HRP20171302T1 - Makrociklički derivati piridazinona - Google Patents
Makrociklički derivati piridazinona Download PDFInfo
- Publication number
- HRP20171302T1 HRP20171302T1 HRP20171302TT HRP20171302T HRP20171302T1 HR P20171302 T1 HRP20171302 T1 HR P20171302T1 HR P20171302T T HRP20171302T T HR P20171302TT HR P20171302 T HRP20171302 T HR P20171302T HR P20171302 T1 HRP20171302 T1 HR P20171302T1
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- Prior art keywords
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- diyl
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- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- -1 3, 3-dimethylbutyl Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 201000006417 multiple sclerosis Diseases 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 2
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000015943 Coeliac disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000005919 1,2,2-trimethylpropyl group Chemical group 0.000 claims 1
- 125000001989 1,3-phenylene group Chemical group [H]C1=C([H])C([*:1])=C([H])C([*:2])=C1[H] 0.000 claims 1
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 1
- 125000006218 1-ethylbutyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006219 1-ethylpentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006176 2-ethylbutyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004493 2-methylbut-1-yl group Chemical group CC(C*)CC 0.000 claims 1
- 125000005916 2-methylpentyl group Chemical group 0.000 claims 1
- 125000005917 3-methylpentyl group Chemical group 0.000 claims 1
- 208000007815 Acquired Hyperostosis Syndrome Diseases 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 208000026326 Adult-onset Still disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010001935 American trypanosomiasis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 206010004659 Biliary cirrhosis Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000024699 Chagas disease Diseases 0.000 claims 1
- 206010008690 Chondrocalcinosis pyrophosphate Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102100026018 Interleukin-1 receptor antagonist protein Human genes 0.000 claims 1
- 101710144554 Interleukin-1 receptor antagonist protein Proteins 0.000 claims 1
- 102100036342 Interleukin-1 receptor-associated kinase 1 Human genes 0.000 claims 1
- 101710199015 Interleukin-1 receptor-associated kinase 1 Proteins 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000000209 Isaacs syndrome Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000000185 Localized scleroderma Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000003250 Mixed connective tissue disease Diseases 0.000 claims 1
- 206010027982 Morphoea Diseases 0.000 claims 1
- 102100022691 NACHT, LRR and PYD domains-containing protein 3 Human genes 0.000 claims 1
- 101710126825 NACHT, LRR and PYD domains-containing protein 3 Proteins 0.000 claims 1
- 206010072359 Neuromyotonia Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 201000004854 SAPHO syndrome Diseases 0.000 claims 1
- 201000010848 Schnitzler Syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010072148 Stiff-Person syndrome Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 208000004631 alopecia areata Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 208000027625 autoimmune inner ear disease Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 208000000594 bullous pemphigoid Diseases 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000002849 chondrocalcinosis Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000002557 hidradenitis Diseases 0.000 claims 1
