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31. 发明专利

PT2280696E MODULADORES DO RECETOR DA PROSTACICLINA (PGI2) ÚTEIS PARA O TRATAMENTO DE DISTÚRBIOS COM ELE RELACIONADOS 未知
公开(公告)号：PT2280696E
公开(公告)日：2014-12-12
申请号：PT09721284
申请日：2009-03-17
申请人： ARENA PHARM INC
发明人： SHIN YOUNG-JUN , TRAN THUY-ANH , CHEN WEICHAO , KRAMER BRYAN A , SADEQUE ABU J M , SHYFRYNA HANNA L , VALLAR PUREZA , ZOU NING
IPC分类号： A61K31/17 , A61K31/27 , A61P43/00 , C07C271/08 , C07C275/18

32. 发明专利

EA019882B1 МОДУЛЯТОРЫ РЕЦЕПТОРА ПРОСТАЦИКЛИНА (PGI2), ПРИГОДНЫЕ ДЛЯ ЛЕЧЕНИЯ СВЯЗАННЫХ С НИМ РАССТРОЙСТВ 未知
公开(公告)号：EA019882B1
公开(公告)日：2014-07-30
申请号：EA201071090
申请日：2009-03-17
申请人： ARENA PHARM INC
发明人： TRAN THUY-ANH , CHEN WEICHAO , KRAMER BRYAN A , SADEQUE ABU J M , SHYFRYNA HANNA L , SHIN YOUNG-JUN , VALLAR PUREZA , ZOU NING
IPC分类号： A61K31/17 , A61K31/27 , A61P43/00 , C07C271/08 , C07C275/18
摘要： Изобретениеотноситсяк амиднымпроизводнымформулы (XIIIa) ифармацевтическимкомпозициямнаосновеэтихсоединений, которыемодулируютактивность PGI2 рецептора. Соединенияпонастоящемуизобретениюи фармацевтическиекомпозициинаосновеэтихсоединенийнаправленынаспособы, полезныедлялечениялегочнойартериальнойгипертензии (РАН); идиопатическойРАН; семейнойРАН; РАН, связаннойс коллагеновымсосудистымзаболеванием, врожденнымсердечнымзаболеванием, портальнойгипертензией, ВИЧинфекцией, приемомлекарственногосредстваилитоксина, наследственнойгеморрагическойтелеангиэктазией, спленэктомией, легочнымвеноокклюзивнымзаболеванием (PVOD) илилегочнымкапиллярнымгемангиоматозом (РСН); РАНс существеннымпоражениемвениликапилляров; агрегациитромбоцитов; заболеваниякоронарныхартерий; инфарктамиокарда; преходящегонарушениямозговогокровобращения; стенокардии; удара; ишемическогореперфузионногопоражения; рестеноза; фибрилляциипредсердия; образованиясгусткакровиу пациентапослеоперацииангиопластикииликоронарногошунтирования, илиу субъекта, страдающегоотфибрилляциипредсердия; атеротромбоза; астмыилиеесимптома; связанныхс диабетомрасстройств, такихкакдиабетическаяпериферическаяневропатия, диабетическаянефропатияилидиабетическаяретинопатия; глаукомыилидругогоглазногозаболеванияс аномальнымвнутриглазнымдавлением; гипертензии; воспаления; псориаза; псориатическогоартрита; ревматоидногоартрита; болезниКрона; отторжениятрансплантата; рассеянногосклероза; системнойкраснойволчанки (SLE); язвенногоколита; атеросклероза; акне; диабетатипа 1; диабетатипа 2; сепсиса

33. 发明专利

AU2009325117B2 Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto 未知
公开(公告)号：AU2009325117B2
公开(公告)日：2014-07-10
申请号：AU2009325117
申请日：2009-11-24
申请人： ARENA PHARM INC
发明人： TRAN THUY-ANH , IBARRA JASON B , SHIN YOUNG-JUN , ULLMAN BRETT , ZOU NING , ZENG XI
IPC分类号： C07D231/12 , A61K31/415 , A61K31/4155 , A61K31/416 , A61P9/00 , A61P11/00 , C07D231/18 , C07D231/54 , C07D231/56 , C07D401/04 , C07D405/04 , C07D409/04
摘要： Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

