ES2530884T3 - Derivados de imidazopiridina o imidazopirimidina como inhibidores de fosfodiesterasa 10A - Google Patents
Derivados de imidazopiridina o imidazopirimidina como inhibidores de fosfodiesterasa 10A Download PDFInfo
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- ES2530884T3 ES2530884T3 ES10760968T ES10760968T ES2530884T3 ES 2530884 T3 ES2530884 T3 ES 2530884T3 ES 10760968 T ES10760968 T ES 10760968T ES 10760968 T ES10760968 T ES 10760968T ES 2530884 T3 ES2530884 T3 ES 2530884T3
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- Prior art keywords
- alkyl
- alkoxy
- fluoroalkyl
- hydroxy
- hydrogen
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- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 title 1
- 101001072037 Homo sapiens cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Proteins 0.000 title 1
- 102100036377 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Human genes 0.000 title 1
- 150000005237 imidazopyrimidines Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 34
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 10
- 125000003545 alkoxy group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical group 0.000 abstract 6
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 5
- -1 oxo-tetrahydrofuranyl Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000002393 azetidinyl group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005961 oxazepanyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
Classifications
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- 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
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- 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
- A61K31/435—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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- 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
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- 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
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- 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
- A61P25/22—Anxiolytics
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- 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
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- 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
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Addiction (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos de fórmula (I)**Fórmula** en los que A es N o C(R6); R1 es hidrógeno, alquilo inferior o fluoroalquilo inferior; R2 es halógeno, C(O)NR7R8 o C(O)OR9; R3 es hidrógeno, NR10R11, alquilo C1-7, alcoxi C1-7, fluoro-alquilo C1-7 o fluoro-alcoxi C1-7; R4 es hidrógeno, alquilo C1-7, fluoroalquilo C1-7, alcoxi C1-7 o fluoro-alcoxi C1-7; R5 es arilo o heteroarilo, que puede estar sustituido opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, alquilo C1-7, alcoxi C1-7, fluoroalquilo C1-7, fluoro-alcoxi C1-7 e hidroxi; R6 es hidrógeno, halógeno, CN, cicloalquilo, alquilo C1-7, cicloalquil-alquilo C1-7, alcoxi C1-7, fluoroalquilo C1-7 o fluoro-alcoxi C1-7; R7 y R8 independientemente el uno del otro se selecciona del grupo que consiste en hidrógeno, alquilo C1-7, alcoxi C1-7-alquilo C1-7, fluoroalquilo C1-7, cicloalquilo, cicloalquil-alquilo C1-7, NH2-alquilo C1-7, N(H,alquilo C1-7)-alquilo C1-C7, N(alquilo C1-7)2-alquilo C1-7, hidroxi-alquilo C1-7, hidroxi-alcoxi C1-7-alquilo C1-7, NH2C(O)-alquilo C1-7, N(H,alquilo C1-7)C(O)-alquilo C1-7, N(alquilo C1-7)2C(O)-alquilo C1-7, alcoxi C1-7, hidroxi-alquilo C1-7-oxetanil-alquilo C1-7, oxo-tetrahidrofuranilo, tetrahidrofuranil-alquilo C1-7, oxo-tetrahidrofuranil-alquilo C1-7, hidroxi-fluoroalquilo C1-7, tetrahidrofuranilo, arilo y heteroarilo, dicho