- 201000007162 hidradenitis suppurativa Diseases 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 claims 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 238000005710 macrocyclization reaction Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 206010072221 mevalonate kinase deficiency Diseases 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000003631 narcolepsy Diseases 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 230000000737 periodic effect Effects 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Classifications
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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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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Claims (16)
1. Spoj s formulom (I)
[image]
naznačen time da
R1, R3 svaki označavaju, neovisno jedan od drugoga H, (CH2)pCON(R5)2, OA, Hal, COOH, COOA, (CH2)pNHCOA, (CH2)pHet1, (CH2)pNR2R5, ili OH;
R2 označava H ili ravni ili razgranati alkil s 1, 2 ili 3 C atoma, pri čemu jedan ili dva H atoma iz alkilne skupine mogu biti zamijenjeni s OR6, NR5R6, NHCOR5, CONR5R6;
R4 označava H ili metil, etil, propil, izopropil, butil, izobutil, sec-butil ili tert-butil, pentil, 1-, 2- ili 3-metilbutil, 1,1- , 1,2- ili 2,2-dimetil-propil, 1-etilpropil, heksil, 1- , 2- , 3- ili 4-metilpentil, 1,1- , 1,2- , 1,3-, 2,2-, 2,3- ili 3,3-dimetilbutil, 1- ili 2-etilbutil, 1-etil-1-metilpropil, 1-etil-2-metilpropil, 1,1,2- ili 1,2,2-trimetilpropil, trifluorometil;
R5 označava H ili ravni ili razgranati alkil s 1, 2 ili 3 C atoma;
R6 označava H ili ravni ili razgranati alkil s 1, 2 ili 3 C atoma;
Z je odsutan ili označava Ar-diil ili Het-diil;
L označava (CH2)n pri čemu jedna ili dvije CH2 skupine mogu biti zamijenjene sa O i/ili a skupinom CH=CH-, i/ili pri čemu jedan ili dva H atoma mogu biti zamijenjeni s OR2, NR2R5 ili Het1;
Ar-diil označava 1,2-, 1,3- ili 1,4-fenilen proizvoljno supstituiran s od 1 do 5 skupina koje su neovisno odabrane od Hal, CN, -CF3, -OCF3, OH, O-A, SO2-A, COOH, COOA, -CO-A, O-fenil, SO2-fenil, SO2-CF3, Het2 i/ili A;
Het-diil označava nezasićen, zasićen ili aromatski 5- ili 6-člani heterocikal koji ima 1 do 2 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili trisupstituirani s Hal, CN, -CF3, -OCF3, O-A, SO2-A, COOH, COOA, -CO-A, O-fenil, SO2-fenil, SO2-CF3, Het2 i/ili A;
A označava nerazgranati ili razgranati alkil koji ima 1 do 10 C atoma, u kojem 1 do 5 H atoma može biti zamijenjeno s F i/ili u kojem jedna ili dvije ne susjedne CH2 skupine mogu biti zamijenjene s O;
Het1 označava morfolinil, piperidinil ili pirolidinil;
Het2 označava morfolinil, piperidinil ili pirolidinil;
Hal označava F, Cl, Br, I;
n označava 1, 2, 3, 4, 5 ili 6;
p označava 0, 1 ili 2;
i njihovi farmaceutski korisni tautomeri, solvati, soli i stereoizomeri, uključujući njihove smjese u svim omjerima.
2. Spoj s formulom (I) prema zahtjevu 1 naznačen time da R4 je H ili metil.
3. Spoj s formulom (I) prema zahtjevima 1 ili 2 naznačen time da Het-diil označava piridin-diil, pirimidin-diil, piridazin-diil, pirazol-diil, imidazol-diil, piperidin-diil ili pirolidin-diil, od kojih je svaki nesupstituiran ili dvostruko supstituiran s A.
4. Spoj s formulom (I) prema zahtjevima 1, 2 ili 3 naznačen time da Z je 1,3-fenilen, koji je nesupstituiran ili jednostruko supstituiran s A, Hal, OH, ili OA.
5. Spoj s formulom (I), prema zahtjevu 1 naznačen time da je odabran iz slijedeće skupine:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i njihovi farmaceutski korisni tautomeri, solvati, soli i stereoizomeri, uključujući njihove smjese u svim omjerima.
6. Spoj s formulom (I) prema gore navedenim patentnim zahtjevima, te njihovi farmaceutski prihvatljivi tautomeri, soli, solvati i stereoizomeri, uključujući njihove smjese u svim omjerima, naznačen time da je za uporabu kao lijek.
7. Spoj prema zahtjevu 6 naznačen time da je za uporabu za liječenje ili prevenciju upalne bolesti, autoimunog poremećaja, raka ili multiple skleroze i povezanih poremećaja.
