DK1633336T3 - Immunosuppressive forbindelser og sammensætninger - Google Patents
Immunosuppressive forbindelser og sammensætninger Download PDFInfo
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- DK1633336T3 DK1633336T3 DK04752597.7T DK04752597T DK1633336T3 DK 1633336 T3 DK1633336 T3 DK 1633336T3 DK 04752597 T DK04752597 T DK 04752597T DK 1633336 T3 DK1633336 T3 DK 1633336T3
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- inhibitor
- kinase
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Claims (8)
1. 1 -{4-[1 -(4-Cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidin-3-carboxylsyre og de farmaceutisk acceptable salte deraf.
2. Forbindelse ifølge krav 1 af formlen:
og de farmaceutisk acceptable salte deraf.
3. Farmaceutisk sammensætning omfattende en terapeutisk effektiv mængde af en forbindelse ifølge krav 1 eller 2 i kombination med et farmaceutisk acceptabelt excipiens.
4. Farmaceutisk sammensætning omfattende en terapeutisk effektiv mængde af forbindelsen ifølge krav 1 eller 2 i kombination med et immunosuppressivt middel, et immunomodulerende middel, et antiinflammatorisk middel eller et kemoterapeutisk middel.
5. Forbindelse ifølge krav 1 eller 2 eller kombinationen ifølge krav 4 til anvendelse ved behandlingen eller forebyggelsen af allo- eller xenotransplantat akut eller kronisk afstødning eller inflammatoriske eller autoimmune lidelser.
6. Farmaceutisk kombination omfattende en terapeutisk effektiv mængde af forbindelsen ifølge krav 1 i kombination med én eller flere af: i. en aromataseinhibitor, ii. en antiøstrogen, en antiandrogen (især i tilfælde af prostatacancer) eller en gonadorelinagonist, iii. en topoisamerase-l-inhibitor eller en topoisamerase-ll-inhibitor, iv. et mikrotubulusaktivt middel, et alkylerende middel, en antineoplastisk antimetabolit eller en platinforbindelse, v. en forbindelse rettet imod/som formindsker en protein- eller lipidkinaseaktivitet eller en protein- eller lipidphosphataseaktivitet, en yderligere antiangiogen-forbindelse eller en forbindelse, som inducerer celledifferentieringsprocesser, vi. en bradykinin-1 -receptor eller en angiotensin-ll-antagonist, vii. en cyclooxygenaseinhibitor, et bisphosphonat, en histondeacetylaseinhibitor, en heparanaseinhibitor (forhindrer heparansulfatnedbrydning), fortrinsvis PI-88, en biologisk reaktionsmodifikator, fortrinsvis et lymphokin eller interferoner, en ubiquitinationsinhibitor, eller en inhibitor, som blokerer antiapoptotiske veje, viii. en inhibitor af Ras-onkogene isoformer, fortrinsvis Η-Ras, K-Ras eller N-Ras, eller en famesyltransferaseinhibitor, fortrinsvis L-744,832 eller DK8G557, ix. en telomeraseinhibitor, fortrinsvis telomestatin, x. en proteaseinhibitor, en matrixmetalloproteinaseinhibitor, en methioninamino-peptidaseinhibitor, fortrinsvis bengamid eller et derivat deraf, eller en proteosom-inhibitor, fortrinsvis PS-341, og/eller xi. en mTOR-inhibitor.
7. Farmaceutisk kombination ifølge krav 4 eller 6, omfattende én eller flere blandt calcineurininhibitor, fortrinsvis cyclosporin A eller FK 506; en mTOR-inhibitor, fortrinsvis rapamycin, 40-O-(2-hydroxyethyl)-rapamycin, CCI779, ABT578 eller AP23573; en ascomycin med immunosuppressive egenskaber, fortrinsvis ABT-281, ASM981; corticosteroider; cyclophosphamid; azathiopren; methotrexate; leflunomid; mizoribin; mycophenolsyre; mycophenolatmofetil; 15-deoxyspergualin eller en immunosuppressiv homolog, analog eller derivat deraf; immunosuppressive monoklonale antistoffer, fortrinsvis monoklonale antistoffer for leukocytreceptorer, fortrinsvis MHC, CD2, CD3, CD4, CD7, CD8, CD25, CD28, CD40, CD45, CD58, CD80, CD86 eller deres ligander; andre immunomodulatoriske forbindelser, fortrinsvis et rekombinant bindende molekyle med i det mindste en del af det ekstracellulære domæne for CTLA4 eller en mutant deraf, fortrinsvis en i det mindste ekstracellulær del af CTLA4 eller en mutant deraf forbundet med en ikke-CTLA4-proteinsekvens, fortrinsvis CTLA4lg eller en mutant deraf, fortrinsvis LEA29Y; adhæsionsmolekyleinhibitorer, fortrinsvis LFA-1-antagonister, ICAM-1- eller-3-antagonister, VCAM-4-antagonister eller VLA-4-antagonister; steroider, især atamestan, exemestan og formestan og, især, ikke-steroider, især aminoglutethimid, roglethimid, pyridoglutethimid, trilostan, testolacton, ketokonazol, vorozol, fadrozol, anastrozol og letrozol; tamoxifen, fulvestrant, raloxifen og raloxifenhydrochlorid; bicalutamid; abarelix, goserelin og goserelinacetat; topotecan, irinotecan, 9-nitrocamptothecin og det makromolekylære camptothecinkonjugat PNU- 166148; anthracycliner såsom doxorubicin, daunorubicin, epirubicin, idarubicin og nemorubicin, anthraquinonerne