AR087628A1 - Inhibidores de pde10 de pirimidina - Google Patents
Inhibidores de pde10 de pirimidinaInfo
- Publication number
- AR087628A1 AR087628A1 ARP120103086A ARP120103086A AR087628A1 AR 087628 A1 AR087628 A1 AR 087628A1 AR P120103086 A ARP120103086 A AR P120103086A AR P120103086 A ARP120103086 A AR P120103086A AR 087628 A1 AR087628 A1 AR 087628A1
- Authority
- AR
- Argentina
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- substituents selected
- group
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 7
- 125000003342 alkenyl group Chemical group 0.000 abstract 7
- 125000000304 alkynyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001624 naphthyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- -1 imidazopyridazinyl Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000000335 thiazolyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 abstract 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 210000004227 basal ganglia Anatomy 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 abstract 1
- 210000001577 neostriatum Anatomy 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
Classifications
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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
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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
-
- 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
- A61P25/22—Anxiolytics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (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)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente se refiere a compuestos de pirimidina que son útiles como agentes terapéuticos para el tratamiento de trastornos del sistema nervioso central asociados con la fosfodiesterasa 10 (PDE10). La presente también se refiere al uso de dichos compuestos para tratar trastornos neurológicos y psiquiátricos, tales como la esquizofrenia, la psicosis o la enfermedad de Huntington, y aquellos asociados con la hipofunción del cuerpo estriado o la disfunción de los ganglios basales. Reivindicación 1: Un compuesto de la fórmula (1) en la que: A se selecciona entre el grupo que consiste en: (i) piridilo, (ii) quinolinilo, (iii) naftiridinilo, (iv) tiazolilo, (v) piridazinilo, (vi) oxazolilo, y (vii) pirazolilo, (viii) dihidropirrolopirazolilo, (ix) dihidrociclopentapiridinilo, (x) imidazopiridazinilo y (xi) pirazolopirimidinilo; B se selecciona entre el grupo que consiste en: (i) tiazolilo, (ii) pirazolilo, (iii) tiadiazolilo, (iv) isoxazolilo, (v) isotiazolilo, (vi) piridilo y (vii) pirimidinilo; R¹ᵃ, R¹ᵇ y R¹ᶜ se seleccionan independientemente entre el grupo que consiste en: (i) hidrógeno, (ii) halógeno, (iii) hidroxilo, (iv) -(C=O)ₘ-Oₙ-alquilo C₁₋₆, en la que m es 0 ó 1, n es 0 ó 1 (en la que si m es 0 o n es 0, está presente un enlace) y en la que el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (v) -(C=O)ₘ-Oₙ-cicloalquilo C₃₋₆, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (vi) -(C=O)ₘ-alquenilo C₂₋₄, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (vii) -(C=O)ₘ-alquinilo