8. Spoj prema zahtjevu 7 naznačen time da je autoimuna bolest odabrana iz skupine koju čine astma, reumatoidni artritis, akutni diseminirani encefalomijelitis (ADEM), Addisonova bolest, alopecija areata, ankilozirajući spondilitis, sindrom antifosfolipidnih protutijela (APS), autoimuna hemolitička anemija, autoimuni hepatitis, autoimuna bolest unutarnjeg uha, bulozni pemfigoid, Behçetova bolest, celijakija, anti-transglutaminaza, Chagasova bolest, kronična opstruktivna plućna bolest, Crohnova bolest, dermatomiozitis, šećerna bolest tip 1, endometrioza, Goodpastureov sindrom, Gravesova bolest, Guillain-Barré sindrom (GBS), Hashimotova bolest, Hidradenitis suppurativa, Kawasakijeva bolest, IgA nefropatija, idiopatska trombocitopenična purpura, intersticijski cistitis, eritemski lupus, miješana bolest vezivnog tkiva, morfea, multipla skleroza (MS), miastenija gravis, narkolepsija, neuromiotonija, pemfigus vulgaris, perniciozna anemija, psorijaza, psorijazni artritis, polimiozitis, primarna bilijarna ciroza, reumatoidni artritis, shizofrenija, sklerodermija, Sjögrenov sindrom, sindrom ukočene osobe, sistemska skleroza, temporalni arteritis, ulcerozni kolitis, vaskulitis, vitiligo, Wegenerova granulomatoza.
9. Spoj prema zahtjevu 7 naznačen time da je bolest odabrana iz skupine koju čine reumatoidni artritis, psorijazni artritis, osteoartritis, sistemski eritemski lupus, lupusni nefritis, ankilozirajući spondilitis, osteoporoza, sistemska skleroza, multipla skleroza, psorijaza, dijabetes tipa I, dijabetes tipa II, upalna bolest crijeva (Crohnova bolest i ulcerozni kolitis), hiperimunoglobulinemija D i sindrom periodične groznice, periodični sindromi vezani za kriopirin, Schnitzlerov sindrom, sistemski juvenilni idiopatski artritis, Stillova bolest odrasle dobi, giht, pseudogiht, SAPHO sindrom, Castlemanova bolest, sepsa, moždani udar, ateroskleroza, celijakija, DIRA (nedostatak antagonista IL-1 receptora), Alzheimerova bolest, Parkinsonova bolest, rak.
10. Spoj prema zahtjevu 7 naznačen time da je bolest odabrana od reumatoidnog artritisa, lupusnog nefritisa, sistemskog eritematoznog lupusa.
11. Spoj s formulom (I) prema zahtjevu 1 naznačen time da je za prevenciju i/ili liječenje bolesti povezanih s prekomjernom ekspresijom IRAK.
12. Komplet naznačen time da sadrži odvojena pakiranja:
(a) učinkovite količine spoja formule (I) prema zahtjevu 1 i/ili njegovih farmaceutski prihvatljivih tautomera, solvata, soli, hidrata i stereoizomera, uključujući njihove smjese u svim omjerima, i
(b) učinkovite količine dodatnog aktivnog sastojka lijeka.
13. Farmaceutski pripravak naznačen time da sadrži barem jedan od spojeva s Formulom (I) prema bilo kojem od zahtjeva 1 do 5 i/ili njihove farmaceutski korisne tautomere, solvate, soli i stereoizomere, uključujući njihove smjese u svim omjerima.
14. Farmaceutski pripravak prema zahtjevu 13 naznačen time da dodatno sadrži barem jedan dodatni lijek korišten u liječenju upalnih bolesti ili poremećaja imuniteta.
15. Farmaceutski pripravak prema zahtjevu 14 naznačen time da dodatno sadrži barem jedno dodatno imunomodulacijsko sredstvo.
