HRP20191944T1 - Soli i polimorfi od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6h-azepino[5,4,3-cd]indol-6-ona - Google Patents

Soli i polimorfi od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6h-azepino[5,4,3-cd]indol-6-ona Download PDF

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HRP20191944T1
HRP20191944T1 HRP20191944TT HRP20191944T HRP20191944T1 HR P20191944 T1 HRP20191944 T1 HR P20191944T1 HR P20191944T T HRP20191944T T HR P20191944TT HR P20191944 T HRP20191944 T HR P20191944T HR P20191944 T1 HRP20191944 T1 HR P20191944T1
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cancer
salt
camsylate
ray powder
diffraction pattern
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HRP20191944TT
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Patricia Ann Basford
Anthony Michael Campeta
Adam Gillmore
Matthew Cameron Jones
Elefherios Kougoulos
Suman Luthra
Robert Wallton
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Pfizer Inc.
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Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of HRP20191944T1 publication Critical patent/HRP20191944T1/hr

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Claims (19)

1. Sol, naznačena time, da se upotrebljava u postupku inhibiranja aktivnosti poli(ADP-riboza)polimeraze (PARP) kod sisavaca, pri čemu postupak obuhvaća davanje sisavcu terapeutski učinkovite količine soli odabrane iz skupine koja se sastoji od kamsilatne soli od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona i maleatne soli od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona.
2. Sol za uporabu u postupku prema patentnom zahtjevu 1, naznačena time, da sisavac ima mutaciju BRCA1 i/ili mutaciju BRCA2.
3. Sol za uporabu u postupku prema patentnom zahtjevu 1 ili zahtjevu 2, naznačena time, da navedeni postupak je postupak liječenja raka.
4. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da sisavac ima rak odabran iz skupine koja se sastoji od sljedećih: mezoteliom, hepatobilijarni rak, primarni tumor centralnog nervnog sustava (CNS), sekundarni tumor CNS sustava, primarni tumor mozga, sekundarni tumor mozga, rak pluća, rak kostiju, rak gušterače, rak kože, rak glave, rak vrata, kutani melanom, intraokularni melanom, rak jajnika, rak debelog crijeva, rak rektuma, rak analnog područja, rak želuca, gastrointestinalni rak, rak dojke, rak maternice, karcinom falopijeve tube, karcinom endometrija, karcinom cerviksa, karcinom vagine, karcinom vulve, Hodgkinova bolest, rak jednjaka, rak malog crijeva, rak endokrinog sustava, rak tiroidne žlijezde, rak paratiroidne žlijezde, rak adrenalne žlijezde, sarkom mekog tkiva, rak mokraćne cijevi, rak penisa, rak prostate, rak testisa, kronična leukemija, akutna leukemija, kronična mijeloidna leukemija, limfocitni limfomi, rak mjehura, rak bubrega, rak mokraćovoda, rak renalne stanice, karcinom renalne karlice, neoplazme CNS sustava, primarni limfom CNS sustava, ne-Hodgkinov limfom, tumori kralježnice, gliom moždanog debla, adenom hipofize, adrenokortikalni rak, rak žučnog mjehura, višestruki mijelom, kolangiokarcinom, fibrosarkom, neuroblastom i retinoblastom.
5. Sol za uporabu u postupku prema patentnom zahtjevu 1, naznačena time, da sisavac ima stanje bolesti odabrano iz skupine koja se sastoji od sljedećih: dijabetička retinopatija, neovaskularni glaukom, reumatoidni artritis, psorijaza i makularna degeneracija vezana uz dob.
6. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da postupak nadalje obuhvaća davanje terapeutski učinkovite količine spoja odabranog iz skupine koja se sastoji od sljedećih: antitumorsko sredstvo, sredstvo antiangiogeneze, inhibitor signalne transdukcije, antiproliferativno sredstvo, mitotički inhibitor, alkilacijsko sredstvo, anti-metabolit, interkalacijski antibiotik, inhibitor faktora rasta, inhibitor staničnog ciklusa, enzim, inhibitor topoizomeraze, modifikator biološkog odgovora, protutijelo, citotoksično sredstvo, anti-hormon i anti-androgen; prema potrebi s time, da je navedeno antitumorsko sredstvo odabrano iz skupine koja se sastoji od temozolomida, irinotekana, topotekana, cisplatina i doksorubicin-hidroklorida.
7. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je sol kristal i ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 12,2 ± 0,2, 14,8 ± 0,2 i 22,4 ± 0,2, pri čemu se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
8. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je navedeni kamsilat S-kamsilat ili R-kamsilat.
9. Sol za uporabu u postupku prema bilo kojem od patentnih zahtjeva 1 do 6, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je navedena kamsilatna sol S-kamsilat polimorfnog Oblika A, dok polimorf ima uzorak difrakcije praha X-zraka koji sadrži jednu ili više ili dvije ili više ili tri vršne vrijednosti s difrakcijskim kutevima (2θ) odabranima iz skupine koju čine: 12,2 ± 0,2, 14,8 ± 0,2 i 22,4 ± 0,2, gdje se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
10. Sol za uporabu u postupku prema bilo kojem od patentnih zahtjeva 1 do 6, naznačena time, da sol je maleatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je navedena maleatna sol odabrana iz skupine koja se sastoji od maleata polimorfnog Oblika A, dok polimorf ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 6,0 ± 0,2, 20,3 ± 0,2 i 21,7 ± 0,2, gdje se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma, i maleata polimorfnog Oblika B, gdje polimorf ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 7,5 ± 0,2, 11,3 ± 0,2 i 24,3 ± 0,2, s time, da se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
11. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da se navedena sol primjenjuje u farmaceutskom pripravku koji se prepisuje u čvrstom obliku za doziranje; prema potrebi s time, da je navedeni čvrsti oblik za doziranje odabran iz skupine koja se sastoji od tablete, praška, zrnca, pastile i tablete za cuclanje dijamantog oblika.
12. Sol za uporabu u postupku prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da doza soli koja se prepisuje, iznosi od oko 0,001 do oko 1000 mg/kg tjelesne težine sisavca; dok prema potrebi doza soli koja se prepisuje, iznosi od oko 0,001 do oko 50 mg/kg tjelesne težine sisavca.
13. Uporaba soli odabrane iz skupine koja se sastoji od kamsilatne soli od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona i maleatne soli od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, naznačena time, da je za proizvodnju lijeka za liječenje stanja bolesti kod sisavaca koje je posredovano putem aktivnosti poli(ADP-riboza)polimeraze.
14. Uporaba prema patentnom zahtjevu 13, naznačena time, da stanje bolesti je rak koji je odabran iz skupine koja se sastoji od sljedećih: mezoteliom, hepatobilijarni rak, primarni tumor centralnog nervnog sustava (CNS), sekundarni tumor CNS sustava, primarni tumor mozga, sekundarni tumor mozga, rak pluća, rak kostiju, rak gušterače, rak kože, rak glave, rak vrata, kutani melanom, intraokularni melanom, rak jajnika, rak debelog crijeva, rak rektuma, rak analnog područja, rak želuca, gastrointestinalni rak, rak dojke, rak maternice, karcinom falopijeve tube, karcinom endometrija, karcinom cerviksa, karcinom vagine, karcinom vulve, Hodgkinova bolest, rak jednjaka, rak malog crijeva, rak endokrinog sustava, rak tiroidne žlijezde, rak paratiroidne žlijezde, rak adrenalne žlijezde, sarkom mekog tkiva, rak mokraćne cijevi, rak penisa, rak prostate, rak testisa, kronična leukemija, akutna leukemija, kronična mijeloidna leukemija, limfocitni limfomi, rak mjehura, rak bubrega, rak mokraćovoda, rak renalne stanice, karcinom renalne karlice, neoplazme CNS sustava, primarni limfom CNS sustava, ne-Hodgkinov limfom, tumori kralježnice, gliom moždanog debla, adenom hipofize, adrenokortikalni rak, rak žučnog mjehura, višestruki mijelom, kolangiokarcinom, fibrosarkom, neuroblastom i retinoblastom.
15. Uporaba prema patentnom zahtjevu 13, naznačena time, da je stanje bolesti odabrano iz skupine koja se sastoji od sljedećih: dijabetička retinopatija, neovaskularni glaukom, reumatoidni artritis, psorijaza i makularna degeneracija vezana uz dob.