mitoxantron og losoxantron, og podophillotoxinerne etoposids og teniposid; taxaner, fortrinsvis paclitaxel og docetaxel, vincaalkaloider, fortrinsvis, vinblastin, især vinblastinsulfat, vincristine, især vincristinsulfat og vinorelbin, discodermolider og epothiloner og derivater deraf, fortrinsvis epothilon B eller et derivat deraf; busulfan, chlorambucil, cyclophosphamid, ifosfamid, melphalan eller nitros-urinstof; 5-fluoruracil, capecitabin, gemcitabin, cytarabin, fludarabin, thioguanin, methotrexat og edatrexat; carboplatin, cis-platin og oxaliplatin; proteintyrosinkinase-og/eller serin- og/eller threoninkinaseinhibitorer eller lipidkinaseinhibitorer, fortrinsvis forbindelser, som er rettet imod, reducerer eller inhiberer aktiviteren af den epidermiske vækstfaktorfamilie af receptortyrosinkinaser (EGFR, ErbB2, ErbB3, ErbB4 som homo-eller heterodimerer), den vaskulære endotheliske vækstfaktorfamilie af receptortyrosinkinaser (VEGFR), de pladeafledte vækstfaktorreceptorer (PDGFR), fibro-blastvækstfaktorreceptorerne (FGFR), den insulinlignende vækstfaktorreceptor 1 (IGF-1R), Trk-receptortyrosinkinasefamilien, Axl-receptortyrosinkinasefamilien, Ret-receptortyrosinkinase, Kit/SCFR-receptortyrosinkinasen, medlemmer af c-Abl-familien og deres genfusionsprodukter, fortrinsvis BCR-Abl, medlemmer af proteinkinase C (PKC) og Raf-familien af serin/threoninkinaser, medlemmer af MEK-, SRC-, JAK-, FAK-, PDK- eller Pl(3)-kinasefamilien, eller af den Pl(3)-kinaserelaterede kinasefamilie, og/eller medlemmer af den cyclinafhængige kinasefamilie (CDK) og antiangiogene forbindelser med en anden mekanisme til disses aktivitet, fortrinsvis ikke-relateret til protein- eller lipidkinaseinhibering; fortrinsvis 1-(4-chloranilino)-4-(4-pyridylmethyl)-phthalazin eller et farmaceutisk acceptabelt salt deraf, fortrinsvis et N-aryl(thio)-anthranilsyreamidderivat, fortrinsvis 2-[(4-pyridyl)methyl]amino-N-[3-methoxy-5-(trifluormethyl)phenyl]benzamid eller 2-[(1-oxido-4-pyridyl)methyl]amino-N-[3-trifluor-methylphenyljbenzamid; endostatin, anthranilinsyreamider; ZD4190; ZD6474; SU5416; SU6668; eller anti-VEGF-antistoffer eller anti-VEGF-receptorantistoffer, fortrinsvis RhuMab; forbindelser, proteiner eller antistoffer, som inhiberer medlemmer af EGF-receptortyrosinkinasefamilien, fortrinsvis EGF-receptor, ErbB2, ErbB3 og ErbB4, eller binder til EGF- eller EGF-relaterede ligander, eller som har en dobbelt inhiberende virkning på ErbB- og VEGF-receptorkinase, såsom fortrinsvis trastuzumab, cetuximab, Iressa, OSI-774, CI-1033, EKB-569, GW-2016, E1.1, E2.4, E2.5, E6.2, E6.4, E2.11, E6.3 eller E7.6.3; forbindelser, som inhiberer PDGF-receptoren, fortrinsvis et N-phenyl- 2-pyrimidinaminderivat, fortrinsvis imatinib; forbindelser, som er rettet imod, reducerer eller inhiberer aktiviteten af c-Abl-familiemedlemmer og deres genfusionsprodukter, fortrinsvis et N-phenyl-2-pyrimidin-aminderivat, fortrinsvis imatinib; PD180970; AG957; eller NSC 680410; forbindelser som er rettede imod, reducerer eller inhiberer aktiviteten af proteinkinase-C-, Raf-, MEK-, SRC-, JAK-, FAK- og PDK-familiemedlemmer, eller Pl(3)-kinase eller Pl(3)-kinaserelaterede familiemedlemmer, og/eller medlemmer af den cyclinafhængige kinasefamilie (CDK), såsom staurosporinderivater, fortrinsvis midostaurin; UCN-01, safingol, BAY 43-9006, Bryostatin 1, Perifosin; llmofosin; RO 318220 og RO 320432; GO 6976; Isis 3521; eller LY333531/LY379196; thalidomid og TNP-470; inhibitorer af phosphatase 1, phosphatase 2A, PTEN eller CDC25, fortrinsvis okadainsyre eller derivater deraf; retinoinsyre, a-, y-, δ-tocopherol eller a-, y- eller δ-tocotrienol; celecoxib, rofecoxib, etoricoxib, valdecoxib eller en 5-alkyl-2-arylaminophenyleddikesyre, fortrinsvis 5-methyl-2-(2'-chlor-6'-fluoranilin)phenyleddike-syre; MS-27-275, SAHA, pyroxamid, FR-901228 eller valproinsyre; etridon-, clodron-, tiludron-, pamidron-, alendron-, ibandron-, risedron- og zoledron-syre; collagenpeptidomimetiske og ikke-peptidomimetiske inhibitorer, tetracyclinderivater, fortrinsvis hydroxamatpeptidomimetisk inhibitor, batimastat og dets oralt biologisk tilgængelige analoge marimastat, prinomastat, BMS-279251, BAY 12-9566, TAA211 eller AAJ996; rapamycin (sirolimus) elleret derivat deraf, fortrinsvis 32-deoxorapamycin, 16-pent-2-ynyloxy-32-deoxorapamycin, 16-pent-2-ynyloxy-32(S)-dihydro-rapamycin, 16-pent-2-ynyloxy-32(S)-dihydro-40-O-(2-hydroxyethyl)-rapamycin og mere fore-trukkent, 40-O-(2-hydroxyethyl)-rapamycin, CCI779 eller 40-[3-hydroxy-2-(hydroxy-methyl)-2-methylpropanoat]-rapamycin eller et farmaceutisk acceptabelt salt deraf, ABT578 eller 40-(tetrazolyl)-rapamycin, især 40-epi-(tetrazolyl)-rapamycin.
