PE20140788A1 - Tetrahidroquinolinas condensadas con cicloalquilo como moduladores de receptores de crth2 - Google Patents

Tetrahidroquinolinas condensadas con cicloalquilo como moduladores de receptores de crth2

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Publication number
PE20140788A1
PE20140788A1 PE2013002820A PE2013002820A PE20140788A1 PE 20140788 A1 PE20140788 A1 PE 20140788A1 PE 2013002820 A PE2013002820 A PE 2013002820A PE 2013002820 A PE2013002820 A PE 2013002820A PE 20140788 A1 PE20140788 A1 PE 20140788A1
Authority
PE
Peru
Prior art keywords
cis
tetrahydroquinolines
alkyl
receptor modulators
crth2 receptor
Prior art date
Application number
PE2013002820A
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English (en)
Inventor
Xianhai Huang
Jason Brubaker
Scott L Peterson
John W Butcher
Joshua T Close
Michelle Martinez
Rachel Nicola Maccoss
Joon O Jung
Phieng Siliphaivanh
Hongjun Zhang
Robert G Aslanian
Purakkattle Johny Biju
Li Dong
Ying Huang
Kevin D Mccormick
Anandan Palani
Ning Shao
Wei Zhou
Original Assignee
Merck Sharp & Dohme
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47357455&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140788(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20140788A1 publication Critical patent/PE20140788A1/es

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    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE TETRAHIDROQUINOLINAS CONDENSADAS CON CICLOALQUILO DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C4), ALQUENILO(C2-C4), ENTRE OTROS; R2 ES -Q-W-V, ENTRE OTROS, EN DONDE Q ES C(O), C(O)O, C(O)N(H), ENTRE OTROS; W ES ALQUILENO(C1-C8), CH=CH- O FENILENO; V ES CO2H, TETRAZOLILO, ENTRE OTROS; Y ES C(O), S(O)2, ENTRE OTROS; Z ES ALQUILENO(C1-C6), -O-, N(H), ENTRE OTROS; E ES FENILO, NAFTILO, INDANILO, ENTRE OTROS; R7 ES HALO, FLUOROALQUILO(C1-C3), CN, ENTRE OTROS; R8 ES ALQUILO(C1-C3), ALQUENILO(C2-C3) O FLUORO; R8a ES H O ALQUILO(C1-C6); n Y u SON CADA UNO DE 0 A 2; t ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: ACIDO 4-[{CIS,CIS-4-[(BENCILOXI)CARBONIL]-2,3,3a,4,9,9a-HEXAHIDRO-1H-CICLOPENTA[b]QUINOLIN-9-IL}(CICLOPROPIL)AMINO]-4-OXOBUTANOICO; ACIDO 4-[{CIS,CIS-4-[(BENCILOXI)CARBONIL]-2,3,3a,4,9,9a-HEXAHIDRO-1H-CICLOPENTA[b]QUINOLIN-9-IL}(FENIL)AMINO]-4-OXOBUTANOICO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR HOMOLOGO QUIMIOATRAYENTE EXPRESADAS EN CELULAS T AUXILIARES DE TIPO 2 (CRTH2) SIENDO UTILES EN EL TRATAMIENTO DE ASMA, RINITIS ALERGICA
PE2013002820A 2011-06-17 2012-06-14 Tetrahidroquinolinas condensadas con cicloalquilo como moduladores de receptores de crth2 PE20140788A1 (es)

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US201161498345P 2011-06-17 2011-06-17

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US (2) US8592383B2 (es)
EP (1) EP2720545B1 (es)
JP (1) JP5629403B2 (es)
KR (1) KR101599157B1 (es)
CN (1) CN103763924B (es)
AR (1) AR086931A1 (es)
AU (1) AU2012271661B8 (es)
BR (1) BR112013032557A2 (es)
CA (1) CA2838731C (es)
CL (1) CL2013003625A1 (es)
CO (1) CO6821958A2 (es)
CR (1) CR20130670A (es)
DO (1) DOP2013000306A (es)
EA (1) EA025100B1 (es)
EC (1) ECSP14013156A (es)
ES (1) ES2613644T3 (es)
IL (1) IL229508A0 (es)
MA (1) MA35188B1 (es)
MX (1) MX2013014900A (es)
NI (1) NI201300133A (es)
PE (1) PE20140788A1 (es)
TN (1) TN2013000471A1 (es)
TW (1) TW201302711A (es)
WO (1) WO2012174176A1 (es)
ZA (1) ZA201308942B (es)

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MX2013007295A (es) 2010-12-23 2013-08-26 Merck Sharp & Dohme Quinoxalinas y aza-quinoxalinas como moduladores del receptor de crth2.
WO2012087872A1 (en) 2010-12-23 2012-06-28 Merck Sharp & Dohme Corp. Quinolines and aza-quinolines as crth2 receptor modulators

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