ZA200407418B - Certain 1-(D-cyclopropylglycinyl)-4-(pipridin-4-yl)piperazine compounds as inhibitors of the serine protease factor Xa. - Google Patents
Certain 1-(D-cyclopropylglycinyl)-4-(pipridin-4-yl)piperazine compounds as inhibitors of the serine protease factor Xa. Download PDFInfo
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- ZA200407418B ZA200407418B ZA200407418A ZA200407418A ZA200407418B ZA 200407418 B ZA200407418 B ZA 200407418B ZA 200407418 A ZA200407418 A ZA 200407418A ZA 200407418 A ZA200407418 A ZA 200407418A ZA 200407418 B ZA200407418 B ZA 200407418B
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- South Africa
- Prior art keywords
- compound
- formula
- composition
- cyclopropylglycinyl
- pharmaceutically acceptable
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- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000002024 ethyl acetate extract Substances 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000003527 fibrinolytic agent Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 230000005802 health problem Effects 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- CVVIJWRCGSYCMB-UHFFFAOYSA-N hydron;piperazine;dichloride Chemical compound Cl.Cl.C1CNCCN1 CVVIJWRCGSYCMB-UHFFFAOYSA-N 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 1
- 235000019341 magnesium sulphate Nutrition 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 238000001819 mass spectrum Methods 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 150000004682 monohydrates Chemical class 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 230000014508 negative regulation of coagulation Effects 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 125000006503 p-nitrobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1[N+]([O-])=O)C([H])([H])* 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- AUYNWRLEXAPZAJ-UHFFFAOYSA-N piperazine;trihydrochloride Chemical compound Cl.Cl.Cl.C1CNCCN1 AUYNWRLEXAPZAJ-UHFFFAOYSA-N 0.000 description 1
- 125000004193 piperazinyl group Chemical class 0.000 description 1
- 229940012957 plasmin Drugs 0.000 description 1
- CHKVPAROMQMJNQ-UHFFFAOYSA-M potassium bisulfate Chemical compound [K+].OS([O-])(=O)=O CHKVPAROMQMJNQ-UHFFFAOYSA-M 0.000 description 1
- 229910000343 potassium bisulfate Inorganic materials 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000012289 standard assay Methods 0.000 description 1
- 238000005556 structure-activity relationship Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical group C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 description 1
- 229960003766 thrombin (human) Drugs 0.000 description 1
- 239000003868 thrombin inhibitor Substances 0.000 description 1
- 229960000103 thrombolytic agent Drugs 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 231100000583 toxicological profile Toxicity 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 229940038773 trisodium citrate Drugs 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 210000005166 vasculature Anatomy 0.000 description 1
Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36852302P | 2002-04-01 | 2002-04-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200407418B true ZA200407418B (en) | 2005-09-15 |
Family
ID=28791889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200407418A ZA200407418B (en) | 2002-04-01 | 2004-09-15 | Certain 1-(D-cyclopropylglycinyl)-4-(pipridin-4-yl)piperazine compounds as inhibitors of the serine protease factor Xa. |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7166606B2 (ja) |
| EP (1) | EP1492767B1 (ja) |
| JP (1) | JP2005531529A (ja) |
| KR (1) | KR20040094892A (ja) |
| CN (1) | CN1288135C (ja) |
| AT (1) | ATE303990T1 (ja) |
| AU (1) | AU2003218147A1 (ja) |
| BR (1) | BR0308870A (ja) |
| CA (1) | CA2478340A1 (ja) |
| CR (1) | CR7497A (ja) |
| DE (1) | DE60301569T2 (ja) |
| DK (1) | DK1492767T3 (ja) |
| EA (1) | EA007300B1 (ja) |
| EC (1) | ECSP045329A (ja) |
| ES (1) | ES2248737T3 (ja) |
| HK (1) | HK1070363A1 (ja) |
| HR (1) | HRP20040900B1 (ja) |
| IL (1) | IL164018A0 (ja) |
| MX (1) | MXPA04009640A (ja) |
| NO (1) | NO20044688L (ja) |
| NZ (1) | NZ535402A (ja) |
| PL (1) | PL373066A1 (ja) |
| UA (1) | UA76849C2 (ja) |
| WO (1) | WO2003084929A1 (ja) |
| ZA (1) | ZA200407418B (ja) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6834308B1 (en) | 2000-02-17 | 2004-12-21 | Audible Magic Corporation | Method and apparatus for identifying media content presented on a media playing device |
| EP1490767B1 (en) | 2001-04-05 | 2014-06-11 | Audible Magic Corporation | Copyright detection and protection system and method |
| US8972481B2 (en) | 2001-07-20 | 2015-03-03 | Audible Magic, Inc. | Playlist generation method and apparatus |
| DE102014108210A1 (de) | 2014-06-11 | 2015-12-17 | Dietrich Gulba | Rodentizid |
| EP3541381B1 (en) | 2016-11-18 | 2022-12-28 | Merck Sharp & Dohme LLC | Inhibitors of factor xiia |
| EP4070658A1 (de) | 2021-04-06 | 2022-10-12 | BIORoxx GmbH | Verwendung von blutgerinnungshemmenden verbindungen als rodentizide |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1009758B1 (en) | 1997-08-29 | 2005-06-01 | Tularik Limited | Meta-benzamidine derivatives as serine protease inhibitors |
| AU5413600A (en) | 1999-06-14 | 2001-01-02 | Eli Lilly And Company | Compounds |
| CA2375920A1 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Compounds |
| GB0030306D0 (en) | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| GB0030304D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| GB0030303D0 (en) | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| GB0030305D0 (en) | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| TWI257389B (en) | 2001-06-12 | 2006-07-01 | Lilly Co Eli | Pharmaceutical compound |
| ES2298386T3 (es) * | 2001-07-26 | 2008-05-16 | Eli Lilly And Company | 1-glicinil-4-(1-metilpiperidin-4-il)piperazinas y -piperidinas como antagonistas del factor xa. |
-
2003
- 2003-03-24 CA CA002478340A patent/CA2478340A1/en not_active Abandoned
- 2003-03-24 KR KR10-2004-7015486A patent/KR20040094892A/ko not_active Application Discontinuation
- 2003-03-24 IL IL16401803A patent/IL164018A0/xx unknown
- 2003-03-24 DK DK03714138T patent/DK1492767T3/da active
- 2003-03-24 AU AU2003218147A patent/AU2003218147A1/en not_active Abandoned
- 2003-03-24 JP JP2003582128A patent/JP2005531529A/ja active Pending
- 2003-03-24 US US10/486,138 patent/US7166606B2/en not_active Expired - Fee Related
- 2003-03-24 MX MXPA04009640A patent/MXPA04009640A/es active IP Right Grant
- 2003-03-24 UA UA20041008649A patent/UA76849C2/uk unknown
- 2003-03-24 NZ NZ535402A patent/NZ535402A/en unknown
- 2003-03-24 BR BR0308870-7A patent/BR0308870A/pt not_active IP Right Cessation
- 2003-03-24 EA EA200401290A patent/EA007300B1/ru not_active IP Right Cessation
- 2003-03-24 CN CNB038074141A patent/CN1288135C/zh not_active Expired - Fee Related
- 2003-03-24 AT AT03714138T patent/ATE303990T1/de not_active IP Right Cessation
- 2003-03-24 DE DE60301569T patent/DE60301569T2/de not_active Expired - Fee Related
- 2003-03-24 PL PL03373066A patent/PL373066A1/xx unknown
- 2003-03-24 ES ES03714138T patent/ES2248737T3/es not_active Expired - Lifetime
- 2003-03-24 EP EP03714138A patent/EP1492767B1/en not_active Expired - Lifetime
- 2003-03-24 WO PCT/US2003/007794 patent/WO2003084929A1/en active IP Right Grant
-
2004
- 2004-09-15 ZA ZA200407418A patent/ZA200407418B/en unknown
- 2004-09-24 CR CR7497A patent/CR7497A/es unknown
- 2004-09-29 EC EC2004005329A patent/ECSP045329A/es unknown
- 2004-09-30 HR HR20040900A patent/HRP20040900B1/xx not_active IP Right Cessation
- 2004-10-29 NO NO20044688A patent/NO20044688L/no not_active Application Discontinuation
-
2005
- 2005-04-11 HK HK05103052A patent/HK1070363A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| NZ535402A (en) | 2006-02-24 |
| ES2248737T3 (es) | 2006-03-16 |
| ECSP045329A (es) | 2004-11-26 |
| NO20044688L (no) | 2004-10-29 |
| EA007300B1 (ru) | 2006-08-25 |
| WO2003084929A8 (en) | 2004-05-21 |
| AU2003218147A1 (en) | 2003-10-20 |
| ATE303990T1 (de) | 2005-09-15 |
| WO2003084929A1 (en) | 2003-10-16 |
| BR0308870A (pt) | 2005-01-04 |
| UA76849C2 (uk) | 2006-09-15 |
| CN1642914A (zh) | 2005-07-20 |
| IL164018A0 (en) | 2005-12-18 |
| US20050096328A1 (en) | 2005-05-05 |
| DE60301569D1 (de) | 2005-10-13 |
| EA200401290A1 (ru) | 2005-02-24 |
| KR20040094892A (ko) | 2004-11-10 |
| MXPA04009640A (es) | 2005-01-11 |
| JP2005531529A (ja) | 2005-10-20 |
| HRP20040900A2 (en) | 2004-12-31 |
| EP1492767A1 (en) | 2005-01-05 |
| DE60301569T2 (de) | 2006-06-14 |
| PL373066A1 (en) | 2005-08-08 |
| CA2478340A1 (en) | 2003-10-16 |
| CN1288135C (zh) | 2006-12-06 |
| EP1492767B1 (en) | 2005-09-07 |
| DK1492767T3 (da) | 2005-11-28 |
| HRP20040900B1 (en) | 2006-02-28 |
| US7166606B2 (en) | 2007-01-23 |
| HK1070363A1 (en) | 2005-06-17 |
| CR7497A (es) | 2005-01-17 |
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