16. Uporaba prema bilo kojem od patentnih zahtjeva 13 do 15, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je sol kristal i ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 12,2 ± 0,2, 14,8 ± 0,2 i 22,4 ± 0,2, gdje se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
17. Uporaba prema bilo kojem od patentnih zahtjeva 13 do 16, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je navedeni kamsilat S-kamsilat ili R-kamsilat.
18. Uporaba prema bilo kojem od patentnih zahtjeva 13 do 15, naznačena time, da sol je kamsilatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je kamsilatna sol S-kamsilat polimorfnog Oblika A, gdje polimorf ima uzorak difrakcije praha X-zraka koji sadrži jednu ili više ili dvije ili više ili tri vršne vrijednosti s difrakcijskim kutevima (2θ) od 12,2 ± 0,2, 14,8 ± 0,2 i 22,4 ± 0,2, pri čemu se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
19. Uporaba prema bilo kojem od patentnih zahtjeva 13 do 15, naznačena time, da navedena sol je maleatna sol od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona, pri čemu je maleatna sol odabrana iz skupine koja se sastoji od maleata polimorfnog Oblika A, gdje polimorf ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 6,0 ± 0,2, 20,3 ± 0,2 i 21,7 ± 0,2, pri čemu se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma, i maleata polimorfnog Oblika B, gdje polimorf ima uzorak difrakcije praha X-zraka koji sadrži vršne vrijednosti s difrakcijskim kutevima (2θ) od 7,5 ± 0,2, 11,3 ± 0,2 i 24,3 ± 0,2, pri čemu se navedeni uzorak rendgenske difrakcije praha dobiva uporabom bakar-K-α1-X-zraka uz valnu duljinu od 1,5406 Angstroma.
HRP20191944TT 2010-02-12 2019-10-25 Soli i polimorfi od 8-fluoro-2-{4-[(metilamino)metil]fenil}-1,3,4,5-tetrahidro-6h-azepino[5,4,3-cd]indol-6-ona HRP20191944T1 (hr)

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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2534153T3 (pl) * 2010-02-12 2017-08-31 Pfizer Inc. Sole i polimorfy 8-fluoro-2-{4-[(metyloamino}metylo]fenylo}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-onu
TW201516636A (zh) * 2013-10-22 2015-05-01 Hon Hai Prec Ind Co Ltd 電子裝置及其供電方法
EP3182975A4 (en) * 2014-08-22 2018-04-18 Clovis Oncology, Inc. High dosage strength tablets of rucaparib
KR20190018643A (ko) * 2016-05-16 2019-02-25 풀마젠 테라퓨틱스 (애즈마) 리미티드 퀴놀린 유도체의 결정
DE102016218772A1 (de) * 2016-09-28 2018-03-29 Bruker Biospin Gmbh Verbesserte Temperierung eines NMR-MAS-Rotors
US10875870B2 (en) 2017-01-24 2020-12-29 Assia Chemical Industries Ltd. Solid state forms of rucaparib and of rucaparib salts
CN109651377B (zh) * 2017-10-12 2020-10-20 成都海创药业有限公司 一种治疗癌症的化合物及其用途
JP2021501771A (ja) * 2017-11-03 2021-01-21 サンド・アクチエンゲゼルシヤフト 三環系ポリ（ａｄｐ−リボース）ポリメラーゼ阻害剤の結晶性塩
WO2019115000A1 (en) * 2017-12-15 2019-06-20 Advitech Advisory And Technologies Sa Process for the preparation of rucaparib and novel synthesis intermediates
WO2019130229A1 (en) 2017-12-28 2019-07-04 Mylan Laboratories Ltd Methods and intermediates for preparing rucaparib
BR112020013672A2 (pt) 2018-01-05 2020-12-01 Cybrexa 1, Inc. compostos, composições, e métodos para tratamento de doenças que envolvem tecidos afetados por ácidos ou hipoxia
