DE10035927A1 - Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel - Google Patents
Neue Heteroaryl-Derivate und deren Verwendung als ArzneimittelInfo
- Publication number
- DE10035927A1 DE10035927A1 DE10035927A DE10035927A DE10035927A1 DE 10035927 A1 DE10035927 A1 DE 10035927A1 DE 10035927 A DE10035927 A DE 10035927A DE 10035927 A DE10035927 A DE 10035927A DE 10035927 A1 DE10035927 A1 DE 10035927A1
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- mono
- radical
- alkylamino
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000003814 drug Substances 0.000 title claims abstract description 6
- 125000001072 heteroaryl group Chemical group 0.000 title claims description 8
- 229940079593 drug Drugs 0.000 title claims description 3
- 229940027998 antiseptic and disinfectant acridine derivative Drugs 0.000 claims abstract description 21
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 9
- 238000004519 manufacturing process Methods 0.000 claims abstract description 6
- 125000000641 acridinyl group Chemical class C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims abstract description 3
- -1 phenylethyloxy, nitro, amino Chemical group 0.000 claims description 362
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 153
- 229910052736 halogen Inorganic materials 0.000 claims description 134
- 150000002367 halogens Chemical class 0.000 claims description 134
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 72
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 71
- 229910052739 hydrogen Inorganic materials 0.000 claims description 70
- 239000001257 hydrogen Substances 0.000 claims description 70
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 69
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 68
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims description 65
- 125000004043 oxo group Chemical group O=* 0.000 claims description 60
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 58
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 57
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 claims description 57
- 229910052731 fluorine Inorganic materials 0.000 claims description 55
- 239000011737 fluorine Substances 0.000 claims description 55
- 125000003282 alkyl amino group Chemical group 0.000 claims description 27
- 150000001251 acridines Chemical class 0.000 claims description 26
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 21
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 13
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 12
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 10
- 125000001153 fluoro group Chemical group F* 0.000 claims description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 5
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 5
- 239000001301 oxygen Substances 0.000 claims description 5
- 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 claims description 4
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims description 4
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims description 4
- 125000004941 pyridazin-5-yl group Chemical group N1=NC=CC(=C1)* 0.000 claims description 4
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims description 4
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 4
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical compound [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 claims description 3
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 2
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
- QCVGMYKWTIPJGT-UHFFFAOYSA-N [C].C1=CC=CC2=NC3=CC=CC=C3C=C12 Chemical group [C].C1=CC=CC2=NC3=CC=CC=C3C=C12 QCVGMYKWTIPJGT-UHFFFAOYSA-N 0.000 claims description 2
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims description 2
- OOGYVVYCCYJADG-UHFFFAOYSA-N acridine-1-carboxylic acid Chemical compound C1=CC=C2C=C3C(C(=O)O)=CC=CC3=NC2=C1 OOGYVVYCCYJADG-UHFFFAOYSA-N 0.000 claims description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 2