arilo o heteroarilo pueden estar sustituidos opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, alquilo C1-7, alcoxi C1-7, fluoroalquilo C1-7, fluoro-alcoxi C1-7 e hidroxi, o R7 y R8, junto con el átomo de nitrógeno al que están unidos, forman un heterociclilo seleccionado de entre el grupo que consiste en pirrolidinilo, azetidinilo, morfolinilo, 5,6-dihidro-8-H- [1,2,4]triazolo [4,3-a]pirazinilo, 3,4-dihidro-1H-pirrolo[1,2-a]pirazinilo, 2-oxa-6-aza-spiro[3,3]heptilo, 5,6-dihidro-8H25 imidazo[1,2-a]pirazinilo, [1,4]oxazepanilo, piperazinilo, tiomorfolinilo y 2-oxa-5-aza-biciclo[2,2,1]heptilo, dicho heterociclilo puede estar sustituidos opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, alquilo C1-7, alquilo C1-7-C(O), alcoxi C1-7-alquilo C1-7, oxo, hidroxi, hidroxi-alquilo C1- 7, N(alquilo C1-7)2, NH2, N(H,alquilo C1-7), fluoroalquilo C1-7, fluoroalquilo C1-7-C(O), alcoxi C1-7 y fluoro-alcoxi C1-7; R9 es hidrógeno, alquilo C1-7, o fluoroalquilo C1-7; R10 y R11 independientemente el uno del otro son hidrógeno, alquilo C1-7 o fluoroalquilo C1-7, o R10 y R11, junto con el átomo de nitrógeno al que están unidos, forman un heterociclilo seleccionado de entre el grupo que consiste en piperidinilo, morfolinilo, pirrolidinilo, azetidinilo y piperazinilo, dicho heterociclilo puede estar sustituido opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, alquilo C1-7, alcoxi C1-7, fluoro-alquilo C1-7 y fluoro-alcoxi C1-7; y sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09171253 | 2009-09-24 | ||
| PCT/EP2010/063830 WO2011036127A1 (en) | 2009-09-24 | 2010-09-21 | Imidazopyridine or imidazopyrimidine derivatives as phosphodiesterase 10a inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2530884T3 true ES2530884T3 (es) | 2015-03-06 |
Family
ID=43416552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10760968T Active ES2530884T3 (es) | 2009-09-24 | 2010-09-21 | Derivados de imidazopiridina o imidazopirimidina como inhibidores de fosfodiesterasa 10A |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8017604B2 (es) |
| EP (1) | EP2480546B1 (es) |
| JP (1) | JP5629322B2 (es) |
| KR (1) | KR101426624B1 (es) |
| CN (1) | CN102548991B (es) |
| AR (1) | AR078437A1 (es) |
| BR (1) | BR112012006531A2 (es) |
| CA (1) | CA2770087C (es) |
| CL (1) | CL2012000708A1 (es) |
| CY (1) | CY1116120T1 (es) |
| DK (1) | DK2480546T3 (es) |
| ES (1) | ES2530884T3 (es) |
| HR (1) | HRP20150345T1 (es) |
| IL (1) | IL218032A (es) |
| MX (1) | MX2012003469A (es) |
| PE (1) | PE20121438A1 (es) |
| PH (1) | PH12012500355A1 (es) |
| PL (1) | PL2480546T3 (es) |
| PT (1) | PT2480546E (es) |
| RU (1) | RU2502737C2 (es) |
| SI (1) | SI2480546T1 (es) |
| TW (1) | TWI402268B (es) |
| WO (1) | WO2011036127A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8470820B2 (en) * | 2010-01-22 | 2013-06-25 | Hoffman-La Roche Inc. | Nitrogen-containing heteroaryl derivatives |
| WO2012105594A1 (ja) * | 2011-02-01 | 2012-08-09 | 協和発酵キリン株式会社 | 縮環複素環誘導体 |
| EP2675791B1 (en) | 2011-02-18 | 2016-02-17 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| US8975276B2 (en) * | 2011-06-29 | 2015-03-10 | Bristol-Myers Squibb Company | Inhibitors of PDE10 |
| EP2574607A1 (en) * | 2011-09-06 | 2013-04-03 | F. Hoffmann-La Roche AG | PDE10 modulators |
| CN103827114B (zh) * | 2011-09-19 | 2016-08-24 | 霍夫曼-拉罗奇有限公司 | 作为pde10a抑制剂的三唑并吡啶化合物 |
| WO2014071044A1 (en) | 2012-11-01 | 2014-05-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| CA2899781A1 (en) * | 2013-01-31 | 2014-08-07 | F.Hoffmann-La Roche Ag | Radiolabeled compounds |
| WO2014133046A1 (ja) | 2013-02-27 | 2014-09-04 | 持田製薬株式会社 | 新規ピラゾール誘導体 |
| KR20160003173A (ko) | 2013-04-29 | 2016-01-08 | 에프. 호프만-라 로슈 아게 | 2-페닐 또는 2-헤트아릴 이미다졸[1,2-a]피리딘 유도체 |
