HRP20150069T1 - Spojevi pirazola kao crth2-antagonisti - Google Patents
Spojevi pirazola kao crth2-antagonisti Download PDFInfo
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- HRP20150069T1 HRP20150069T1 HRP20150069AT HRP20150069T HRP20150069T1 HR P20150069 T1 HRP20150069 T1 HR P20150069T1 HR P20150069A T HRP20150069A T HR P20150069AT HR P20150069 T HRP20150069 T HR P20150069T HR P20150069 T1 HRP20150069 T1 HR P20150069T1
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- alkyl
- pyrazole compounds
- alkoxy
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- 150000003217 pyrazoles Chemical class 0.000 title claims 26
- 239000005557 antagonist Substances 0.000 title claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 19
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 8
- -1 C1-C6- alkoxy Chemical group 0.000 claims 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 7
- 150000001721 carbon Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- HCMJWOGOISXSDL-UHFFFAOYSA-N (2-isothiocyanato-1-phenylethyl)benzene Chemical compound C=1C=CC=CC=1C(CN=C=S)C1=CC=CC=C1 HCMJWOGOISXSDL-UHFFFAOYSA-N 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims 1
- 208000012659 Joint disease Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 102000009389 Prostaglandin D receptors Human genes 0.000 claims 1
- 108050000258 Prostaglandin D receptors Proteins 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000808 adrenergic beta-agonist Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 1
- 230000004957 immunoregulator effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002458 infectious effect Effects 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
Classifications
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- 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
- C07D403/02—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
- C07D403/12—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 chain containing hetero atoms as chain links
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
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- 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
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- 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
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- 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
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- 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
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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
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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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- 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]
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- C07D405/02—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
- 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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- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Dermatology (AREA)
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- Ophthalmology & Optometry (AREA)
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- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
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- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Claims (23)
1. Spojevi pirazola, naznačeni time, da imaju formulu (Ia) ili (Ib) i njihove farmaceutski prihvatljive soli,
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gdje su
Rai Rb neovisno odabrani od sljedećih: vodik, hidroksi, halogen, C1-C6-alkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-haloalkoksi i C3-C8-cikloalkil, ili Ra i Rb zajedno s atomom ugljika na kojega su vezani za tvorbu, mogu tvoriti karbonilnu skupinu, ili Ra i Rb zajedno s atomom ugljika na kojega su vezani, tvore 3-člani do 8-člani prsten, pri čemu navedeni prsten može sadržavati 1 ili 2 heteroatoma odabrana od Ο, N i S kao člana prstena i gdje članovi prstena od navedenog prstena mogu biti opcijski neovisno supstituirani sa sljedećima: hidroksi, halogen, C1-C6-alkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-haloalkoksi i C3-C8-cikloalkil;