8. Forbindelse ifølge kravene 1 eller 2 og sammensætningen ifølge krav 3 til anvendelse ved behandlingen og/eller forebyggelsen af sygdomme eller lidelser, hvor sygdommene eller lidelserne vælges blandt sygdomme eller lidelser medierede af vekselvirkninger af lymphocyter, akut eller kronisk transplantatafstødning af celle-, væv- eller organallo-eller xenotransplantater eller forsinket transplantatfunktion, graft-versus-host-sygdom, autoimmune sygdomme, rheumatoid arthritis, systemisk lupus erythematosus, hashimoto's thyroidis, multipel sclerose, myasthenia gravis, diabetes type I eller II og lidelserne knyttede dertil, vasculitis, perniciøs anæmi, Sjøgren syndrom, uveitis, psoriasis, Graves ophthalmopati, alopecia areata og andre, allergiske sygdomme, allergisk astma, atopisk dermatitis, allergisk rhinitis/konjunktivitis, allergisk kontakt-dermatitis, inflammatoriske sygdomme, inflammatorisk tarmsygdom, Crohn's sygdom eller ulcerativ colitis, intrinsisk astma, inflammatorisk lungebeskadigelse, inflammatorisk leverbeskadigelse, inflammatorisk glomerulumbeskadigelse, atheroscleroe, osteoarthritis, irriteret kontaktdermatitis og yderligere eksematøse dermatitiser, seborrhoisk dermatitis, cutane manifestationer af immunologisk-medierede lidelser, inflammatorisk øjensygdom, keratokonjunktivitis, myocarditis eller hepatitis, iskæmi/reperfusionsskade, myocardial infarkt, slagtilfælde, tarmiskæmi, nyresvigt eller hemorrhagisk chok, traumatisk chok, T-cellelymphomaer eller T-celleleukæmi, infektiøse sygdomme, toksisk chok, septisk chok, voksen åndenødssyndrom eller virale infektioner, AIDS, viral hepatitis, kronisk bakteriel infektion, eller senil demens.
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1546110A4 (en) | 2002-07-30 | 2008-03-26 | Univ Virginia | ACTIVE COMPOUNDS IN THE SIGNALING OF SPHINGOSINE 1-PHOSPHATE |
MY150088A (en) * | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
AU2011224085B2 (en) * | 2003-05-19 | 2013-03-07 | Novartis Ag | Immunosuppressant compounds and compositions |
CA2537093C (en) * | 2003-08-29 | 2013-11-12 | Ono Pharmaceutical Co., Ltd. | Compound capable of binding s1p receptor and pharmaceutical use thereof |
WO2005041899A2 (en) | 2003-11-03 | 2005-05-12 | University Of Virginia Patent Foundation | Orally available sphingosine 1-phosphate receptor agonists and antagonists |
GB0500020D0 (en) | 2005-01-04 | 2005-02-09 | Novartis Ag | Organic compounds |
CA2553572A1 (en) * | 2004-02-24 | 2005-09-09 | Irm Llc | Immunosuppressant compounds and compositions |
TW200538433A (en) * | 2004-02-24 | 2005-12-01 | Irm Llc | Immunosuppressant compounds and compositiions |
RU2478384C2 (ru) | 2004-11-29 | 2013-04-10 | Новартис Аг | Курс лечения с использованием агониста рецептора s1p |
AU2006214314B2 (en) | 2005-02-14 | 2012-02-09 | University Of Virginia Patent Foundation | Sphingosine 1- phos phate agonists comprising cycloalkanes and 5 -membered heterocycles substituted by amino and phenyl groups |
GB0504544D0 (en) * | 2005-03-04 | 2005-04-13 | Novartis Ag | Organic compounds |
EP1873153B1 (en) * | 2005-04-22 | 2010-07-07 | Daiichi Sankyo Company, Limited | 3-azetidinecarboxylic acid derivatives for use as immunosuppressants |
GB0510390D0 (en) * | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
JP2009528274A (ja) | 2006-01-27 | 2009-08-06 | ユニバーシティ オブ バージニア パテント ファンデーション | 神経因性疼痛の治療法 |
WO2007092638A1 (en) | 2006-02-09 | 2007-08-16 | University Of Virginia Patent Foundation | Bicyclic sphingosine 1-phosphate analogs |
US8097644B2 (en) | 2006-03-28 | 2012-01-17 | Allergan, Inc. | Indole compounds having sphingosine-1-phosphate (S1P) receptor antagonist |
GB0612721D0 (en) | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
NZ574012A (en) | 2006-08-08 | 2012-02-24 | Kyorin Seiyaku Kk | Aminoalcohol derivative and immunosuppressant containing the same as active ingredient |
KR101339976B1 (ko) | 2006-08-08 | 2013-12-10 | 교린 세이야꾸 가부시키 가이샤 | 아미노인산에스테르 유도체 및 그들을 유효성분으로 하는 s1p 수용체 조절제 |
