AR081627A1 - Compuestos heterociclicos de nitrogeno insaturados utiles como inhibidores de pde10 - Google Patents
Compuestos heterociclicos de nitrogeno insaturados utiles como inhibidores de pde10Info
- Publication number
- AR081627A1 AR081627A1 ARP110101668A ARP110101668A AR081627A1 AR 081627 A1 AR081627 A1 AR 081627A1 AR P110101668 A ARP110101668 A AR P110101668A AR P110101668 A ARP110101668 A AR P110101668A AR 081627 A1 AR081627 A1 AR 081627A1
- Authority
- AR
- Argentina
- Prior art keywords
- alq
- ring
- nrara
- halo
- independently
- Prior art date
Links
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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/36—Opioid-abuse
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
- C07C53/16—Halogenated acetic acids
- C07C53/18—Halogenated acetic acids containing fluorine
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
-
- 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
- C07D471/08—Bridged systems
-
- 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
-
- 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
- C07D487/08—Bridged systems
-
- 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Abstract
Composiciones que los contienen, y procesos para preparar tales compuestos. También se proporcionan en la presente métodos para tratar trastornos o enfermedades tratables por inhibición de PDE10, tales como obesidad, enfermedad de Huntington, diabetes no dependiente a insulina, esquizofrenia, trastorno bipolar, trastorno obsesivo-compulsivo, y similares.Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque: X1 es N o CR6; X2 es N o CR2; X3 es N o CR3; X4 es N o CR6; X5 es N o CR6; en donde 1 hasta 2 de X1, X2, X3, X4 y X5 son N; R1 es halo, alq C1-8, haloalq C1-4, -ORc, -N(Ra)C(=O)Rb, -C(=O)Ra, -C(=O)Rc, -C(=O)-O-Ra, -NRaRc, -N(Rc)C(=O)Rb, -N(Ra)C(=O)Rc, -C(=O)NRaRb, -C(=O)NRaRc, o Alq C0-4-L1; en donde el grupo alq C1-8 se sustituye por 0, 1, 2 ó 3 grupos los cuales son halo, haloalq C1-3, -OH, -Oalq C1-4, -NH2, -NHalq C1-4, -OC(=O)alq C1-4, o -N(alq C1-4)alq C1-4; Y es un alq C0-4, -C(=O), SO, o SO2; cada R2 y R3 es independientemente R1, H, halo, CN, OH, -Oalq C1-4, alq C1-4, haloalq C1-4, -alq C1-6ORa, -C(=O)alq C1-4, -C(=O)NRaRa, -alq C0-4NHC(=O)Ra, o Rc; o alternativamente el anillo que contiene X1, X2, X3, X4 y X5 se puede fusionar al anillo A, anillo B, o anillo C; que tiene la fórmula (2), (3) ó (4); en donde cada anillo A, anillo B, o anillo C es un anillo carbocíclico o heterocíclico saturado, parcialmente saturado o no saturado de 4 a 6 miembros fusionado que contiene 0, 1, 2 ó 3 heteroátomos; y se sustituyen por 0, 1 ó 2 grupos R10; R4a es H, OH, halo, alq C1-4, o haloalq C1-4; R4b es halo, CN, OH, Oalq C1-4, alq C1-4, haloalq C1-4, u oxo; R5 es -alq C1-6ORa, anillo heteroarilo de 5 a 6 miembros, biciclo-heterocíclico no saturado de 9 a 10 miembros, o anillo triciclo-heterocíclico de 11 a 15 miembros; anillo R5 se sustituye por 0, 1, 2, 3 ó 4 grupos R8; R6 es independientemente R1, H, halo, CN, OH, Oalq C1-4, alq C1-4 o haloalq C1-4; m es 0, 1, 2, 3 ó 4; cada uno de p y