ZA200106337B - Heterocyclic derivatives as inhibitors of Factor Xa. - Google Patents
Heterocyclic derivatives as inhibitors of Factor Xa. Download PDFInfo
- Publication number
- ZA200106337B ZA200106337B ZA200106337A ZA200106337A ZA200106337B ZA 200106337 B ZA200106337 B ZA 200106337B ZA 200106337 A ZA200106337 A ZA 200106337A ZA 200106337 A ZA200106337 A ZA 200106337A ZA 200106337 B ZA200106337 B ZA 200106337B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- compound
- formula
- hydroxy
- carboxy
- Prior art date
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- 125000000623 heterocyclic group Chemical group 0.000 title claims description 24
- 108010074860 Factor Xa Proteins 0.000 title claims description 21
- 239000003112 inhibitor Substances 0.000 title description 6
- -1 trifluromethy] Chemical group 0.000 claims description 100
- 150000001875 compounds Chemical class 0.000 claims description 72
- 125000000217 alkyl group Chemical group 0.000 claims description 54
- 238000000034 method Methods 0.000 claims description 30
- 239000001257 hydrogen Substances 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 16
- 125000003282 alkyl amino group Chemical group 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 9
- 230000002401 inhibitory effect Effects 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
- 239000001301 oxygen Substances 0.000 claims description 8
- 241000282414 Homo sapiens Species 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 7
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 7
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 7
- 125000002947 alkylene group Chemical group 0.000 claims description 7
- 125000005842 heteroatom Chemical group 0.000 claims description 7
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 5
- 125000003302 alkenyloxy group Chemical group 0.000 claims description 5
- 125000004414 alkyl thio group Chemical group 0.000 claims description 5
- 125000005133 alkynyloxy group Chemical group 0.000 claims description 5
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 5
- 238000002560 therapeutic procedure Methods 0.000 claims description 5
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 239000005864 Sulphur Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 3
- 125000005236 alkanoylamino group Chemical group 0.000 claims description 3
- 125000001589 carboacyl group Chemical group 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 3
- 150000002431 hydrogen Chemical group 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 3
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 3
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims description 3
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- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 5
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/435—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
- 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
-
- 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
- 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
- A61P9/10—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9902989.4A GB9902989D0 (en) | 1999-02-11 | 1999-02-11 | Heterocyclic derivatives |
Publications (1)
Publication Number | Publication Date |
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ZA200106337B true ZA200106337B (en) | 2002-11-01 |
Family
ID=10847476
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ZA200106337A ZA200106337B (en) | 1999-02-11 | 2001-08-01 | Heterocyclic derivatives as inhibitors of Factor Xa. |
Country Status (24)
Country | Link |
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US (1) | US6723723B1 (hu) |