- 150000001412 amines Chemical class 0.000 claims description 2
- DZBUGLKDJFMEHC-UHFFFAOYSA-N benzoquinolinylidene Natural products C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 claims description 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 125000004942 pyridazin-6-yl group Chemical group N1=NC=CC=C1* 0.000 claims description 2
- 150000003254 radicals Chemical group 0.000 claims description 2
- 239000011593 sulfur Substances 0.000 claims description 2
- 125000004434 sulfur atom Chemical group 0.000 claims description 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000004306 triazinyl group Chemical group 0.000 claims description 2
- 229940126601 medicinal product Drugs 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 1
- 150000005840 aryl radicals Chemical class 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 210000004027 cell Anatomy 0.000 description 12
- 239000000203 mixture Substances 0.000 description 9
- 239000000126 substance Substances 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 5
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 4
- 230000001028 anti-proliverative effect Effects 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 210000004881 tumor cell Anatomy 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
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- SIROSARMEVWQGM-UHFFFAOYSA-N acridin-9-yl-[4-(3,5-dimethoxyphenyl)piperazin-1-yl]methanone Chemical compound COC1=CC(OC)=CC(N2CCN(CC2)C(=O)C=2C3=CC=CC=C3N=C3C=CC=CC3=2)=C1 SIROSARMEVWQGM-UHFFFAOYSA-N 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
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- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
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- 241000282412 Homo Species 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
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- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 2
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- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 2
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 2
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- 239000003826 tablet Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D219/00—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems
- C07D219/04—Heterocyclic compounds containing acridine or hydrogenated acridine ring systems 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 carbon atoms of the ring system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (32)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10035927A DE10035927A1 (de) | 2000-07-21 | 2000-07-21 | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| NZ524155A NZ524155A (en) | 2000-07-21 | 2001-07-18 | Acridine derivatives and their use as medicaments |
| HU0303729A HUP0303729A3 (en) | 2000-07-21 | 2001-07-18 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals and process for their preparation |
| AU8967501A AU8967501A (en) | 2000-07-21 | 2001-07-18 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals |
| EP01969410A EP1301485B1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
| UA2003021451A UA75085C2 (en) | 2000-07-21 | 2001-07-18 | Heteroaryl derivatives and use thereof as pharmaceutical preparations |
| PL01358808A PL358808A1 (en) | 2000-07-21 | 2001-07-18 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals |
| HK04100290.3A HK1057549B (en) | 2000-07-21 | 2001-07-18 | Heteroaryl derivatives and the use thereof as pharmaceuticals |
| AU2001289675A AU2001289675B2 (en) | 2000-07-21 | 2001-07-18 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals |
| PCT/EP2001/008263 WO2002008194A1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
| SK193-2003A SK1932003A3 (en) | 2000-07-21 | 2001-07-18 | Acridin derivatives and the use thereof as pharmaceuticals |
| CZ2003427A CZ2003427A3 (cs) | 2000-07-21 | 2001-07-18 | Nové deriváty akridinu a jejich použití jako léčiv |