q es independientemente 0, 1, 2, 3, 4, 5 ó 6; en donde la suma de p y q es 2 hasta 6; el anillo que contiene p y q contiene 0, 1 ó 2 enlaces dobles; Ra es independientemente H o Rb; Rb es independientemente fenilo, bencilo, o alq C1-6, en donde el fenilo, bencilo, y alq C1-6 se sustituyen por 0, 1, 2 ó 3 sustituyentes los cuales son, independientemente, halo, alq C1-4, haloalq C1-3, -OH, -Oalq C1-4, -NH2, -NHalq C1-4, -OC(=O)alq C1-4, o -N(alq C1-4)alq C1-4; Rc es alq C0-4-L2; cada L1 es independientemente un anillo monocíclico ligado al carbono o ligado al nitrógeno saturado, parcialmente saturado o no saturado de 3, 4, 5, 6 ó 7 miembros o anillo bicíclico saturado, parcialmente saturado o no saturado de 6, 7, 8, 9, 10, 11 ó 12 miembros, el anillo contiene 0, 1, 2, 3 ó 4 átomos N y 0, 1 ó 2 átomos los cuales son O ó S; L1 es independientemente sustituido por 0, 1, 2 ó 3 grupos R9; cada L2 es independientemente un anillo monocíclico ligado al carbono o ligado al nitrógeno saturado, parcialmente saturado o no saturado de 3, 4, 5, 6 ó 7 miembros o anillo bicíclico saturado, parcialmente saturado o no saturado de 6, 7, 8, 9, 10, 11 ó 12 miembros, el anillo contiene 0, 1, 2, 3 ó 4 átomos N y 0, 1 ó 2 átomos los cuales son O ó S; L2 es independientemente sustituido por 0, 1, 2 ó 3 grupos R11; R8 es halo, CN, OH, Oalq C1-4, alq C1-4, haloalq C1-4, Ohaloalq C1-4, -C(=O)Rb, C(=O)Rc, C(=O)NHRb, C(=O)NHRc, -S(=O)2Rb, -S(=O)2Rc, -S(=O)2NRaRa, Rb, Rc, NO2, ORb, ORc; R9 es halo, alq C1-6, haloalq C1-4, -ORa, -Ohaloalq C1-4, CN, -C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -Oalq C1-6NRaRa, -Oalq C1-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaalq C1-6NRaRa, -NRaalq C1-6ORa, -alq C1-6NRaRa, -alq C1-6ORa, -alq C1-6N(Ra)C(=O)Rb, -alq C1-6OC(=O)Rb, -alq C1-6C(=O)NRaRa, -alq C1-6C(=O)ORa, oxo, o Rc; R10 es oxo, alq C1-6, haloalq C1-3, -OH, -Oalq C1-4, -NH2, -NHalq C1-4, -OC(=O)alq C1-4, o -N(alq C1-4)alq C1-4; y R11 es halo, alq C1-6, haloalq C1-4, -ORa, -Ohaloalq C1-4, CN, -C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -Oalq C1-6NRaRa, -Oalq C1-6ORa, SRa, S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaalq C1-6NRaRa, -NRaalq C1-6ORa, -alq C1-6NRaRa, -alq C1-6ORa, -alq C1-6N(Ra)C(=O)Rb, -alq C1-6OC(=O)Rb, -alq C1-6C(=O)NRaRa, -alq C1-6C(=O)ORa, u oxo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33452510P | 2010-05-13 | 2010-05-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR081627A1 true AR081627A1 (es) | 2012-10-10 |
Family
ID=44278966
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110101668A AR081627A1 (es) | 2010-05-13 | 2011-05-13 | Compuestos heterociclicos de nitrogeno insaturados utiles como inhibidores de pde10 |
Country Status (25)
Country | Link |
---|---|
US (3) | US8957073B2 (es) |
EP (1) | EP2569300A1 (es) |
JP (1) | JP5702855B2 (es) |
KR (1) | KR101564806B1 (es) |
CN (1) | CN103221404B (es) |
AR (1) | AR081627A1 (es) |
AU (1) | AU2011253057B2 (es) |
BR (1) | BR112012029026A2 (es) |
CA (1) | CA2798490A1 (es) |
CL (1) | CL2012003178A1 (es) |
CO (1) | CO6630189A2 (es) |
CR (1) | CR20120635A (es) |