C₂₋₄, donde el alquinilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (viii) -(C=O)ₘ-Oₙ-fenilo o -(C=O)ₘ-Oₙ-naftilo, donde el fenilo o el naftilo están sin sustituir o sustituidos con uno o más sustituyentes seleccionados entre R¹³, (ix) -(C=O)ₘ-Oₙ-heteroarilo, donde el heteroarilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (x) -(C=O)ₘ-NR¹⁰R¹¹, (xi) -S(O)₂-NR¹⁰R¹¹, (xii) -S(O)q-R¹², donde q es 0, 1 ó 2 y donde R¹² se selecciona entre las definiciones de R¹⁰ y R¹¹, (xiii) -CO₂H, (xiv) -CN y (xv) -NO₂; R²ᵃ, R²ᵇ y R²ᶜ se seleccionan independientemente entre el grupo que consiste en: (i) hidrógeno, (ii) halógeno, (iii) hidroxilo, (iv) -(C=O)ₘ-Oₙ-alquilo C₁₋₆, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (v) -(C=O)ₘ-Oₙ-cicloalquilo C₃₋₆, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (vi) -(C=O)ₘ-alquenilo C₂₋₄, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (vii) -(C=O)ₘ-alquinilo C₂₋₄, donde el alquinilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (viii) -(C=O)ₘ-Oₙ-fenilo o -(C=O)ₘ-Oₙ-naftilo, donde el fenilo o el naftilo están sin sustituir o sustituidos con uno o más sustituyentes seleccionados entre R¹³, (ix) -(C=O)ₘ-Oₙ-heterociclilo, donde el heterociclilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹³, (x) -(C=O)ₘ-NR¹⁰R¹¹, (xi) -S(O)₂-NR¹⁰R¹¹, (xii) -S(O)q-R¹², (xiii) -CO₂H, (xiv) -CN y (xv) -NO₂; R³ se selecciona entre el grupo que consiste en: (i) CH₃, (ii) CF₃, (iii) CH₂F, (iv) CH₂CH₃, (v) ciclopropilo, (vi) ciano, (vii) hidrógeno, (viii) NH₂, (ix) C(O)OR⁵, (x) -O-alquilo C₁₋₆, (xi) -(CO)NH₂, (xii) alquil C₁₋₆OH, (xiii) C(O)alquilo C₁₋₆, y (xiv) halógeno; R⁴ se selecciona entre el grupo que consiste en: (i) hidrógeno, (ii) halo, (iii) -alquilo C₁₋₆, y (iv) ciano; R⁵ se selecciona entre el grupo que consiste en: (i) hidrógeno y (ii) alquilo C₁₋₆; R⁶ se selecciona entre el grupo que consiste en: (i) hidrógeno, (ii) alquilo C₁₋₆, y (iii) O-alquilo C₁₋₆; R¹⁰ y R¹¹ se seleccionan independientemente entre el grupo que consiste en: (a) hidrógeno, (b) alquilo C₁₋₆, que está sin sustituir o sustituido con R¹⁴, (c) alquenilo C₃₋₆, que está sin sustituir o sustituido con R¹⁴, (d) alquinilo C₃₋₆, que está sin sustituir o sustituido con R¹⁴, (e) cicloalquilo C₃₋₆, que está sin sustituir o sustituido con R¹⁴, (f) alcoxilo C₁₋₆, que está sin sustituir o sustituido con R¹⁴, (g) fenilo, que está sin sustituir o sustituido con R¹⁴, y (h) heteroarilo, que está sin sustituir o sustituido con R¹⁴; R¹³ se selecciona entre el grupo que consiste en: (i) halógeno, (ii) hidroxilo, (iii) -(C=O)ₘ-Oₙ-alquilo C₁₋₆, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹⁴, (iv) -Oₙ-perfluoroalquilo C₁₋₃, (v) -(C=O)ₘ-Oₙ-cicloalquilo C₃₋₆, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹⁴, (vi) -(C=O)ₘ-alquenilo C₂₋₄, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹⁴, (vii) -(C=O)ₘ-alquinilo C₂₋₄, donde el alquinilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹⁴, (viii) -(C=O)ₘ-Oₙ-fenilo o -(C=O)ₘ-Oₙ-naftilo, donde el fenilo o el naftilo están sin sustituir o sustituidos con uno