AR065311A1 - Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceutica - Google Patents
Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceuticaInfo
- Publication number
- AR065311A1 AR065311A1 ARP080100597A ARP080100597A AR065311A1 AR 065311 A1 AR065311 A1 AR 065311A1 AR P080100597 A ARP080100597 A AR P080100597A AR P080100597 A ARP080100597 A AR P080100597A AR 065311 A1 AR065311 A1 AR 065311A1
- Authority
- AR
- Argentina
- Prior art keywords
- groups
- optionally substituted
- group
- heterocyclyl
- alkyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 18
- 125000000217 alkyl group Chemical group 0.000 abstract 17
- 125000001072 heteroaryl group Chemical group 0.000 abstract 16
- 125000003342 alkenyl group Chemical group 0.000 abstract 13
- 125000000304 alkynyl group Chemical group 0.000 abstract 13
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 13
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 13
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 11
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 11
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000004104 aryloxy group Chemical group 0.000 abstract 10
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 10
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 8
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 8
- 125000005843 halogen group Chemical group 0.000 abstract 8
- -1 -OH Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 3
- 125000002883 imidazolyl group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 102000030484 alpha-2 Adrenergic Receptor Human genes 0.000 abstract 2
- 108020004101 alpha-2 Adrenergic Receptor Proteins 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 2
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 239000000048 adrenergic agonist Substances 0.000 abstract 1
- 229940126157 adrenergic receptor agonist Drugs 0.000 abstract 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 125000003387 indolinyl group Chemical class N1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- WCESRWVTCVMYMU-GFCCVEGCSA-N n-[2,4-dimethoxy-5-[[(2r)-2-methyl-2,3-dihydroindol-1-yl]sulfonyl]phenyl]acetamide Chemical group C1=C(NC(C)=O)C(OC)=CC(OC)=C1S(=O)(=O)N1C2=CC=CC=C2C[C@H]1C WCESRWVTCVMYMU-GFCCVEGCSA-N 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/02—Nasal agents, e.g. decongestants
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- A61P25/00—Drugs for disorders of the nervous system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- C07—ORGANIC CHEMISTRY
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- 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
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- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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- 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
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- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
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- Pulmonology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
La presente provee una nueva clase de indolinas como inhibidores de los agonistas del receptor alfa2C adrenérgico, y composiciones farmacéuticas que contienen uno o más de dichos compuestos. Estos compuestos actuan como receptores alfa2C adrenérgicos siendo utiles en el tratamiento del dolor, la migrana, trastornos psicofísicos e isquemia. Reivindicacion 1: Un compuesto representado por la estructura (1) o una sal, éster, solvato o prodroga farmacéuticamente aceptable del mismo, en donde: A es un anillo heterocíclico de 5 miembros que contiene 1-3 heteroátomos, y está opcionalmente sustituido con al menos un grupo R5 y/o 1 o 2 grupos (=O); J1, J2, y J3 son independientemente -N-, -N(O) o -C(R2)-; J4 es C o N; J5 es -C(R6)- o -N(R6)-; ------ es un enlace simple o doble; R1 está seleccionado del grupo integrado por -[C(Ra)(Rb)]qYR7', -[C(Ra)(Rb)]qN(R7)YR7', -[C(Ra)(Rb)]qNR7R7', -[C(Ra)(Rb)]qOYR7', -[C(Ra)(Rb)]qON=CR7R7', -P(=O)(OR7)(OR7'), -P(=O)(NR7R7')2, y -P(=O)R82; Y está seleccionado del grupo integrado por un enlace, -C(=O)-, -C(=O)NR7-; -C(=O)O-, -C(=O)-[C(Ra)(Rb)]n-O-C(=O)-, -C(=O)N(Rc)-O-, -C(=NR7)-, -C(=NOR7)-, -C(=NR7)NR7-, -C(=NR7)NR7O-, -S(O)p-, SO2NR7-, y -C(=S)NR7-, en donde Ra y Rb están independientemente seleccionados del grupo integrado por H, alquilo, alcoxi, y halo, y Rc es H o alquilo; R2 está independientemente seleccionado del grupo integrado por H, -OH, halo, -CN, -NO2, S(O)pR7, -NR7R7', (CH2)qYR7', (CH2)qN(R7)YR7', (CH2)qOYR7',-(CH2)qON=CR7R7', P(=O)(OR7)(OR7'), P(=O)NR7R7', y P(=O)R82, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5; R3 está independientemente seleccionado del grupo integrado por H, halo y (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5, siempre que cuando w sea 3, no más de 2 de los grupos R3 puedan ser (=O); R4 está independientemente seleccionado del grupo integrado por H, -CN y halo, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con al menos un R5; R5 está independientemente seleccionado del grupo integrado por H, halo, -OH, -CN, -NO2, -NR7R7', y -S(O)pR7, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -S(O)pR7 y/o 1 o 2 grupos (=O); R6 está independientemente seleccionado del grupo integrado por H y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, NR7R7', y -S(O)pR7 y/o 1 o 2 grupos (=O), y -C(=O)R7, -C(=O)OR7, C(=O)NR7R7', -SO2R7 y -SO2NR7R7'; R7 está independientemente seleccionado del grupo integrado por H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, ciclociclenilo, ciclociclenilalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heterociclenilo, heterociclenilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido una o más veces con R12; R7' está independientemente seleccionado del grupo integrado por H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, ciclociclenilo, ciclociclenilalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heterociclenilo, heterociclenilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido una o más veces con R12; R7 y R7' conjuntamente con el átomo de nitrogeno al cual ellos están unidos forman un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros que tiene, además del átomo de N, 1 o 2 heteroátomos adicionales seleccionados del grupo integrado por O, N, -N(R9)- y S, en donde dichos anillos están opcionalmente sustituidos con 1 a 5 restos R5 independientemente seleccionados y/o 1 o 2 grupos (=O), R8 está independientemente seleccionado del grupo integrado por grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, alcoxi, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R9 está independientemente seleccionado del grupo integrado por H, -C(O)-R10, -C(O)-OR10, y -S(O)p-OR10 y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); y R10 está seleccionado del grupo integrado por grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R11 es un resto independientemente seleccionado del grupo integrado por H y alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con al menos un sustituyente independientemente seleccionado del grupo integrado por halo, -OH, -CN, -NO2, -N(R11')2, y -S(O)pR11 y/o 1 o 2 grupos (=O); R11' está independientemente seleccionado del grupo integrado por H, alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo; R12 está independientemente seleccionado del grupo integrado por H, halo, -OH, -CN, -NO2, -N(R11)2 , y -S(O)pR11 y/o 1 o 2 