ZA200404147B - Pyrrolidine-2-ones as factor Xa inhibitors. - Google Patents
Pyrrolidine-2-ones as factor Xa inhibitors. Download PDFInfo
- Publication number
- ZA200404147B ZA200404147B ZA200404147A ZA200404147A ZA200404147B ZA 200404147 B ZA200404147 B ZA 200404147B ZA 200404147 A ZA200404147 A ZA 200404147A ZA 200404147 A ZA200404147 A ZA 200404147A ZA 200404147 B ZA200404147 B ZA 200404147B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- halogen
- optionally substituted
- heteroatom
- hydrogen
- Prior art date
Links
- 229940123583 Factor Xa inhibitor Drugs 0.000 title claims description 10
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical class O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims description 76
- 229910052736 halogen Inorganic materials 0.000 claims description 58
- 125000005842 heteroatom Chemical group 0.000 claims description 53
- 229910052760 oxygen Inorganic materials 0.000 claims description 45
- 229910052717 sulfur Inorganic materials 0.000 claims description 45
- 229910052739 hydrogen Inorganic materials 0.000 claims description 42
- 239000001257 hydrogen Substances 0.000 claims description 40
- 229910052757 nitrogen Inorganic materials 0.000 claims description 33
- 150000001875 compounds Chemical class 0.000 claims description 28
- 150000002367 halogens Chemical class 0.000 claims description 27
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 25
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 23
- -1 substituent halogen Chemical class 0.000 claims description 21
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000004450 alkenylene group Chemical group 0.000 claims description 13
- 125000002947 alkylene group Chemical group 0.000 claims description 13
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 11
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 11
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims description 11
- 150000002431 hydrogen Chemical class 0.000 claims description 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 11
- 125000001424 substituent group Chemical group 0.000 claims description 10
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 238000002560 therapeutic procedure Methods 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- XFGMPZRFMGBTDI-POFDKVPJSA-N (2s)-n-[(2s)-1-[[(2s)-1-[(2s)-2-[[2-[[(2s)-1-amino-3-(1h-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2s)-4-methyl-2-[[(2s)-5-oxopyrrolidine-2-carbonyl]amino]pe Chemical compound N([C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(N)=O)C(=O)[C@@H]1CCC(=O)N1 XFGMPZRFMGBTDI-POFDKVPJSA-N 0.000 claims 1
- 101800001365 Red pigment-concentrating hormone Proteins 0.000 claims 1
- XFGMPZRFMGBTDI-UHFFFAOYSA-N p-Glu-Leu-Asn-Phe-Ser-Pro-Gly-Trp-NH2 Natural products C=1C=CC=CC=1CC(C(=O)NC(CO)C(=O)N1C(CCC1)C(=O)NCC(=O)NC(CC=1C2=CC=CC=C2NC=1)C(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CC(C)C)NC(=O)C1CCC(=O)N1 XFGMPZRFMGBTDI-UHFFFAOYSA-N 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 description 5
- 229960004072 thrombin Drugs 0.000 description 5
- 102000009123 Fibrin Human genes 0.000 description 4
- 108010073385 Fibrin Proteins 0.000 description 4
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- 208000007536 Thrombosis Diseases 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 229950003499 fibrin Drugs 0.000 description 4
- 210000005166 vasculature Anatomy 0.000 description 4
- 230000001154 acute effect Effects 0.000 description 3
- 239000003146 anticoagulant agent Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 3
- 206010002388 Angina unstable Diseases 0.000 description 2
- 208000005189 Embolism Diseases 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108010074860 Factor Xa Proteins 0.000 description 2
- 206010027476 Metastases Diseases 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 208000010378 Pulmonary Embolism Diseases 0.000 description 2
- 208000007814 Unstable Angina Diseases 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 230000015271 coagulation Effects 0.000 description 2
- 238000005345 coagulation Methods 0.000 description 2
- 238000007887 coronary angioplasty Methods 0.000 description 2
- 229940088598 enzyme Drugs 0.000 description 2
- 239000003527 fibrinolytic agent Substances 0.000 description 2
- 201000004332 intermediate coronary syndrome Diseases 0.000 description 2
