CY1107184T1 - Τρικυκλικοι ανταγωνιστες υποδοχεα θρομβινης - Google Patents
Τρικυκλικοι ανταγωνιστες υποδοχεα θρομβινηςInfo
- Publication number
- CY1107184T1 CY1107184T1 CY20081100152T CY081100152T CY1107184T1 CY 1107184 T1 CY1107184 T1 CY 1107184T1 CY 20081100152 T CY20081100152 T CY 20081100152T CY 081100152 T CY081100152 T CY 081100152T CY 1107184 T1 CY1107184 T1 CY 1107184T1
- Authority
- CY
- Cyprus
- Prior art keywords
- n6nhc
- n6nhso2r16
- or16b
- nr28r29
- alkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Αποκαλύπτονται ετεροκυκλικά-υποκατεστημένα τρικυκλικά του τύπου (Ι) ή φαρμακευτικώς αποδεκτό άλας αυτών, όπου: η διακεκομμένη γραμμή αντιπροσωπεύει έναν προαιρετικό απλό δεσμό, το (a) αντιπροσωπεύει προαιρετικό διπλό δεσμό, το n είναι 0-2, το Q είναι κυκλοαλκυλ, προαιρετικά υποκατεστημένο από R13 και R14, έκαστο R13 ανεξαρτήτως επιλέγεται από Η, (C1-C6)αλκυλ, (C3-C8)κυκλοαλκυλ, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5 και -(CH2)n6C(O)NR28R29 όπου το n6 είναι 0-4, αλογονοαλκυλ και αλογόνο, έκαστο R14 ανεξαρτήτως επιλέγεται από Η, (C1-C6)αλκυλ, -OH, (C1-C6)αλκοξυ, R27-αρυλ (C1-C6)αλκυλ, ετεροαρυλ, ετεροαρυλαλκυλ, ετεροκυκλυλ, ετεροκυκλυλαλκυλ, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5 και -(CH2)n6C(O)NR28R29 όπου το n6 είναι 0-4, αλογόνο και αλογονοαλκυλ ή τα R13 και R14 λαμβανόμενα μαζί σχηματίζουν σπειροκυκλικό ή ετεροσπειροκυκλικό δακτύλιο 3-6 ατόμων, όπου τουλάχιστον ένα των R13 ή R14 επιλέγεται από την ομάδα που αποτελείται από -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, -(CH2)n6NHSO2NR4R5 και -(CH2)n6C(O)NR28R29 όπου το n6 είναι 0-4, το Het είναι μονο- ή δι-κυκλική προαιρετικώς υποκατεστημένη ετεροαρυλ ομάδα και το Β είναι ένας δεσμός, αλκυλενο ή προαιρετικά υποκατεστημένο αλκενυλενο ή αλκυνυλενο, όπου οι υπόλοιποι υποκατάστατες είναι όπως ορίζεται στην περιγραφή, καθώς επίσης φαρμακευτικές συνθέσεις που περιέχουν αυτά και μέθοδος θεραπείας ασθενειών που συνδυάζονται με θρόμβωση, αθηροσκλήρωση, επαναστένωση, υπέρταση, στηθάγχη, αρρυθμία, καρδιακή ανεπάρκεια και καρκίνο με χορήγηση των αναφερθεισών ενώσεων. Αξιώνεται επίσης θεραπεία συνδυασμού με άλλους καρδιαγγειακούς παράγοντες.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US37307202P | 2002-04-16 | 2002-04-16 | |
EP03718393A EP1495018B3 (en) | 2002-04-16 | 2003-04-14 | Tricyclic thrombin receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1107184T1 true CY1107184T1 (el) | 2012-10-24 |
Family
ID=29250954
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20081100152T CY1107184T1 (el) | 2002-04-16 | 2008-02-07 | Τρικυκλικοι ανταγωνιστες υποδοχεα θρομβινης |
CY20111100338T CY1111363T1 (el) | 2002-04-16 | 2011-03-30 | Τρικυκλικος ανταγωνιστης υποδοχεων θρομβινης |
CY2015029C CY2015029I2 (el) | 2002-04-16 | 2015-07-10 | Τρικυκλικοι ανταγωνιστες υποδοχεα θρομβινης |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20111100338T CY1111363T1 (el) | 2002-04-16 | 2011-03-30 | Τρικυκλικος ανταγωνιστης υποδοχεων θρομβινης |
CY2015029C CY2015029I2 (el) | 2002-04-16 | 2015-07-10 | Τρικυκλικοι ανταγωνιστες υποδοχεα θρομβινης |
Country Status (34)
Country | Link |
---|---|
US (3) | US7304078B2 (el) |
EP (5) | EP2062890B1 (el) |
JP (2) | JP4558331B2 (el) |
KR (1) | KR101026929B1 (el) |
CN (1) | CN1659162B (el) |
AR (1) | AR039570A1 (el) |
AT (3) | ATE378330T1 (el) |
AU (1) | AU2003221932B2 (el) |
BR (1) | BRPI0309309B8 (el) |
CA (1) | CA2482858C (el) |
CY (3) | CY1107184T1 (el) |
DE (3) | DE60317493T3 (el) |
DK (2) | DK2065384T3 (el) |
EC (1) | ECSP045368A (el) |
ES (3) | ES2357876T3 (el) |
FR (1) | FR15C0047I2 (el) |
HK (3) | HK1070887A1 (el) |
IL (1) | IL164585A (el) |
LT (1) | LTC1495018I2 (el) |
LU (1) | LU92759I2 (el) |
MX (1) | MXPA04010308A (el) |
MY (1) | MY144040A (el) |
NL (1) | NL300746I1 (el) |
NO (2) | NO330500B1 (el) |
NZ (2) | NZ535880A (el) |
PE (1) | PE20040412A1 (el) |
PL (1) | PL214718B1 (el) |
PT (2) | PT1495018E (el) |
RU (2) | RU2329264C9 (el) |
SG (1) | SG164279A1 (el) |
SI (2) | SI1495018T1 (el) |
TW (1) | TWI343919B (el) |
WO (1) | WO2003089428A1 (el) |
ZA (1) | ZA200408342B (el) |
Families Citing this family (62)
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US8563511B2 (en) * | 2004-10-06 | 2013-10-22 | University Of Rochester | Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway |
ES2535534T3 (es) * | 2005-01-14 | 2015-05-12 | Merck Sharp & Dohme Corp. | Una síntesis exo-selectiva de los análogos de himbacina |