EA (1) | EA201291236A1 (es) |
IL (1) | IL222898A (es) |
MA (1) | MA34300B1 (es) |
MX (1) | MX2012013130A (es) |
NZ (1) | NZ603876A (es) |
PE (1) | PE20130576A1 (es) |
SG (1) | SG185515A1 (es) |
TN (1) | TN2012000530A1 (es) |
TW (1) | TW201206902A (es) |
UA (1) | UA109438C2 (es) |
UY (1) | UY33382A (es) |
WO (1) | WO2011143365A1 (es) |
ZA (1) | ZA201208510B (es) |
Families Citing this family (64)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MA34300B1 (fr) * | 2010-05-13 | 2013-06-01 | Amgen Inc | Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10 |
AU2011253143A1 (en) | 2010-05-13 | 2012-12-06 | Amgen Inc. | Nitrogen- heterocyclic compounds as phosphodiesterase 10 inhibitors |
WO2011143366A1 (en) | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxycarbocyclyl compounds as pde10 inhibitors |
CA2798325A1 (en) | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as pde10 inhibitors |
US8772316B2 (en) | 2011-02-18 | 2014-07-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE10A) |
JP2014517016A (ja) | 2011-06-10 | 2014-07-17 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害活性を有するピリミジンおよびピリミジン化合物の組成物と製造方法 |
US8623860B2 (en) * | 2011-12-30 | 2014-01-07 | Boehringer Ingelheim International Gmbh | Azetidine derivatives, pharmaceutical compositions and uses thereof |
TW201348231A (zh) * | 2012-02-29 | 2013-12-01 | Amgen Inc | 雜雙環化合物 |
CN104271568B (zh) * | 2012-05-09 | 2016-05-04 | 硕腾服务有限责任公司 | 作为抗寄生虫剂的氮杂环丁烷衍生物 |
UY34858A (es) | 2012-06-14 | 2013-11-29 | Amgen Inc | Compuestos de azetidina y piperidina útiles como inhibidores de pde10 |
WO2014071044A1 (en) | 2012-11-01 | 2014-05-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
CA2894399A1 (en) | 2012-12-06 | 2014-06-12 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
CA2900303A1 (en) * | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4 |
US9200016B2 (en) | 2013-12-05 | 2015-12-01 | Allergan, Inc. | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) |
ES2672797T3 (es) | 2014-02-13 | 2018-06-18 | Incyte Corporation | Ciclopropilaminas como inhibidores de LSD1 |
ME03580B (me) | 2014-02-13 | 2020-07-20 | Incyte Corp | Ciklopropilamini kao lsd1 inhibitori |
CA2939082C (en) | 2014-02-13 | 2022-06-07 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
MA39337B1 (fr) * | 2014-02-14 | 2019-11-29 | Takeda Pharmaceuticals Co | Modulateurs de pyrazines de gpr6 |
CN104016911A (zh) * | 2014-04-03 | 2014-09-03 | 定陶县友帮化工有限公司 | 一种2-氨基-3,5-二溴吡啶的合成方法 |
CN104016909B (zh) * | 2014-04-03 | 2016-04-20 | 定陶县友帮化工有限公司 | 一种2-氨基-3-溴-5-氯吡啶的合成方法 |
JP6616786B2 (ja) * | 2014-05-19 | 2019-12-04 | メリアル インコーポレイテッド | 駆虫性化合物 |
WO2016007731A1 (en) * | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
JP6769963B2 (ja) | 2014-08-29 | 2020-10-14 | ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ | α−アミノ−β−カルボキシムコン酸セミアルデヒド脱炭酸酵素の阻害剤 |
WO2016054560A1 (en) * | 2014-10-02 | 2016-04-07 | Flatley Discovery Lab | Isoxazole compounds and methods for the treatment of cystic fibrosis |
TWI714567B (zh) | 2015-04-03 | 2021-01-01 | 美商英塞特公司 | 作為lsd1抑制劑之雜環化合物 |
WO2017009751A1 (en) | 2015-07-15 | 2017-01-19 | Pfizer Inc. | Pyrimidine derivatives |