o más sustituyentes seleccionados entre R¹⁴, (ix) -(C=O)ₘ-Oₙ-heteroarilo, donde el heteroarilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R¹⁴, (x) -(C=O)ₘ-NR¹⁰R¹¹, (xi) -S(O)₂-NR¹⁰R¹¹, (xii) -S(O)q-R¹², (xiii) -CO₂H, (xiv) -CN y (xv) -NO₂; R¹⁴ se selecciona entre el grupo que consiste en: (i) hidroxilo, (ii) halógeno, (iii) alquilo C₁₋₆, (iv) -cicloalquilo C₃₋₆, (v) -O-alquilo C₁₋₆, (vi) -O(C=O)-alquilo C₁₋₆, (vii) -NH-alquilo C₁₋₆, (viii) fenilo, (ix) heteroarilo, (x) -CO₂H y (xi) -CN; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161527392P | 2011-08-25 | 2011-08-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087628A1 true AR087628A1 (es) | 2014-04-09 |
Family
ID=47746797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103086A AR087628A1 (es) | 2011-08-25 | 2012-08-22 | Inhibidores de pde10 de pirimidina |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US9062059B2 (es) |
| EP (1) | EP2748151B1 (es) |
| JP (1) | JP5648147B2 (es) |
| KR (1) | KR101655635B1 (es) |
| CN (1) | CN103917528B (es) |
| AR (1) | AR087628A1 (es) |
| AU (1) | AU2012299080B2 (es) |
| BR (1) | BR112014004310B8 (es) |
| CA (1) | CA2845578C (es) |
| CL (1) | CL2014000450A1 (es) |
| CO (1) | CO6890101A2 (es) |
| CR (1) | CR20140085A (es) |
| CY (1) | CY1117622T1 (es) |
| DK (1) | DK2748151T3 (es) |
| DO (1) | DOP2014000039A (es) |
| EA (1) | EA023685B1 (es) |
| ES (1) | ES2572527T3 (es) |
| HR (1) | HRP20160635T1 (es) |
| HU (1) | HUE028451T2 (es) |
| IL (1) | IL230997A (es) |
| MA (1) | MA35508B1 (es) |
| ME (1) | ME02419B (es) |
| MX (1) | MX357241B (es) |
| MY (1) | MY157301A (es) |
| NI (1) | NI201400014A (es) |
| PE (1) | PE20141535A1 (es) |
| PH (1) | PH12014500424A1 (es) |
| PL (1) | PL2748151T3 (es) |
| RS (1) | RS54788B1 (es) |
| SG (1) | SG2014013536A (es) |
| SI (1) | SI2748151T1 (es) |
| TN (1) | TN2014000070A1 (es) |
| TW (1) | TWI450895B (es) |
| UA (1) | UA109735C2 (es) |
| WO (1) | WO2013028590A1 (es) |
| ZA (1) | ZA201401272B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9200001B2 (en) | 2011-10-06 | 2015-12-01 | Merck Sharp & Dohme Corp. | Triazolyl PDE10 inhibitors |
| CA2851082A1 (en) | 2011-10-06 | 2013-04-11 | Merck Sharp & Dohme Corp. | 1,3-substituted azetidine pde10 inhibitors |
| US9359348B2 (en) | 2012-11-15 | 2016-06-07 | Merck Sharp & Dohme Corp. | Cyclopropyl imidazopyridine PDE10 inhibitors |
| WO2014078216A1 (en) | 2012-11-15 | 2014-05-22 | Merck Sharp & Dohme Corp. | Cyclobutyl benzimidazoles as pde10 inhibitors |
| TW201422610A (zh) * | 2012-11-15 | 2014-06-16 | Merck Sharp & Dohme | 作爲ｐｄｅ１０抑制劑之經二級醇取代之三唑 |
| WO2014081617A1 (en) | 2012-11-20 | 2014-05-30 | Merck Sharp & Dohme Corp. | Substituted pyridone derivatives as pde10 inhibitors |
| EP2922823B1 (en) * | 2012-11-20 | 2018-10-31 | Merck Sharp & Dohme Corp. | Pyrimidine pde10 inhibitors |
| WO2014139150A1 (en) | 2013-03-15 | 2014-09-18 | Merck Sharp & Dohme Corp. | Substituted pyridizinone derivatives as pde10 inhibitors |
| AU2015236369B2 (en) | 2014-03-24 | 2017-02-16 | Novartis Ag | Monobactam organic compounds for the treatment of bacterial infections |
