HRP20201927T1 - PIRIMIDINONI KAO INHIBITORI FAKTORA XIa - Google Patents
PIRIMIDINONI KAO INHIBITORI FAKTORA XIa Download PDFInfo
- Publication number
- HRP20201927T1 HRP20201927T1 HRP20201927TT HRP20201927T HRP20201927T1 HR P20201927 T1 HRP20201927 T1 HR P20201927T1 HR P20201927T T HRP20201927T T HR P20201927TT HR P20201927 T HRP20201927 T HR P20201927T HR P20201927 T1 HRP20201927 T1 HR P20201927T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutical composition
- oral pharmaceutical
- image
- composition according
- independently selected
- Prior art date
Links
- 108010080805 Factor XIa Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title 1
- 239000008203 oral pharmaceutical composition Substances 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 230000009424 thromboembolic effect Effects 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 229940127218 antiplatelet drug Drugs 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 239000003527 fibrinolytic agent Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010037437 Pulmonary thrombosis Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000003416 antiarrhythmic agent Substances 0.000 claims 1
- 239000003529 anticholesteremic agent Substances 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 229940127090 anticoagulant agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 239000003524 antilipemic agent Substances 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 210000005242 cardiac chamber Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 229960000103 thrombolytic agent Drugs 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/61—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (15)
1. Oralna farmaceutska kompozicija koja sadrži spoj sa formulom (I):
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog, gdje:
prsten A je nezavisno odabran od
[image]
prsten B je nezavisno odabran od
[image]
R1 je nezavisno odabran od H i C1-4 alkil;
R2 je nezavisno odabran od F, Cl, CF3, CHF2, i COOH;
R3 je nezavisno odabran od H, CHF2, CD3, CH3, i
[image]
R4 je nezavisno odabran od H i F; i
R5 je nezavisno odabran od H, F, Cl, CH3, i OCH3;
i farmaceutski prihvatljiv nosač ili razblaživač.
2. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1, gdje R2 je nezavisno odabran od F, Cl, CF3, i CHF2.
3. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1 gdje spoj sa Formulom (I) je odabrano iz grupe koja se sastoji od:
[image]
[image]
[image]
[image]
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog.
4. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1, gdje spoj sa Formulom (I) ima strukturu:
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog.
5. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1. gdje spoj sa Formulom (I) ima strukturu:
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog.
6. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1, gdje spoj sa Formulom (I) ima strukturu:
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog.
7. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 1, gdje spoj sa Formulom (I) ima strukturu:
[image]
ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog.
8. Oralna farmaceutska kompozicija u skladu sa bilo kojim od patentnih zahtjeva 1 do 7 u obliku tableta, kapsula, pilula, praška, granula, eliksira, tinktura, suspenzija, sirupa ili emulzija.
9. Oralna farmaceutska kompozicija u skladu sa bilo kojim od patentnih zahtjeva 1 do 8 koja dalje sadrži jedan ili više dodatnih terapijskih agenasa odabranih od antiartimijskog agensa, antihipertenzivnog agensa, antikoagulantnog agensa, antitrombocitnog agensa, trombin inhibirajućeg agensa, trombolitičkog agensa, fibrinolitičkog agensa, blokatora kalcijevog kanala, blokatora kalijevog kanala, agensa za snižavanje kolesterola/lipida, ili kombinaciju istih.
10. Oralna farmaceutska kompozicija u skladu sa patentnim zahtjevom 9 gdje jedan ili više dodatnih terapijskih agenasa je antitrobocitni agens ili kombinacija istih.
11. Oralna farmaceutska kompozicija u skladu sa bilo kojim od patentnih zahtjeva 1 do 10 za primjenu kao lijek.
12. Oralna farmaceutska kompozicija u skladu sa bilo kojim od patentnih zahtjeva 1 do 10 za primjenu u liječenju tromboembolijskog poremećaja.
13. Oralna farmaceutska kompozicija u skladu sa bilo kojim od patentnih zahtjeva 1 do 8 za primjenu u liječenju tromboembolijskog poremećaja u kombinaciji sa antitrombocitnim agensom, pri dnevnoj dozi od oko 0.01 do oko 300 miligrama spoja (I) i oko 50 do oko 150 miligrama antitrombocitnog agensa, po kilogramu tjelesne težine pacijenta.