CR20180152A (es) | 2015-08-12 | 2018-08-09 | Incyte Corp | Sales de un inhibidor de lsd1 |
MX2018012901A (es) | 2016-04-22 | 2019-06-06 | Incyte Corp | Formulaciones de inhibidor de demetilasa 1 especifica para lisina (lsd1). |
WO2017205425A1 (en) * | 2016-05-24 | 2017-11-30 | President And Fellows Of Harvard College | Compounds for organic light emitting diode materials |
AU2017275657B2 (en) | 2016-06-02 | 2021-08-19 | Novartis Ag | Potassium channel modulators |
DK3555064T5 (da) * | 2016-12-16 | 2023-05-01 | Pfizer | GLP-1 receptoragonister og anvendelser deraf |
US9975886B1 (en) | 2017-01-23 | 2018-05-22 | Cadent Therapeutics, Inc. | Potassium channel modulators |
CN106957300A (zh) * | 2017-04-12 | 2017-07-18 | 苏州汉德创宏生化科技有限公司 | 抗肿瘤杂环药物中间体2‑(3‑氮杂环丁基)吡啶二盐酸盐的合成方法 |
WO2019084338A1 (en) * | 2017-10-25 | 2019-05-02 | University Of South Florida | DRUG-INDUCED ACTIVATION OF THE REELIN SIGNALING SYSTEM |
CA3078769A1 (en) | 2017-10-27 | 2019-05-02 | Boehringer Ingelheim International Gmbh | Pyridine carbonyl derivatives and therapeutic uses thereof as trpc6 inhibitors |
CN109956931B (zh) * | 2017-12-26 | 2021-07-16 | 迈第康(上海)生物医药科技有限公司 | 四氢吡咯类化合物、其制备方法、药物组合物及用途 |
IL277071B1 (en) | 2018-03-08 | 2024-03-01 | Incyte Corp | Aminopyrizine diol compounds as PI3K–y inhibitors |
TWI707683B (zh) * | 2018-06-13 | 2020-10-21 | 美商輝瑞股份有限公司 | Glp-1受體促效劑及其用途 |
BR112020024956A2 (pt) * | 2018-06-15 | 2021-03-09 | Pfizer Inc. | Agonistas de receptor de glp-1 e usos dos mesmos |
US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
ES2958917T3 (es) | 2018-10-02 | 2024-02-16 | Syngenta Participations Ag | Compuestos de benceno-amida y azina-amida con actividad plaguicida |
US11161838B2 (en) | 2018-11-13 | 2021-11-02 | Incyte Corporation | Heterocyclic derivatives as PI3K inhibitors |
WO2020102216A1 (en) | 2018-11-13 | 2020-05-22 | Incyte Corporation | Substituted heterocyclic derivatives as pi3k inhibitors |
EP3883928A4 (en) * | 2018-11-22 | 2022-06-29 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
CN113165139B (zh) | 2018-11-26 | 2023-06-09 | 京瓷株式会社 | 气体喷嘴和气体喷嘴的制造方法以及等离子体处理装置 |
WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
TW202102489A (zh) | 2019-03-29 | 2021-01-16 | 瑞士商先正達農作物保護公司 | 殺有害生物活性之二𠯤-醯胺化合物 |
KR20210149113A (ko) | 2019-04-05 | 2021-12-08 | 신젠타 크롭 프로텍션 아게 | 살충 활성 디아진-아미드 화합물 |
CA3131861A1 (en) | 2019-04-11 | 2020-10-15 | Jurgen Harry Schaetzer | Pesticidally active diazine-amide compounds |
US10954221B2 (en) | 2019-04-12 | 2021-03-23 | Qilu Regor Therapeutics Inc. | GLP-1R agonists and uses thereof |
CR20210562A (es) * | 2019-04-12 | 2022-02-18 | Qilu Regor Therapeutics Inc | Agonistas de glp-1r y usos de los mismos |
US20220289715A1 (en) | 2019-08-23 | 2022-09-15 | Syngenta Crop Protection Ag | Pesticidally active pyrazine-amide compounds |
JP2022547707A (ja) * | 2019-09-12 | 2022-11-15 | ディスアーム セラピューティクス, インコーポレイテッド | Sarm1の阻害剤 |
CN114728939B (zh) * | 2019-11-15 | 2023-12-08 | 日东制药株式会社 | Glp-1受体激动剂及其用途 |
CN115279750A (zh) * | 2020-03-18 | 2022-11-01 | 株式会社Lg化学 | Glp-1受体激动剂、包含该激动剂的药物组合物及其制备方法 |
