HRP20120476T1 - Derivati 4-benzilamino-1-karboksiacil-piperidina kao cetp inhibitori korisni za liječenje bolesti kao što su hiperlipidemija ili arterioskleroza - Google Patents
Derivati 4-benzilamino-1-karboksiacil-piperidina kao cetp inhibitori korisni za liječenje bolesti kao što su hiperlipidemija ili arterioskleroza Download PDFInfo
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- HRP20120476T1 HRP20120476T1 HRP20120476AT HRP20120476T HRP20120476T1 HR P20120476 T1 HRP20120476 T1 HR P20120476T1 HR P20120476A T HRP20120476A T HR P20120476AT HR P20120476 T HRP20120476 T HR P20120476T HR P20120476 T1 HRP20120476 T1 HR P20120476T1
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 5
- 201000010099 disease Diseases 0.000 title claims 3
- 206010003210 Arteriosclerosis Diseases 0.000 title claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 title claims 2
- 208000011775 arteriosclerosis disease Diseases 0.000 title claims 2
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 9
- 229910052736 halogen Inorganic materials 0.000 claims abstract 5
- 150000002367 halogens Chemical class 0.000 claims abstract 5
- 125000001424 substituent group Chemical group 0.000 claims abstract 4
- 125000005842 heteroatom Chemical group 0.000 claims abstract 3
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 3
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims 18
- 230000003287 optical effect Effects 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 3
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims 2
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 2
- 102000003729 Neprilysin Human genes 0.000 claims 2
- 108090000028 Neprilysin Proteins 0.000 claims 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 claims 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 1
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000037487 Endotoxemia Diseases 0.000 claims 1
- 208000010496 Heart Arrest Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010021024 Hypolipidaemia Diseases 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229940123934 Reductase inhibitor Drugs 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 229960002478 aldosterone Drugs 0.000 claims 1
- 239000002170 aldosterone antagonist Substances 0.000 claims 1
- 229940083712 aldosterone antagonist Drugs 0.000 claims 1
- 150000003973 alkyl amines Chemical class 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 238000002399 angioplasty Methods 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 229940126317 angiotensin II receptor antagonist Drugs 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 201000009101 diabetic angiopathy Diseases 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000009977 dual effect Effects 0.000 claims 1
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 208000029498 hypoalphalipoproteinemia Diseases 0.000 claims 1
- 230000007574 infarction Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Spoj, naznačen time, da ima formulu (I): gdje, R1 je (C1-C7)alkil-O-C(O)-, ili 5- ili 6-člani heteroaril koji ima 1, 2 ili 3 heteroatoma odabranih od N, O ili S, pri čemu je spomenuti heteroaril opcijski supstituiran s jednim do tri supstituenta odabranih od halogena, di(C1-C4)
Claims (8)
1. Spoj, naznačen time, da ima formulu (I):
[image]
gdje,
R1 je (C1-C7)alkil-O-C(O)-, ili 5- ili 6-člani heteroaril koji ima 1, 2 ili 3 heteroatoma odabranih od N, O ili S, pri čemu je spomenuti heteroaril opcijski supstituiran s jednim do tri supstituenta odabranih od halogena, di(C1-C4)alkilamina, (C1-C7)alkoksi, ili 5- ili 6-člani heterociklil koji ima 1, 2 ili 3 heteroatoma odabranih od N, O ili S, gdje je spomenuti heterociklil nadalje opcijski supstituiran s jednim do tri supstituenta odabranih od
(C1-C4)alkila, (C1C7)alkanoila ili hidroksi;
R2 je (C1-C7)alkil;
R3 je HO(O)C-R9-O-C(O)-;
R4 je (C1-C7)alkil ili fenil-(C1-C4)alkil, pri čemu je spomenuti fenil opcijski supstituiran s jednim do tri supstituenta odabranih od (C1-C4)alkila ili halogena;
R5 je vodik;
R6 i R7 su neovisno halogen, (C1-C7)alkil ili (C1-C7)alkoksi, gdje je spomenuti alkil supstituiran s jednim do tri halogena; i
R9 je (C1-C4)alkil, (C3-C6)cikloalkil, (C1-C4)alkil-(C3-C6)cikloalkil ili (C3-C6)cikloalkil-(C1C4)alkil; ili
njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili mješavina optičkih izomera.
2. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili mješavina optičkih izomera; naznačen time, da R9 je
[image]
ili
[image]
3. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je odabran od sljedećih
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
,
[image]
i
[image]
.
4. Spoj prema zahtjevu 3, ili njegova farmaceutski prihvatljiva sol, naznačen time, da on je
[image]
.
5. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 4, ili njegovu farmaceutski prihvatljivu sol; ili njegov optički izomer; ili mješavinu optičkih izomera; kao i farmaceutski prihvatljivi nosač.
6. Kombinacija spoja prema bilo kojem od zahtjeva 1 do 4, ili njegove farmaceutski prihvatljive soli, ili njegovog optičkog izomera; ili mješavine optičkih izomera; naznačena time, da je zajedno s daljnjim aktivnim počelom odabrana iz skupine koju čine:
(i) inhibitor reduktaze HMG-Co-A ili njegova farmaceutski prihvatljiva sol,
(ii) antagonist receptora angiotenzina II ili njegova farmaceutski prihvatljiva sol,
(iii) inhibitor angiotenzina koji pretvara enzime (ACE) ili njegova farmaceutski prihvatljiva sol,
(iv) blokator kanala kalcija ili njegova farmaceutski prihvatljiva sol,
(v) inhibitor sinteze aldosterona ili njegova farmaceutski prihvatljiva sol,
(vi) antagonist aldosterona ili njegova farmaceutski prihvatljiva sol,
(vii) dvojni inhibitor angiotenzina koji pretvara enzime / neutralne endopeptidaze (ACE/NEP) ili njegova farmaceutski prihvatljiva sol,
(viii) antagonist endotelina ili njegova farmaceutski prihvatljiva sol,
(ix) inhibitor renina ili njegova farmaceutski prihvatljiva sol,
(x) diuretik ili njegova farmaceutski prihvatljiva sol, i
(xi) ApoA-I-mimetik.
7. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol; ili njegov optički izomer; ili mješavina optičkih izomera; naznačen time, da se upotrebljava kao lijek.
8. Uporaba spoja formule (I) prema bilo kojem od zahtjeva 1 do 4, ili njegove farmaceutski prihvatljive soli; ili njegovog optičkog izomera; ili mješavine optičkih izomera; naznačena time, da je za proizvodnju lijeka za liječenje poremećaja ili bolesti, pri čemu je poremećaj ili bolest odabrana iz skupine koju čine hiperlipidemija, arterioskleroza, ateroskleroza, periferalna vaskularna bolest, dislipidemija, hiperbetalipoproteinemija, hipoalfalipoproteinemija, hiperkolesterolemija, hipertrigliceridemija, porodična hiperkolesterolemija, kardiovaskularni poremećaj, koronarna srčana bolest, koronarna arterijska bolest, koronarna vaskularna bolest, angina, ishemija, srčana ishemija, tromboza, kardijski infarkt kao primjerice miokardijski infarkt, udar, periferalna vaskularna bolest, reperfuzijska ozljeda, angioplastična restinoza, hipertenzija, kongestivni srčani zastoj, dijabetes kao primjerice dijabetes melitus tipa II, dijabetske vaskularne komplikacije, pretilost ili endotoksemija.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98545607P | 2007-11-05 | 2007-11-05 | |
| PCT/EP2008/064859 WO2009059943A1 (en) | 2007-11-05 | 2008-11-03 | 4-benzylamino-1-carboxyacyl-piperidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120476T1 true HRP20120476T1 (hr) | 2012-06-30 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120476AT HRP20120476T1 (hr) | 2007-11-05 | 2012-06-05 | Derivati 4-benzilamino-1-karboksiacil-piperidina kao cetp inhibitori korisni za liječenje bolesti kao što su hiperlipidemija ili arterioskleroza |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8193349B2 (hr) |
| EP (2) | EP2207775B1 (hr) |
| JP (1) | JP5555635B2 (hr) |
| KR (1) | KR101564793B1 (hr) |
| CN (1) | CN101910150B (hr) |
| AR (1) | AR069165A1 (hr) |
| AT (1) | ATE550333T1 (hr) |
| AU (1) | AU2008324243B2 (hr) |
| BR (1) | BRPI0819223A2 (hr) |
| CA (1) | CA2704633C (hr) |
| CL (1) | CL2008003284A1 (hr) |
| CY (1) | CY1112706T1 (hr) |
| DK (1) | DK2207775T3 (hr) |
| EA (1) | EA022912B1 (hr) |
| ES (2) | ES2381518T3 (hr) |
| HK (1) | HK1168096A1 (hr) |
| HR (1) | HRP20120476T1 (hr) |
| JO (1) | JO2732B1 (hr) |
| MX (1) | MX2010004929A (hr) |
| PE (1) | PE20090982A1 (hr) |
| PL (2) | PL2463282T3 (hr) |
| PT (2) | PT2463282E (hr) |
| SI (1) | SI2207775T1 (hr) |
| TW (1) | TWI426910B (hr) |
| WO (1) | WO2009059943A1 (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2229356B1 (en) | 2007-12-03 | 2011-10-12 | Novartis AG | 1,2-disubstituted-4-benzylamino-pyrrolidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperli pidemia or arteriosclerosis |
| KR101702609B1 (ko) | 2009-06-17 | 2017-02-03 | 버텍스 파마슈티칼스 인코포레이티드 | 인플루엔자 바이러스 복제의 억제제 |
| JO3340B1 (ar) | 2010-05-26 | 2019-03-13 | Regeneron Pharma | مضادات حيوية لـعامل تمايز النمو 8 البشري |
| US8877815B2 (en) | 2010-11-16 | 2014-11-04 | Novartis Ag | Substituted carbamoylcycloalkyl acetic acid derivatives as NEP |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| CN103391939B (zh) | 2010-12-03 | 2016-03-09 | Epizyme股份有限公司 | 作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物 |
| EP2668507B1 (en) | 2011-01-26 | 2017-08-23 | INSERM - Institut National de la Santé et de la Recherche Médicale | Method for assessing a subject's risk of having a cardiovascular disease. |
| DK3141548T3 (da) * | 2011-07-05 | 2020-07-06 | Vertex Pharma | Fremgangsmåder og mellemprodukter til fremstilling af azaindoler |
| ES2683350T3 (es) * | 2011-07-08 | 2018-09-26 | Novartis Ag | Método para tratar la aterosclerosis en sujetos con alto nivel de triglicéridos |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| PT2780368T (pt) | 2011-11-14 | 2018-03-22 | Regeneron Pharma | Composições e métodos para aumentar a massa muscular e a força muscular antagonizando especificamente gdf8 e/ou activina a |
| US10538475B2 (en) | 2012-05-25 | 2020-01-21 | Nutech Ventures | Amphiphilic cyclobutenes and cylobutanes |
| UY35144A (es) | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| US9340582B2 (en) | 2013-07-25 | 2016-05-17 | Novartis Ag | Bioconjugates of synthetic apelin polypeptides |
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