JP2009269819A (ja) * | 2006-08-25 | 2009-11-19 | Asahi Kasei Pharma Kk | アミン化合物 |
JP2010510250A (ja) | 2006-11-21 | 2010-04-02 | ユニバーシティ オブ バージニア パテント ファンデーション | スフィンゴシン=1−燐酸受容体アゴニスト活性を有するヒドリンダンアナログ |
CA2669102A1 (en) | 2006-11-21 | 2008-05-29 | University Of Virginia Patent Foundation | Tetralin analogs having sphingosine 1-phosphate agonist activity |
JP2010510251A (ja) | 2006-11-21 | 2010-04-02 | ユニバーシティ オブ バージニア パテント ファンデーション | スフィンゴシン=1−燐酸受容体活性を有するベンゾシクロヘプチルアナログ |
US8524917B2 (en) | 2007-01-11 | 2013-09-03 | Allergan, Inc. | 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity |
CN104337808A (zh) * | 2007-05-04 | 2015-02-11 | 诺华股份有限公司 | S1p受体调节剂的用途 |
BRPI0817397A2 (pt) | 2007-09-24 | 2015-04-07 | Allergan Inc | Compostos indol contendo grupos arila ou heteroarila com atividade biológica do receptor de esfingosina-1-fosfato (sip) |
BRPI0818161B8 (pt) | 2007-10-12 | 2021-05-25 | Novartis Ag | mistura estável compreendendo agonista de receptores de s1p, sua forma de dosagem final e seu uso |
GB0725101D0 (en) * | 2007-12-21 | 2008-01-30 | Glaxo Group Ltd | Compounds |
WO2009099174A1 (ja) | 2008-02-07 | 2009-08-13 | Kyorin Pharmaceutical Co., Ltd. | アミノアルコール誘導体を有効成分とする炎症性腸疾患の治療剤又は予防剤 |
SI2278960T2 (sl) | 2008-03-17 | 2020-02-28 | Actelion Pharmaceuticals Ltd. | Režim odmerjanja za selektivni agonist receptorja sip1 |
GB0807910D0 (en) * | 2008-04-30 | 2008-06-04 | Glaxo Group Ltd | Compounds |
AU2009244538A1 (en) | 2008-05-08 | 2009-11-12 | Allergan, Inc. | Therapeutically useful substituted 1, 7-diphenyl-l, 2, 3, 5, 6, 7-hexahydropyrido [ 3, 2, 1-I J ] quinoline compounds |
US8143291B2 (en) | 2008-05-09 | 2012-03-27 | Allergan, Inc. | Indole compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor biological activity |
SI2300013T1 (en) | 2008-05-21 | 2018-03-30 | Adriad Pharmacaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
CN104311472B9 (zh) | 2008-07-23 | 2020-03-17 | 艾尼纳制药公司 | 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物 |
AU2013209344B2 (en) * | 2008-07-23 | 2015-12-24 | Novartis Ag | Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation |
JP5878015B2 (ja) | 2008-07-23 | 2016-03-08 | ノバルティス アーゲー | スフィンゴシン一リン酸受容体調節因子および筋肉炎症を治療するためのその使用 |
CN102186473B (zh) * | 2008-08-18 | 2014-07-02 | 诺华股份有限公司 | 用于治疗周围神经病的化合物 |
MX2011002199A (es) * | 2008-08-27 | 2011-05-10 | Arena Pharm Inc | Derivados de acidos triciclicos substituidos como agonistas del receptor s1p1 utiles en el tratamiento de trastornos autoinmunes e inflamatorios. |
SG171785A1 (en) | 2008-12-18 | 2011-07-28 | Novartis Ag | Hemifumarate salt of 1- [4- [1- ( 4 -cyclohexyl-3 -trifluoromethyl-benzyloxyimino ) -ethyl] -2 -ethyl-benzyl] -a zetidine-3-carboxylic acid |
AU2009327405A1 (en) | 2008-12-18 | 2011-06-30 | Novartis Ag | New polymorphic form of 1- (4- { l- [ (E) -4-cyclohexyl--3-trifluoromethyl-benzyloxyimino] -ethyl) -2-ethyl-benzy l) -azetidine-3-carboxylic |
BRPI0922466A2 (pt) | 2008-12-18 | 2018-10-23 | Novartis Ag | sais |
RU2561681C2 (ru) * | 2008-12-22 | 2015-08-27 | Новартис Аг | Схема приема агониста рецептора s1p |
US8399451B2 (en) | 2009-08-07 | 2013-03-19 | Bristol-Myers Squibb Company | Heterocyclic compounds |
CN103221391B (zh) | 2010-01-27 | 2018-07-06 | 艾尼纳制药公司 | (R)-2-(7-(4-环戊基-3-(三氟甲基)苄基氧基)-1,2,3,4-四氢环戊二烯并[b]吲哚-3-基)乙酸及其盐的制备方法 |
CA2789480A1 (en) | 2010-03-03 | 2011-09-09 | Arena Pharmaceuticals, Inc. | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
WO2011116091A1 (en) | 2010-03-17 | 2011-09-22 | Novartis Ag | Dispenser |
US8835470B2 (en) | 2010-04-23 | 2014-09-16 | Bristol-Myers Squibb Company | Mandelamide heterocyclic compounds |
EP2619190B1 (en) | 2010-09-24 | 2015-08-12 | Bristol-Myers Squibb Company | Substituted oxadiazole compounds and their use as s1p1 agonists |
CA2819609A1 (en) | 2010-12-03 | 2012-06-07 | Allergan, Inc. | Novel oxime azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators |
CA2819603A1 (en) | 2010-12-03 | 2012-06-07 | Allergan, Inc. | Novel oxime derivatives as sphingosine 1-phosphate (s1p) receptor modulators |