grupos (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalquenilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroariloxi, heteroarilalquilo, heterociclilo, heterociclenilo, heterocicleniloxi, heterociclilalquilo, heterociclenilalquilo, arilalcoxi, heteroarilalcoxi, heterociclilalcoxi, y heterociclenilalcoxi, cada uno de los cuales a su vez está opcionalmente sustituido al menos una vez con un sustituyente seleccionado del grupo integrado por H, alquilo, haloalquilo, halo, -OH, alcoxi opcionalmente sustituido, ariloxi opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, heteroariloxi opcionalmente sustituido, heterocicleniloxi opcionalmente sustituido, -CN, -NO2, -N(R11)2, y -S(O)pR11 y/o 1 o 2 grupos (=O), en donde dichos ariloxi, alcoxi opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, heterocicleniloxi y heteroariloxi opcionalmente sustituido, cuando están sustituidos están sustituidos una o más veces con R11, m es 1-5; n es independientemente 1-3; p es independientemente 0-2; q es independientemente 0-6; y w es 1-3; con las siguientes condiciones: (a) si J1-J3 son -C(H)-, R1 es -[C(Ra)(Rb)]qYR7', q es 0, y A es imidazolilo no sustituido, entonces Y es distinto a un enlace; (b) si J1-J3 son -C(H)-, R1 es [C(Ra)(Rb)]qYR7', q es 0, y A es imidazolilo no sustituido, entonces Y es distinto a un enlace; (c) si J4 es N, entonces J5 es -C(R6)-; (d) si J4 es C, entonces J5 es -N(R6)- y (e) si A es imidazolilo no sustituido, R1 es -[C(RA)(Rb)]qYR7', q es 0, Y es -C(=O)- o -C(=O)O-, entonces R7 es distinto a H o alquilo, (f) si R1 es -[C(Ra)(Rb)]qYR7', q =0, e Y = - C(=NR7)-, -C(=NOR7)-, -C(NR7)NR7-, o C(=NR7)N(Rc)O, entonces R7 y R7' pueden no tomarse conjuntamente para formar un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros; y (g) si R1 es -[C(Ra)(Rb)]qN(R7)YR7 o -[C(Ra)(Rb)]qNR7R7' y q = 0, entonces R7 y R7' pueden no tomarse conjuntamente para formar un anillo heterociclilo, heterociclenilo o heteroarilo de 3 a 8 miembros.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US11/705,683 US8003624B2 (en) | 2005-08-25 | 2007-02-13 | Functionally selective ALPHA2C adrenoreceptor agonists |
Publications (1)
Publication Number | Publication Date |
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AR065311A1 true AR065311A1 (es) | 2009-05-27 |
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ARP080100597A AR065311A1 (es) | 2007-02-13 | 2008-02-12 | Agonistas del adrenoreceptor alfa2c funcionalmente selectivos y composicion farmaceutica |
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US (1) | US8003624B2 (es) |
EP (1) | EP2125784A2 (es) |
KR (1) | KR20090110938A (es) |
CN (1) | CN101903373A (es) |
AR (1) | AR065311A1 (es) |
AU (1) | AU2008216798A1 (es) |
CA (1) | CA2679849A1 (es) |
CL (1) | CL2008000439A1 (es) |
IL (1) | IL200424A0 (es) |
PE (1) | PE20090069A1 (es) |
TW (1) | TW200836721A (es) |
WO (1) | WO2008100457A2 (es) |
Families Citing this family (45)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2678036A1 (en) * | 2007-02-13 | 2008-08-21 | Schering Corporation | Functionally selective alpha2c adrenoreceptor agonists |
MX2009008777A (es) * | 2007-02-13 | 2009-08-25 | Schering Corp | Derivados y analogos de cromano como agonistas de los receptores alfa2c adrenergicos funcionalmente selectivos. |
CL2008000431A1 (es) * | 2007-02-13 | 2008-08-18 | Schering Corp | Compuestos derivados de biciclos o heterociclos condensados; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar afecciones relacionadas con los a2c adrenegicos, tales como congestion relacionada con rinitis, polipos o re |
EP2257546B1 (en) * | 2008-02-21 | 2012-08-15 | Merck Sharp & Dohme Corp. | Functionally selective alpha2c adrenoreceptor agonists |