US7541471B2 (en) * | 2005-01-14 | 2009-06-02 | Schering Corporation | Synthesis of himbacine analogs |
AR056919A1 (es) * | 2005-01-14 | 2007-11-07 | Schering Corp | SíNTESIS EXO- Y DIASTEREO- SELECTIVAS DE ANÁLOGOS DE HIMBACINA |
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EP1863778B1 (en) * | 2005-03-31 | 2015-12-30 | Merck Sharp & Dohme Corp. | Spirocyclic thrombin receptor antagonists |
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TW200812619A (en) * | 2006-04-06 | 2008-03-16 | Schering Corp | TRA combination therapies |
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KR20090031544A (ko) * | 2006-06-29 | 2009-03-26 | 쉐링 코포레이션 | 치환된 비사이클릭 및 트리사이클릭 트롬빈 수용체 길항제 |
AR061727A1 (es) * | 2006-06-30 | 2008-09-17 | Schering Corp | Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato |
TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
DE102006036023A1 (de) | 2006-08-02 | 2008-02-07 | Sanofi-Aventis | Imino-imidazo-pyridinderivate mit antithrombotischer Aktivität |
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JP2010505842A (ja) * | 2006-10-04 | 2010-02-25 | シェーリング コーポレイション | トロンビン受容体拮抗薬としての二環式誘導体および三環式誘導体 |
AU2007320029A1 (en) * | 2006-10-04 | 2008-05-22 | Schering Corporation | Thrombin receptor antagonists based on the modified tricyclic unit of himbacine |
WO2008079260A2 (en) * | 2006-12-22 | 2008-07-03 | Schering Corporation | Disintegration promoters in solid dose wet granulation formulations |
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PT2240487E (pt) | 2008-02-05 | 2012-03-08 | Sanofi Sa | Triazolopiridazinas como inibidores do par1, sua preparação e utilização como produtos farmacêuticos |
ES2553588T3 (es) | 2008-02-05 | 2015-12-10 | Sanofi | Sales de triazolio como inhibidores de PAR1, su preparación y uso como medicamento |
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CN102099340A (zh) | 2008-05-19 | 2011-06-15 | 先灵公司 | 作为因子ixa抑制剂的杂环化合物 |
PL2438060T3 (pl) * | 2009-06-04 | 2014-03-31 | Merck Sharp & Dohme | Aktywny metabolit antagonisty receptora trombiny |
EP2440191A2 (en) | 2009-06-08 | 2012-04-18 | Schering Corporation | A thrombin receptor antagonist and clopidogrel fixed dose tablet |
AR077695A1 (es) | 2009-08-04 | 2011-09-14 | Schering Corp | Derivados de pirimidina como inhibidores del factor ixa |
WO2011128421A1 (de) | 2010-04-16 | 2011-10-20 | Sanofi | Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren |
ES2527535T3 (es) | 2010-04-16 | 2015-01-26 | Sanofi | Piridil-vinil-pirazolo-quinolinas como inhibidores de PAR1 |
KR101303348B1 (ko) | 2010-06-25 | 2013-09-03 | 한국화학연구원 | 트롬빈 수용체 길항제인 [6+5]접합 바이사이클, 그의 제조방법 및 그를 포함하는 약제학적 조성물 |
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FR3090317B1 (fr) | 2018-12-19 | 2021-05-07 | Cvasthera | Utilisation d’un antagoniste de par-1 pour le traitement d’une maladie inflammatoire chronique intestinale |
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US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
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FR3134314A1 (fr) | 2022-04-08 | 2023-10-13 | Cvasthera | Composition pharmaceutique à base de vorapaxar et son utilisation pour le traitement des maladies inflammatoires intestinales |
Family Cites Families (10)
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FR2623810B2 (fr) | 1987-02-17 | 1992-01-24 | Sanofi Sa | Sels de l'alpha-(tetrahydro-4,5,6,7 thieno(3,2-c) pyridyl-5) (chloro-2 phenyl) -acetate de methyle dextrogyre et compositions pharmaceutiques en contenant |
IL106197A (en) | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
US5576328A (en) | 1994-01-31 | 1996-11-19 | Elf Sanofi | Method for the secondary prevention of ischemic events |
US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
ATE266025T1 (de) * | 1997-11-25 | 2004-05-15 | Schering Corp | Thrombin-rezeptor antagonisten |
FR2779726B1 (fr) | 1998-06-15 | 2001-05-18 | Sanofi Sa | Forme polymorphe de l'hydrogenosulfate de clopidogrel |
US20040192753A1 (en) | 2000-06-15 | 2004-09-30 | Samuel Chackalamannil | Methods of use of thrombin receptor antagonists |
US7488742B2 (en) | 2000-06-15 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
US6645987B2 (en) * | 2000-06-15 | 2003-11-11 | Schering Corporation | Nor-seco himbacine derivatives useful as thrombin receptor antagonists |
PL371948A1 (en) | 2001-10-18 | 2005-07-11 | Schering Corporation | Himbacine analogues as thrombin receptor antagonists |
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