34. 发明专利

CA2532152C TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 未知
公开(公告)号：CA2532152C
公开(公告)日：2013-10-01
申请号：CA2532152
申请日：2004-07-09
申请人： ARENA PHARM INC
发明人： JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , CALDERON IMELDA , CHOI JIN SUN KAROLINE , FIORAVANTI BEATRIZ , LEHMANN JUERG , BRUCE MARC A
IPC分类号： C07D401/12 , A61K31/4439 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P3/10 , C07D239/52 , C07D239/54 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

35. 发明专利

ZA201103813B PYRAZOLYL SUBSTITUTED CARBONIC ACID DERIVATIVES AS MODULATORS OF THE PROSTACYCLIN (PG12) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 未知
公开(公告)号：ZA201103813B
公开(公告)日：2012-10-31
申请号：ZA201103813
申请日：2011-05-24
申请人： ARENA PHARM INC
发明人： TRAN THUY-ANH , SHIN YOUNG-JUN , ZOU NING , IBARRA JASON B , ULLMAN BRETT R , ZENG XI
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101
摘要： Pyrazole derivatives of Formula la and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

36. 发明专利

ZA201006694B MODULATORS OF THE PROSTACYCLIN (PG12) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 未知
公开(公告)号：ZA201006694B
公开(公告)日：2012-03-28
申请号：ZA201006694
申请日：2010-09-17
申请人： ARENA PHARM INC
发明人： TRAN THUY-ANH , CHEN WEICHAO , KRAMER BRYAN A , SADEQUE ABU JM , SHYFRYNA HANNA L , SHIN YOUNG-JUN , VALLAR PUREZA , ZOU NING
IPC分类号： A61P20060101 , A61K20060101 , C07C20060101
摘要： The present invention relates to amide derivatives of Formula (Xllla) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

37. 发明专利

NZ578505A Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto 未知
公开(公告)号：NZ578505A
公开(公告)日：2011-03-31
申请号：NZ57850504
申请日：2004-07-09
申请人： ARENA PHARM INC
发明人： JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , CALDERON IMELDA , CHOI JIN SUN KAROLINE , FIORAVANTI BEATRIZ , LEHMANN JUERG , BRUCE MARC A
IPC分类号： C07D401/12 , A61K31/4439 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P3/10 , C07D239/52 , C07D239/54 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Disclosed herein is the use of trisubstituted aryl and heteroaryl compounds of formula (I), wherein the substituents are as defined in the specification. Such compounds are useful in the treatment of conditions ameliorated by promoting beta-cell proliferation, condition ameliorated by inhibiting beta-cell death, idiopathic type 1 diabetes (Type 1 b), latent autoimmune diabetes in adults (LAD A), early-onset type 2 diabetes (EOD), youth-onset atypical diabetes (YOAD), maturity onset diabetes of the young (MODY), malnutrition-related diabetes, gestational diabetes, coronary hear disease, ischemia, a transient ischemic event, stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction, necrosis, apoptosis, post-prandial lipemia, a condition of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity, osteoporosis, hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetic retinopathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, metabolic syndrome, premenstrual syndrome, coronary hear disease, angina pectoris, thrombosis, atherosclerosis, vascular restenosis, hyperinsulinemia, impaired glucose metabolism, erectile dysfunction, a skin or connective tissue disorder, foot ulceration, ulcerative colitis, endothelial dysfunction, or impaired vascular compliance. (62) Divided Out of 544140