14. Oralna farmaceutska kompozicija za primjenu u skladu sa patentnim zahtjevom 12 gdje je tromboembolijski poremećaj odabran od arterijskih kardiovaskularnih tromboembolijskih poremećaja, venskih kardiovaskularnih tromboembolijskih poremećaja, i tromboembolijskih poremećaja u srčanim komorama ili u perifernoj cirkulaciji.
15. Oralna farmaceutska kompozicija za primjenu u skladu sa patentnim zahtjevom 12 gdje je tromboembolijski poremećaj odabran od nestabilne angine, akutnog koronarnog sindroma, atrijalne fibrilacije, infarkta miokarda, prolaznog ishemičnog napada, moždanog udara, ateroskleroze, periferne okluzivne arterijske bolesti, venske tromboze, tromboze dubokih vena, tromboflebitisa, arterijske embolije, koronarne arterijske tromboze, cerebralne arterijske tromboze, cerebralne embolije, bubrežne embolije, plućne embolije, i tromboze koja je posljedica medicinskih implantata, uređaja, ili procedura u kojima je krv izložena umjetnoj površini koja potiče trombozu.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462058316P | 2014-10-01 | 2014-10-01 | |
EP17189935.4A EP3293186B1 (en) | 2014-10-01 | 2015-07-29 | Pyrimidinones as factor xia inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20201927T1 true HRP20201927T1 (hr) | 2021-02-05 |
Family
ID=53784023
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20171950TT HRP20171950T1 (hr) | 2014-10-01 | 2017-12-18 | Pirimidinoni kao inhibitori faktora xia |
HRP20201927TT HRP20201927T1 (hr) | 2014-10-01 | 2020-12-03 | PIRIMIDINONI KAO INHIBITORI FAKTORA XIa |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20171950TT HRP20171950T1 (hr) | 2014-10-01 | 2017-12-18 | Pirimidinoni kao inhibitori faktora xia |
Country Status (33)
Country | Link |
---|---|
EP (4) | EP3089979B1 (hr) |
JP (4) | JP6462865B2 (hr) |
KR (2) | KR101921436B1 (hr) |
CN (3) | CN110734435B (hr) |
AR (1) | AR101367A1 (hr) |
AU (3) | AU2015324530B2 (hr) |
CA (1) | CA2963395C (hr) |
CL (1) | CL2017000712A1 (hr) |
CO (1) | CO2017003833A2 (hr) |
CY (2) | CY1119678T1 (hr) |
DK (2) | DK3089979T3 (hr) |
EA (1) | EA031590B1 (hr) |
ES (3) | ES2963267T3 (hr) |
HR (2) | HRP20171950T1 (hr) |
HU (2) | HUE052812T2 (hr) |
IL (2) | IL251434B (hr) |
LT (2) | LT3293186T (hr) |
MA (1) | MA40123A1 (hr) |
MX (2) | MX2017003695A (hr) |
MY (1) | MY183987A (hr) |
NO (1) | NO2721243T3 (hr) |
PE (2) | PE20170939A1 (hr) |
PH (2) | PH12017500580B1 (hr) |
PL (1) | PL3089979T3 (hr) |
PT (2) | PT3089979T (hr) |
RS (2) | RS61183B1 (hr) |
SG (2) | SG11201702576QA (hr) |
SI (2) | SI3089979T1 (hr) |
TN (2) | TN2018000229A1 (hr) |
TW (3) | TWI769442B (hr) |
UY (1) | UY36244A (hr) |
WO (1) | WO2016053455A1 (hr) |
ZA (1) | ZA201702478B (hr) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
NO2760821T3 (hr) | 2014-01-31 | 2018-03-10 | ||
HUE040226T2 (hu) * | 2014-01-31 | 2019-02-28 | Bristol Myers Squibb Co | Makrociklusok heterociklusos P2' csoportokkal XIA faktor inhibitorokként |
WO2016036893A1 (en) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
NO2721243T3 (hr) * | 2014-10-01 | 2018-10-20 | ||
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
CN107001391B (zh) | 2014-10-01 | 2020-11-27 | 默克专利股份公司 | 硼酸衍生物 |
JOP20160086B1 (ar) | 2015-05-08 | 2021-08-17 | 2 Katholieke Univ Leuven Ku Leuven Research And Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
EP3310777B1 (en) | 2015-06-19 | 2019-10-09 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