US10442813B2 (en) 2018-01-30 2019-10-15 RK Pharma Solutions LLC Polymorphs of rucaparib camsylate and methods of making same
WO2019207498A1 (en) * 2018-04-25 2019-10-31 Biophore India Pharmaceuticals Pvt. Ltd Solid forms of 8-fluoro-2-{4-[(methylamino)methyl] phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd] indol-6-one ((1s,4r)-7,7dimethyl-2-oxobicyclo [2.2.1] hept-1-yl) methanesulfonic acid salt (rucaparib camsylate) and the prerparation thereof
WO2019207596A1 (en) 2018-04-25 2019-10-31 Mylan Laboratories Limited Novel crystalline forms of rucaparib (s)-camsylate salt and rucaparib free base
CN108743557A (zh) * 2018-06-27 2018-11-06 李莉 一种磷酸瑞卡帕布软胶囊及其制备方法
CN109111454A (zh) * 2018-08-01 2019-01-01 宁波金未生物科技有限公司 一种瑞卡帕布s-樟脑磺酸盐
CN111217818A (zh) * 2018-11-27 2020-06-02 台耀化学股份有限公司 芦卡帕尼樟脑磺酸盐的结晶、及制备三环化合物、芦卡帕尼及其樟脑磺酸盐结晶的方法
WO2020113500A1 (zh) * 2018-12-06 2020-06-11 上海诚妙医药科技有限公司 芦卡帕利樟脑磺酸盐的新晶型和制备方法及其用途
WO2021007435A1 (en) 2019-07-10 2021-01-14 Cybrexa 2, Inc. Peptide conjugates of cytotoxins as therapeutics
AU2020311925A1 (en) 2019-07-10 2022-02-03 Cybrexa 3, Inc. Peptide conjugates of microtubule-targeting agents as therapeutics
CN111004244A (zh) * 2019-12-27 2020-04-14 重庆市碚圣医药科技股份有限公司 一种瑞卡帕布樟脑磺酸盐的合成方法
EP4100125A1 (en) 2020-02-03 2022-12-14 Sandoz AG Polymorph of rucaparib mesylate
CA3179912A1 (en) * 2020-04-24 2021-10-28 Astrazeneca Ab Pharmaceutical formulations
CN115485271A (zh) 2020-04-28 2022-12-16 理森制药股份公司 用作聚(adp-核糖)聚合酶（parp）抑制剂的新型化合物
WO2022010537A1 (en) 2020-07-10 2022-01-13 The Regents Of The University Of Michigan Gas41 inhibitors and methods of use thereof
EP4182318A1 (en) 2020-07-14 2023-05-24 Assia Chemical Industries Ltd Solid state forms of rucaparib salts
WO2022090938A1 (en) 2020-10-31 2022-05-05 Rhizen Pharmaceuticals Ag Phthalazinone derivatives useful as parp inhibitors
IL307339A (en) 2021-04-08 2023-11-01 Rhizen Pharmaceuticals Ag Poly(ADP-ribose) polymerase inhibitors
WO2023137060A1 (en) 2022-01-11 2023-07-20 Assia Chemical Industries Ltd. Solid state forms of rucaparib tosylate
WO2023152754A1 (en) * 2022-02-08 2023-08-17 Sawant, Mohit Manikrao Crystalline form of rosuvastatin allyl ester

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4489011A (en) 1983-05-16 1984-12-18 Merrell Dow Pharmaceuticals Inc. Hypoglycemic N-(2-substituted-3-dialkylamino-2-propenylidene)-N-alkylalkanaminium camsylate salts
GB8607683D0 (en) 1986-03-27 1986-04-30 Ici Plc Anti-tumor agents
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
DE4125292A1 (de) * 1991-07-31 1993-02-04 Kali Chemie Pharma Gmbh 6-oxo-azepinoindol-verbindungen sowie verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
US5587458A (en) 1991-10-07 1996-12-24 Aronex Pharmaceuticals, Inc. Anti-erbB-2 antibodies, combinations thereof, and therapeutic and diagnostic uses thereof
EP0625200B1 (en) 1992-02-06 2005-05-11 Chiron Corporation Biosynthetic binding protein for cancer marker
US6177401B1 (en) 1992-11-13 2001-01-23 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften Use of organic compounds for the inhibition of Flk-1 mediated vasculogenesis and angiogenesis
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DE69519751T2 (de) 1995-04-20 2001-04-19 Pfizer Arylsulfonamido-substituierte hydroxamsäure derivate als inhibitoren von mmp und tnf
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
GB9520822D0 (en) 1995-10-11 1995-12-13 Wellcome Found Therapeutically active compounds
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
KR100489174B1 (ko) 1996-03-05 2005-09-30 제네카-파마 소시에떼아노님 4-아닐리노퀴나졸린유도체
JP3195756B2 (ja) 1996-07-04 2001-08-06 公子 吉水 潤滑補助体
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
BR9710362A (pt) 1996-07-13 1999-08-17 Glaxo Group Ltd Composto formula-ao farmaceutica utiliza-ao de um composto processos de tratamento de um ser humano ou animal sofrendo de uma mediada por atividade anormal de cinase de proteina tirosina e para a prepara-ao de um composto
AU3766897A (en) 1996-07-13 1998-02-09 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
WO1998003516A1 (en) 1996-07-18 1998-01-29 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
SK21499A3 (en) 1996-08-23 2000-05-16 Pfizer Arylsulfonylamino hydroxamic acid derivatives
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
EP0977733B1 (en) 1997-02-03 2003-09-03 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
CN1247531A (zh) 1997-02-11 2000-03-15 辉瑞大药厂 芳基磺酰基异羟肟酸衍生物
ATE292623T1 (de) 1997-05-07 2005-04-15 Sugen Inc 2-indolinonderivate als modulatoren der proteinkinase-ativität
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
US5835420A (en) 1997-06-27 1998-11-10 Aplus Flash Technology, Inc. Node-precise voltage regulation for a MOS memory system
ID23668A (id) 1997-08-08 2000-05-11 Pfizer Prod Inc Turunan asam ariloksiarilsulfonilamino hidroksamat
DE69838172T2 (de) 1997-08-22 2008-04-10 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
EP1017682A4 (en) 1997-09-26 2000-11-08 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
KR100446363B1 (ko) 1997-11-11 2004-09-01 화이자 프로덕츠 인코포레이티드 항암제로 유용한 티에노피리미딘 및 티에노피리딘 유도체
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
JP4462654B2 (ja) 1998-03-26 2010-05-12 ソニー株式会社 映像素材選択装置及び映像素材選択方法
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
EP1082305A4 (en) 1998-05-29 2001-09-26 Sugen Inc PYRROL SUBSTITUTED 2-INDOLINONE EFFECTIVE AS A PROTEIN KINASE INHIBITOR
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
US6114361A (en) 1998-11-05 2000-09-05 Pfizer Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
US6649645B1 (en) 1998-12-23 2003-11-18 Pharmacia Corporation Combination therapy of radiation and a COX-2 inhibitor for treatment of neoplasia
JP2002533416A (ja) 1998-12-23 2002-10-08 ジー．ディー．サール ＆ カンパニー 新形成の治療における組み合わせ治療としてのシクロオキシゲナーゼ−２インヒビターおよび一つまたはそれ以上の抗腫瘍薬の使用方法
HU229875B1 (en) * 1999-01-11 2014-11-28 Agouron Pharmaceuticals Inc La Jolla Tricyclic inhibitors of poly(adp-ribose) polymerases
KR100452491B1 (ko) 2001-03-29 2004-10-12 한미약품 주식회사 신규한 결정형 암로디핀 캠실레이트 염 및 그의 제조방법
KR20040011751A (ko) 2002-07-30 2004-02-11 씨제이 주식회사 암로디핀의 유기산염
RU2005122659A (ru) † 2002-12-19 2006-01-20 Пфайзер Продактс Инк. (Us) Комплексы е-2-метокси-n-(3-{4-[3-метил-4-(6-метилпиридин-3-илокси) фениламино] хиназолин-6-ил} аллил) ацетамида, способ получения и применения указанных комплексов
JP2006522088A (ja) * 2003-03-31 2006-09-28 ファイザー・インク ポリ（ａｄｐ−リボース）ポリメラーゼの三環系阻害剤の塩
ES2339663T3 (es) 2003-07-25 2010-05-24 Cancer Research Technology Limited Inhibidores de parp triciclicos.