IL296336A (en) * | 2020-03-18 | 2022-11-01 | Lg Chemical Ltd | A agonist for the glp-1 receptor, a pharmaceutical preparation containing it and a method for its preparation |
EP4247241A1 (en) * | 2020-11-19 | 2023-09-27 | Cerecin Inc. | Radiopharmaceutical ketone and dual tracer imaging in alzheimer's disease, cognitive impairment, and other conditions of altered cerebral metabolism |
BR112023025644A2 (pt) | 2021-06-09 | 2024-02-27 | Syngenta Crop Protection Ag | Compostos de diazina-amida pesticidamente ativos |
CA3217423A1 (en) * | 2021-06-16 | 2022-12-22 | Jeffrey M. Schkeryantz | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
Family Cites Families (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
HN2002000266A (es) * | 2001-09-24 | 2003-11-16 | Bayer Corp | Preparacion y uso de derivados de imidazol para el tratamiento de la obesidad. |
JP4568603B2 (ja) * | 2002-05-31 | 2010-10-27 | プロテオテック・インコーポレイテッド | アミロイド疾患およびシヌクレイノパチー(例えばアルツハイマー病、タイプ2型糖尿病、およびパーキンソン病)を処置するための化合物、組成物、および方法 |
CA2501539A1 (en) | 2002-10-17 | 2004-04-29 | Amgen Inc. | Benzimidazole derivatives and their use as vanilloid receptor ligands |
US20070032404A1 (en) | 2003-07-31 | 2007-02-08 | Bayer Pharmaceuticals Corporation | Methods for treating diabetes and related disorders using pde10a inhibitors |
GB0325287D0 (en) * | 2003-10-29 | 2003-12-03 | Merck Sharp & Dohme | Therapeutic agents |
KR100907354B1 (ko) * | 2004-05-18 | 2009-07-10 | 쉐링 코포레이션 | Pde4 억제제로서 유용한 치환된 2-퀴놀릴-옥사졸 |
US20060019975A1 (en) | 2004-07-23 | 2006-01-26 | Pfizer Inc | Novel piperidyl derivatives of quinazoline and isoquinoline |
US20070072908A1 (en) | 2005-06-08 | 2007-03-29 | Japan Tobacco Inc. | Heterocyclic compounds |
US7709501B2 (en) * | 2005-12-23 | 2010-05-04 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
US20100222353A1 (en) | 2006-01-27 | 2010-09-02 | Pfizer Products Inc. | Aminophthalazine derivative compounds |
AU2008339572B2 (en) | 2007-12-21 | 2012-05-10 | Astrazeneca Ab | Bicyclic derivatives for use in the treatment of androgen receptor associated conditions |
JP2011524917A (ja) | 2008-06-20 | 2011-09-08 | メタボレックス, インコーポレイテッド | アリールgpr119作動薬およびその使用 |
US20100041663A1 (en) * | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
RS53075B (en) | 2009-05-12 | 2014-04-30 | Janssen Pharmaceuticals Inc. | 1,2,4-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS |
AU2010289397B2 (en) * | 2009-09-03 | 2016-05-26 | Bioenergenix | Heterocyclic compounds for the inhibition of PASK |
EP2479165B1 (en) | 2009-09-16 | 2017-10-25 | Astellas Pharma Inc. | Glycine compound |
CA2798325A1 (en) | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as pde10 inhibitors |
WO2011143366A1 (en) | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxycarbocyclyl compounds as pde10 inhibitors |
MA34300B1 (fr) * | 2010-05-13 | 2013-06-01 | Amgen Inc | Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10 |
AU2011253143A1 (en) | 2010-05-13 | 2012-12-06 | Amgen Inc. | Nitrogen- heterocyclic compounds as phosphodiesterase 10 inhibitors |
UY34858A (es) * | 2012-06-14 | 2013-11-29 | Amgen Inc | Compuestos de azetidina y piperidina útiles como inhibidores de pde10 |