ES2937156T3 (es) | 2015-07-29 | 2023-03-24 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que llevan un grupo P2' no aromático |
ES2803659T3 (es) | 2015-07-29 | 2021-01-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor xia que contienen restos alquilo o cicloalquilo p2 |
JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JO3633B1 (ar) | 2015-09-16 | 2020-08-27 | Katholieke Univ Leuven Ku Leuven Research & Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
EP3423458A1 (en) | 2016-03-02 | 2019-01-09 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
SG11201808138YA (en) | 2016-03-31 | 2018-10-30 | Janssen Pharmaceuticals Inc | Substituted indole derivatives as dengue viral replication inhibitors |
MA44498A (fr) | 2016-03-31 | 2019-02-06 | Janssen Pharmaceuticals Inc | Dérivés d'indoline substituée utilisés en tant qu'inhibiteurs de la réplication du virus de la dengue |
JOP20170069B1 (ar) | 2016-04-01 | 2021-08-17 | 1 Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
EA201892200A1 (ru) | 2016-04-01 | 2019-03-29 | Янссен Фармасьютикалз, Инк. | Замещенные производные соединений индола в качестве ингибиторов репликации вирусов денге |
WO2018133793A1 (zh) * | 2017-01-18 | 2018-07-26 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
KR102625991B1 (ko) | 2017-05-22 | 2024-01-16 | 얀센 파마슈티칼즈, 인코포레이티드 | 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체 |
US11407715B2 (en) | 2017-05-22 | 2022-08-09 | Janssen Pharmaceuticals, Inc. | Substituted indoline derivatives as dengue viral replication inhibitors |
MX2021012286A (es) * | 2019-04-11 | 2022-04-06 | Bristol Myers Squibb Co | Nuevas opciones sinteticas hacia la manufactura de (6r,10s)-10-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1-il)fenil]-6 -oxo-1(6h)-pirimidinil}-1-(difluorometil)-6-metil-1,4,7,8,9,10-he xahidro-11,15-(meteno)pirazol[4,3-b][1,7]diazaciclotetradecin-5(6 h)-ona. |
EA202192753A1 (ru) * | 2019-04-11 | 2022-01-11 | Бристол-Маерс Сквибб Компани | Повышенная эффективность аморфных твердых и солюбилизированных составов для достижения терапевтических концентраций в плазме |
WO2020211781A1 (zh) | 2019-04-16 | 2020-10-22 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
US20220281868A1 (en) * | 2019-07-23 | 2022-09-08 | Medshine Discovery Inc. | Macrocyclic derivatives as factor xia inhibitors |
JP7450024B2 (ja) * | 2019-09-27 | 2024-03-14 | シェンヅェン サルブリス ファーマシューティカルズ カンパニー リミテッド | FXIa阻害剤及びその調製方法と医薬用途 |
PE20231071A1 (es) * | 2020-04-10 | 2023-07-17 | Bristol Myers Squibb Co | Formas cristalinas de (9r,13s)-13-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1- il)fenil]-6-oxo-1,6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3,4,7,15- tetraazatriciclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-ona |
TW202229280A (zh) * | 2020-10-12 | 2022-08-01 | 美商必治妥美雅史谷比公司 | (6r,10s)-10-{4-[5-氯-2-(4-氯-1h-1,2,3-三唑-1-基)苯基]-6-側氧基-1(6h)-嘧啶基}-1-(二氟甲基)-6-甲基-1,4,7,8,9,10-六氫-11,15-(亞甲橋基)吡唑并[4,3-b][1,7]二氮雜環十四炔-5(6h)-酮之製備方法 |
CN115215867B (zh) * | 2021-04-21 | 2023-12-26 | 上海美悦生物科技发展有限公司 | FXIa抑制剂及其药物组合物、制备方法和用途 |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | Beecham Group Plc | Enzyme derivatives, and their preparation |
PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
WO2000076970A2 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Serine protease inhibitors |
DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