- 230000009401 metastasis Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 2
- 229960000103 thrombolytic agent Drugs 0.000 description 2
- 230000002537 thrombolytic effect Effects 0.000 description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 208000031104 Arterial Occlusive disease Diseases 0.000 description 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 description 1
- 206010003658 Atrial Fibrillation Diseases 0.000 description 1
- 108010039209 Blood Coagulation Factors Proteins 0.000 description 1
- 102000015081 Blood Coagulation Factors Human genes 0.000 description 1
- 108010017384 Blood Proteins Proteins 0.000 description 1
- 102000004506 Blood Proteins Human genes 0.000 description 1
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 1
- 206010053567 Coagulopathies Diseases 0.000 description 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 description 1
- 102000005927 Cysteine Proteases Human genes 0.000 description 1
- 108010005843 Cysteine Proteases Proteins 0.000 description 1
- 206010051055 Deep vein thrombosis Diseases 0.000 description 1
- 108010049003 Fibrinogen Proteins 0.000 description 1
- 102000008946 Fibrinogen Human genes 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 206010053159 Organ failure Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 108010094028 Prothrombin Proteins 0.000 description 1
- 102100027378 Prothrombin Human genes 0.000 description 1
- 206010040070 Septic Shock Diseases 0.000 description 1
- 208000001435 Thromboembolism Diseases 0.000 description 1
- 208000032109 Transient ischaemic attack Diseases 0.000 description 1
- 206010047249 Venous thrombosis Diseases 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 206010000891 acute myocardial infarction Diseases 0.000 description 1
- 229940127090 anticoagulant agent Drugs 0.000 description 1
- 208000021328 arterial occlusion Diseases 0.000 description 1
- 210000005249 arterial vasculature Anatomy 0.000 description 1
- 230000001164 bioregulatory effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000023555 blood coagulation Effects 0.000 description 1
- 208000015294 blood coagulation disease Diseases 0.000 description 1
- 239000003114 blood coagulation factor Substances 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 208000002528 coronary thrombosis Diseases 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 210000003414 extremity Anatomy 0.000 description 1
- 229940012952 fibrinogen Drugs 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 230000003176 fibrotic effect Effects 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 230000023597 hemostasis Effects 0.000 description 1
- 230000002439 hemostatic effect Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 210000002241 neurite Anatomy 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 229940039716 prothrombin Drugs 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000001732 thrombotic effect Effects 0.000 description 1
- 201000010875 transient cerebral ischemia Diseases 0.000 description 1
- 108010036927 trypsin-like serine protease Proteins 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—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
- C07D207/18—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
- 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
- A61P9/06—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
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D405/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyrrole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0130705.7A GB0130705D0 (en) | 2001-12-21 | 2001-12-21 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200404147B true ZA200404147B (en) | 2005-06-21 |
Family
ID=9928210
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200404147A ZA200404147B (en) | 2001-12-21 | 2004-05-27 | Pyrrolidine-2-ones as factor Xa inhibitors. |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20050059726A1 (https=) |
| EP (1) | EP1456172A1 (https=) |
| JP (1) | JP2005519885A (https=) |
| KR (1) | KR20040072666A (https=) |
| CN (1) | CN100364971C (https=) |
| AR (1) | AR037928A1 (https=) |
| AU (1) | AU2002366747A1 (https=) |
| BR (1) | BR0215200A (https=) |
| CA (1) | CA2471461A1 (https=) |
| CO (1) | CO5590896A2 (https=) |
| GB (1) | GB0130705D0 (https=) |
| HU (1) | HUP0500137A2 (https=) |
| IL (1) | IL162454A0 (https=) |