| DE50112669T DE50112669D1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
| MXPA02012564A MXPA02012564A (es) | 2000-07-21 | 2001-07-18 | Derivados de acridina y su uso como medicina. |
| CNB018131379A CN1296359C (zh) | 2000-07-21 | 2001-07-18 | 杂芳基衍生物及其作为药物的应用 |
| IL15347601A IL153476A0 (en) | 2000-07-21 | 2001-07-18 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals |
| KR10-2003-7000878A KR20030022296A (ko) | 2000-07-21 | 2001-07-18 | 신규한 헤테로아릴 유도체 및 약제로서의 이의 용도 |
| AT01969410T ATE365717T1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
| BR0112591-5A BR0112591A (pt) | 2000-07-21 | 2001-07-18 | Derivados de acridina e sua aplicação como medicamento |
| RU2003105283/04A RU2267488C2 (ru) | 2000-07-21 | 2001-07-18 | Производные акридина, способ их получения и фармацевтическая композиция на их основе |
| ES01969410T ES2291349T3 (es) | 2000-07-21 | 2001-07-18 | Derivados de acridina y su uso como medicamentos. |
| SI200130756T SI1301485T1 (sl) | 2000-07-21 | 2001-07-18 | Derivati akridina in njihova uporaba kot zdravila |
| JP2002514101A JP2004504382A (ja) | 2000-07-21 | 2001-07-18 | アクリジン誘導体および医薬としてのその使用 |
| DK01969410T DK1301485T3 (da) | 2000-07-21 | 2001-07-18 | Nye heteroaryl-derivater og disses anvendelse som lægemiddel |
| PT01969410T PT1301485E (pt) | 2000-07-21 | 2001-07-18 | Derivados de acridina e sua utilização como agentes farmacêuticos |
| US09/910,142 US6706722B2 (en) | 2000-07-21 | 2001-07-20 | Heteroaryl derivatives and their use as medicaments |
| ARP010103480A AR033383A1 (es) | 2000-07-21 | 2001-07-20 | Derivados de acridina, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y los medicamentos que contienen dichos derivados |
| CA002353360A CA2353360A1 (en) | 2000-07-21 | 2001-07-20 | Novel heteroaryl derivatives and their use as medicaments |
| ZA200210411A ZA200210411B (en) | 2000-07-21 | 2002-12-23 | Novel heteroaryl derivatives and the use thereof as pharmaceuticals. |
| NO20030301A NO324939B1 (no) | 2000-07-21 | 2003-01-20 | Akridinderivater, anvendelse derav, fremgangsmate for fremstilling derav samt medikament inneholdende minst ett akridinderivat |
| BG107507A BG107507A (bg) | 2000-07-21 | 2003-01-30 | Акридинови производни и тяхното използване като лекарствени средства |
| CY20071101236T CY1106890T1 (el) | 2000-07-21 | 2007-09-26 | Παραγωγα της ακριδινης και η χρηση τους ως φαρμακων |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10035927A DE10035927A1 (de) | 2000-07-21 | 2000-07-21 | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE10035927A1 true DE10035927A1 (de) | 2002-03-07 |
Family
ID=7649979
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE10035927A Withdrawn DE10035927A1 (de) | 2000-07-21 | 2000-07-21 | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| DE50112669T Expired - Fee Related DE50112669D1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE50112669T Expired - Fee Related DE50112669D1 (de) | 2000-07-21 | 2001-07-18 | Acridin-derivate und deren verwendung als arzneimittel |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US6706722B2 (https=) |
| EP (1) | EP1301485B1 (https=) |
| JP (1) | JP2004504382A (https=) |
| KR (1) | KR20030022296A (https=) |
| CN (1) | CN1296359C (https=) |
| AR (1) | AR033383A1 (https=) |
| AT (1) | ATE365717T1 (https=) |
| AU (2) | AU2001289675B2 (https=) |
| BG (1) | BG107507A (https=) |
| BR (1) | BR0112591A (https=) |
| CA (1) | CA2353360A1 (https=) |
| CY (1) | CY1106890T1 (https=) |
| CZ (1) | CZ2003427A3 (https=) |
| DE (2) | DE10035927A1 (https=) |
| DK (1) | DK1301485T3 (https=) |
| ES (1) | ES2291349T3 (https=) |
| HU (1) | HUP0303729A3 (https=) |
| IL (1) | IL153476A0 (https=) |
| MX (1) | MXPA02012564A (https=) |
| NO (1) | NO324939B1 (https=) |
| NZ (1) | NZ524155A (https=) |
| PL (1) | PL358808A1 (https=) |
| PT (1) | PT1301485E (https=) |
| RU (1) | RU2267488C2 (https=) |
| SK (1) | SK1932003A3 (https=) |
| UA (1) | UA75085C2 (https=) |
| WO (1) | WO2002008194A1 (https=) |