WO2010017120A1 (en) * | 2008-08-04 | 2010-02-11 | Schering Corporation | Cyclopropylchromene derivatives as modulators of the alpha-2c receptor |
UA103195C2 (uk) | 2008-08-11 | 2013-09-25 | Глаксосмитклайн Ллк | Похідні пурину для застосування у лікуванні алергій, запальних та інфекційних захворювань |
WO2010033495A2 (en) * | 2008-09-16 | 2010-03-25 | Schering Corporation | Functionally selective azanitrile alpha2c adrenoreceptor agonists |
EP2356106A1 (en) | 2008-10-07 | 2011-08-17 | Schering Corporation | Biaryl spiroaminooxazoline analogues as alpha2c adrenergic receptor modulators |
US9512111B2 (en) | 2010-11-08 | 2016-12-06 | Lycera Corporation | N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease |
US8921559B2 (en) * | 2010-12-01 | 2014-12-30 | Janssen Pharmaceutica Nv | 4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of CCR2 |
US10112946B2 (en) | 2011-07-22 | 2018-10-30 | Glaxosmithkline Llc | Composition |
BR112014028017A2 (pt) | 2012-05-08 | 2017-06-27 | Lycera Corp | composto, composição farmacêutica, método para tratar um distúrbio, método para reduzir a quantidade il-17 em um indivíduo e método para inibir a atividade de ror |
EP2847198B1 (en) | 2012-05-08 | 2016-12-14 | Lycera Corporation | Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of ror-gamma and the treatment of disease |
US9555036B2 (en) | 2012-08-24 | 2017-01-31 | Glaxosmithkline Llc | Pyrazolopyrimidine compounds |
WO2014081644A1 (en) | 2012-11-20 | 2014-05-30 | Glaxosmithkline Llc | Novel compounds |
PT2922549T (pt) | 2012-11-20 | 2017-09-01 | Glaxosmithkline Llc | Novos compostos |
ES2625023T3 (es) | 2012-11-20 | 2017-07-18 | Glaxosmithkline Llc | Compuestos novedosos |
WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease |
US9663502B2 (en) | 2013-12-20 | 2017-05-30 | Lycera Corporation | 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease |
WO2015131035A1 (en) | 2014-02-27 | 2015-09-03 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods |
US9896441B2 (en) | 2014-05-05 | 2018-02-20 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
JP6523337B2 (ja) | 2014-05-05 | 2019-05-29 | リセラ・コーポレイションLycera Corporation | RORγのアゴニストとしての使用及び疾患治療のためのベンゼンスルホンアミド及び関連化合物 |
EP3256450B1 (en) | 2015-02-11 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof |
US9745253B2 (en) | 2015-03-13 | 2017-08-29 | Forma Therapeutics, Inc. | Alpha-cinnamide compounds and compositions as HDAC8 inhibitors |
JP2018515491A (ja) | 2015-05-05 | 2018-06-14 | リセラ・コーポレイションLycera Corporation | RORγの作動薬及び疾患の療法として使用するジヒドロ−2H−ベンゾ[b][1,4]オキサジンスルホンアミド及び関連化合物 |
MX2017016134A (es) | 2015-06-11 | 2018-08-15 | Lycera Corp | Aril dihidro-2h-benzo[b][1,4]oxazina sulfonamida y compuestos relacionados para uso como agonistas de rory y el tratamiento de enfermedad. |
WO2017040963A1 (en) | 2015-09-03 | 2017-03-09 | Forma Therapeutics, Inc. | [6,6] fused bicyclic hdac8 inhibitors |
WO2017075182A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
JP2018531957A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としての置換二環式ピラゾール化合物及びその使用 |
EP3368535B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
CN107098845A (zh) * | 2017-07-06 | 2017-08-29 | 贵州大学 | 一种5‑氰基‑6‑硝基吲哚的制备工艺 |
US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
CR20220066A (es) | 2019-08-14 | 2022-11-28 | Incyte Corp | Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2 |
CN115298177A (zh) | 2019-10-11 | 2022-11-04 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
AU2021215709A1 (en) | 2020-02-04 | 2022-09-01 | Mindset Pharma Inc. | 3-pyrrolidine-indole derivatives as serotonergic psychedelic agents for the treatment of CNS disorders |
US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