EP (1) | EP1150974B1 (hu) |
JP (1) | JP2002536443A (hu) |
KR (1) | KR20010102072A (hu) |
AT (1) | ATE223402T1 (hu) |
AU (1) | AU757738B2 (hu) |
BR (1) | BR0008130A (hu) |
CA (1) | CA2362392A1 (hu) |
CZ (1) | CZ20012867A3 (hu) |
DE (1) | DE60000410T2 (hu) |
DK (1) | DK1150974T3 (hu) |
ES (1) | ES2181637T3 (hu) |
GB (1) | GB9902989D0 (hu) |
HU (1) | HUP0105102A3 (hu) |
IL (1) | IL144792A0 (hu) |
NO (1) | NO20013921L (hu) |
NZ (1) | NZ513350A (hu) |
PL (1) | PL349220A1 (hu) |
PT (1) | PT1150974E (hu) |
RU (1) | RU2226193C2 (hu) |
SK (1) | SK11462001A3 (hu) |
TR (1) | TR200102306T2 (hu) |
WO (1) | WO2000047573A1 (hu) |
ZA (1) | ZA200106337B (hu) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL115420A0 (en) | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
TWI290136B (en) | 2000-04-05 | 2007-11-21 | Daiichi Seiyaku Co | Ethylenediamine derivatives |
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-
1999
- 1999-02-11 GB GBGB9902989.4A patent/GB9902989D0/en not_active Ceased
-
2000
- 2000-02-08 ES ES00902725T patent/ES2181637T3/es not_active Expired - Lifetime
- 2000-02-08 TR TR2001/02306T patent/TR200102306T2/xx unknown
- 2000-02-08 DE DE60000410T patent/DE60000410T2/de not_active Expired - Lifetime
- 2000-02-08 JP JP2000598493A patent/JP2002536443A/ja active Pending
- 2000-02-08 AU AU24470/00A patent/AU757738B2/en not_active Ceased
- 2000-02-08 WO PCT/GB2000/000354 patent/WO2000047573A1/en not_active Application Discontinuation
- 2000-02-08 US US09/913,071 patent/US6723723B1/en not_active Expired - Fee Related
- 2000-02-08 KR KR1020017010184A patent/KR20010102072A/ko not_active Application Discontinuation
- 2000-02-08 CA CA002362392A patent/CA2362392A1/en not_active Abandoned
- 2000-02-08 EP EP00902725A patent/EP1150974B1/en not_active Expired - Lifetime
- 2000-02-08 DK DK00902725T patent/DK1150974T3/da active
- 2000-02-08 SK SK1146-2001A patent/SK11462001A3/sk unknown
- 2000-02-08 NZ NZ513350A patent/NZ513350A/xx unknown
- 2000-02-08 AT AT00902725T patent/ATE223402T1/de active
- 2000-02-08 IL IL14479200A patent/IL144792A0/xx unknown
- 2000-02-08 BR BR0008130-2A patent/BR0008130A/pt not_active IP Right Cessation
- 2000-02-08 HU HU0105102A patent/HUP0105102A3/hu unknown
- 2000-02-08 PL PL00349220A patent/PL349220A1/xx not_active Application Discontinuation
- 2000-02-08 RU RU2001124855/04A patent/RU2226193C2/ru not_active IP Right Cessation
- 2000-02-08 PT PT00902725T patent/PT1150974E/pt unknown
- 2000-02-08 CZ CZ20012867A patent/CZ20012867A3/cs unknown
-
2001
- 2001-08-01 ZA ZA200106337A patent/ZA200106337B/en unknown
- 2001-08-10 NO NO20013921A patent/NO20013921L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
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AU757738B2 (en) | 2003-03-06 |
NZ513350A (en) | 2003-01-31 |
CZ20012867A3 (cs) | 2001-10-17 |
HUP0105102A3 (en) | 2003-01-28 |
KR20010102072A (ko) | 2001-11-15 |
AU2447000A (en) | 2000-08-29 |
SK11462001A3 (sk) | 2001-12-03 |
US6723723B1 (en) | 2004-04-20 |
DK1150974T3 (da) | 2002-12-02 |
JP2002536443A (ja) | 2002-10-29 |
EP1150974A1 (en) | 2001-11-07 |
CA2362392A1 (en) | 2000-08-17 |
NO20013921L (no) | 2001-10-10 |
NO20013921D0 (no) | 2001-08-10 |
PT1150974E (pt) | 2003-01-31 |
DE60000410T2 (de) | 2003-06-05 |
RU2226193C2 (ru) | 2004-03-27 |
PL349220A1 (en) | 2002-07-01 |
BR0008130A (pt) | 2002-02-05 |
GB9902989D0 (en) | 1999-03-31 |
ES2181637T3 (es) | 2003-03-01 |
EP1150974B1 (en) | 2002-09-04 |
HUP0105102A2 (hu) | 2002-05-29 |
DE60000410D1 (de) | 2002-10-10 |
WO2000047573A1 (en) | 2000-08-17 |
ATE223402T1 (de) | 2002-09-15 |
TR200102306T2 (tr) | 2001-12-21 |
IL144792A0 (en) | 2002-06-30 |
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