-
2011
- 2011-05-11 MA MA35440A patent/MA34300B1/fr unknown
- 2011-05-11 KR KR1020127032541A patent/KR101564806B1/ko not_active IP Right Cessation
- 2011-05-11 NZ NZ603876A patent/NZ603876A/en not_active IP Right Cessation
- 2011-05-11 CA CA2798490A patent/CA2798490A1/en not_active Abandoned
- 2011-05-11 WO PCT/US2011/036148 patent/WO2011143365A1/en active Application Filing
- 2011-05-11 PE PE2012002159A patent/PE20130576A1/es not_active Application Discontinuation
- 2011-05-11 EA EA201291236A patent/EA201291236A1/ru unknown
- 2011-05-11 BR BR112012029026A patent/BR112012029026A2/pt not_active Application Discontinuation
- 2011-05-11 JP JP2013510285A patent/JP5702855B2/ja not_active Expired - Fee Related
- 2011-05-11 CN CN201180034741.6A patent/CN103221404B/zh not_active Expired - Fee Related
- 2011-05-11 MX MX2012013130A patent/MX2012013130A/es unknown
- 2011-05-11 AU AU2011253057A patent/AU2011253057B2/en not_active Ceased
- 2011-05-11 US US13/105,860 patent/US8957073B2/en active Active
- 2011-05-11 EP EP11721618A patent/EP2569300A1/en not_active Withdrawn
- 2011-05-11 SG SG2012082939A patent/SG185515A1/en unknown
- 2011-05-12 UY UY0001033382A patent/UY33382A/es not_active Application Discontinuation
- 2011-05-13 AR ARP110101668A patent/AR081627A1/es unknown
- 2011-05-13 TW TW100116952A patent/TW201206902A/zh unknown
- 2011-11-05 UA UAA201214182A patent/UA109438C2/uk unknown
-
2012
- 2012-11-06 IL IL222898A patent/IL222898A/en not_active IP Right Cessation
- 2012-11-07 TN TNP2012000530A patent/TN2012000530A1/en unknown
- 2012-11-12 ZA ZA2012/08510A patent/ZA201208510B/en unknown
- 2012-11-13 CL CL2012003178A patent/CL2012003178A1/es unknown
- 2012-11-15 CO CO12207172A patent/CO6630189A2/es active IP Right Grant
- 2012-12-13 CR CR20120635A patent/CR20120635A/es unknown
-
2014
- 2014-04-01 US US14/242,432 patent/US20140213572A1/en not_active Abandoned
-
2015
- 2015-12-17 US US14/973,491 patent/US9718803B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
UA109438C2 (uk) | 2015-08-25 |
US20160102075A1 (en) | 2016-04-14 |
US8957073B2 (en) | 2015-02-17 |
US20140213572A1 (en) | 2014-07-31 |
KR20130065666A (ko) | 2013-06-19 |
US9718803B2 (en) | 2017-08-01 |
CA2798490A1 (en) | 2011-11-17 |
CO6630189A2 (es) | 2013-03-01 |
TW201206902A (en) | 2012-02-16 |
CL2012003178A1 (es) | 2013-07-05 |
CN103221404A (zh) | 2013-07-24 |
JP5702855B2 (ja) | 2015-04-15 |
US20110306587A1 (en) | 2011-12-15 |
ZA201208510B (en) | 2017-11-29 |
UY33382A (es) | 2011-10-31 |
TN2012000530A1 (en) | 2014-04-01 |
MA34300B1 (fr) | 2013-06-01 |
AU2011253057B2 (en) | 2014-11-20 |
EA201291236A1 (ru) | 2013-11-29 |
KR101564806B1 (ko) | 2015-10-30 |
WO2011143365A1 (en) | 2011-11-17 |
IL222898A (en) | 2015-11-30 |
PE20130576A1 (es) | 2013-05-19 |
EP2569300A1 (en) | 2013-03-20 |
JP2013526536A (ja) | 2013-06-24 |
IL222898A0 (en) | 2012-12-31 |
CR20120635A (es) | 2013-01-30 |
NZ603876A (en) | 2015-02-27 |
MX2012013130A (es) | 2013-04-11 |
SG185515A1 (en) | 2012-12-28 |
AU2011253057A1 (en) | 2012-11-29 |
BR112012029026A2 (pt) | 2016-08-02 |