| CN105164126B (zh) | 2013-04-30 | 2017-05-31 | 豪夫迈·罗氏有限公司 | 吡唑酰胺的Pd‑催化偶联 |
| US10039764B2 (en) | 2013-07-12 | 2018-08-07 | University Of South Alabama | Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression |
| CN105579453B (zh) * | 2013-09-26 | 2017-12-22 | 豪夫迈·罗氏有限公司 | 作为成像工具的咪唑并[1，2‑a]吡啶‑7‑胺类 |
| US9200016B2 (en) | 2013-12-05 | 2015-12-01 | Allergan, Inc. | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) |
| SG11201901729YA (en) | 2016-09-02 | 2019-03-28 | Ironwood Pharmaceuticals Inc | Fused bicyclic sgc stimulators |
| CN113698406A (zh) * | 2021-08-30 | 2021-11-26 | 成都药明康德新药开发有限公司 | 6-甲基吡唑并[1,5-a]嘧啶-3-胺的合成方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1140939B1 (en) * | 1999-11-10 | 2005-02-09 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted 2-aryl-3-(heteroaryl)-imidazo[1,2-alpha]pyrimidines, and related pharmaceutical compositions and methods |
| SE0102808D0 (sv) * | 2001-08-22 | 2001-08-22 | Astrazeneca Ab | New compounds |
| ES2393333T3 (es) * | 2002-07-12 | 2012-12-20 | Astellas Pharma Inc. | Derivado de N-fenil-(2R,5S)dimetilpiperazina |
| CA2508194C (en) * | 2002-12-03 | 2011-05-24 | Kyorin Pharmaceutical Co., Ltd. | Use of ibudilast as a phosphodiesterase 10a inhibitor |
| EP1651251A4 (en) | 2003-07-31 | 2008-06-18 | Bayer Pharmaceuticals Corp | METHOD FOR THE TREATMENT OF DIABETES AND RELATED DISEASES USING PDE 10A INHIBITORS |
| EP1748048A4 (en) * | 2004-05-10 | 2010-05-26 | Banyu Pharma Co Ltd | imidazopyridine |
| CA2599987A1 (en) * | 2005-03-03 | 2006-09-08 | Sirtris Pharmaceuticals, Inc. | Fused heterocyclic compounds and their use as sirtuin modulators |
| BRPI0706560A2 (pt) * | 2006-01-17 | 2011-03-29 | Hoffmann La Roche | derivados de aril-isoxazol-4-il-imidazo [1,2-a] piridina úteis para o tratamento de doença de alzheimer por intermédio de receptores gaba |
| WO2007098169A1 (en) * | 2006-02-21 | 2007-08-30 | Amgen Inc. | Cinnoline derivatives as phosphodiesterase 10 inhibitors |
| DE102007012645A1 (de) * | 2007-03-16 | 2008-09-18 | Bayer Healthcare Ag | Substituierte Imidazo- und Triazolopyrimidine |
| FR2926556B1 (fr) * | 2008-01-22 | 2010-02-19 | Sanofi Aventis | Derives de carboxamides n-azabicycliques, leur preparation et leur application en therapeutique |
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2010
- 2010-09-21 JP JP2012530234A patent/JP5629322B2/ja not_active Expired - Fee Related
- 2010-09-21 EP EP10760968.7A patent/EP2480546B1/en not_active Not-in-force
- 2010-09-21 CN CN201080042292.5A patent/CN102548991B/zh not_active Expired - Fee Related
- 2010-09-21 PE PE2012000365A patent/PE20121438A1/es not_active Application Discontinuation
- 2010-09-21 PL PL10760968T patent/PL2480546T3/pl unknown
- 2010-09-21 TW TW099132094A patent/TWI402268B/zh not_active IP Right Cessation
- 2010-09-21 PH PH1/2012/500355A patent/PH12012500355A1/en unknown
- 2010-09-21 CA CA2770087A patent/CA2770087C/en not_active Expired - Fee Related
- 2010-09-21 DK DK10760968.7T patent/DK2480546T3/en active
- 2010-09-21 SI SI201030869T patent/SI2480546T1/sl unknown
- 2010-09-21 PT PT107609687T patent/PT2480546E/pt unknown
- 2010-09-21 ES ES10760968T patent/ES2530884T3/es active Active
- 2010-09-21 BR BR112012006531A patent/BR112012006531A2/pt not_active IP Right Cessation
- 2010-09-21 WO PCT/EP2010/063830 patent/WO2011036127A1/en active Application Filing
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- 2010-09-21 MX MX2012003469A patent/MX2012003469A/es active IP Right Grant
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- 2010-09-23 AR ARP100103465A patent/AR078437A1/es not_active Application Discontinuation
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- 2015-03-27 HR HRP20150345TT patent/HRP20150345T1/hr unknown
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