EP1799685B1 (en) * 2004-09-22 2012-03-28 Pfizer Inc. Polymorphic forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
CN101384264B (zh) * 2004-09-22 2012-03-14 辉瑞大药厂 含有聚（adp-核糖）聚合酶抑制剂的治疗组合物
PL1794163T3 (pl) 2004-09-22 2010-06-30 Pfizer Sposób wytwarzania inhibitorów poli(adp-rybozo)polimerazy
EP1793830A2 (en) 2004-09-22 2007-06-13 Pfizer, Inc. Therapeutic combinations comprising poly(adp-ribose) polymerases inhibitor
GB0502509D0 (en) 2005-02-07 2005-03-16 Pfizer Ltd Novel salt form of a dopamine agonist
CA2600011C (en) * 2005-02-23 2015-11-10 Teva Pharmaceutical Industries Ltd. Rasagiline formulations of improved content uniformity
EP1886670A1 (en) * 2006-07-05 2008-02-13 Teva Pharmaceutical Industries Ltd Pharmaceutical compositions of memantine
KR100843401B1 (ko) 2006-12-04 2008-07-04 씨제이제일제당 (주) 결정성 ｓ-(-)-암로디핀 캠실레이트 무수물 및 이의제조방법
ES2524021T3 (es) * 2006-12-06 2014-12-03 Conatus Pharmaceuticals, Inc. Formas cristalinas del ácido (3S)-3-[N-(N'-(2-terc-butilfenil)oxamil)alaninil]amino-5-(2',3',5',6'-tetrafluorofenoxi)-4-oxopentanoico
WO2008114114A2 (en) 2007-03-16 2008-09-25 Pfizer Products Inc. Poly(adp-ribose) polymerases inhibitor for treating ophthalmic condition
EP2065385A1 (en) † 2007-11-28 2009-06-03 Laboratorios SALVAT, S.A. Stable crystalline salt of (R)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabiciyclo [2.2.2]oct-3-yl ester
JP2011506315A (ja) * 2007-12-05 2011-03-03 バイアル−ポルテラ アンド シーエー，エス．エー． 新たな塩、及び結晶形
KR20090060674A (ko) 2007-12-10 2009-06-15 씨제이제일제당 (주) 결정형의 지프라시돈 술폰산염, 그 제조방법, 및 그것를포함하는 약제학적 조성물
RU2495035C2 (ru) 2008-01-08 2013-10-10 Мерк Шарп Энд Домэ Лтд Фармацевтически приемлемые соли 2-{4-[(3s)-пиперидин-3-ил]фенил}-2н-индазол-7-карбоксамида
EP2387539B1 (en) 2009-01-17 2019-12-11 Boomerang Systems. Inc. Automated storage system with transport vehicle
PL2534153T3 (pl) * 2010-02-12 2017-08-31 Pfizer Inc. Sole i polimorfy 8-fluoro-2-{4-[(metyloamino}metylo]fenylo}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-onu
US9539930B2 (en) 2011-09-23 2017-01-10 Gentex Corporation Systems and methods for rear view mirror displays
US9221946B2 (en) 2011-12-26 2015-12-29 Wintech Polymer Ltd. Polybutylene terephthalate resin pellets, and production method for said polybutylene terephthalate resin pellets
US9384339B2 (en) 2012-01-13 2016-07-05 Telecommunication Systems, Inc. Authenticating cloud computing enabling secure services
US10181126B2 (en) 2012-03-13 2019-01-15 American Express Travel Related Services Company, Inc. Systems and methods for tailoring marketing
KR101984831B1 (ko) 2013-01-31 2019-05-31 삼성전자 주식회사 반도체 패키지 및 그 제조 방법
CN103309115B (zh) 2013-05-30 2016-03-23 京东方科技集团股份有限公司 彩色电泳显示面板及其制造方法、显示装置
US9501163B2 (en) 2014-05-06 2016-11-22 Symbol Technologies, Llc Apparatus and method for activating a trigger mechanism
US10884952B2 (en) 2016-09-30 2021-01-05 Intel Corporation Enforcing memory operand types using protection keys
JP6943759B2 (ja) 2017-12-28 2021-10-06 株式会社東海理化電機製作所 シフト装置

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