CH1427415H1 (de) | 2001-09-21 | 2023-12-21 | Bristol Myers Squibb Holdings Ireland | Lactamhaltige verbindungen und ihre derivate als faktor-xa-hemmer |
US20040180855A1 (en) | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
TWI577665B (zh) * | 2010-02-11 | 2017-04-11 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之巨環類 |
US9327839B2 (en) | 2011-08-05 | 2016-05-03 | General Atomics | Method and apparatus for inhibiting formation of and/or removing ice from aircraft components |
TW201311689A (zh) * | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子xia抑制劑之新穎巨環化合物 |
TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為xia因子抑制劑之環狀p1接合劑 |
EP3290413B9 (en) * | 2011-12-21 | 2020-04-29 | ONO Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
CN108250199B (zh) * | 2012-08-03 | 2021-07-16 | 百时美施贵宝公司 | 二氢吡啶酮p1作为凝血因子xia抑制剂 |
UY34959A (es) * | 2012-08-03 | 2014-01-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Dihidropiridona p1 como inhibidores del factor xia |
HUE040226T2 (hu) * | 2014-01-31 | 2019-02-28 | Bristol Myers Squibb Co | Makrociklusok heterociklusos P2' csoportokkal XIA faktor inhibitorokként |
NO2760821T3 (hr) * | 2014-01-31 | 2018-03-10 | ||
NO2721243T3 (hr) * | 2014-10-01 | 2018-10-20 |
-
2012
- 2012-06-14 NO NO12801069A patent/NO2721243T3/no unknown
-
2015
- 2015-07-29 LT LTEP17189935.4T patent/LT3293186T/lt unknown
- 2015-07-29 MA MA40123A patent/MA40123A1/fr unknown
- 2015-07-29 ES ES20197284T patent/ES2963267T3/es active Active
- 2015-07-29 PE PE2017000527A patent/PE20170939A1/es unknown
- 2015-07-29 CN CN201910882473.1A patent/CN110734435B/zh active Active
- 2015-07-29 TN TNP/2018/000229A patent/TN2018000229A1/en unknown
- 2015-07-29 HU HUE17189935A patent/HUE052812T2/hu unknown
- 2015-07-29 UY UY0001036244A patent/UY36244A/es active IP Right Grant
- 2015-07-29 SG SG11201702576QA patent/SG11201702576QA/en unknown
- 2015-07-29 AU AU2015324530A patent/AU2015324530B2/en active Active
- 2015-07-29 DK DK15747721.7T patent/DK3089979T3/en active
- 2015-07-29 MX MX2017003695A patent/MX2017003695A/es active IP Right Grant
- 2015-07-29 SG SG10201911652TA patent/SG10201911652TA/en unknown
- 2015-07-29 SI SI201530123T patent/SI3089979T1/sl unknown
- 2015-07-29 PE PE2020001966A patent/PE20210922A1/es unknown
- 2015-07-29 LT LTEP15747721.7T patent/LT3089979T/lt unknown
- 2015-07-29 EP EP15747721.7A patent/EP3089979B1/en active Active
- 2015-07-29 EA EA201790595A patent/EA031590B1/ru not_active IP Right Cessation
- 2015-07-29 PL PL15747721T patent/PL3089979T3/pl unknown
- 2015-07-29 TW TW109111475A patent/TWI769442B/zh active
- 2015-07-29 TW TW111120670A patent/TWI834182B/zh active
- 2015-07-29 RS RS20201472A patent/RS61183B1/sr unknown
- 2015-07-29 CN CN201580053079.7A patent/CN106795161B/zh active Active
- 2015-07-29 PT PT157477217T patent/PT3089979T/pt unknown
- 2015-07-29 MY MYPI2017701150A patent/MY183987A/en unknown
- 2015-07-29 CN CN202210580097.2A patent/CN114957255A/zh active Pending
- 2015-07-29 TW TW104124664A patent/TWI692478B/zh active
- 2015-07-29 SI SI201531423T patent/SI3293186T1/sl unknown
- 2015-07-29 ES ES15747721.7T patent/ES2655884T3/es active Active
- 2015-07-29 TN TN2017000112A patent/TN2017000112A1/en unknown
- 2015-07-29 EP EP23185426.6A patent/EP4286372A3/en active Pending
- 2015-07-29 PT PT171899354T patent/PT3293186T/pt unknown
- 2015-07-29 DK DK17189935.4T patent/DK3293186T3/da active