| ZA (1) | ZA200210411B (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10035928A1 (de) * | 2000-07-21 | 2002-03-07 | Asta Medica Ag | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| DE10037310A1 (de) * | 2000-07-28 | 2002-02-07 | Asta Medica Ag | Neue Indolderivate und deren Verwendung als Arzneimittel |
| CN100509790C (zh) * | 2002-06-29 | 2009-07-08 | 赞塔里斯有限公司 | 芳基羰基哌嗪和杂芳基羰基哌嗪及其治疗良性和恶性肿瘤疾病的用途 |
| AU2003232785A1 (en) * | 2002-07-17 | 2004-02-02 | Zentaris Gmbh | Novel anthracene derivatives and the use thereof as a medicament |
| US7125461B2 (en) * | 2003-05-07 | 2006-10-24 | L & L Products, Inc. | Activatable material for sealing, baffling or reinforcing and method of forming same |
| FR2855825B1 (fr) * | 2003-06-04 | 2008-08-22 | Aventis Pharma Sa | Produits aryl-heteroaromatiques, compositions les contenant et utilisation |
| PE20050226A1 (es) * | 2003-06-04 | 2005-05-18 | Aventis Pharma Sa | Productos aril-heteroaromaticos y composiciones que los contienen |
| US7249415B2 (en) * | 2003-06-26 | 2007-07-31 | Zephyros, Inc. | Method of forming members for sealing or baffling |
| DE10331500A1 (de) * | 2003-07-11 | 2005-02-24 | Zentaris Gmbh | Neue Acridin-Derivate und deren Verwendung als Arzneimittel |
| WO2006080043A2 (en) * | 2005-01-27 | 2006-08-03 | Alma Mater Studiorum- Universita' Di Bologna | Organic compounds useful for the treatment of alzheimer's disease, their use and method of preparation |
| US20070299093A1 (en) * | 2005-01-27 | 2007-12-27 | Alma Mater Studiorum-Universitá Di Bologna | Organic Compounds Useful for the Treatment of Alzheimer's Disease, Their Use and Method of Preparation |
| CA2678577A1 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| EP2183228B1 (en) * | 2007-07-26 | 2014-08-20 | Vitae Pharmaceuticals, Inc. | CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1 |
| AR069207A1 (es) * | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW200934490A (en) * | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| WO2009094169A1 (en) * | 2008-01-24 | 2009-07-30 | Vitae Pharmaceuticals, Inc. | Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| US8598160B2 (en) * | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| JP5538356B2 (ja) * | 2008-03-18 | 2014-07-02 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤 |
| AR071236A1 (es) | 2008-05-01 | 2010-06-02 | Vitae Pharmaceuticals Inc | Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2723032A1 (en) * | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CL2009001059A1 (es) * | 2008-05-01 | 2010-11-12 | Boehringer Ingelheim Int | Compuestos derivados de 1,3-oxazin-2-ona-3,6 sustituidos, inhibidores de la actividad de la 11-beta-hidroxiesteroide deshidrogenasa i; composicion farmaceutica que los comprende; utiles en el tratamiento de enfermedades tales como diabetes mellitus, entre otras. |
| US8846668B2 (en) | 2008-07-25 | 2014-09-30 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2010011314A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| TW201039034A (en) * | 2009-04-27 | 2010-11-01 | Chunghwa Picture Tubes Ltd | Pixel structure and the method of forming the same |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1 |
| KR20120061771A (ko) * | 2009-04-30 | 2012-06-13 | 비타이 파마슈티컬즈, 인코포레이티드 | 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제 |
| EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| WO2011002910A1 (en) | 2009-07-01 | 2011-01-06 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8933072B2 (en) | 2010-06-16 | 2015-01-13 | Vitae Pharmaceuticals, Inc. | Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use |
| JP5813106B2 (ja) | 2010-06-25 | 2015-11-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン |
| PH12013500808A1 (en) | 2010-11-02 | 2015-10-07 | Boehringer Ingelheim Int | Pharmaceutical combinations for the treatment of metabolic disorders |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2538388B1 (fr) | 1982-12-24 | 1985-06-21 | Pharmuka Lab | Nouveaux derives de naphtalene- ou azanaphtalenecarboxamide, leurs procedes de preparation et leur utilisation comme medicaments |
