HRP20200253T1 - Benzoimidazol-2-il pirimidinski modulatori histaminskog h4 receptora - Google Patents
Benzoimidazol-2-il pirimidinski modulatori histaminskog h4 receptora Download PDFInfo
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- HRP20200253T1 HRP20200253T1 HRP20200253TT HRP20200253T HRP20200253T1 HR P20200253 T1 HRP20200253 T1 HR P20200253T1 HR P20200253T T HRP20200253T T HR P20200253TT HR P20200253 T HRP20200253 T HR P20200253T HR P20200253 T1 HRP20200253 T1 HR P20200253T1
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- disease
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- pruritus
- hemitartrate tetrahydrate
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- 102000004187 Histamine H4 receptors Human genes 0.000 title claims 3
- 108090000796 Histamine H4 receptors Proteins 0.000 title claims 3
- WTZRQYJHRXQWTK-UHFFFAOYSA-N 2-pyrimidin-2-yl-1h-benzimidazole Chemical compound N=1C2=CC=CC=C2NC=1C1=NC=CC=N1 WTZRQYJHRXQWTK-UHFFFAOYSA-N 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 24
- 208000003251 Pruritus Diseases 0.000 claims 16
- JJXABLRAISJPTN-UHFFFAOYSA-N 2,3-dihydroxybutanedioic acid octahydrate Chemical compound O.O.O.O.O.O.O.O.OC(C(O)C(O)=O)C(O)=O JJXABLRAISJPTN-UHFFFAOYSA-N 0.000 claims 14
- 208000035475 disorder Diseases 0.000 claims 14
- 201000010099 disease Diseases 0.000 claims 10
- 208000006673 asthma Diseases 0.000 claims 6
- 239000012535 impurity Substances 0.000 claims 6
- -1 Hemitartrate tetrahydrate [5-(4,6-Dimethyl-1H-benzoimidazol-2-yl)-4-methyl-pyrimidin-2-yl]-[3-(1-methyl-piperidin-4-yl)-propyl ]-amine Chemical compound 0.000 claims 5
- 238000002441 X-ray diffraction Methods 0.000 claims 5
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 206010020751 Hypersensitivity Diseases 0.000 claims 4
- 208000026935 allergic disease Diseases 0.000 claims 4
- 230000007815 allergy Effects 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 208000020576 Adrenal disease Diseases 0.000 claims 2
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 2
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 206010008635 Cholestasis Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 208000001840 Dandruff Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 206010012442 Dermatitis contact Diseases 0.000 claims 2
- 206010012468 Dermatitis herpetiformis Diseases 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 206010015943 Eye inflammation Diseases 0.000 claims 2
- 206010017533 Fungal infection Diseases 0.000 claims 2
- 208000007465 Giant cell arteritis Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 201000002980 Hyperparathyroidism Diseases 0.000 claims 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000006877 Insect Bites and Stings Diseases 0.000 claims 2
- 206010022971 Iron Deficiencies Diseases 0.000 claims 2
- 206010023126 Jaundice Diseases 0.000 claims 2
- 208000018501 Lymphatic disease Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000031888 Mycoses Diseases 0.000 claims 2
- 208000000592 Nasal Polyps Diseases 0.000 claims 2
- 206010052437 Nasal discomfort Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000030852 Parasitic disease Diseases 0.000 claims 2
- 201000011152 Pemphigus Diseases 0.000 claims 2
- 208000031845 Pernicious anaemia Diseases 0.000 claims 2
- 208000008601 Polycythemia Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000003699 Punctate palmoplantar keratoderma Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 206010039509 Scab Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 2
- 208000006045 Spondylarthropathies Diseases 0.000 claims 2
- 206010042496 Sunburn Diseases 0.000 claims 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 2
- 208000024799 Thyroid disease Diseases 0.000 claims 2
- 241000159241 Toxicodendron Species 0.000 claims 2
- 241000159243 Toxicodendron radicans Species 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 206010047642 Vitiligo Diseases 0.000 claims 2
- 206010048222 Xerosis Diseases 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 208000007502 anemia Diseases 0.000 claims 2
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- 208000010668 atopic eczema Diseases 0.000 claims 2
- 230000001363 autoimmune Effects 0.000 claims 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 2
- 201000004339 autoimmune neuropathy Diseases 0.000 claims 2
- 208000006424 autoimmune oophoritis Diseases 0.000 claims 2
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 2
- 201000004982 autoimmune uveitis Diseases 0.000 claims 2