CN103221404B (zh) | 2015-12-16 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR081627A1 (es) | Compuestos heterociclicos de nitrogeno insaturados utiles como inhibidores de pde10 | |
AR082699A1 (es) | Sales de fenotiazindiaminio, composicion farmaceutica en base al compuesto y proceso de preparacion del compuesto | |
AR095823A1 (es) | Compuesto de ciclopropanamina y uso del mismo | |
AR067762A1 (es) | Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma | |
AR059380A1 (es) | Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina, composiciones farmaceuticas | |
CO6811860A2 (es) | 4-aril-n-fenil-1,3,5-triazin-2-aminas que contienen un grupo sulfoximina | |
AR074358A1 (es) | Derivados de pirazina como inhibidores de la fosfodiesterasa 10 | |
ES2770058T3 (es) | Compuestos y composiciones destinados a modular las actividades de quinasa de EGFR mutante | |
ECSP13012892A (es) | IMIDAZO[5,1-f][1,2,4]TRIAZINAS PARA EL TRATAMIENTO DE TRASTORNOS NEUROLÓGICOS | |
AR090203A1 (es) | Compuestos heterobiciclicos como inhibidores de pde10 | |
ES2655391T3 (es) | Inhibidores isoindolinona de fosfatidilinositol 3-quinasa | |
AR072819A1 (es) | Derivados de triazolo[4,3-a]piridina,procedimiento de preparacion,intermediarios de dicho proceso,composiciones farmaceuticas que los comprenden y uso de los mismos, como inhibidores de la proteinquinasa met,para el tratamiento de canceres,psoriasis,enfermedades del sistema nervioso central y otras | |
AR074775A1 (es) | Compuestos aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10 | |
AR082154A1 (es) | DERIVADOS DE PIRAZOLO[1,5-a]PIRIMIDINA COMO MODULADORES DE IRAK4 | |
ECSP13012891A (es) | Derivados de heteroarilo como moduladores de nachr alfa 7 | |
PE20142081A1 (es) | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos | |
AR074608A1 (es) | Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas | |
AR078321A1 (es) | Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9) | |
AR087915A1 (es) | N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1 | |
PE20110196A1 (es) | 5-alquinil-pirimidinas | |
AR075368A1 (es) | Inhibidores de glicosilceramida sintasa | |
CL2015001319A1 (es) | Compuestos derivados de n-(piridin-2-il)pirimidin-4-amina que contienen un grupo sulfoximina; compuestos intermediarios; composicion farmaceutica; combinacion farmaceutica; y metodo para la preparacion de compuestos. | |
AR086036A1 (es) | DERIVADOS DE ETINILO COMO MODULADORES ALOSTERICOS POSITIVOS DE (mGluR5) | |
AR072820A1 (es) | Derivados de imidazo[1,2-a]pirimidina,procedimiento de preparacion,intermediarios de dicho proceso,composiciones farmaceuticas que los comprenden y uso de los mismos, como inhibidores de la proteinquinasa met,para el tratamiento de canceres,psoriasis,enfermedades del sistema nervioso central y otras | |
CL2013003646A1 (es) | Compuestos derivados de trans-1-(3s.1r)-6-cloro-3-fenilindan-1-il)-1,2,2-trimetilpiperazina deuterados, con actividad en los receptores 5ht2, d1 y d2; proceso de preparacion; compuesto intermediario; composicion y combinacion farmaceutica; y su uso para el tratamiento de la psicosis, entre otros. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |