HRP20120993T1 - Anacetrapib i drugi inhibitori cetp - Google Patents

Anacetrapib i drugi inhibitori cetp Download PDF

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Publication number
HRP20120993T1
HRP20120993T1 HRP20120993TT HRP20120993T HRP20120993T1 HR P20120993 T1 HRP20120993 T1 HR P20120993T1 HR P20120993T T HRP20120993T T HR P20120993TT HR P20120993 T HRP20120993 T HR P20120993T HR P20120993 T1 HRP20120993 T1 HR P20120993T1
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Croatia
Prior art keywords
image
group
alkyl
pharmaceutically acceptable
acceptable salt
Prior art date
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HRP20120993TT
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English (en)
Inventor
Amjad Ali
Joann M. Napolitano
Qiaolin Deng
Zhijian Lu
Peter J. Sinclair
Gayle E. Taylor
Christopher F. Thompson
Nazia Quraishi
Cameron J. Smith
Julianne A. Hunt
Adrian A. Dowst
Yi-Heng Chen
Hong Li
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Merck Sharp & Dohme Corp.
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Application filed by Merck Sharp & Dohme Corp. filed Critical Merck Sharp & Dohme Corp.
Publication of HRP20120993T1 publication Critical patent/HRP20120993T1/hr

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Claims (17)

1. Spoj koje ima formulu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što: [image] Y je -(CRR1)-; X je izabran iz grupe koju čine -O-, -NH- i -N(C1-C3alkil); Z je -C(=O)-; svako R je nezavisno izabrano iz grupe koju čine H i C1-C2 alkil; B je izabran iz grupe koju čine A1 i A2, pri čemu A1 ima strukturu: [image] R1 je izabran iz grupe koju čine H, -C1-C3 alkil i -(C(R)2)nA2, pri čemu je -C1-C3 alkil izborno supstituiran sa 1-5 halogena; R2 je izabran iz grupe koju čine H, -C1-C3 alkil, A1, i -(C(R)2)nA2, pri čemu je -C1-C3 alkil izborno supstituiran sa 1-5 halogena; gdje je jedan od B i R2 jednak A1; i jedan od B, R1 i R2 je A2 ili -(C(R)2)nA2; tako da spoj formule I sadrži jednu grupu A1 i jednu grupu A2; A3 je izabran iz grupe koju čine: (a) fenil; (b) 5-6-člani aromatični heterociklični prsten koji ima 1-2 heteroatoma nezavisno izabrana od N, S, O i -N(O)-, gdje je točka vezivanja A3 za fenil prsten za koji je vezan A3 – atom ugljika; i (c) benzoheterocikličan prsten koji sadrži fenil prsten fuzioniran sa 5-članim aromatičnim heterocikličnim prstenom koji ima 1-2 heteroatoma nezavisno izabrana od O, N i -S(O)x, gdje je točka vezivanja A3 za fenil prsten za koji je vezan A3 – atom ugljika; A2 je izabran iz grupe koju čine: (a) fenil; (b) 5-6-člani heterociklični prsten koji ima 1-4 heteroatoma nezavisno izabrana od N, S, O i -N(O)-, i izborno također sadrži 1-3 dvogube veze; (c) benzoheterocikličan prsten koji sadrži fenil prsten fuzioniran sa 5-članim heterocikličnim prstenom koji ima 1-2 heteroatoma nezavisno izabrana od O, N i S; i (d) -C5-C6 cikloalkil prsten; gdje su svako A3 i A2 izborno supstituirani sa 1-4 supstituirajuće grupe nezavisno izabrane od Ra; svako Ra je nezavisno izabrano iz grupe koju čine -C1-C4 alkil, -C2-C4 alkenil, ciklopropil, -OC1-C2alkil, -C(=O)C1-C2alkil, -C(=O)H, -CO2C1-C4alkil, -OH, -NR3R4, - NR3C(=O)OC1-C4 alkil, -S(O)xC1-C2 alkil, halogen, -CN, -NO2 i 5-6-člani heterociklični prsten koji ima 1-2 heteroatoma nezavisno izabrana od N, S i O, gdje je točka vezivanja navedenog heterocikličnog prstena za prsten za koji je Ra veezan – atom ugljika, pri čemu je navedeni heterociklični prsten izborno supstituiran sa 1-5 supstituišuće grupe nezavisno izabrane od halogena; gdje je za spojeve u kojima je Ra izabran iz grupe koju čine -C1-C4 alkil, -C2-C4 alkenil, -OC1-C2alkil, -C(=O)C1-C2alkil, -CO2C1-C4alkil, -NR3C(=O)OC1-C4alkil i - S(O)xC1-C2 alkil, alkil grupa iz Ra - izborno supstituirana sa 1-5 halogena i izborno je također supstituirana sa jednom supstituirajućom grupom koja je izabrana od (a) -OH, (b) -NR3R4, (c) -OCH3 izborno supstituiranom sa 1-3 atoma fluora i izborno također supstituirana sa jednom fenil grupom, i (d) fenila koji je izborno supstituiran sa 1-3 grupe nezavisno izabrane od halogena, -CH3, -CF3, -OCH3 i -OCF3; n je 0 ili 1; p je cijeli broj od 0-2; x je 0, 1 ili 2; i svako R3, R4 i R5 nezavisno su izabrani od H i -C1-C3 alkil.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine spojevi koji imaju formulu Ia, Ib i Id, ili njegova farmaceutski prihvatljiva sol: [image] [image] i [image]
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što A3 je izabran iz grupe koju čine fenil, tienil, imidazolil, pirolil, pirazolil, piridil, N-oksido-piridil, tiazolil, piridazinil, pirimidinil, pirazinil, benzotienil, benzotienil-S-oksid i benzotienil-S-dioksid; i A2 je izabran iz grupe koju čine fenil, tienil, imidazolil, tiazolil, pirolil, pirazolil, 1,2,4-triazolil, tetrazolil, benzodioksolil, piridil, N-oksido-piridil, piridazinil, pirimidinil, pirazinil, ciklopentil, cikloheksil i tetrahidropiranil.
4. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što su i A2 i A3 - fenil; i Ra je izabran iz grupe koju čine -C1-C4 alkil koji je izborno susptituiran sa 1-5 atoma fluora i izborno je takođe supstituiran sa jednom grupom koja je izabrana od -OH i -OCH3; -OC1-C2alkil, koji je izborno supstituiran sa 1-3 atoma fluora; -C2-C4 alkenil; -C1-C2 alkil koji je supstituiran sa jednom grupom -NR3R4; ciklopropil; -C(=O)H; -OH; -NR3R4; -S(O)xC1-C2 alkil; halogen; -CN; i -NO2.
5. Spoj prema patentnom zahtjevu 4 koje formulu Ii, ili njegova farmaceutski prihvatljiva sol, naznačen time što: [image] R7 je izabran iz grupe koju čine Cl i -CF3; svako Rb je nezavisno izabrano iz grupe koju čine -C1-C3 alkil, -OCH3 i F; R1 je izabran iz grupe koju čine H i -C1-C2 alkil; Rc je izabran iz grupe koju čine halogen, -CH3, -CF3 i -CN; q je 2 ili 3; i t je cijeli broj od 0-2.
6. Spoj prema patentnom zahtjevu 4 koje ima formulu Ij, ili njegova farmaceutski prihvatljiva sol, naznačen time što: [image] R7 je izabran iz grupe koju čine Cl i -CF3; svako Rb je nezavisno izabrano iz grupe koju čine -C1-C3 alkil, -OCH3 i F; R1 je izabran iz grupe koju čine H i -C1-C2 alkil; Rc je izabran iz grupe koju čine halogen, -CH3 -CF3 i -CN; q je 2 ili 3; i t je cijeli broj od 0-2.
7. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine slijedeći spojevi, ili njegova farmaceutski prihvatljiva sol: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
8. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine spojevi sa formulom (a) do (c), ili njegova farmaceutski prihvatljiva sol: (a) [image] gdje je R izabran iz grupe koju čine [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image] (b) [image] gdje je R izabran iz grupe koju čine [image] [image] [image] [image] i [image] i (c) [image] gdje je R izabran iz grupe koju čine [image] [image] [image] [image] [image] [image] i [image]
9. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine slijedeći spojevi, ili njegova farmaceutski prihvatljiva sol: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image]
10. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine spojevi koji imaju formulu (a) do (k), ili njegova farmaceutski prihvatljiva sol: (a) [image] gdje su A3, A2 i Z za spojeve (1) do (5) izabrana iz grupe koju čine: [image] (b) [image] gdje je A3 izabrano iz grupe koju čine: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image] (c) [image] gdje su A3 i A2 za jedinjenja (1) do (6) izabrani iz grupe koju čine: [image] (d) [image] gdje je R izabran iz grupe koju čine [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image] (e) [image] gdje je R jednako Et ili n-Pr; (f) [image] gdje su R i A3 za spojeve (1) do (4) izabrani iz grupe koju čine [image] (g) [image] gdje je R izabran iz grupe koju čine: [image] [image] [image] [image] (h) [image] gdje je A2 izabran iz grupe koju čine [image] [image] [image] [image] [image] i [image] (i) [image] gdje je R izabran iz grupe koju čine [image] [image] [image] [image] [image] [image] (j) [image] gdje je A3 izabran iz grupe koju čine: [image] [image] [image] [image] i (k) [image] gdje su A3, R2 i R3 za spojeve (1) do (3) izabrani iz grupe koju čine: [image]
11. Spoj prema patentnom zahtjevu 1, naznačen time što ima formulu: [image] ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema patentnom zahtjevu 1, naznačen time što ima formulu: [image]
13. Farmaceutska kompozicija naznačena time što sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem prethodnom patentnom zahtjevu, i farmaceutski prihvatljiv nosač.
14. Spoj ili farmaceutski prihvatljiva so prema bilo kojem od patentnih zahtjeva 1 do 12, za uporabu u terapiji.
15. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 12, za uporabu u povećanju HDL-C ili liječenju ateroskleroze, periferne vaskularne bolesti, dislipidemije, hiperbetalipoproteinemije, hipoalfalipoproteinemije, hiperholesterolemije, hipertrigliceridemije, porodične-hiperholesterolemije, kardiovaskularnih poremećaja, angine, ishemije, srčane ishemije, moždanog udara, infarkta miokarda, reperfuzione povrede, angioplastične restenoze, hipertenzije, vaksularnih komplikacija dijabetesa, debljine, endotoksemije ili metaboličkog sindroma.
16. Spoj ili farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 12, za upotrebu u povećanju HDL-C ili liječenju ateroskleroze.
17. Upotreba spoja ili farmaceutski prihvatljive soli prema bilo kojem od patentnih zahtjeva 1 do 12, za proizvodnju lijeka za liječenje ateroskleroze ili za povećanje HDL-C.
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Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7270971B2 (en) * 2003-10-16 2007-09-18 Merck & Co., Inc. Fluorescence assay for measuring the rate of cholesterol ester transfer
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
WO2007005572A1 (en) * 2005-07-01 2007-01-11 Merck & Co., Inc. Process for synthesizing a cetp inhibitor
ATE516016T1 (de) * 2005-12-05 2011-07-15 Merck Sharp & Dohme Selbstemulgierende formulierungen von cetp- hemmern
AR057218A1 (es) * 2005-12-15 2007-11-21 Astra Ab Compuestos de oxazolidinona y su uso como pontenciadores del receptor metabotropico de glutamato
CA2635010A1 (en) * 2005-12-30 2007-07-19 Amjad Ali Oxazolidinone derivatives as cetp inhibitors
US7910592B2 (en) * 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
KR20140107671A (ko) 2005-12-30 2014-09-04 머크 샤프 앤드 돔 코포레이션 Ｃｅｔｐ 억제제로서 유용한 1,3-옥사졸리딘-2-온 유도체
CA2635087A1 (en) * 2005-12-30 2007-07-19 Merck & Co., Inc. Cholesteryl ester transfer protein inhibitors
CN101378731B (zh) * 2006-02-09 2014-03-05 默沙东公司 Cetp抑制剂的聚合物制剂
US8383660B2 (en) * 2006-03-10 2013-02-26 Pfizer Inc. Dibenzyl amine compounds and derivatives
US7919506B2 (en) * 2006-03-10 2011-04-05 Pfizer Inc. Dibenzyl amine compounds and derivatives
WO2007136672A2 (en) * 2006-05-19 2007-11-29 Merck & Co., Inc. Synthesis of a biaryl synthetic intermediate
WO2008082567A1 (en) * 2006-12-29 2008-07-10 Merck & Co., Inc. Process for synthesizing a cetp inhibitor
ES2547386T3 (es) 2007-01-26 2015-10-05 Kaneq Pharma Inc. Inhibidores de la PTP-1B aromáticos condensados
EP2125750B1 (en) 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2136637B1 (en) * 2007-03-16 2015-11-11 Concert Pharmaceuticals, Inc. Inhibitors of cholesterol ester transfer protein
US8338458B2 (en) 2007-05-07 2012-12-25 Merck Sharp & Dohme Corp. Method of treatment using fused aromatic compounds having anti-diabetic activity
CN103450077B (zh) 2007-06-08 2016-07-06 满康德股份有限公司 IRE-1α抑制剂
EP2166847B1 (en) * 2007-06-20 2014-11-19 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
CA2689523A1 (en) * 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
EP2170058B1 (en) * 2007-06-20 2013-07-03 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
WO2009003861A1 (en) 2007-07-02 2009-01-08 F. Hoffmann-La Roche Ag Imidazole derivatives as ccr2 receptor antagonists
ES2395081T3 (es) * 2007-07-26 2013-02-08 Vitae Pharmaceuticals, Inc. Síntesis de inhibidores de la 11beta-hidroxiesteroide deshidrogenasa de tipo 1
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
US8440658B2 (en) 2007-12-11 2013-05-14 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
EP2252601B1 (en) * 2008-01-24 2012-12-19 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009099901A1 (en) * 2008-02-01 2009-08-13 Amira Pharmaceuticals, Inc. N,n-disubstituted aminoalkylbiphenyl antagonists of prostaglandin d2 receptors
BRPI0907364A2 (pt) * 2008-02-01 2015-07-14 Amira Pharmaceuticals Inc Antagonistas aminoalquilbifenil n,n-disubstituídos de receptores d2 de prostaglandina
CA2714532A1 (en) * 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2009102893A2 (en) 2008-02-14 2009-08-20 Amira Pharmaceuticals, Inc. CYCLIC DIARYL ETHER COMPOUNDS AS ANTAGONISTS OF PROSTAGLANDIN D2 receptors
WO2009102460A2 (en) * 2008-02-15 2009-08-20 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP2011513242A (ja) 2008-02-25 2011-04-28 アミラ ファーマシューティカルズ，インク． プロスタグランジンｄ２受容体アンタゴニスト
CA2718264A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
US8426449B2 (en) 2008-04-02 2013-04-23 Panmira Pharmaceuticals, Llc Aminoalkylphenyl antagonists of prostaglandin D2 receptors
ES2421537T3 (es) 2008-05-01 2013-09-03 Vitae Pharmaceuticals Inc Inhibidores cíclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
US8569292B2 (en) 2008-05-01 2013-10-29 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
US8063088B2 (en) * 2008-06-11 2011-11-22 Hoffmann-La Roche Inc. Imidazolidine derivatives
PL2324018T3 (pl) 2008-07-25 2014-02-28 Boehringer Ingelheim Int Cykliczne inhibitory dehydrogenazy 11 beta-hydroksysteroidowej typu 1
EP2323994A1 (en) 2008-07-25 2011-05-25 Boehringer Ingelheim International GmbH Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の阻害剤
GB2463788B (en) 2008-09-29 2010-12-15 Amira Pharmaceuticals Inc Heteroaryl antagonists of prostaglandin D2 receptors
DE102008049675A1 (de) 2008-09-30 2010-04-01 Markus Dr. Heinrich Verfahren zur Herstellung von 3-Aminobiphenylen
US8378107B2 (en) 2008-10-01 2013-02-19 Panmira Pharmaceuticals, Llc Heteroaryl antagonists of prostaglandin D2 receptors
EP2348859B1 (en) * 2008-10-01 2013-12-04 Merck Sharp & Dohme Corp. Prodrugs of oxazolidinone cetp inhibitors
US8524748B2 (en) 2008-10-08 2013-09-03 Panmira Pharmaceuticals, Llc Heteroalkyl biphenyl antagonists of prostaglandin D2 receptors
CN102264228A (zh) 2008-10-22 2011-11-30 默沙东公司 用于抗糖尿病药的新的环状苯并咪唑衍生物
AU2009309037A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010057118A2 (en) 2008-11-17 2010-05-20 Amira Pharmaceuticals, Inc. Heterocyclic antagonists of prostaglandin d2 receptors
TW201028414A (en) 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
EP2389226B1 (en) 2009-01-23 2013-11-20 Merck Sharp & Dohme Corp. Bridged and fused heterocyclic antidiabetic compounds
CA2749891A1 (en) 2009-01-23 2010-07-29 Hubert B. Josien Bridged and fused antidiabetic compounds
EP2393807B1 (en) 2009-02-04 2013-08-14 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1
WO2010091176A1 (en) 2009-02-05 2010-08-12 Schering Corporation Phthalazine-containing antidiabetic compounds
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
JP5656986B2 (ja) 2009-06-11 2015-01-21 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １，３−オキサジナン−２−オン構造に基づく１１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
EP2448928B1 (en) 2009-07-01 2014-08-13 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN102596902A (zh) * 2009-08-05 2012-07-18 潘米拉制药公司 Dp2拮抗剂及其用途
JP2011057661A (ja) 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
US8552212B2 (en) 2009-11-05 2013-10-08 Boehringer Ingelheim International Gmbh Chiral phosphorus ligands
US8754099B2 (en) 2010-01-15 2014-06-17 Merck Sharp & Dohme Corp Oxadiazole beta carboline derivatives as antidiabetic compounds
AU2011218830B2 (en) 2010-02-25 2014-07-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP2013531636A (ja) 2010-05-26 2013-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ２−オキソ−１，２−ジヒドロピリジン−４−イルボロン酸誘導体
EP2397473A1 (en) 2010-06-14 2011-12-21 LEK Pharmaceuticals d.d. A stable highly crystalline anacetrapib
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
EP2626351A4 (en) 2010-10-04 2014-03-12 Kowa Co AGENT CAPABLE OF INHIBITING THE EXPRESSION OF LIPID METABOLISM-RELATED MRNA
AU2011320665B2 (en) 2010-10-29 2015-09-03 Merck Sharp & Dohme Corp. Cyclic amine substituted oxazolidinone CETP inhibitor
CA2813671A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
EP2468735A1 (en) * 2010-12-23 2012-06-27 LEK Pharmaceuticals d.d. Synthesis of intermediates for preparing anacetrapib and derivates thereof
EP2468736A1 (en) * 2010-12-23 2012-06-27 LEK Pharmaceuticals d.d. Synthesis of intermediates for preparing anacetrapib and derivates thereof
ES2648788T3 (es) 2011-01-26 2018-01-08 Inserm - Institut National De La Santé Et De La Recherche Médicale Método para evaluar el riesgo de un sujeto de tener una enfermedad cardiovascular
PE20140859A1 (es) 2011-02-25 2014-07-25 Merck Sharp & Dohme Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos
DK2697207T3 (en) 2011-04-12 2017-03-27 Chong Kun Dang Pharmaceutical Corp 3- (2-ARYL-CYCLOALKENYLMETHYL) -OXAZOLIDIN-2-ON DERIVATIVES AS CHOLESTEROL ESTER-TRANSFER PROTEIN (CETP) INHIBITORS
WO2013005834A1 (ja) * 2011-07-07 2013-01-10 持田製薬株式会社 高純度ｅｐａを含有する抗肥満剤
TWI627167B (zh) 2011-07-08 2018-06-21 諾華公司 用於高三酸甘油酯個體治療動脈粥狀硬化之方法
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
US9145348B2 (en) 2011-10-31 2015-09-29 Merck Sharpe & Dohme Corp. Process for synthesizing a CETP inhibitor
WO2013064188A1 (en) 2011-11-03 2013-05-10 Lek Pharmaceuticals D.D. A stable highly crystalline anacetrapib
EP2789347A4 (en) 2011-11-29 2015-12-16 Kowa Co AGENT FOR INHIBITING THE EXPRESSION OF NPC1L1 AND / OR LIPG MRA AND AGENT FOR PREVENTING AND / OR TREATING OBESITY
AU2012346754B2 (en) * 2011-11-30 2016-09-22 Daewoong Pharmaceutical Co., Ltd. Pharmaceutical composition for preventing or treating hyperlipidemia
WO2013091696A1 (en) * 2011-12-21 2013-06-27 Lek Pharmaceuticals D.D. Synthesis of intermediates for preparing anacetrapib and derivatives thereof
US9353101B2 (en) 2012-05-02 2016-05-31 Merck Sharp & Dohme Corp. Cyclic amine substituted heterocyclic CETP inhibitors
MX347400B (es) 2012-06-29 2017-04-18 Univ Nac Autónoma De México Vacuna de aplicacion nasal contra el desarrollo de la enfermedad aterosclerotica y el higado graso.
WO2014012428A1 (zh) * 2012-07-19 2014-01-23 上海恒瑞医药有限公司 噁唑烷酮类衍生物、其制备方法及其在医药上的应用
WO2014031465A1 (en) 2012-08-22 2014-02-27 Merck Sharp & Dohme Corp. Novel azabenzimidazole tetrahydropyran derivatives
US9717714B2 (en) 2012-12-19 2017-08-01 Merck Sharp & Dohme Corp. Spirocyclic CETP inhibitors
US9376408B2 (en) 2012-12-20 2016-06-28 Merck Sharp & Dohme Corp. Therapeutic thiazolidinone compounds
WO2014111953A1 (en) * 2013-01-17 2014-07-24 Glenmark Pharmaceuticals Limited; Glenmark Generics Limited Process for preparation of anacetrapib and intermediates thereof
NZ708079A (en) 2013-01-31 2016-07-29 Chong Kun Dang Pharm Corp Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as cetp inhibitors
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
EP3027619B1 (en) 2013-07-30 2019-01-02 Merck Sharp & Dohme Corp. Bicyclic ureas and thiadiazolidine-1,1-dioxides as cetp inhibitors
US9688630B2 (en) 2013-10-10 2017-06-27 Merck Sharp & Dohme Corp. 3,3′-disubstituted indolines as inhibitors of cholesterol ester transfer protein
WO2015094932A1 (en) 2013-12-17 2015-06-25 Merck Sharp & Dohme Corp. Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein
CN104955816B (zh) * 2014-01-14 2016-08-31 杭州普晒医药科技有限公司 一种安塞曲匹的晶型及其制备方法、其药物组合物和用途
CN103923030B (zh) * 2014-03-27 2015-07-22 汕头经济特区鮀滨制药厂 一种安塞曲匹的关键中间体的合成方法
CN103923031A (zh) * 2014-04-01 2014-07-16 汕头经济特区鮀滨制药厂 一种安塞曲匹的中间体的合成方法
WO2016018729A1 (en) * 2014-07-29 2016-02-04 Merck Sharp & Dohme Corp. Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
JP6854752B2 (ja) 2014-07-30 2021-04-07 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｈｄｌ上昇剤又はｈｄｌ模倣剤を用いた治療に対する応答性を予測するための遺伝マーカー
CN104230835B (zh) * 2014-09-01 2017-01-25 福建师范大学 一种合成n‑苯乙烯基恶唑烷‑2‑酮衍生物的方法
WO2016067194A1 (en) * 2014-10-27 2016-05-06 Sun Pharmaceutical Industries Limited Process for the preparation of anacetrapib and an intermediate thereof
CN106032362B (zh) * 2015-03-10 2018-06-19 湖南千金湘江药业股份有限公司 安塞曲匹的制备方法
MX2018015872A (es) 2016-06-29 2019-04-22 Orion Corp Derivados de benzodioxano y su uso farmaceutico.
KR101902002B1 (ko) * 2016-07-19 2018-09-27 재단법인 대구경북첨단의료산업진흥재단 Cetp 억제제로서의 옥사졸리딘온 유도체 화합물
JP6945619B2 (ja) * 2016-08-17 2021-10-06 ノバルティス アーゲー Ｎｅｐ阻害剤合成のための新規な方法および中間体
CN106496211A (zh) * 2016-10-18 2017-03-15 湖南德魅信息技术有限公司 二氟甲基取代的噁唑烷酮化合物及其用途
CN106496154A (zh) * 2016-10-18 2017-03-15 湖南德魅信息技术有限公司 安塞曲匹的制备方法
CN106749075A (zh) * 2016-11-24 2017-05-31 山东新华制药股份有限公司 阿那曲波的恶唑烷酮中间体的晶型及其制备方法
WO2019043018A1 (en) 2017-08-29 2019-03-07 Dalcor Pharma Uk Ltd., Stockport Zug Branch METHODS OF TREATING OR PREVENTING CARDIOVASCULAR DISORDERS AND REDUCING THE RISK OF CARDIOVASCULAR EVENTS
JOP20180092A1 (ar) 2017-10-13 2019-04-13 Gilead Sciences Inc مثبطات hiv بروتياز
CN112888432A (zh) 2018-08-09 2021-06-01 英国达科(莱得海德)制药有限公司-楚歌分公司 用于延迟新发作2型糖尿病的发生和用于减慢2型糖尿病的进展和治疗2型糖尿病的方法
SG11202107468YA (en) 2019-03-07 2021-08-30 Dalcor Pharma Uk Ltd Leatherhead Methods for treating or preventing heart failure and reducing risk of heart failure
TW202104210A (zh) 2019-04-17 2021-02-01 美商基利科學股份有限公司 Hiv蛋白酶抑制劑
CA3148300A1 (en) 2019-07-19 2021-01-28 Biosynth Ag Method of making nicotinamide ribofuranoside salts, nicotinamide ribofuranoside salts as such, and uses thereof
WO2022075645A1 (ko) * 2020-10-08 2022-04-14 재단법인 대구경북첨단의료산업진흥재단 Pcsk9 억제제로서 아미노알콜 유도체 및 이를 함유하는 고콜레스테롤 혈증의 예방 또는 치료용 약학적 조성물
WO2023278698A1 (en) * 2021-06-30 2023-01-05 Apellis Pharmaceuticals, Inc. Complement inhibition

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4179442A (en) * 1975-08-29 1979-12-18 York Hartleben 4-(Alpha-hydroxy-isopropyl)-5-phenyl-oxazolidin-2-one
DE2655369A1 (de) * 1976-12-03 1978-06-08 Schering Ag 5-(subst. phenyl)-oxazolidinone und deren schwefelanaloga sowie verfahren zu deren herstellung
US4851423A (en) 1986-12-10 1989-07-25 Schering Corporation Pharmaceutically active compounds
HU203330B (en) * 1987-06-10 1991-07-29 Pfizer Process for producing oxazolidin-2-one derivatives and hypoglychemic pharmaceutical compositions containing them
US5480899A (en) * 1992-04-30 1996-01-02 Taiho Pharmaceutical Co., Ltd. Oxazolidine derivatives and pharmaceutically acceptable salts thereof
US5482971A (en) * 1993-10-01 1996-01-09 American Cyanamid Company Beta3 -adrenergic agents and their use in pharmaceutical compositions
AU684316B2 (en) * 1993-10-15 1997-12-11 Shionogi & Co., Ltd. Oxazolinone derivative having intracellular phospholipase A2 inhibitor activity
PT758233E (pt) * 1994-04-21 2004-04-30 Schering Ag Inibidores pde iv para o tratamento da esclerose multipla
FR2729954B1 (fr) * 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
CN1173818A (zh) * 1995-02-10 1998-02-18 舍林股份公司 用于tnf抑制的药物制剂
JP2002515014A (ja) * 1995-05-17 2002-05-21 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺菌・殺カビ性の環式アミド類
US5612363A (en) 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
MX9710259A (es) 1995-06-20 1998-03-29 Du Pont Amidas ciclicas fungicidas y artropodicidas.
US5846990A (en) * 1995-07-24 1998-12-08 Bristol-Myers Squibb Co. Substituted biphenyl isoxazole sulfonamides
US6310095B1 (en) * 1995-11-06 2001-10-30 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
DE19647380A1 (de) * 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
WO1998023155A1 (en) 1996-11-26 1998-06-04 E.I. Du Pont De Nemours And Company Arthropodicidal and fungicidal cyclic amides
DE19704243A1 (de) * 1997-02-05 1998-08-06 Bayer Ag Neue 2-Amino-substituierte Pyridine
BR9811260A (pt) * 1997-03-03 2000-08-08 Boehringer Ingelheim Pharma Pequenas moléculas úteis no tratamento de doença inflamatória
CA2288330C (en) 1997-05-07 2014-02-11 University Of Pittsburgh Benzoyl amino acid derivatives useful as inhibitors of protein isoprenyl tranferases
DE19741400A1 (de) * 1997-09-19 1999-03-25 Bayer Ag Benzyl-biphenyle
KR20010015910A (ko) 1998-01-23 2001-02-26 로렌스 티. 마이젠헬더 옥사졸리디논 조합 라이브러리, 조성물 및 제조 방법
DE19816880A1 (de) * 1998-04-17 1999-10-21 Boehringer Ingelheim Pharma Neue Diphenyl-substituierte 5-Ring-Heterocyclen, Verfahren zu ihrer Herstellung sowie deren Verwendung als Arzneimittel
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
KR20020047175A (ko) 1999-09-17 2002-06-21 밀레니엄 파머슈티컬스 인코퍼레이티드 Ｘａ 인자의 억제제
HN2000000203A (es) * 1999-11-30 2001-06-13 Pfizer Prod Inc Procedimiento para la obtencion de 1,2,3,4-tetrahidroquinolinas 4-carboxiamino-2- sustituidas.
US6462063B1 (en) 2000-02-04 2002-10-08 Fibrogen, Inc. C-proteinase inhibitors
AU4456601A (en) 2000-03-28 2001-10-08 Nippon Soda Co., Ltd. Oxa(thia)zolidine derivative and anti-inflammatory drug
DE50111751D1 (de) * 2000-12-21 2007-02-08 Sanofi Aventis Deutschland Neue diphenzylazetidinone, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung zur behandlung von lipidstoffwechselstörungen
BR0212458A (pt) 2001-09-11 2004-10-19 Astrazeneca Ab Composto ou sal farmaceuticamente aceitável, ou um éster hidrolizável in vivo deste, pró-droga, método para a produção de um efeito antibacteriano em um animal de sangue quente, uso de um composto ou sal farmaceuticamente aceitável, ou um éster hidrolizável in vivo deste, composição farmacêutica, e, processo para a preparação de um composto ou sais farmaceuticamente aceitável, ou ésteres hidrolizáveis in vivo deste
NZ532288A (en) * 2001-10-16 2005-12-23 Memory Pharm Corp 4-(4-alkoxy-3-hydroxyphenyl)-2-pyrrolidone derivatives as PDE-4 inhibitors for the treatment of neurological syndromes
US7091196B2 (en) * 2002-09-26 2006-08-15 Rib-X Pharmaceuticals, Inc. Bifunctional heterocyclic compounds and methods of making and using same
PL1603553T3 (pl) 2003-03-17 2012-04-30 Japan Tobacco Inc Kompozycje farmaceutyczne inhibitorów CETP
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
DOP2005000123A (es) * 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
WO2006103527A1 (en) 2005-03-31 2006-10-05 Council Of Scientific And Industrial Research Aromatic substituted pentadienoic acid amide for combination with anti-infective drugs
US7910592B2 (en) * 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
KR20140107671A (ko) * 2005-12-30 2014-09-04 머크 샤프 앤드 돔 코포레이션 Ｃｅｔｐ 억제제로서 유용한 1,3-옥사졸리딘-2-온 유도체
CA2635010A1 (en) * 2005-12-30 2007-07-19 Amjad Ali Oxazolidinone derivatives as cetp inhibitors

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