JP5617799B2 (ja) | 2010-12-07 | 2014-11-05 | 信越化学工業株式会社 | 化学増幅レジスト材料及びパターン形成方法 |
JO3619B1 (ar) | 2011-01-07 | 2020-08-27 | Novartis Ag | صياغات مثبطة للمناعة |
WO2012095853A1 (en) | 2011-01-10 | 2012-07-19 | Novartis Pharma Ag | Modified release formulations comprising sip receptor modulators |
EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
WO2013057212A1 (en) | 2011-10-21 | 2013-04-25 | Novartis Ag | Dosage regimen for an s1p receptor modulator or agonist |
US9604914B2 (en) * | 2012-02-03 | 2017-03-28 | Novartis Ag | Process for preparing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester |
US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
CA2900844C (en) * | 2013-04-04 | 2022-05-03 | Novartis Ag | Identifying patient response to s1p receptor modulator administration |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
US9629834B2 (en) | 2013-04-26 | 2017-04-25 | Kyoto University | Medicinal composition for inhibiting formation and/or enlargement of cerebral aneurysm or shrinking same |
EP2862574A1 (en) | 2013-10-15 | 2015-04-22 | Sanofi | {4-[5-(3-chloro-phenoxy)-oxazolo[5,4 d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid for use in the prevention or treatment of acute kidney injury |
US10441654B2 (en) | 2014-01-24 | 2019-10-15 | Children's Hospital Of Eastern Ontario Research Institute Inc. | SMC combination therapy for the treatment of cancer |
CA2938311C (en) | 2014-02-03 | 2023-03-07 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ror-gamma |
SI3207043T1 (sl) | 2014-10-14 | 2019-04-30 | Vitae Pharmaceuticals, Inc. | Dihidropirolopiridinovi inhibitorji za ROR-gama |
US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
AU2016205361C1 (en) | 2015-01-06 | 2021-04-08 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
CA2973540A1 (en) | 2015-02-26 | 2016-09-01 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
KR102603199B1 (ko) | 2015-06-22 | 2023-11-16 | 아레나 파마슈티칼스, 인크. | S1p1 수용체-관련 장애에서의 사용을 위한 (r)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[b]인돌-3-일)아세트산 (화합물 1)의 결정성 l-아르기닌 염 |
US10301261B2 (en) | 2015-08-05 | 2019-05-28 | Vitae Pharmaceuticals, Llc | Substituted indoles as modulators of ROR-gamma |
CN108463458B (zh) | 2015-11-20 | 2022-02-01 | 生命医药有限责任公司 | ROR-γ的调节剂 |
EP3400211A1 (en) | 2016-01-04 | 2018-11-14 | Auspex Pharmaceuticals, Inc. | Azetidine modulators of the sphingosine 1-phosphate receptor |
TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
MX2019009841A (es) | 2017-02-16 | 2020-01-30 | Arena Pharm Inc | Compuestos y metodos para el tratamiento de la colangitis biliar primaria. |
KR20190113955A (ko) | 2017-02-16 | 2019-10-08 | 아레나 파마슈티칼스, 인크. | 장-외 증상을 갖는 염증성 장질환의 치료를 위한 화합물 및 방법 |
US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
US11958805B2 (en) | 2017-03-09 | 2024-04-16 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
WO2019023207A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF RORƳ |
MX2020007270A (es) * | 2017-09-27 | 2020-08-17 | Novartis Ag | Formulacion parenteral que comprende siponimod. |
CN111405897A (zh) | 2017-09-27 | 2020-07-10 | 雷迪博士实验室有限公司 | 辛波莫德、其盐及其固态形式的制备方法 |
AU2018341154A1 (en) | 2017-09-29 | 2020-03-12 | Novartis Ag | Dosing regimen of siponimod |
MX2020007326A (es) | 2017-09-29 | 2020-09-07 | Novartis Ag | Regimen de dosificacion de siponimod. |
US11673860B2 (en) | 2018-01-22 | 2023-06-13 | Teva Pharmaceuticals International Gmbh | Crystalline siponimod fumaric acid and polymorphs thereof |
US11555015B2 (en) | 2018-09-06 | 2023-01-17 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
WO2020114477A1 (zh) * | 2018-12-06 | 2020-06-11 | 上海济煜医药科技有限公司 | 作为免疫调节剂的化合物及其制备方法和应用 |
EP3947348A1 (en) | 2019-03-29 | 2022-02-09 | Synthon B.V. | Process for making siponimod and intermediate thereof |
EP3953326A1 (en) | 2019-04-11 | 2022-02-16 | Synthon B.V. | Solid forms of siponimod |