- 2015-07-29 KR KR1020177011233A patent/KR101921436B1/ko active IP Right Grant
- 2015-07-29 WO PCT/US2015/042576 patent/WO2016053455A1/en active Application Filing
- 2015-07-29 JP JP2017517766A patent/JP6462865B2/ja active Active
- 2015-07-29 EP EP17189935.4A patent/EP3293186B1/en active Active
- 2015-07-29 CA CA2963395A patent/CA2963395C/en active Active
- 2015-07-29 RS RS20180046A patent/RS56786B1/sr unknown
- 2015-07-29 AR ARP150102426A patent/AR101367A1/es active IP Right Grant
- 2015-07-29 EP EP20197284.1A patent/EP3828186B1/en active Active
- 2015-07-29 ES ES17189935T patent/ES2836270T3/es active Active
- 2015-07-29 HU HUE15747721A patent/HUE038061T2/hu unknown
- 2015-07-29 KR KR1020187033199A patent/KR102269999B1/ko active IP Right Grant
-
2017
- 2017-03-21 MX MX2020010840A patent/MX2020010840A/es unknown
- 2017-03-24 CL CL2017000712A patent/CL2017000712A1/es unknown
- 2017-03-28 IL IL251434A patent/IL251434B/en active IP Right Grant
- 2017-03-29 PH PH12017500580A patent/PH12017500580B1/en unknown
- 2017-04-07 ZA ZA2017/02478A patent/ZA201702478B/en unknown
- 2017-04-20 CO CONC2017/0003833A patent/CO2017003833A2/es unknown
- 2017-12-15 CY CY20171101314T patent/CY1119678T1/el unknown
- 2017-12-18 HR HRP20171950TT patent/HRP20171950T1/hr unknown
-
2018
- 2018-12-27 JP JP2018244086A patent/JP6937734B2/ja active Active
-
2020
- 2020-01-20 AU AU2020200376A patent/AU2020200376B2/en active Active
- 2020-01-27 PH PH12020500195A patent/PH12020500195A1/en unknown
- 2020-08-03 IL IL276470A patent/IL276470B/en active IP Right Grant
- 2020-12-03 HR HRP20201927TT patent/HRP20201927T1/hr unknown
- 2020-12-04 CY CY20201101149T patent/CY1123663T1/el unknown
-
2021
- 2021-08-31 JP JP2021140618A patent/JP7317905B2/ja active Active
- 2021-10-05 AU AU2021245098A patent/AU2021245098B2/en active Active
-
2023
- 2023-07-19 JP JP2023117409A patent/JP2023134734A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20201927T1 (hr) | PIRIMIDINONI KAO INHIBITORI FAKTORA XIa | |
HRP20161378T1 (hr) | Dihidropiridon kao faktor xia inhibitora | |
JP2014521700A5 (hr) | ||
JP2011520967A5 (hr) | ||
RU2019107938A (ru) | Производное оксопиколинамида, способ его получения и его фармацевтическое применение | |
IL298983B2 (en) | Macrocyclines with P2' heterocyclic groups as factor XIA inhibitors | |
HRP20180465T1 (hr) | Kristalni oblici inhibitora faktora xia | |
JP2017504640A5 (hr) | ||
RU2014129797A (ru) | Соединения | |
EP3658538A1 (en) | Compounds and compositions for treating conditions associated with nlrp activity | |
JP2016530259A5 (hr) | ||
HRP20171122T1 (hr) | Novi makrociklusi kao inhibitori faktora xia | |
JP2017525744A5 (hr) | ||
JP2014530240A5 (hr) | ||
JP2014532070A5 (hr) | ||
JP2007537273A5 (hr) | ||
JP2016515096A5 (hr) | ||
MA38323B1 (fr) | Dérivés pyrimidone et leur utilisation dans le traitement, l'amélioration ou la prévention d'une maladie virale | |
JP2009536218A5 (hr) | ||
RU2011143741A (ru) | Производное индолизина и его применение в медицинских целях | |
JP2016518434A5 (hr) | ||
RU2017121460A (ru) | Производные пиридинкарбоксамида, способ их получения и их фармацевтическое применение | |
RU2014120477A (ru) | Производные пиримидин-4-она и их применение в лечении, облегчении или профилактике вирусного заболевания | |
EA201391558A1 (ru) | Тетрагидропиразоло[1,5-а]пиримидины как противотуберкулезные соединения | |
JP2017514809A5 (hr) |