AR080496A1 - Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad - Google Patents
Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedadInfo
- Publication number
- AR080496A1 AR080496A1 ARP110100765A ARP110100765A AR080496A1 AR 080496 A1 AR080496 A1 AR 080496A1 AR P110100765 A ARP110100765 A AR P110100765A AR P110100765 A ARP110100765 A AR P110100765A AR 080496 A1 AR080496 A1 AR 080496A1
- Authority
- AR
- Argentina
- Prior art keywords
- heterocycloalkyl
- aminoalkyl
- cycloalkyl
- aryl
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000000543 Histamine Receptors Human genes 0.000 title 1
- 108010002059 Histamine Receptors Proteins 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 10
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 4
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- -1 C-amido Chemical group 0.000 abstract 2
- 125000003368 amide group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 101100240528 Caenorhabditis elegans nhr-23 gene Proteins 0.000 abstract 1
- 208000022873 Ocular disease Diseases 0.000 abstract 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 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
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
- 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
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Abstract
Compuestos y métodos que pueden ser utiles como inhibidores de la H4R para el tratamiento y la prevencion de enfermedades inflamatorias, autoinmunes, alérgicas y oculares. Reivindicacion 1: El compuesto caracterizado porque tiene la formula estructural (1), o una sal del mismo, donde el anillo que comprende X1-5 es aromático; X1 y X5 se seleccionan independientemente de C, CH y N; X2 se selecciona de [C(R6)(R7)], NR8, O y S; X3 se selecciona de [C(R9)(R10)], NR11, O, y S; X4 se selecciono de [C(R12)(R13)], NR14, O y S; X6 se selecciona de CR18 y N; X7 se selecciona de CR19 y N; Y1 se selecciona de un enlace, alquilo inferior, alcoxi inferior, OR15, NR16R17, y aminoalquilo inferior; Y2 se selecciona de un enlace, alquilo inferior, alcoxi inferior, OR20, NR21R22, S, C(O)NH2, C(O)NHR23, C(O)NR23R24 y aminoalquilo inferior; R1 se selecciono del grupo que consiste en: arilo, heterocicloalquilo, cicloalquilo, y heteroarilo, donde cualquiera puede estar opcionalmente sustituido, cuando Y1 es un enlace; y ninguno, cuando Y1 se selecciona de OR15, NR16R17, alquilo inferior, alcoxi inferior, o aminoalquilo inferior; R2, se selecciona de alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterocicloalquilo y heteroarilodonde cualquiera puede estar opcionalmente sustituido; R6, R7, R9, R10, R12, R13, R18 y R19 se seleccionan independientemente de ninguno, hidrogeno, alquilo, alquenilo, alquinilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcíonalmente sustituido; R8, R11, y R14 se seleccionan independientemente de ninguno, hidrogeno, alquilo, heteroalquilo, alcoxi, haloalquilo, perhaloalquilo, aminoalquilo, C-amido, carboxilo, acilo, hidroxi, arilo, arilalquilo, cicloalquilo, cicloaIquiIaIquiIo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; R15, R16, R20 y R21 se seleccionan independientemente de aminoalquilo, alquilaminoalquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilaminoheterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; R17 y R22 se selecciona independientemente de hidrogeno, aminoalquilo, alquilaminoalquil arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilaminoheterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido; y R23 y R24 se seleccionan independientemente de hidrogeno, alquilo, alquenilo, alquinilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, perhaloalcoxi, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, donde cualquiera puede estar opcionalmente sustituido.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31261510P | 2010-03-10 | 2010-03-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR080496A1 true AR080496A1 (es) | 2012-04-11 |
Family
ID=44564108
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110100765A AR080496A1 (es) | 2010-03-10 | 2011-03-11 | Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad |
Country Status (17)
Country | Link |
---|---|
US (1) | US8569300B2 (es) |
EP (1) | EP2545058B1 (es) |
JP (1) | JP5888654B2 (es) |
KR (1) | KR20130016253A (es) |
CN (1) | CN102869666B (es) |
AR (1) | AR080496A1 (es) |
AU (1) | AU2011224316B2 (es) |
BR (1) | BR112012022211A2 (es) |
CA (1) | CA2791417A1 (es) |
ES (1) | ES2607125T3 (es) |
IL (1) | IL221829A (es) |
MX (1) | MX2012010404A (es) |
NZ (1) | NZ602041A (es) |
RU (1) | RU2012137180A (es) |
TW (1) | TW201200518A (es) |
UY (1) | UY33271A (es) |
WO (1) | WO2011112766A2 (es) |
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EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
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WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
TW201625635A (zh) | 2014-11-21 | 2016-07-16 | 默沙東藥廠 | 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物 |
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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 |
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-
2011
- 2011-03-07 TW TW100107575A patent/TW201200518A/zh unknown
- 2011-03-10 CN CN201180019492.3A patent/CN102869666B/zh not_active Expired - Fee Related
- 2011-03-10 MX MX2012010404A patent/MX2012010404A/es active IP Right Grant
- 2011-03-10 NZ NZ602041A patent/NZ602041A/en not_active IP Right Cessation
- 2011-03-10 KR KR1020127026253A patent/KR20130016253A/ko not_active Application Discontinuation
- 2011-03-10 US US13/044,661 patent/US8569300B2/en not_active Expired - Fee Related
- 2011-03-10 JP JP2012557231A patent/JP5888654B2/ja not_active Expired - Fee Related
- 2011-03-10 CA CA2791417A patent/CA2791417A1/en not_active Abandoned
- 2011-03-10 BR BR112012022211A patent/BR112012022211A2/pt active Search and Examination
- 2011-03-10 ES ES11754043.5T patent/ES2607125T3/es active Active
- 2011-03-10 RU RU2012137180/04A patent/RU2012137180A/ru not_active Application Discontinuation
- 2011-03-10 WO PCT/US2011/027817 patent/WO2011112766A2/en active Application Filing
- 2011-03-10 EP EP11754043.5A patent/EP2545058B1/en not_active Not-in-force
- 2011-03-10 AU AU2011224316A patent/AU2011224316B2/en not_active Ceased
- 2011-03-10 UY UY0001033271A patent/UY33271A/es not_active Application Discontinuation
- 2011-03-11 AR ARP110100765A patent/AR080496A1/es not_active Application Discontinuation
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2012
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AU2011224316A1 (en) | 2012-09-13 |
EP2545058B1 (en) | 2016-08-24 |
JP5888654B2 (ja) | 2016-03-22 |
AU2011224316B2 (en) | 2016-09-15 |
BR112012022211A2 (pt) | 2017-07-18 |
MX2012010404A (es) | 2013-05-20 |
US8569300B2 (en) | 2013-10-29 |
KR20130016253A (ko) | 2013-02-14 |
CN102869666A (zh) | 2013-01-09 |
WO2011112766A3 (en) | 2012-01-19 |
RU2012137180A (ru) | 2014-04-20 |
CA2791417A1 (en) | 2011-09-15 |
EP2545058A4 (en) | 2013-07-24 |
WO2011112766A2 (en) | 2011-09-15 |
ES2607125T3 (es) | 2017-03-29 |
JP2013522222A (ja) | 2013-06-13 |
IL221829A (en) | 2014-11-30 |
EP2545058A2 (en) | 2013-01-16 |
UY33271A (es) | 2011-10-31 |
US20110237565A1 (en) | 2011-09-29 |
TW201200518A (en) | 2012-01-01 |
CN102869666B (zh) | 2015-09-09 |
NZ602041A (en) | 2014-08-29 |
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