16. Postupak za sintezu spoja s formulom (I) prema zahtjevu 1 naznačen time da se spoj s formulom (I) dobiva makrociklizacijom spoja s formulom (II) pri čemu R1, R2, R3, R4, Z i L su kako je definirano u zahtjevu 1 i A1 je H, Li, Na ili K:
[image]
.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13154391 | 2013-02-07 | ||
| EP14706474.5A EP2953952B1 (en) | 2013-02-07 | 2014-02-07 | Macrocyclic pyridazinone derivatives |
| PCT/EP2014/000337 WO2014121942A1 (en) | 2013-02-07 | 2014-02-07 | Macrocyclic pyridazinone derivatives |
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| Publication Number | Publication Date |
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| HRP20171302T1 true HRP20171302T1 (hr) | 2017-10-20 |
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| US (2) | US9550794B2 (hr) |
| EP (1) | EP2953952B1 (hr) |
| JP (1) | JP6267729B2 (hr) |
| KR (1) | KR102216812B1 (hr) |
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| HR (1) | HRP20171302T1 (hr) |
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| PT (1) | PT2953952T (hr) |
| RS (1) | RS56269B1 (hr) |
| RU (1) | RU2660435C2 (hr) |
| SG (1) | SG11201506099XA (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PT2953944T (pt) * | 2013-02-07 | 2017-08-01 | Merck Patent Gmbh | Derivados de piridazinona-amidas |
| EP3253764B1 (en) * | 2015-02-05 | 2021-06-09 | Merck Patent GmbH | Macrocyclic compounds as irak1/4 inhibitors and uses thereof |
| EP3253763B1 (en) * | 2015-02-06 | 2020-09-30 | Merck Patent GmbH | Pyridazinone macrocycles as irak inhibitors and uses thereof |
| LT3286181T (lt) | 2015-04-22 | 2021-04-26 | Rigel Pharmaceuticals, Inc. | Pirazolo junginiai ir junginių gamybos bei naudojimo būdas |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| EP3684366A4 (en) | 2017-09-22 | 2021-09-08 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES OF THE LATEST |
| IL273432B (en) | 2017-09-22 | 2022-09-01 | Kymera Therapeutics Inc | Protein compounds and their uses |
| WO2019111218A1 (en) | 2017-12-08 | 2019-06-13 | Cadila Healthcare Limited | Novel heterocyclic compounds as irak4 inhibitors |
| SG11202005912PA (en) | 2017-12-26 | 2020-07-29 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| US11485743B2 (en) | 2018-01-12 | 2022-11-01 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CA3102762A1 (en) * | 2018-06-04 | 2019-12-12 | Ohio State Innovation Foundation | Eaat2 activators and methods of using thereof |
| WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
| TWI721483B (zh) | 2018-07-13 | 2021-03-11 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| US11352350B2 (en) | 2018-11-30 | 2022-06-07 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| WO2020260252A1 (en) | 2019-06-24 | 2020-12-30 | Boehringer Ingelheim International Gmbh | New macrocyclic compounds and derivatives as egfr inhibitors |
| CA3152264A1 (en) | 2019-08-30 | 2021-03-04 | Rigel Pharmaceuticals, Inc. | Pyrazole compounds, formulations thereof, and a method for using the compounds and/or formulations |
| BR112022011651A2 (pt) | 2019-12-17 | 2022-08-23 | Kymera Therapeutics Inc | Degradadores de irak e usos dos mesmos |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| CN114057771B (zh) * | 2020-12-03 | 2023-10-03 | 北京鞍石生物科技有限责任公司 | 大环化合物及其制备方法和应用 |
| WO2024099395A1 (en) * | 2022-11-10 | 2024-05-16 | Beigene, Ltd. | Compounds for the degradation of egfr kinase |
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| CA2458533C (en) * | 2001-10-09 | 2011-01-04 | Tularik Inc. | Imidazole derivates as anti-inflammatory agents |
| MXPA05009972A (es) * | 2003-03-18 | 2005-11-04 | Kowa Co | Derivado de fenilpiridazina soluble en agua y medicina que contiene el mismo. |
| JP2010502717A (ja) * | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン１受容体関連キナーゼの調節物質 |
| MX2011002470A (es) * | 2008-09-08 | 2011-04-05 | Merck Patent Gmbh | Pirimidinas macrociclicas como inhibidores de aurora cinasa. |
| SI2655357T1 (sl) * | 2010-12-20 | 2016-10-28 | Merck Serono S.A. | Derivati indazolil triazola kot zaviralci IRAK |
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