| EP0318235A3 (en) * | 1987-11-25 | 1991-05-02 | Takeda Chemical Industries, Ltd. | Paf antagonist, 1,4-disubstituted piperazine compounds and production thereof |
| US5030631A (en) * | 1989-11-27 | 1991-07-09 | Schering Corporation | Tricylclic arylsulfonamides |
| RU2126001C1 (ru) * | 1995-01-10 | 1999-02-10 | Самдзин Фармасьютикал Ко., Лтд | Производные пиперазина и фармацевтическая композиция на их основе |
| NZ329847A (en) * | 1996-06-29 | 1999-01-28 | Samjin Pharm Co Ltd | Piperazine derivatives and process for the preparation thereof |
| US5861395A (en) | 1996-09-13 | 1999-01-19 | Schering Corporation | Compounds useful for inhibition of farnesyl proteins transferase |
| FR2753706B1 (fr) | 1996-09-20 | 1998-10-30 | Nouvelles amines cycliques n-substituees, leur procede de preparation et les compositions pharmaceutiques les renfermant | |
| DE19743435A1 (de) | 1997-10-01 | 1999-04-08 | Merck Patent Gmbh | Benzamidinderivate |
| CA2342251A1 (en) | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
| WO2000051614A1 (en) | 1999-03-03 | 2000-09-08 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferases |
-
2000
- 2000-07-21 DE DE10035927A patent/DE10035927A1/de not_active Withdrawn
-
2001
- 2001-07-18 CN CNB018131379A patent/CN1296359C/zh not_active Expired - Fee Related
- 2001-07-18 PT PT01969410T patent/PT1301485E/pt unknown
- 2001-07-18 AT AT01969410T patent/ATE365717T1/de not_active IP Right Cessation
- 2001-07-18 KR KR10-2003-7000878A patent/KR20030022296A/ko not_active Ceased
- 2001-07-18 WO PCT/EP2001/008263 patent/WO2002008194A1/de not_active Ceased
- 2001-07-18 MX MXPA02012564A patent/MXPA02012564A/es active IP Right Grant
- 2001-07-18 NZ NZ524155A patent/NZ524155A/en unknown
- 2001-07-18 BR BR0112591-5A patent/BR0112591A/pt not_active IP Right Cessation
- 2001-07-18 HU HU0303729A patent/HUP0303729A3/hu unknown
- 2001-07-18 EP EP01969410A patent/EP1301485B1/de not_active Expired - Lifetime
- 2001-07-18 DE DE50112669T patent/DE50112669D1/de not_active Expired - Fee Related
- 2001-07-18 DK DK01969410T patent/DK1301485T3/da active
- 2001-07-18 AU AU2001289675A patent/AU2001289675B2/en not_active Ceased
- 2001-07-18 AU AU8967501A patent/AU8967501A/xx active Pending
- 2001-07-18 ES ES01969410T patent/ES2291349T3/es not_active Expired - Lifetime
- 2001-07-18 SK SK193-2003A patent/SK1932003A3/sk not_active Application Discontinuation
- 2001-07-18 PL PL01358808A patent/PL358808A1/xx not_active Application Discontinuation
- 2001-07-18 UA UA2003021451A patent/UA75085C2/uk unknown
- 2001-07-18 CZ CZ2003427A patent/CZ2003427A3/cs unknown
- 2001-07-18 IL IL15347601A patent/IL153476A0/xx unknown
- 2001-07-18 JP JP2002514101A patent/JP2004504382A/ja not_active Withdrawn
- 2001-07-18 RU RU2003105283/04A patent/RU2267488C2/ru not_active IP Right Cessation
- 2001-07-20 AR ARP010103480A patent/AR033383A1/es unknown
- 2001-07-20 US US09/910,142 patent/US6706722B2/en not_active Expired - Fee Related
- 2001-07-20 CA CA002353360A patent/CA2353360A1/en not_active Abandoned
-
2002
- 2002-12-23 ZA ZA200210411A patent/ZA200210411B/xx unknown
-
2003
- 2003-01-20 NO NO20030301A patent/NO324939B1/no not_active IP Right Cessation
- 2003-01-30 BG BG107507A patent/BG107507A/bg unknown
-
2007
- 2007-09-26 CY CY20071101236T patent/CY1106890T1/el unknown
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| EP1484329A1 (de) | Indolderivate mit Apoptose induzierender Wirkung |
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Free format text: GUENTHER, ECKHARD, DR., 63477 MAINTAL, DE EMIG, PETER, DR., 63486 BRUCHKOEBEL, DE NICKEL, BERND, DR., 64367 MUEHLTAL, DE BAASNER, SILKE, DR., 61137 SCHOENECK, DE BACHER, GERALD, DR., 82110 GERMERING, DE AUE, BEATE, 63762 GROSSOSTHEIM, DE BECKERS, THOMAS, DR., 60596 FRANKFURT, DE |
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