| EP3544958B1 (en) | 2016-11-28 | 2021-03-24 | Boehringer Ingelheim International GmbH | Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
| IL279725B2 (en) | 2018-06-27 | 2024-04-01 | Eth Zuerich | Novel pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2 |
| CN116640118A (zh) | 2018-06-27 | 2023-08-25 | 豪夫迈·罗氏有限公司 | 放射性标记的大麻素受体2配体 |
| EP3814328A1 (en) | 2018-06-27 | 2021-05-05 | F. Hoffmann-La Roche AG | Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2 |
| AU2021285225A1 (en) * | 2020-06-05 | 2023-01-19 | Noema Pharma Ag | Use of a phosphodiesterase 10 inhibitor for the treatment of Tourette Syndrome |
| JP2024509991A (ja) | 2021-03-17 | 2024-03-05 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｐｄｅ１０化合物のプロドラッグ |
| WO2023184486A1 (en) * | 2022-04-01 | 2023-10-05 | Merck Sharp & Dohme Llc | Process for preparing ( (1s, 2s) -2- (5-methylpyridin-2-yl) cyclopropyl) -methanol |
| CN115403527B (zh) * | 2022-07-20 | 2024-03-29 | 西安近代化学研究所 | 一种还原胺化法合成杀菌剂乙嘧酚的方法 |
| WO2024049721A1 (en) * | 2022-08-31 | 2024-03-07 | Merck Sharp & Dohme Llc | Sustained release delivery of a pde10 inhibitor |
| CN120187717A (zh) * | 2022-11-11 | 2025-06-20 | 杭州中美华东制药有限公司 | 1,5-萘啶类cGAS抑制剂及其用途 |
| WO2024206200A1 (en) * | 2023-03-29 | 2024-10-03 | Merck Sharp & Dohme Llc | Controlled release pde10a formulations |
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| JP4302762B2 (ja) | 2005-01-07 | 2009-07-29 | ファイザー・プロダクツ・インク | 複素環式芳香族キノリン化合物およびｐｄｅ１０阻害剤としてのその使用 |
| GB0506883D0 (en) * | 2005-04-05 | 2005-05-11 | Astrazeneca Ab | Chemical compounds |
| CA2602372A1 (en) * | 2005-04-05 | 2006-10-12 | Astrazeneca Ab | Pyrimidine derivatives for use as anticancer agents |
| NL2000397C2 (nl) * | 2006-01-05 | 2007-10-30 | Pfizer Prod Inc | Bicyclische heteroarylverbindingen als PDE10 inhibitoren. |
| CA2650976A1 (en) | 2006-05-02 | 2007-11-15 | Pfizer Products Inc. | Bicyclic heteroaryl compounds as pde10 inhibitors |
| US20110230472A1 (en) * | 2008-08-29 | 2011-09-22 | Shionogi & Co., Ltd. | Ring-fused azole derivative having pi3k-inhibiting activity |
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| JP2012501962A (ja) | 2008-09-10 | 2012-01-26 | 田辺三菱製薬株式会社 | 芳香族含窒素六員環化合物及びその使用 |
| TW201030001A (en) * | 2008-11-14 | 2010-08-16 | Amgen Inc | Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors |
| US8637500B2 (en) * | 2008-12-17 | 2014-01-28 | Amgen Inc. | Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors |
| WO2011008931A2 (en) * | 2009-07-15 | 2011-01-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders |
| TWI481607B (zh) * | 2009-12-17 | 2015-04-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物 |
| US8470820B2 (en) * | 2010-01-22 | 2013-06-25 | Hoffman-La Roche Inc. | Nitrogen-containing heteroaryl derivatives |
| EP2621276B1 (en) * | 2010-09-30 | 2017-12-27 | Merck Sharp & Dohme Corp. | 2-alkoxy pyrimidine pde10 inhibitors |
| WO2012044562A2 (en) * | 2010-09-30 | 2012-04-05 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine pde10 inhibitors |
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