HUP0200242A2 - Pyrazole-3-on-derivatives as factor xa inhibitors, pharmaceutical compositions containing them, their preparation and their use - Google Patents
Pyrazole-3-on-derivatives as factor xa inhibitors, pharmaceutical compositions containing them, their preparation and their useInfo
- Publication number
- HUP0200242A2 HUP0200242A2 HU0200242A HUP0200242A HUP0200242A2 HU P0200242 A2 HUP0200242 A2 HU P0200242A2 HU 0200242 A HU0200242 A HU 0200242A HU P0200242 A HUP0200242 A HU P0200242A HU P0200242 A2 HUP0200242 A2 HU P0200242A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- substituted
- cr7r7
- het
- naphthyl
- Prior art date
Links
- 229940123583 Factor Xa inhibitor Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000001624 naphthyl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000006267 biphenyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D413/08—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 alicyclic rings
-
- 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
- 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
- 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
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D231/08—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A találmány tárgya új (I) általános képletű vegyületek - ahol R1 és R2jelentése egymástól függetlenül hidrogénatom, A, cikloalkil-[C(R7R7')]n- vagy Ar-[C(R7R7')]n-; R3 és R4 egymástól függetlenülhidrogénatom, Ar, Het, R5, ahol a két szubsztituens közül az egyiklegalább R5-öt jelent; R5 jelentése egyszeresen -COA, Ar-[C(R7R7')]n-CO-, COOA, OH vagy szokásos amino-védőcsoporttal adott esetbenszubsztituált -C(=NH)-NH2 csoporttal, vagy -NH-C(=NH)-NH2, -CO-N=C(NH2)2 vagy a) vagy b) képletű csoporttal szubsztituált fenil-,naftil- vagy bifenilcsoport, amelyek adott esetben még szubsztituálvalehetnek egyszer vagy kétszer A, Ar', Het, OR6, NR6R6', NO2, CN, Hal,NR6COA, NR6COAr', NR6SO2A, NR6SO2Ar', COOR6, CO-NR6R6', COR7, CO-Ar',SO2NR6R6', S(O)nAr' vagy S(O)nA csoporttal; R6 és R6' jelentéseegymástól függetlenül hidrogénatom vagy A, CR7R7'-Ar' vagy CR7R7'-Het;R7 és R7' jelentése egymástól függetlenül hidrogénatom vagy A; X és Yjelentése egymástól függetlenül (CR7R7')n; A jelentése 1-20 szénatomosalkilcsoport, ahol egy vagy két metiléncsoportot oxigén- vagy kénatomés/vagy -CH=CH- csoport és/vagy 1-7 hidrogénatomot fluoratomhelyettesíthet; Ar jelentése szubsztituálatlan vagy szubsztituáltfenil-, naftil- vagy bifenil-csoport; Ar' jelentése szubsztituálatlanvagy szubsztituált fenil- vagy naftilcsoport; n értéke 0, 1 vagy 2. Avegyületek Xa faktor véralvadásgátlók és tromboembóliás betegségekmegelőzésére és/vagy gyógyítására alkalmazhatók. A találmány kiterjeda vegyületek előállítására, ezeket tartalmazó gyógyszerkészítményekreés alkalmazásukra is. ÓThe subject of the invention is new compounds of general formula (I) - where R1 and R2 are independently hydrogen atom, A, cycloalkyl-[C(R7R7')]n- or Ar-[C(R7R7')]n-; R3 and R4 independently of each other are a hydrogen atom, Ar, Het, R5, where at least one of the two substituents represents R5; R5 is -COA, Ar-[C(R7R7')]n-CO-, COOA, OH or a -C(=NH)-NH2 group optionally substituted with a conventional amino-protecting group, or -NH-C(=NH)- NH2, -CO-N=C(NH2)2 or a phenyl-, naphthyl- or biphenyl group substituted with a group of the formula a) or b), which may optionally be substituted once or twice with A, Ar', Het, OR6, NR6R6', NO2 , CN, Hal,NR6COA, NR6COAr', NR6SO2A, NR6SO2Ar', COOR6, CO-NR6R6', COR7, CO-Ar', SO2NR6R6', S(O)nAr' or S(O)nA; R6 and R6' are independently hydrogen or A, CR7R7'-Ar' or CR7R7'-Het; R7 and R7' are independently hydrogen or A; X and Y independently mean (CR7R7'); A is an alkyl group with 1-20 carbon atoms, where one or two methylene groups can be replaced by oxygen or sulfur atoms and/or -CH=CH- groups and/or 1-7 hydrogen atoms by fluorine atoms; Ar is an unsubstituted or substituted phenyl, naphthyl or biphenyl group; Ar' is unsubstituted or substituted phenyl or naphthyl; The value of n is 0, 1 or 2. The compounds can be used for the prevention and/or treatment of factor Xa anticoagulants and thromboembolic diseases. The invention also covers the production of compounds, pharmaceutical preparations containing them and their use. HE
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19909237A DE19909237A1 (en) | 1999-03-03 | 1999-03-03 | Pyrazol-3-one derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0200242A2 true HUP0200242A2 (en) | 2002-11-28 |
| HUP0200242A3 HUP0200242A3 (en) | 2002-12-28 |
Family
ID=7899522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0200242A HUP0200242A3 (en) | 1999-03-03 | 2000-02-29 | Pyrazole-3-on-derivatives as factor xa inhibitors, pharmaceutical compositions containing them, their preparation and their use |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1157010A1 (en) |
| JP (1) | JP2002538143A (en) |
| KR (1) | KR20010102428A (en) |
| CN (1) | CN1342148A (en) |
| AU (1) | AU2916500A (en) |
| BR (1) | BR0008608A (en) |
| CA (1) | CA2364908A1 (en) |
| CZ (1) | CZ20013164A3 (en) |
| DE (1) | DE19909237A1 (en) |
| HU (1) | HUP0200242A3 (en) |
| MX (1) | MXPA01008844A (en) |
| NO (1) | NO20014234L (en) |
| PL (1) | PL350941A1 (en) |
| RU (1) | RU2001126566A (en) |
| SK (1) | SK12152001A3 (en) |
| WO (1) | WO2000051989A1 (en) |
| ZA (1) | ZA200108064B (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6455525B1 (en) | 1999-11-04 | 2002-09-24 | Cephalon, Inc. | Heterocyclic substituted pyrazolones |
| JP4744149B2 (en) | 2002-12-03 | 2011-08-10 | ファーマサイクリックス インコーポレイテッド | 2- (2-Hydroxybiphenyl-3-yl) -1H-benzimidazole-5-carboxamidine derivatives as factor VIIA inhibitors |
| WO2005012255A1 (en) * | 2003-08-01 | 2005-02-10 | Mitsubishi Pharma Corporation | Remedy for inflammatory joint diseases |
| DE102008020113A1 (en) | 2008-04-23 | 2009-10-29 | Bayer Schering Pharma Aktiengesellschaft | Substituted dihydropyrazolones and their use |
| DE102005019712A1 (en) | 2005-04-28 | 2006-11-09 | Bayer Healthcare Ag | Dipyridyl-dihydropyrazolone and its use |
| DE102006050513A1 (en) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | New substituted dihydropyrazolone derivatives are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful to treat/prevent e.g. cardiovascular diseases, heart-circulation diseases, heart failure and anemia |
| DE102006050515A1 (en) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | New substituted dipyridiyl-dihydropyrazolone derivatives are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful to treat/prevent e.g. cardiovascular diseases, heart-circulation diseases, heart failure and anemia |
| DE102006050516A1 (en) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | New pyrazol-3-one compounds are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful e.g. to treat and/or prophylaxis heart-circulation diseases, heart failure, anemia, chronic kidney diseases and renal failure |
| DE102007044032A1 (en) | 2007-09-14 | 2009-03-19 | Bayer Healthcare Ag | New substituted heteroaryl compounds are hypoxia-inducible factor prolyl-4-hydroxylase inhibitors useful to treat and/or prevent e.g. circulatory heart diseases, heart failure, anemia, chronic kidney diseases and renal failure |
| DE102007048447A1 (en) | 2007-10-10 | 2009-04-16 | Bayer Healthcare Ag | New substituted dihydropyrazole-3-thione compounds are hypoxia inducible factor-prolyl-4-hydroxylase inhibitor, useful for preparing medicament to treat and/or prevent e.g. cardiovascular diseases, wound healing and anemia |
| DE102010044131A1 (en) | 2010-11-18 | 2012-05-24 | Bayer Schering Pharma Aktiengesellschaft | Substituted sodium 1H-pyrazole-5-olate |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5612353A (en) * | 1995-06-07 | 1997-03-18 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds |
| JP3994453B2 (en) * | 1995-10-13 | 2007-10-17 | 日産化学工業株式会社 | Pyrazolones |
-
1999
- 1999-03-03 DE DE19909237A patent/DE19909237A1/en not_active Withdrawn
-
2000
- 2000-02-29 HU HU0200242A patent/HUP0200242A3/en unknown
- 2000-02-29 CZ CZ20013164A patent/CZ20013164A3/en unknown
- 2000-02-29 CN CN00804521A patent/CN1342148A/en active Pending
- 2000-02-29 BR BR0008608-8A patent/BR0008608A/en not_active Application Discontinuation
- 2000-02-29 JP JP2000602216A patent/JP2002538143A/en active Pending
- 2000-02-29 MX MXPA01008844A patent/MXPA01008844A/en unknown
- 2000-02-29 CA CA002364908A patent/CA2364908A1/en not_active Abandoned
- 2000-02-29 EP EP00907650A patent/EP1157010A1/en not_active Withdrawn
- 2000-02-29 RU RU2001126566/04A patent/RU2001126566A/en unknown