- 231100000359 cholestasis Toxicity 0.000 claims 2
- 230000007870 cholestasis Effects 0.000 claims 2
- 206010009887 colitis Diseases 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 201000001981 dermatomyositis Diseases 0.000 claims 2
- 238000000502 dialysis Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
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- 230000000694 effects Effects 0.000 claims 2
- 208000014617 hemorrhoid Diseases 0.000 claims 2
- 208000002557 hidradenitis Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 208000018555 lymphatic system disease Diseases 0.000 claims 2
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- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 206010028417 myasthenia gravis Diseases 0.000 claims 2
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- 230000003071 parasitic effect Effects 0.000 claims 2
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 2
- 208000005987 polymyositis Diseases 0.000 claims 2
- 230000035935 pregnancy Effects 0.000 claims 2
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- 206010043207 temporal arteritis Diseases 0.000 claims 2
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- 238000004128 high performance liquid chromatography Methods 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 230000014759 maintenance of location Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
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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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Claims (13)
1. Hemitartarat tetrahidrat [5-(4,6-Dimetil-1H-benzoimidazol-2-il)-4-metil-pirimidin-2-il]-[3-(1-metil-piperidin-4-il)-propil]-amina formule:
[image]
2. Hemitartarat tetrahidrat prema zahtjevu 1, gdje profil difrakcije X-zraka spomenutog hemitartarat tetrahidrata obuhvaća sljedeće signale :
[image]
3. Hemitartarat tetrahidrat prema zahtjevu 1, gdje profil difrakcije X-zraka spomenutog hemitartarat tetrahidrata obuhvaća sljedeće signale :
[image]
4. Hemitartarat tetrahidrat prema zahtjevu 1, gdje profil difrakcije X-zraka spomenutog hemitartarat tetrahidrata obuhvaća sljedeće signale :
[image]
(nastavak)
[image]
5. Hemitartarat tetrahidrat prema zahtjevu 1, gdje profil difrakcije X-zraka spomenutog hemitartarat tetrahidrata obuhvaća sljedeće signale:
[image]
6. Hemitartarat tetrahidrat prema zahtjevu 1, gdje profil difrakcije X-zraka spomenutog hemitartarat tetrahidrata obuhvaća sljedeće signale :
[image]
(nastavak)
[image]
7. Hemitartarat tetrahidrat [5-(4,6-Dimetil-1H-benzoimidazol-2-il)-4-metil-pirimidin-2-il]-[3-(1-metil-piperidin-4-il)-propil]-amina formule:
[image]
gdje spomenuti hemitartarat tetrahidrat je suštinski bez nečistoća I1, I3 i I8 formula:
[image]
gdje izraz "suštinski bez" označava da nečistoća ne može biti otkrivena korištenjem visokoefikasne tekuće kromatografije (HPLC) kao detektorom s masenim spektrometrom (MS) ili ultra-ljubičastim spektroskopom (UV), nalaženjem jedne ili više masa nečistoća, relativnih vremena retencije i količine (kao postotka relativne površine).
8. Hemitartarat tetrahidrat [5-(4,6-Dimetil-1H-benzoimidazol-2-il)-4-metil-pirimidin-2-il]-[3-(1-metil-piperidin-4-il)-propil]-amina prema zahtjevu 7, gdje je spomenuti hemitartarat tetrahidrat dalje suštinski slobodan bar od nečistoće I5 formule:
[image]
9. Hemitartarat tetrahidrat [5-(4,6-Dimetil-1H-benzoimidazol-2-il)-4-metil-pirimidin-2-il]-[3-(1-metil-piperidin-4-il)-propil]-amina prema zahtjevu 8, gdje spomenuti hemitartarat tetrahidrat ne sadrži više od oko 0.2% nečistoće I7 formule:
[image]
10. Hemitartarat tetrahidrat [5-(4,6-dimetil-1H-benzoimidazol-2-il)-4-metil-pirimidin-2-il]-[3-(1-metil-piperidin-4-il)-propil]-amina prema zahtjevu 9, gdje spomenuti hemitartarat tetrahidrat ne sadrži više od oko 0.06% nečistoće I7 formule:
[image]
11. Farmaceutski sastav za upotrebu u liječenju bolesti, poremećaja ili medicinskog stanja u kojem posreduje aktivnost receptora histamina H4 , koji sadrži efikasnu količinu bar spoja prema bilo kojem od zahtjeva 1 ili 7 do 10, gdje bolest, poremećaj, ili medicinsko stanje je upala,
ili gdje bolest, poremećaj ili medicinsko stanje je izabrano iz grupe koju čine: upalni poremećaji, alergijski poremećaji, dermatološki poremećaji, autoimuna bolest, limfatični poremećaji i imunodeficijentni poremećaji,
ili gdje bolest, poremećaj ili medicinsko stanje je izabrano između: alergije, astme, autoimunih bolesti i pruritusa,