Rc i Rd su neovisno odabrani od sljedećih: vodik, hidroksi, halogen, C1-C6-alkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-haloalkoksi i C3-C8-cikloalkil, ili
Rc i Rd zajedno s atomom ugljika na kojega su vezani za tvorbu, mogu tvoriti karbonilnu skupinu, ili Rc i Rd zajedno s atomom ugljika na kojega su vezani, tvore 3-člani do 8-člani prsten, gdje navedeni prsten može sadržavati 1 ili 2 heteroatoma odabrana od O, N i S kao člana prstena i pri čemu članovi prstena od toga prstena mogu opcijski biti neovisno supstituirani sa sljedećima: hidroksi, halogen, C1-C6-alkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-haloalkoksi i C3-C8-cikloalkil;
Υ1, Υ2, Υ3, Y4 i Y5 su neovisno odabrani od N i CRy, gdje je svaki Ry neovisno odabran od sljedećih: H, hidroksi, halogen, cijano, nitro, SF5, C(0)NRfRg, C1-C6-alkil, hidroksi-C1-C6-alkil, C1-C6alkoksi-C1-C6-alkil, C3-C8-cikloalkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-alkoksi-C1-C6-alkoksi, C1-C6-haloalkoksi, C3-C8-cikloalkoksi, C1-C6-alkilamino, di-C1-C6-alkilamino, C1-C6-alkilsulfonil, fenil, fenoksi, 5-člani ili 6-člani heterociklil i 5-člani ili 6-člani heterocikliloksi, pri čemu su Rf i Rg međusobno neovisno odabrani od sljedećih: H, C1-C6-alkil, C1-C6-haloalkil, C3-C8-cikloalkil, C3-C8-cikloalkenil i 5-člani ili 6-člani heterociklil ili Rf i Rg zajedno s atomom dušika na kojega su vezani, tvore ciklički amin koji može sadržavati sljedeći heteroatom odabran od Ο, N i S kao člana prstena;
Z je odabran od O, S i NRZ, gdje Rz je H, C1-C6-alkil ili benzil;
R1 i R2 su međusobno neovisno odabrani od sljedećih: H, halogen, C1-C6-alkil, C2-C6-alkenil, C2-C6-alkinil, C1-C6-alkoksi, C1-C6-alkiltio, -NRfRg, C3-C8-cikloalkil, C3-C8-cikloalkil-C1-C6-alkil, C3-C8-cikloalkil-C2-C6-alkenil, C3-C8-cikloalkenil, C3-C8-cikloalkenil-C2-C6-alkil, C3-C8-cikloalkenil-C2-C6-alkenil, fenil, fenil-C1-C6-alkil, fenil-C2-C6-alkenil, naftil, naftil-C1-C6-alkil, naftil-C2-C6-alkenil, heterociklil, heterociklil-C1-C6-alkil, i heterociklil-C2-C6-alkenil,
pri čemu su dijelovi molekula od C1-C6-alkila, C2-C6-alkenila i C2-C6-alkinila u gore navedenim radikalima R1 i R2, nesupstituirani ili nose barem jedan supstituent odabran od sljedećih: hidroksi, halogen, cijano, nitro, C1-C6-alkoksi, C1-C6-haloalkoksi, C1-C6-alkilamino, di-C1-C6-alkilamino i C1-C6alkilsulfonil i/ili pri čemu dva radikala vezana na isti atom ugljika od navedenih dijelova molekula C1-C6-alkila, C2-C6-alkenila i C2-C6-alkinila u gore navedenim radikalima R1 i R2 zajedno s navedenim atomom ugljika, mogu tvoriti karbonilnu skupinu, i gdje su dijelovi molekula C3-C8-cikloalkila, cikloalkenila, fenila, naftila i heterociklila u gore navedenim radikalima R1 i R2, nesupstituirani ili nose barem jedan supstituent odabran od sljedećih: hidroksi, halogen, cijano, nitro, C1-C6-alkil, C3-C8-cikloalkil, C1-C6-haloalkil, C1-C6-alkoksi, C1-C6-haloalkoksi, C1-C6-alkilamino, di-C1-C6-alkilamino, C1-C6-alkilsulfonil, fenil i 5-člani ili 6-člani hetaril i/ili pri čemu dva radikala koja su vezana na isti atom ugljika od spomenutih dijelova molekula C3-C8-cikloalkila, C3-C8-cikloalkenila i heterociklila od radikala R1 i R2 zajedno s navedenim atomom ugljika, mogu tvoriti karbonilnu skupinu, i gdje Rf i Rg su međusobno neovisno odabrani od sljedećih: H, C1-C6-alkil, C1-C6-haloalkil, C3-C8-cikloalkil, C3-C8-cikloalkenil i heterociklil ili
Rf i Rg zajedno s atomom dušika na kojega su vezani, tvore ciklički amin koji može sadržavati sljedeći heteroatom odabran od Ο, N i S kao člana prstena; nje cijeli broj od 0, 1, 2 ili 3; i
ako su prisutni R3, odabrani su neovisno od sljedećih: halogen, C1-C6-alkoksi i C1-C6-haloalkoksi.
2. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 1, naznačeni time, da oba Ra i Rb su vodik.
3. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da oba Rc i Rd su vodik.
4. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da Υ1 je CRy1 ili N, pri čemu Ry1 ima jedno od značenja navedenih za Ry u zahtjevu 1.
5. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 4, naznačeni time, da Υ1 je CRy1.
6. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 5, naznačeni time, da Ry1 je odabran od sljedećih: H, C1-C6-alkil, C1-C6alkoksi-C1-C6alkil i C1-C6-haloalkil.
7. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da Y2 je CRy2, Y3 je CRy3, Y4 je CRy4 i Y5 je CRy5, gdje Ry2, Ry3, Ry4 i Ry5 međusobno neovisno imaju značenja kako su definirana za Ry u zahtjevu 1.
8. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 7, naznačeni time, da Ry2, Ry3, Ry4 i Ry5 su neovisno odabrani od sljedećih: H, C1-C6-alkoksi, C1-C6-alkoksi-C1-C6-alkoksi, C1-C6-haloalkoksi.
9. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da Z je O.
10. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od zahtjeva 1 do 8, naznačeni time, da Z je S.
11. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od zahtjeva 1 do 8, naznačeni time, da Z je NRZ.
12. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da R1 i R2 su međusobno neovisno odabrani od sljedećih: H, C1-C6-alkil, C3-C8-cikloalkil, fenil i naftil.
13. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 12, naznačeni time, da R1 i R2 su međusobno neovisno odabrani od sljedećih: H, C1-C4-alkil, C3-C6-cikloalkil i fenil.
14. Spojevi pirazola formule (Ia) ili (Ib) prema zahtjevu 13, naznačeni time, da R1 i R2 su odabrani od C1-C4-alkila.
15. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da n je 0 ili 1.
16. Spojevi pirazola formule (Ia) ili (Ib) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da ako su prisutni R3, tada su oni neovisno odabrani od halogena.
17. Spojevi pirazola formule (Ia) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da su spojevi pirazola odabrani od spojeva formule (Ia'),
[image]
gdje Z, R1, R2, R3, Ry1, Ry2, Ry3, Ry4 i Ry5 imaju jedno od značenja iznesenih u bilo kojem od prethodnih zahtjeva i n je 0 ili 1.
18. Spojevi pirazola formule (Ib) prema bilo kojem od zahtjeva. 1 do 16, naznačeni time, da su spojevi pirazola odabrani od spojeva formule (Ib'),
[image]
gdje Z, R1, R2, R3, Ry1, Ry2, Ry3, Ry4 i Ry5 imaju jedno od značenja iznesenih u bilo kojem od prethodnih zahtjeva i n je 0 ili 1.
19. Spojevi pirazola formule (Ia) ili (lb) prema bilo kojem od prethodnih zahtjeva, naznačeni time, da se upotrebljavaju kao lijekovi.
20. Spojevi pirazola formule (Ia) ili (lb) prema bilo kojem od zahtjeva 1 do 18, naznačeni time, da se upotrebljavaju za liječenje bolesti povezanih s djelovanjem CRTH2.
21. Spojevi pirazola formule (Ia) ili (lb) prema bilo kojem od zahtjeva 1 do 18, naznačeni time, da se upotrebljavaju za prevenciju i/ili liječenje upalnih, infektivnih i imunoregulacijskim poremećaja, respiratornih ili gastrointestinalnih bolesti ili smetnji, upalnih bolesti zglobova i alergijskih bolesti nosa i ždrijela te očiju i kože.
22. Farmaceutske formulacije, naznačene time, da sadrže jedan ili više spojeva pirazola formule (Ia) i/ili (lb) prema bilo kojem od zahtjeva 1 do 18.
23. Farmaceutske formulacije, naznačene time, da sadrže jedan ili više spojeva pirazola formule (Ia) i/ili (lb) prema bilo kojem od zahtjeva 1 do 18 u kombinaciji s jednom ili više djelotvornih tvari odabranih između sljedećih: betamimetici, antikolinergici, kortikosteroidi,
PDE4-inhibitori, LTD4-antagonisti, EGFR-inhibitori, CCR3-antagonisti, CCR5-antagonisti, CCR9-antagonisti, 5-LO-inhibitori, antagonisti histaminskog receptora, SYK-inhibitori i sulfonamidi.