- 2000-02-29 AU AU29165/00A patent/AU2916500A/en not_active Abandoned
- 2000-02-29 KR KR1020017011000A patent/KR20010102428A/en not_active Application Discontinuation
- 2000-02-29 WO PCT/EP2000/001695 patent/WO2000051989A1/en not_active Application Discontinuation
- 2000-02-29 SK SK1215-2001A patent/SK12152001A3/en unknown
- 2000-02-29 PL PL00350941A patent/PL350941A1/en unknown
-
2001
- 2001-08-31 NO NO20014234A patent/NO20014234L/en not_active Application Discontinuation
- 2001-10-01 ZA ZA200108064A patent/ZA200108064B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0200242A3 (en) | 2002-12-28 |
| WO2000051989A1 (en) | 2000-09-08 |
| JP2002538143A (en) | 2002-11-12 |
| MXPA01008844A (en) | 2002-05-14 |
| SK12152001A3 (en) | 2002-03-05 |
| AU2916500A (en) | 2000-09-21 |
| ZA200108064B (en) | 2003-01-02 |
| NO20014234D0 (en) | 2001-08-31 |
| EP1157010A1 (en) | 2001-11-28 |
| BR0008608A (en) | 2002-01-02 |
| PL350941A1 (en) | 2003-02-24 |
| RU2001126566A (en) | 2004-02-27 |
| NO20014234L (en) | 2001-10-24 |
| CA2364908A1 (en) | 2000-09-08 |
| KR20010102428A (en) | 2001-11-15 |
| DE19909237A1 (en) | 2000-09-07 |
| CN1342148A (en) | 2002-03-27 |
| CZ20013164A3 (en) | 2001-12-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HUP0004306A2 (en) | Benzamidine derivatives as factor xa inhibitors and process for their preparation | |
| HUP0300832A2 (en) | Novel, slow-acting betamimetics, a method for their production and their use as medicaments and pharmaceutical compositions containing them | |
| HUP9802694A1 (en) | Benzamide derivatives, process for producing them and pharmaceutical compositions containing them | |
| HUP0200242A2 (en) | Pyrazole-3-on-derivatives as factor xa inhibitors, pharmaceutical compositions containing them, their preparation and their use | |
| MXPA04001240A (en) | Antitumoral analogs. | |
| ES2196396T3 (en) | HETEROAROMATIC COMPOUNDS OF 5 MEMBERS CONTAINING OXYGEN OR SULFUR AS INHIBITORS OF THE XA FACTOR. | |
| HUP0402458A2 (en) | Chemokine receptor binding heterocyclic compounds with enhanced efficacy | |
| HUP0400636A2 (en) | Pharmaceutical compositions containing azetidine derivatives, novel azetidine derivatives and preparation thereof | |
| HUP0301745A2 (en) | Cyclopentanoindoles, compositions containing such compounds and their use | |
| HUP0204410A2 (en) | Pyrimidine-4-one derivatives, process for their preparation, pharmaceutical compositions containing them and their use | |
| HUP0200312A2 (en) | Substituted 2-phenylbenzimidazoles, pharmaceutical compositions containing them, the production thereof and their use | |
| HUP0204418A2 (en) | Nhe-1 inhibitor n-[(substituted five-membered di- or triaza diunsaturated ring)carbonyl] guanidine derivatives and use thereof | |
| HUP0303729A2 (en) | Novel heteroaryl derivatives and the use thereof as pharmaceuticals and process for their preparation | |
| HUP0303724A2 (en) | Chemokine receptors inhibitor bipiperidinyl-derivatives and pharmaceutical compositions containing them and process for preparation of the compounds | |
| MY142018A (en) | Thiophene derivatives as chk 1 inihibitors | |
| HUP0400527A2 (en) | Benzoylpyridine derivative or its salt, fungicide containing it as an active ingredient, its production process and intermediate for producing it | |
| HUP0301817A2 (en) | Kahalalide compounds, process for preparing thereof, pharmaceutical compositions comprising them and their use | |
| HUP0500497A2 (en) | Phenoxy piperidines pharmaceutical compositions containing them and process for producing them | |
| HUP0000762A2 (en) | 2-amino-6-(2-substituted-4-phenoxy)-substituted-pyridines, and pharmaceutical compositions containing them | |
| ZA200409379B (en) | Cationically substituted diphenyl azetidinones, method for their production, medicaments containing said compounds and use thereof | |
| RS97004A (en) | Benzoxazine derivatives as 5-ht6 modulators and uses thereof | |
| RS101204A (en) | N-acylaminobenzene derivatives as selective monoamine oxidase b inhibitors | |
| IL178360A0 (en) | 2-substituted pyrimidines and their use as pesticides | |
| DK1644389T3 (en) | Pyrinidine compounds with phosphonate groups as antiviral nucleotide analogues | |
| HUP0402341A2 (en) | Compositions containing thiazol-2-ylamines for the treatment of cancer |