ili gdje spomenuta upalna bolest je jedna od kolitisa, Crohnove bolesti i ulceroznog kolitisa,
ili gdje je bolest, poremećaj ili medicinsko stanje izabrano između : alergije, astme, eozinofilne astme, suhog oka, kronične opstruktivne bolesti pluća (COPD), ateroskleroze, reumatoidnog artritisa, multipla skleroze, upalnih bolesti crijeva, psorijaze, pruritusa, svrbeža kože, atopijskog dermatitisa, urtikarije, očne upale, konjuktivitisa, nazalnih polipa, alergijskog rinitisa, nazalnog svrbeža, parazitskih ili gljivičnih infekcija, gnojnog hidradenitisa, maligniteta, kao što su limfomi, žutice, policitemije, punktatne palmoplantarne keratoderme, bolesti štitnjače/hiperparatiroidizam, dijabetesa, vodenih kozica, anemije uslijed nedostatka željeza, psihijatrijskih bolesti, lijekovima izazvanog svrbeža; kolestaze; svrbeža u trudnoći, kseroze, opekotina od sunca, peruti, krasta/ožiljaka, ugriza od insekata, otrovnog bršljana, otrovnog hrasta, hemoroida, kontaktnog dermatitisa, svrbeža u vezi s godinama, svrbeža u vezi s dijalizom, skleroderme, autoimunih bolesti štitnjače, imuno-posredovane šećerne bolesti, lupusa, mijastenije gravis, autoimunih neuropatija, autoimunog uveitisa, autoimune hemolitičke anemije, perniciozne anemije, autoimune trombocitopenije, temporalnog arteritisa, anti-fosfolipidnog sindroma, vaskulitida, Behcetove bolesti, herpetiformnog dermatitisa, pemfigus vulgarisa, vitiliga, primarne bilijarne ciroze, autoimunog hepatitisa, autoimunog ooforitisa i orhitisa, autoimune bolesti nadbubrežne žlijezde, polimiozitisa, dermatomiozitisa, spondiloartropatije, Sjogrenovog sindroma i pruritusa.
12. Spoj prema bilo kojem od zahtjeva 1-10 za upotrebu u terapiji.
13. Spoj prema zahtjevu 1 za upotrebu u postupku liječenja subjekta koji pati od ili kod kojeg je dijagnosticirana bolest, poremećaj ili medicinsko stanje u kojem posreduje aktivnost receptora histamina H4, gdje postupak obuhvaća davanje subjektu kojem je potrebno takvo liječenje efikasne količine spoja prema zahtjevu 1,
gdje bolest, poremećaj ili medicinsko stanje je upala,
ili gdje bolest, poremećaj ili medicinsko stanje je izabrano iz grupe koju čine: upalni poremećaji, alergijski poremećaji, dermatološki poremećaji, autoimuna bolest, limfatični poremećaji i imunodeficijentni poremećaji ,
ili gdje bolest, poremećaj ili medicinsko stanje je izabrano između: alergije, astme, autoimunih bolesti, i pruritusa,
ili gdje spomenuta upalna bolest crijeva je jedna od kolitisa, Crohnove bolesti i ulceroznog kolitisa,
ili gdje bolest, poremećaj, ili medicinsko stanje je izabrano između: alergije, astme, eozinofilne astme, suhog oka, kronične opstruktivne bolesti pluća (COPD), ateroskleroze, reumatoidnog artritisa, multipla skleroze, upalnih bolesti crijeva, psorijaze, pruritusa, svrbeža kože, atopijskog dermatitisa, urtikarije, očne upale, konjuktivitisa, nazalnih polipa, alergijskog rinitisa, nazalnog svrbeža, parazitskih i gljivičnih infekcija, gnojnog hidradenitisa, maligniteta, kao što su limfomi, žutica, policitemija, punktatne palmoplantarne keratoderme, bolesti štitnjače/hiperparatiroidizma, dijabetesa, vodene kozice, anemije uslijed nedostatka željeza, psihijatrijskih bolesti, svrbeža izazvanog lijekovima; kolestaze; svrbeža u trudnoći, kseroze, opekotina od sunca, peruti, krasta/ožiljaka, ugriza insekata, otrovnog bršljana, otrovnog hrasta, hemoroida, kontaktnog dermatitisa, svrbeža u vezi s godinama, svrbeža u vezi s dijalizom, skleroderme, autoimunih bolesti štitnjače, imuno-posredovane šećerne bolesti, lupusa, mijastenije gravis, autoimunih neuropatija, autoimunog uveitisa, autoimune hemolitičke anemije, perniciozne anemije, autoimune trombocitopenije, temporalnog arteritisa, anti-fosfolipidnog sindroma, vaskulitida, Behcetove bolesti, herpetiformnog dermatitisa, pemfigus vulgarisa, vitiliga, primarne bilijarne ciroze, autoimunog hepatitisa, autoimunog ooforitisa i orhitisa, autoimune bolesti nadbubrežne žlijezde, polimiozitisa, dermatomiozitisa, spondiloartropatije, Sjogrenovog sindroma i pruritusa.
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| EP14760540.6A EP2964229B1 (en) | 2013-03-06 | 2014-03-06 | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
| PCT/US2014/021130 WO2014138368A1 (en) | 2013-03-06 | 2014-03-06 | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
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| JO3773B1 (ar) | 2013-03-14 | 2021-01-31 | Janssen Pharmaceutica Nv | معدلات p2x7 |
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