GB202112240D0 (en) * | 2021-08-26 | 2021-10-13 | Univ Court Univ St Andrews | Inhibitor compounds |
US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
WO2023115002A1 (en) * | 2021-12-16 | 2023-06-22 | Terran Biosciences Inc. | Analogs of 4-bromo-2,5-dimethoxyphenethylamine |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5393771A (en) | 1993-05-12 | 1995-02-28 | Brisol-Myers Squibb Company | 4-substituted benzopyran and related compounds |
RU2124511C1 (ru) * | 1993-05-14 | 1999-01-10 | Фармасьютикал Ко., Лтд | Производные пиперазина |
US5778302A (en) | 1995-09-14 | 1998-07-07 | Tosoh Smd, Inc. | Methods of making Cr-Me sputter targets and targets produced thereby |
WO1997048697A1 (en) | 1996-06-19 | 1997-12-24 | Rhone-Poulenc Rorer Limited | Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase |
US5977134A (en) * | 1996-12-05 | 1999-11-02 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
TW527355B (en) * | 1997-07-02 | 2003-04-11 | Bristol Myers Squibb Co | Inhibitors of farnesyl protein transferase |
US6841684B2 (en) | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
TWI283669B (en) | 1999-06-10 | 2007-07-11 | Allergan Inc | Compounds and method of treatment having agonist-like activity selective at alpha 2B or 2B/2C adrenergic receptors |
NZ521185A (en) * | 2000-07-14 | 2005-02-25 | Allergan Inc | Compositions containing alpha-2-adrenergic agonist components |
US7091232B2 (en) | 2002-05-21 | 2006-08-15 | Allergan, Inc. | 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds |
FI20022159A0 (fi) | 2002-12-05 | 2002-12-05 | Orion Corp | Uusia farmaseuttisia yhdisteitä |
WO2005014543A1 (ja) | 2003-08-06 | 2005-02-17 | Japan Tobacco Inc. | 縮合環化合物及びそのhcvポリメラーゼ阻害剤としての利用 |
EP1791832A1 (en) * | 2004-09-24 | 2007-06-06 | Allergan, Inc. | 4-(heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists |
AU2006283104A1 (en) | 2005-08-25 | 2007-03-01 | Pharmacopeia, Inc. | Imidazole derivatives as functionally selective alpha2C adrenoreceptor agonists |
GB0608928D0 (en) | 2006-05-08 | 2006-06-14 | Angeletti P Ist Richerche Bio | Therapeutic agents |
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2007
- 2007-02-13 US US11/705,683 patent/US8003624B2/en not_active Expired - Fee Related
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2008
- 2008-02-11 WO PCT/US2008/001767 patent/WO2008100457A2/en active Application Filing
- 2008-02-11 AU AU2008216798A patent/AU2008216798A1/en not_active Abandoned
- 2008-02-11 CA CA002679849A patent/CA2679849A1/en not_active Abandoned
- 2008-02-11 CN CN2008800127607A patent/CN101903373A/zh active Pending
- 2008-02-11 KR KR1020097018935A patent/KR20090110938A/ko not_active Application Discontinuation
- 2008-02-11 EP EP08714239A patent/EP2125784A2/en not_active Withdrawn
- 2008-02-12 TW TW097104878A patent/TW200836721A/zh unknown
- 2008-02-12 PE PE2008000308A patent/PE20090069A1/es not_active Application Discontinuation
- 2008-02-12 AR ARP080100597A patent/AR065311A1/es not_active Application Discontinuation
- 2008-02-12 CL CL200800439A patent/CL2008000439A1/es unknown
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2009
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Also Published As
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US8003624B2 (en) | 2011-08-23 |
EP2125784A2 (en) | 2009-12-02 |
WO2008100457A3 (en) | 2008-12-18 |
CA2679849A1 (en) | 2008-08-21 |
CN101903373A (zh) | 2010-12-01 |
KR20090110938A (ko) | 2009-10-23 |
CL2008000439A1 (es) | 2008-08-22 |
TW200836721A (en) | 2008-09-16 |
PE20090069A1 (es) | 2009-02-13 |
WO2008100457A2 (en) | 2008-08-21 |
AU2008216798A2 (en) | 2009-09-24 |
US20080027100A1 (en) | 2008-01-31 |
IL200424A0 (en) | 2010-04-29 |
AU2008216798A1 (en) | 2008-08-21 |
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