗生物制药有限公司 | 4-氨基嘧啶衍生物和它们作为腺苷a2a 受体拮抗剂 |
Non-Patent Citations (2)
| Title |
|---|
| Distinct Roles of PDE4 and PDE10A in the Regulation of cAMP/PKA Signaling in the Striatum;Akinori Nishi et al.;《The Journal of Neuroscience》;20081015;第28卷(第42期);第10460-10471页 * |
| PDE10A and PDE10A-dependent cAMP catabolism are dysregulated oppositely in striatum and nucleus accumbens after lesion of midbrain dopamine neurons in rat: A key step in parkinsonism physiopathology;M. Giorgi et al.;《Neurobiology of Disease》;20110416;第43卷;第293-303页 * |
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| GR01 | Patent grant | ||
| GR01 | Patent grant |