WO2020234423A1 (en) | 2019-05-21 | 2020-11-26 | Synthon B.V. | Siponimod maleic acid and fumaric acid salt |
CN112745244B (zh) * | 2019-10-30 | 2024-05-03 | 苏州科伦药物研究有限公司 | 一种辛波莫德的中间体及其合成方法 |
IL292529A (en) | 2019-10-31 | 2022-06-01 | Idorsia Pharmaceuticals Ltd | Combination of cxcr7 antagonist with s1p1 receptor modulator |
AR121276A1 (es) | 2020-02-06 | 2022-05-04 | Mitsubishi Tanabe Pharma Corp | Agente terapéutico para la encefalomielitis miálgica / síndrome de fatiga crónica |
US11135197B2 (en) | 2020-02-07 | 2021-10-05 | Argentum Pharmaceuticals Llc | Dosage regimen of an S1P receptor modulator |
WO2021214717A1 (en) | 2020-04-23 | 2021-10-28 | Novartis Ag | Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome |
EP4139282A2 (en) | 2020-05-29 | 2023-03-01 | Cipla Limited | Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof |
IT202000019897A1 (it) | 2020-08-10 | 2022-02-10 | Olon Spa | Procedimento per la preparazione di un intermedio chiave del siponimod |
US20240010616A1 (en) | 2020-09-25 | 2024-01-11 | Synthon B.V. | Siponimod salts and cocrystals |
EP4313941A1 (en) | 2021-03-26 | 2024-02-07 | OLON S.p.A. | Novel crystalline compound of siponimod hemifumarate |
EP4212156A1 (en) | 2022-01-13 | 2023-07-19 | Abivax | Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a s1p receptor modulator |
WO2024126409A1 (en) | 2022-12-12 | 2024-06-20 | Synthon B.V. | Pharmaceutical composition of siponimod |
Family Cites Families (74)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR901228A (fr) | 1943-01-16 | 1945-07-20 | Deutsche Edelstahlwerke Ag | Système d'aimant à entrefer annulaire |
CH540247A (de) * | 1967-04-21 | 1973-09-28 | Ciba Geigy Ag | Verfahren zur Herstellung von heterocyclischen, Asthylendoppelbindungen enthaltenden Verbindungen |
US3872113A (en) * | 1972-05-30 | 1975-03-18 | Endo Lab | Hydroxy- and acetoxy-phthalaldehydric acid, O-(substituted) oximes |
IL86632A0 (en) | 1987-06-15 | 1988-11-30 | Ciba Geigy Ag | Derivatives substituted at methyl-amino nitrogen |
NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
EP0528762B1 (de) | 1991-08-15 | 1997-05-07 | Novartis AG | N-Acyl-N-Heterocyclyl- oder Naphthylalkyl-Aminosäuren als Angiotensin II Antagonisten |
AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
TW225528B (da) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
HU221343B1 (en) | 1992-10-28 | 2002-09-28 | Genentech Inc | Use of anti-vegf antibodies for the treatment of cancer |
IL109161A0 (en) | 1993-03-31 | 1994-06-24 | Cell Therapeutics Inc | Amino alcohol derivatives, methods for the preparation thereof, and pharmaceutical compositions containing the same |
GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
IL110172A (en) | 1993-07-22 | 2001-10-31 | Lilly Co Eli | Bicycle compounds and pharmaceuticals containing them |
US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
JPH10504569A (ja) | 1994-08-24 | 1998-05-06 | イーライ・リリー・アンド・カンパニー | 向代謝性グルタメート受容体拮抗剤としてのピロリジニルジカルボン酸誘導体 |
WO1996030347A1 (en) | 1995-03-30 | 1996-10-03 | Pfizer Inc. | Quinazoline derivatives |
GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
DK0836605T3 (da) | 1995-07-06 | 2002-05-13 | Novartis Ag | Pyrrolopyrimidiner og fremgangsmåder til deres fremstilling |
US5688798A (en) | 1995-10-10 | 1997-11-18 | Hoffmann-La Roche Inc. | Pyrimidine compounds |
US6008220A (en) * | 1995-12-22 | 1999-12-28 | Warner Lambert Company | Aromatic keto-acids and their derivatives as inhibitors of matrix metalloproteinases |
WO1997024119A1 (en) | 1995-12-29 | 1997-07-10 | Smithkline Beecham Corporation | Vitronectin receptor antagonists |
US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
EP0892789B2 (en) | 1996-04-12 | 2009-11-18 | Warner-Lambert Company LLC | Irreversible inhibitors of tyrosine kinases |
DE69734513T2 (de) | 1996-06-24 | 2006-07-27 | Pfizer Inc. | Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten |
AU735648B2 (en) | 1996-07-12 | 2001-07-12 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