38. 发明专利

RS50540B SUBSTITUISANI PIRIDINIL I PIRIMIDINIL DERIVATI KAO MODULATORI METABOLIZMA I LEČENJE POREMEĆAJA PROISTEKLIH IZ TOGA 未知
公开(公告)号：RS50540B
公开(公告)日：2010-05-07
申请号：RSP20080068
申请日：2006-01-09
申请人： ARENA PHARM INC
发明人： HURST DAVID , JONES ROBERT , WONG AMY , LEHMANN JUERG , SHIN YOUNG-JUN
IPC分类号： C07D401/14 , A61K31/44 , A61K31/505
摘要： Jedinjenje odabrano od jedinjenja formule (la) i njihove farmaceutski prihvatljive soli, solvati i hidrati: naznačena time, što:X je N ili CR8 pri čemu je R8 H ili halogen; Y je NH ili O; Z je CH ili N;R1 je karbo-C1-C6-alkoksi, oksadiazolii ili pirimidinil gde su navedeni karbo-C1-C6-alkoksi, oksadiazolil ili pirimidinil svaki opciono supstituisani sa 1 ili 2 supstituentima nezavisno odabranim od grupe koja se sastoji od -C1-4 alkil, -C1-4-alkoksi i C3-5 cikloalkil; R2 je H ili C1-4 alkil;R3 je C1-4 alkoksi, O-C2-4-alkinil ili hidroksil;R4 je odabran od grupe koja se sastoji od H, C1-4 alkoksi, C1-4 alkil, C2-4 alkinil i halogen;R5 je odabran od grupe koja se sastoji od C1-4 acilsulfonamid, C1-4 alkoksi, C1-4 alkil, C1-4 alkilamino, C1-4 alkilsulfonil, C1-4 alkiltio, cijano, heterociklil, di-C1-4-dialkilamino i silfonamid, pri čemu su navedeni C1-4 alkoksi, C1-4 alkil, C1-4 alkilamino, C1-4 alkilsulfonil, C1-4 alkiltio, di- C1-4 dialkilamino i heterociklil svaki opciono supstituisani sa 1 ili 2 supstituenata nezavisno odabranih od grupe koja se sastoji od C2-4.alkinil, C1.4alkoksi, C1.4alkilkarboksamid, C1-4 alkilsulfonil, C3-5cikloalkil, C3-5cikloalkiloksi, di-C1-4-alkilkaboksamid, hidroksil i fosfonooksi, pri čemu je navedeni C1-4 alkilkarboksamid opciono supstituisan sa hidroksil; ili R5 je grupa Formule (A): pri čemu su:m, n i q svaki nezavisno 0, 1, 2 ili 3;r je 0, 1 ili 2; i t je 0 ili 1; R6 je H ili halogen; i R7 je H ili C1-4alkilPrijava sadrži još 61 patentni zahtev.

39. 发明专利

MY141116A TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 未知
公开(公告)号：MY141116A
公开(公告)日：2010-03-15
申请号：MYPI20042770
申请日：2004-07-09
申请人： ARENA PHARM INC
发明人： JONES ROBERT M , BRUCE MARC A , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , CALDERON IMELDA , FIORAVANTI BEATRIZ , CHOI JIN SUN KAROLINE , LEHMANN JUERG
IPC分类号： C07D401/12 , A61K31/4439 , A61K31/513 , A61P3/10 , C07D239/52 , C07D239/54 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： THE PRESENT INVENTION RELATES TO CERTAIN TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES OF FORMULA (I) THAT ARE MODULATORS OF METABOLISM. ACCORDINGLY, COMPOUNDS OF THE PRESENT INVENTION ARE USEFUL IN THE PROPHYLAXIS OR TREATMENT OF METABOLIC DISORDERS AND COMPLICATIONS THEREOF, SUCH AS, DIABETES AND OBESITY.

40. 发明专利

DK1911756T3 Substituerede pyridinyl- og pyrimidinylderivater som modulatorer af metabolisme og behandling af forstyrrelser relateret dertil 未知
公开(公告)号：DK1911756T3
公开(公告)日：2010-02-08
申请号：DK07023528
申请日：2006-01-09
申请人： ARENA PHARM INC
发明人： WONG AMY SIU-TING , HURST DAVID , JONES ROBERT M , LEHMANN JUERG , SHIN YOUNG-JUN
IPC分类号： C07D401/12 , A61K31/4545 , A61K31/506 , A61P3/00 , C07D401/14 , C07D413/14

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