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| EP11151876 | 2011-01-24 | ||
| EP12700695.5A EP2668181B1 (en) | 2011-01-24 | 2012-01-20 | Pyrazole compounds as crth2 antagonists |
| PCT/EP2012/050830 WO2012101043A1 (en) | 2011-01-24 | 2012-01-20 | Pyrazole compounds as crth2 antagonists |
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| US8759386B2 (en) * | 2011-01-24 | 2014-06-24 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CRTH2 antagonists |
| EP2688882B1 (en) * | 2011-03-25 | 2015-05-13 | Boehringer Ingelheim International GmbH | Pyrazole compounds as crth2 antagonists |
| US20140148484A1 (en) * | 2012-11-23 | 2014-05-29 | Boehringer Ingelheim International Gmbh | Pyrazole compounds for treating hairloss |
| WO2014079803A1 (en) | 2012-11-23 | 2014-05-30 | Boehringer Ingelheim International Gmbh | Bicyclosubstituted pyrazole compounds for treating hairloss |
| EP3768245A4 (en) * | 2018-03-23 | 2023-10-18 | Palatin Technologies, Inc. | MELANOCORTIN RECEPTOR-SPECIFIC PEPTIDE FORMULATIONS AND METHODS OF ADMINISTRATION SPECIFIC TO THE GASTROINTESTINAL TRACT |
| CN113874015B (zh) | 2018-12-21 | 2024-05-24 | 细胞基因公司 | Ripk2的噻吩并吡啶抑制剂 |
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| US5260322A (en) | 1990-10-08 | 1993-11-09 | Merck & Co., Inc. | Angiotension II antagonists in the treatment of hyperuricemia |
| PL356487A1 (en) | 1999-11-10 | 2004-06-28 | Takeda Chemical Industries, Ltd. | 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity |
| DE60303238T2 (de) | 2003-04-25 | 2006-09-14 | Actimis Pharmaceuticals, Inc., La Jolla | Pyrimidin-Essigsäure Derivate geeignet zur Behandlung von CRTH2-bedingten Krankheiten |
| JP2007509104A (ja) * | 2003-10-24 | 2007-04-12 | グラクソ グループ リミテッド | 複素環式化合物 |
| CN101084209A (zh) * | 2004-12-21 | 2007-12-05 | 德福根有限公司 | 具有Kv4离子通道活性的化合物 |
| JP4950542B2 (ja) * | 2006-04-07 | 2012-06-13 | 岩手東芝エレクトロニクス株式会社 | 固体撮像装置およびその製造方法 |
| WO2007141267A1 (en) | 2006-06-06 | 2007-12-13 | Glaxo Group Limited | N- (phenylmethyl) -2- (1h-pyraz0l-4-yl) acetamide derivatives as p2x7 antagonists for the treatment of pain, inflammation and neurodegeneration |
| EP2097407A1 (en) * | 2006-11-27 | 2009-09-09 | Pfizer Products Inc. | Pyrazole analogs |
| MX2010003178A (es) * | 2007-09-25 | 2010-04-30 | Actimis Pharmaceuticals Inc | Primidinas sustituidas con 2-s-bencilo como antagonistas de crth2. |
| TW200922587A (en) | 2007-09-25 | 2009-06-01 | Actimis Pharmaceuticals Inc | Alkylthio pyrimidines as CRTH2 antagonists |
| JP2011088826A (ja) * | 2008-01-31 | 2011-05-06 | Astellas Pharma Inc | 芳香族カルボン酸化合物 |
| US20110144160A1 (en) * | 2008-07-03 | 2011-06-16 | Amira Pharmaceuticals, Inc. | Antagonists of Prostaglandin D2 Receptors |
| GB2463788B (en) * | 2008-09-29 | 2010-12-15 | Amira Pharmaceuticals Inc | Heteroaryl antagonists of prostaglandin D2 receptors |
| WO2010057118A2 (en) | 2008-11-17 | 2010-05-20 | Amira Pharmaceuticals, Inc. | Heterocyclic antagonists of prostaglandin d2 receptors |
| WO2010089391A1 (en) * | 2009-02-09 | 2010-08-12 | Boehringer Ingelheim International Gmbh | New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
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