JPH11209277A (ja) | 1998-01-19 | 1999-08-03 | Yoshitomi Pharmaceut Ind Ltd | 医薬組成物 |
DE19638745C2 (de) | 1996-09-11 | 2001-05-10 | Schering Ag | Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR) |
WO1998010767A2 (en) | 1996-09-13 | 1998-03-19 | Sugen, Inc. | Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders |
EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
DE69825056T2 (de) | 1997-04-04 | 2005-08-25 | Mitsubishi Pharma Corp. | 2-aminopropan-1,3-diol-verbindungen, ihre medizinische anwendung und zwischenprodukte zu ihrer synthese |
CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
TW557297B (en) | 1997-09-26 | 2003-10-11 | Abbott Lab | Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same |
GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
ZA99252B (en) * | 1998-01-16 | 1999-07-14 | Centaur Pharmaceuticals Inc | Thioether furan nitrone compounds. |
WO1999046277A1 (en) * | 1998-03-09 | 1999-09-16 | Smithkline Beecham Corporation | HUMAN EDG-1c POLYNUCLEOTIDES AND POLYPEPTIDES AND METHODS OF USE |
DE69942097D1 (de) | 1998-08-11 | 2010-04-15 | Novartis Ag | Isochinoline derivate mit angiogenesis-hemmender wirkung |
US6630998B1 (en) * | 1998-08-13 | 2003-10-07 | Acushnet Company | Apparatus and method for automated game ball inspection |
GB9824579D0 (en) | 1998-11-10 | 1999-01-06 | Novartis Ag | Organic compounds |
UA71587C2 (uk) | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
WO2000034228A1 (en) * | 1998-12-04 | 2000-06-15 | Neurosearch A/S | Ion channel modulating agents |
WO2000037502A2 (en) | 1998-12-22 | 2000-06-29 | Genentech, Inc. | Vascular endothelial cell growth factor antagonists and uses thereof |
EP1165085B1 (en) | 1999-03-30 | 2006-06-14 | Novartis AG | Phthalazine derivatives for treating inflammatory diseases |
MXPA01009871A (es) | 1999-04-01 | 2002-04-24 | Pfizer Prod Inc | Aminopiridinas como inhibidores de la sorbitol deshidrogenasa. |
UA73307C2 (uk) | 1999-08-05 | 2005-07-15 | Куміаі Кемікал Індастрі Ко., Лтд. | Похідна карбамату і фунгіцид сільськогосподарського/садівницького призначення |
EP1212331B1 (en) | 1999-08-24 | 2004-04-21 | Ariad Gene Therapeutics, Inc. | 28-epirapalogs |
JP2001151771A (ja) | 1999-09-10 | 2001-06-05 | Kyowa Hakko Kogyo Co Ltd | 含窒素芳香族複素環誘導体 |
EP1315735A4 (en) | 2000-08-31 | 2005-04-06 | Merck & Co Inc | Phosphate derivatives as immunoregulatory compounds |
JP2002167371A (ja) * | 2000-09-21 | 2002-06-11 | Sankyo Co Ltd | フェニルプロピオン酸誘導体 |
US20020147198A1 (en) | 2001-01-12 | 2002-10-10 | Guoqing Chen | Substituted arylamine derivatives and methods of use |
TWI311133B (en) * | 2001-04-20 | 2009-06-21 | Eisai R&D Man Co Ltd | Carboxylic acid derivativeand the salt thereof |
WO2002092068A1 (fr) | 2001-05-10 | 2002-11-21 | Ono Pharmaceutical Co., Ltd. | Derives d'acide carboxylique et medicaments contenant ces derives comme principe actif |
JP3714205B2 (ja) | 2001-07-10 | 2005-11-09 | ソニー株式会社 | 非水電解液二次電池 |
CN1545514A (zh) | 2001-08-27 | 2004-11-10 | 阿拉宾度药业有限公司 | β型晶体无水氨曲南的生产方法 |
JP2003073357A (ja) | 2001-09-03 | 2003-03-12 | Mitsubishi Pharma Corp | アミド化合物を含有するRhoキナーゼ阻害剤 |
US20040235866A1 (en) | 2001-09-05 | 2004-11-25 | Takahisa Hanada | Lymphocytic activation inhibitor and remedial agent for autoimmune disease |
AU2002363236A1 (en) | 2001-10-30 | 2003-05-12 | Millennium Pharmaceuticals, Inc. | Compounds, pharmaceutical compositions and methods of use therefor |
JP4430941B2 (ja) | 2002-01-18 | 2010-03-10 | メルク エンド カムパニー インコーポレーテッド | Edg受容体作動薬 |
AU2003216054B2 (en) | 2002-01-18 | 2007-01-04 | Merck & Co., Inc. | Selective S1P1/Edg1 receptor agonists |
US20030207924A1 (en) | 2002-03-07 | 2003-11-06 | Xue-Min Cheng | Compounds that modulate PPAR activity and methods of preparation |
PL373697A1 (en) | 2002-04-26 | 2005-09-05 | F.Hoffmann-La Roche Ag | Isoquinoline derivatives |
AU2003241601A1 (en) * | 2002-05-24 | 2003-12-12 | Pharmacia Corporation | Anilino liver x-receptor modulators |
CA2486853A1 (en) * | 2002-05-27 | 2003-12-04 | Novartis Ag | Bis-aromatic alkanols |