| IS (1) | IS7316A (https=) |
| MX (1) | MXPA04006139A (https=) |
| MY (1) | MY141579A (https=) |
| NO (1) | NO20042990L (https=) |
| NZ (1) | NZ533129A (https=) |
| PL (1) | PL371008A1 (https=) |
| RU (1) | RU2318807C2 (https=) |
| TW (1) | TWI262075B (https=) |
| WO (1) | WO2003053925A1 (https=) |
| ZA (1) | ZA200404147B (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200307667A (en) | 2002-05-06 | 2003-12-16 | Bristol Myers Squibb Co | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
| JP2006527732A (ja) | 2003-06-19 | 2006-12-07 | グラクソ グループ リミテッド | Ｘａ因子の阻害剤としての３−スルホニルアミノ−ピロリジン−２−オン誘導体 |
| GB0314373D0 (en) | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| GB0314299D0 (en) | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| GB0314370D0 (en) * | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| US7169795B2 (en) * | 2003-09-30 | 2007-01-30 | Bristol Myers Squibb Company | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
| PE20060574A1 (es) * | 2004-07-28 | 2006-06-24 | Glaxo Group Ltd | Derivados de arilpiperazina sulfonamida como agonistas de los receptores de secretagogos de la hormona del crecimiento (ghs) |
| DE102004062544A1 (de) * | 2004-12-24 | 2006-07-06 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue substituierte Pyrrolidinone, deren Herstellung und deren Verewendung als Arzneimittel |
| DE102005008649A1 (de) * | 2005-02-25 | 2006-09-07 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue substituierte Pyrrolidinone, deren Herstellung und deren Verwendung als Arzneimittel |
| US20090099231A1 (en) * | 2005-04-11 | 2009-04-16 | John David Harling | 3-Sulfonylamino-Pyrrolidine-2-One Derivatives as Factor Xa Inhibitors |
| EP1894930A4 (en) | 2005-06-23 | 2010-06-23 | Kyowa Hakko Kirin Co Ltd | THIAZOLE DERIVATIVE |
| US7928098B2 (en) | 2005-08-02 | 2011-04-19 | Kyowa Hakko Kirin Co., Ltd. | Therapeutic and/or preventive agents for a sleep disorder |
| US7622492B2 (en) | 2005-08-31 | 2009-11-24 | Hoffmann-La Roche Inc. | Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase |
| EP1951712A2 (en) * | 2005-11-24 | 2008-08-06 | Glaxo Group Limited | Chemical compounds |
| ES2379989T3 (es) | 2006-04-07 | 2012-05-07 | Bactiguard Ab | Sustratos antimicrobianos novedosos y usos de los mismos |
| CA2662574A1 (en) * | 2006-09-22 | 2008-03-27 | Novartis Ag | Heterocyclic organic compounds |
| CN116003280B (zh) * | 2022-12-30 | 2024-11-19 | 合肥工业大学 | 一种芳基甲酰胺类化合物的光化学合成方法 |
| CN116712596A (zh) * | 2023-05-30 | 2023-09-08 | 北京福爱乐科技发展有限公司 | 一种用于体内创面喷涂型医用胶及其制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5202344A (en) * | 1990-12-11 | 1993-04-13 | G. D. Searle & Co. | N-substituted lactams useful as cholecystokinin antagonists |
| EP1384725A3 (en) * | 1994-04-26 | 2007-02-21 | Aventis Pharmaceuticals Inc. | Factor Xa inhibitors |
| US6034093A (en) * | 1995-06-07 | 2000-03-07 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds |
| US5731315A (en) * | 1995-06-07 | 1998-03-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Substituted sulfonic acid n- (aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds |
| DE69718194T2 (de) * | 1996-08-16 | 2003-10-16 | Bristol-Myers Squibb Pharma Co., Wilmington | Amidinophenyl-pyrrolidine, -pyrroline und -isoxazolidine und ihre derivate |
| GB9715894D0 (en) * | 1997-07-29 | 1997-10-01 | Zeneca Ltd | Heterocyclic derivatives |
| US6403632B1 (en) * | 2000-03-01 | 2002-06-11 | Bristol Myers Squibb Pharma Co | Lactam metalloprotease inhibitors |
| US6025358A (en) * | 1998-06-11 | 2000-02-15 | G. D. Searle & Co. | Double prodrugs of potent GP IIb/IIIa antagonists |
| GB0114005D0 (en) * | 2001-06-08 | 2001-08-01 | Glaxo Group Ltd | Chemical compounds |
| TW200307667A (en) * | 2002-05-06 | 2003-12-16 | Bristol Myers Squibb Co | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
| US7169795B2 (en) * | 2003-09-30 | 2007-01-30 | Bristol Myers Squibb Company | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
-
2001
- 2001-12-21 GB GBGB0130705.7A patent/GB0130705D0/en not_active Ceased
-
2002
- 2002-12-19 AR ARP020105014A patent/AR037928A1/es not_active Application Discontinuation
- 2002-12-19 TW TW091136597A patent/TWI262075B/zh not_active IP Right Cessation
- 2002-12-19 MY MYPI20024789A patent/MY141579A/en unknown
- 2002-12-20 JP JP2003554642A patent/JP2005519885A/ja active Pending
- 2002-12-20 RU RU2004122427/04A patent/RU2318807C2/ru not_active IP Right Cessation
- 2002-12-20 US US10/499,529 patent/US20050059726A1/en not_active Abandoned
- 2002-12-20 EP EP02805350A patent/EP1456172A1/en not_active Withdrawn
- 2002-12-20 NZ NZ533129A patent/NZ533129A/en unknown
- 2002-12-20 WO PCT/EP2002/014826 patent/WO2003053925A1/en not_active Ceased
- 2002-12-20 AU AU2002366747A patent/AU2002366747A1/en not_active Abandoned
- 2002-12-20 CA CA002471461A patent/CA2471461A1/en not_active Abandoned
- 2002-12-20 IL IL16245402A patent/IL162454A0/xx unknown
- 2002-12-20 KR KR10-2004-7009675A patent/KR20040072666A/ko not_active Ceased
- 2002-12-20 MX MXPA04006139A patent/MXPA04006139A/es active IP Right Grant
- 2002-12-20 BR BR0215200-2A patent/BR0215200A/pt not_active IP Right Cessation
- 2002-12-20 HU HU0500137A patent/HUP0500137A2/hu unknown
- 2002-12-20 PL PL02371008A patent/PL371008A1/xx not_active Application Discontinuation
- 2002-12-20 CN CNB028282248A patent/CN100364971C/zh not_active Expired - Fee Related
-
2004
- 2004-05-27 ZA ZA200404147A patent/ZA200404147B/en unknown
- 2004-06-16 IS IS7316A patent/IS7316A/is unknown
- 2004-06-18 CO CO04057414A patent/CO5590896A2/es not_active Application Discontinuation
- 2004-07-13 NO NO20042990A patent/NO20042990L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AR037928A1 (es) | 2004-12-22 |
| CN100364971C (zh) | 2008-01-30 |
| WO2003053925A1 (en) | 2003-07-03 |
| NZ533129A (en) | 2006-12-22 |
| IS7316A (is) | 2004-06-16 |
| US20050059726A1 (en) | 2005-03-17 |
| TW200306178A (en) | 2003-11-16 |
| JP2005519885A (ja) | 2005-07-07 |
| CN1620434A (zh) | 2005-05-25 |
| RU2004122427A (ru) | 2006-01-20 |
| KR20040072666A (ko) | 2004-08-18 |
| HUP0500137A2 (en) | 2006-02-28 |
| BR0215200A (pt) | 2004-10-13 |
| TWI262075B (en) | 2006-09-21 |
| CO5590896A2 (es) | 2005-12-30 |
| GB0130705D0 (en) | 2002-02-06 |
| IL162454A0 (en) | 2005-11-20 |
| CA2471461A1 (en) | 2003-07-03 |
| RU2318807C2 (ru) | 2008-03-10 |
| MY141579A (en) | 2010-05-14 |
| NO20042990L (no) | 2004-09-20 |
| MXPA04006139A (es) | 2004-11-01 |
| EP1456172A1 (en) | 2004-09-15 |
| AU2002366747A1 (en) | 2003-07-09 |
| PL371008A1 (en) | 2005-06-13 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200404147B (en) | Pyrrolidine-2-ones as factor Xa inhibitors. | |
| US20250051303A1 (en) | Substituted oxopyridine derivatives for the treatment and/or prophylaxis of thrombotic or thromboembolic disorders and/or thrombotic or thromboembolic complications | |
| US20040067938A1 (en) | Quaternary amines and related inhibitors of factor xa | |
| EE200300306A (et) | Oksübensamiidi derivaadid, nende valmistamine ja kasutamine Xa-teguri inhibiitoritena ning neid sisaldav ravimpreparaat | |
| MEP43008A (en) | Indole-2-carboxamides as factor xa inhibitors | |
| JP2003500386A (ja) | Ｘａ因子阻害剤 | |
| AU784426B2 (en) | Tissue factor antagonists and methods of use thereof | |
| RU2125450C1 (ru) | Применение 2-фенил-3-ароилбензотиофенов для увеличения экспрессии тромбомодулина | |
| MX2007010682A (es) | Derivados del acido 2-[isoquinolin-s-carbonil)amino]-propionico como inhibidores de los factores xi y ix para el tratamiento de la trombosis. | |
| CL2004001080A1 (es) | COMPUESTOS DERIVADOS DE INDAZOL, INHIBIDORES DEL FACTOR Xa, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION, UTILES PARA PREPARAR UN MEDICAMENTO PARA TRATAR INFARTO DE MIOCARDIO AGUDO, TRASTORNOS CARDIOVASCULARES, APOPLEJIA Y OTRAS. | |
| ZA200303847B (en) | Guanidine and amidine derivatives as factor XA inhibitors. | |
| AU6264699A (en) | Pharmaceutically active compounds and methods of use thereof | |
| KR20090128581A (ko) | 혈전증 병상을 치료하고 예방하기 위한 디오스메틴 유도체 | |
| PL201793B1 (pl) | Zestaw leczniczy, sposób wytwarzania tego zestawu, preparat farmaceutyczny i zastosowania takiego zestawu leczniczego i preparatu farmaceutycznego | |
| US5089634A (en) | Isocoumarins with cationic substituents | |
| ZA200309367B (en) | Pyrrolidine derivatives as factor Xa inhibitors. | |
| US20080051388A1 (en) | Novel Compounds That Inhibit Factor Xa Activity | |
| US5932603A (en) | Thrombolytic agents | |
| KOSAKI et al. | Application of a Synthetic Serine Protease Inhibitor in the | |
| EP0811377A1 (en) | Thrombolytic agent | |
| Mayweg | Synthesis of Novel Anticoagulants | |
| JPWO1996020706A1 (ja) | 血栓溶解薬 | |
| ZA200407903B (en) | Semicarbazide derivatives and their use as antithrombotics. | |
| CA2209619A1 (en) | Thrombolytic agents |