CY1119466T1 - Παραγωγα ιμιδαζοθειαδιαζολης και ιμιδαζοπυραζινης ως αναστολεις του ενεργοποιουμενου απο πρωτεαση υποδοχεα 4 (par 4) για αγωγη συσσωματωσης αιμοπεταλιων - Google Patents
Παραγωγα ιμιδαζοθειαδιαζολης και ιμιδαζοπυραζινης ως αναστολεις του ενεργοποιουμενου απο πρωτεαση υποδοχεα 4 (par 4) για αγωγη συσσωματωσης αιμοπεταλιωνInfo
- Publication number
- CY1119466T1 CY1119466T1 CY20171101023T CY171101023T CY1119466T1 CY 1119466 T1 CY1119466 T1 CY 1119466T1 CY 20171101023 T CY20171101023 T CY 20171101023T CY 171101023 T CY171101023 T CY 171101023T CY 1119466 T1 CY1119466 T1 CY 1119466T1
- Authority
- CY
- Cyprus
- Prior art keywords
- inhibitors
- imidazothiadiazole
- par
- action
- activated protease
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- BOXRDDIXJOUZLV-UHFFFAOYSA-N 2h-imidazo[4,5-d]thiadiazole Chemical compound N1SC2=NC=NC2=N1 BOXRDDIXJOUZLV-UHFFFAOYSA-N 0.000 title 1
- 102100040853 PRKC apoptosis WT1 regulator protein Human genes 0.000 title 1
- 101710162991 PRKC apoptosis WT1 regulator protein Proteins 0.000 title 1
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
- 150000005235 imidazopyrazines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract 1
- 150000003557 thiazoles Chemical class 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/433—Thidiazoles
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A—HUMAN NECESSITIES
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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- 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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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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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
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
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- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0453—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Proteomics, Peptides & Aminoacids (AREA)
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- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Η παρούσα εφεύρεση παρέχει ενώσεις θειαζόλης του Χημικού Τύπου I όπου τα W, Υ, R0, R2, R4, R5, R6, R7, Χ1, Χ2, Χ3 και Χ4 είναι όπως καθορίζεται εις το παρόν, ή ένα στερεοϊσομερές, ταυτομερές, φαρμακευτικώς αποδεκτό άλας, εστέρα προφαρμάκου ή μορφή επιδιαλυτωμένου άλατος εξ' αυτών, όπου όλες οι μεταβλητές είναι όπως καθορίζεται εις το παρόν. Αυτές οι ενώσεις είναι αναστολείς της συσσωμάτωσης αιμοπεταλίων και τοιουτοτρόπως μπορούν να χρησιμοποιηθούν ως φάρμακα για αγωγή ή πρόληψη θρομβοεμβολικών διαταραχών.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201261638577P | 2012-04-26 | 2012-04-26 | |
US201361787680P | 2013-03-15 | 2013-03-15 | |
PCT/US2013/037956 WO2013163279A1 (en) | 2012-04-26 | 2013-04-24 | Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
Publications (1)
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CY1119466T1 true CY1119466T1 (el) | 2018-03-07 |
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CY20171101023T CY1119466T1 (el) | 2012-04-26 | 2017-09-29 | Παραγωγα ιμιδαζοθειαδιαζολης και ιμιδαζοπυραζινης ως αναστολεις του ενεργοποιουμενου απο πρωτεαση υποδοχεα 4 (par 4) για αγωγη συσσωματωσης αιμοπεταλιων |
CY20201100069T CY1122625T1 (el) | 2012-04-26 | 2020-01-24 | Παραγωγα ιμιδαζοθειαδιαζολης και ιμιδαζοπυραζινης ως αναστολεις του ενεργοποιουμενου απο πρωτεαση υποδοχεα 4 (par4) για αγωγη συσσωματωσης αιμοπεταλιων |
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CY20201100069T CY1122625T1 (el) | 2012-04-26 | 2020-01-24 | Παραγωγα ιμιδαζοθειαδιαζολης και ιμιδαζοπυραζινης ως αναστολεις του ενεργοποιουμενου απο πρωτεαση υποδοχεα 4 (par4) για αγωγη συσσωματωσης αιμοπεταλιων |
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US (5) | US9688695B2 (el) |
EP (3) | EP3632919B1 (el) |
JP (1) | JP6073464B2 (el) |
KR (3) | KR20200127273A (el) |
CN (2) | CN104583218B (el) |
AR (1) | AR090834A1 (el) |
AU (1) | AU2013251632B2 (el) |
BR (1) | BR112014026643B1 (el) |
CA (1) | CA2871650C (el) |
CL (1) | CL2014002915A1 (el) |
CO (1) | CO7160040A2 (el) |
CY (2) | CY1119466T1 (el) |
DK (3) | DK3243826T3 (el) |
EA (1) | EA026724B1 (el) |
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FI (1) | FI3632919T3 (el) |
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PL (3) | PL3243826T3 (el) |
PT (3) | PT3243826T (el) |
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SI (3) | SI3243826T1 (el) |
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UY (1) | UY34763A (el) |
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KR20200127273A (ko) * | 2012-04-26 | 2020-11-10 | 브리스톨-마이어스 스큅 컴퍼니 | 혈소판 응집을 치료하기 위한 프로테아제 활성화 수용체 4 (par4) 억제제로서의 이미다조티아디아졸 및 이미다조피라진 유도체 |
JP6101343B2 (ja) | 2012-04-26 | 2017-03-22 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピリダジン誘導体 |
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