US6846832B2 (en) | 2002-08-07 | 2005-01-25 | Hoffman-La Roche Inc. | 2,3-dihydro-isoindol-1-one derivatives |
TW200408393A (en) | 2002-10-03 | 2004-06-01 | Ono Pharmaceutical Co | Antagonist of lysophosphatidine acid receptor |
JP4505449B2 (ja) * | 2003-02-11 | 2010-07-21 | アイアールエム・リミテッド・ライアビリティ・カンパニー | 新規二環式化合物および組成物 |
TW200505442A (en) | 2003-05-19 | 2005-02-16 | Genomics Inst Of The Novartis Res Foundation | Immunosuppressant compounds and compositions |
MY150088A (en) * | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
CA2537093C (en) | 2003-08-29 | 2013-11-12 | Ono Pharmaceutical Co., Ltd. | Compound capable of binding s1p receptor and pharmaceutical use thereof |
ES2346665T3 (es) | 2004-05-07 | 2010-10-19 | Warner-Lambert Company Llc | Derivados de fenol y tiofenol 3- o 4-monosustituidos utiles como ligandos de h3. |
WO2006021884A2 (en) | 2004-08-26 | 2006-03-02 | Pfizer Inc. | Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors |
BRPI0720048A8 (pt) | 2006-12-14 | 2023-02-07 | Dow Agrosciences Llc | Proteínas de dedo de zinco não-canônicas otimizadas |
-
2004
- 2004-05-18 MY MYPI20041871A patent/MY150088A/en unknown
- 2004-05-19 CN CN2012103237490A patent/CN102875413A/zh active Pending
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- 2004-05-19 PE PE2004000513A patent/PE20050626A1/es active IP Right Grant
- 2004-05-19 PL PL04752597T patent/PL1633336T3/pl unknown
- 2004-05-19 SI SI200432347A patent/SI1633336T1/sl unknown
- 2004-05-19 LT LTEP04752597.7T patent/LT1633336T/lt unknown
- 2004-05-19 CL CL200401119A patent/CL2004001119A1/es unknown
- 2004-05-19 US US10/849,323 patent/US20050014728A1/en not_active Abandoned
- 2004-05-19 EP EP16166665.6A patent/EP3138835A1/en not_active Withdrawn
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- 2004-05-19 EP EP11183758.9A patent/EP2514743B1/en not_active Expired - Lifetime
- 2004-05-19 IS IS8153A patent/IS3007B/is unknown
- 2004-05-19 NZ NZ543241A patent/NZ543241A/en unknown
- 2004-05-19 AR ARP040101736A patent/AR044403A1/es active IP Right Grant
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- 2004-05-19 PT PT47525977T patent/PT1633336T/pt unknown
- 2004-05-19 KR KR1020057022058A patent/KR101118779B1/ko active IP Right Grant
- 2004-05-19 WO PCT/US2004/015603 patent/WO2004103306A2/en active Search and Examination
- 2004-05-19 EP EP16202251.1A patent/EP3272736A1/en not_active Withdrawn
- 2004-05-19 MX MXPA05012462A patent/MXPA05012462A/es active IP Right Grant
- 2004-05-19 DK DK04752597.7T patent/DK1633336T3/da active
- 2004-05-19 CA CA2524047A patent/CA2524047C/en not_active Expired - Lifetime
- 2004-05-19 TW TW093114151A patent/TWI355931B/zh active
- 2004-05-19 HU HUE04752597A patent/HUE030772T2/en unknown
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2005
- 2005-10-31 IL IL171683A patent/IL171683A/en not_active IP Right Cessation
- 2005-11-10 EC EC2005006148A patent/ECSP056148A/es unknown
- 2005-11-15 MA MA28608A patent/MA27807A1/fr unknown
- 2005-11-18 TN TNP2005000294A patent/TNSN05294A1/en unknown
- 2005-12-08 NO NO20055837A patent/NO334457B1/no unknown
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2006
- 2006-07-27 HK HK06108361.8A patent/HK1087929A1/zh not_active IP Right Cessation
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2008
- 2008-02-01 US US12/024,992 patent/US7939519B2/en not_active Expired - Lifetime
- 2008-07-11 AU AU2008203087A patent/AU2008203087A1/en not_active Abandoned
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2009
- 2009-08-26 RU RU2009132108/04A patent/RU2009132108A/ru not_active Application Discontinuation
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2010
- 2010-08-20 JP JP2010185021A patent/JP2011012069A/ja active Pending
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2016
- 2016-09-07 HR HRP20161156TT patent/HRP20161156T1/hr unknown
- 2016-09-20 CY CY20161100933T patent/CY1118299T1/el unknown
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