MXPA04010608A - Derivados de 7-aril-3,9-diazabiciclo(3.3.1)non-6-eno y sus usos como inhibidores de renina en el tratamiento de enfermedades de hipertension, cardiovasculares o renales. - Google Patents
Derivados de 7-aril-3,9-diazabiciclo(3.3.1)non-6-eno y sus usos como inhibidores de renina en el tratamiento de enfermedades de hipertension, cardiovasculares o renales.Info
- Publication number
- MXPA04010608A MXPA04010608A MXPA04010608A MXPA04010608A MXPA04010608A MX PA04010608 A MXPA04010608 A MX PA04010608A MX PA04010608 A MXPA04010608 A MX PA04010608A MX PA04010608 A MXPA04010608 A MX PA04010608A MX PA04010608 A MXPA04010608 A MX PA04010608A
- Authority
- MX
- Mexico
- Prior art keywords
- acid
- diazabicyclo
- phenyl
- rae
- propyl
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims description 14
- 206010020772 Hypertension Diseases 0.000 title claims description 10
- 208000024172 Cardiovascular disease Diseases 0.000 title claims description 4
- 239000002461 renin inhibitor Substances 0.000 title description 10
- 229940086526 renin-inhibitors Drugs 0.000 title description 10
- 230000002526 effect on cardiovascular system Effects 0.000 title description 3
- 208000017169 kidney disease Diseases 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 269
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 5
- -1 racemates Chemical class 0.000 claims description 1331
- 239000002253 acid Substances 0.000 claims description 978
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 550
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 243
- 239000000203 mixture Substances 0.000 claims description 231
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 178
- 150000002148 esters Chemical class 0.000 claims description 170
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 134
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 122
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 106
- SASNBVQSOZSTPD-UHFFFAOYSA-N n-methylphenethylamine Chemical compound CNCCC1=CC=CC=C1 SASNBVQSOZSTPD-UHFFFAOYSA-N 0.000 claims description 99
- GCJYLAWVUWEHLW-UHFFFAOYSA-N n-[(2-chlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC=C1CNC1CC1 GCJYLAWVUWEHLW-UHFFFAOYSA-N 0.000 claims description 97
- 239000002904 solvent Substances 0.000 claims description 74
- PLKFDECOAXOQRN-UHFFFAOYSA-N FC1=C(OCCCC2=CC=C(C=C2)C23CNCC(C(=CC2)C(=O)O)N3)C(=CC=C1F)F Chemical compound FC1=C(OCCCC2=CC=C(C=C2)C23CNCC(C(=CC2)C(=O)O)N3)C(=CC=C1F)F PLKFDECOAXOQRN-UHFFFAOYSA-N 0.000 claims description 59
- 150000004702 methyl esters Chemical class 0.000 claims description 59
- 125000000217 alkyl group Chemical group 0.000 claims description 51
- IVEWTCACRDEAOB-UHFFFAOYSA-N 2-(2-methoxyphenyl)acetic acid Chemical compound COC1=CC=CC=C1CC(O)=O IVEWTCACRDEAOB-UHFFFAOYSA-N 0.000 claims description 33
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 30
- SSJXIUAHEKJCMH-WDSKDSINSA-N (1s,2s)-cyclohexane-1,2-diamine Chemical compound N[C@H]1CCCC[C@@H]1N SSJXIUAHEKJCMH-WDSKDSINSA-N 0.000 claims description 27
- BTBDLUOYLCXSMK-UHFFFAOYSA-N n-[(3,5-dimethoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC(OC)=CC(CNC2CC2)=C1 BTBDLUOYLCXSMK-UHFFFAOYSA-N 0.000 claims description 26
- 125000006179 2-methyl benzyl group Chemical group [H]C1=C([H])C(=C(C([H])=C1[H])C([H])([H])*)C([H])([H])[H] 0.000 claims description 25
- CRGTXQJSJVBJPN-UHFFFAOYSA-N 5-[4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl]-7,9-diazabicyclo[3.3.1]non-2-ene-2-carboxylic acid Chemical compound C1=C(C)C(C)=CC(Cl)=C1OCCOC1=CC=C(C23NC(CNC2)C(=CC3)C(O)=O)C=C1 CRGTXQJSJVBJPN-UHFFFAOYSA-N 0.000 claims description 25
- QWMNTOVGKJAROU-UHFFFAOYSA-N n-[(2-chlorophenyl)methyl]ethanamine Chemical compound CCNCC1=CC=CC=C1Cl QWMNTOVGKJAROU-UHFFFAOYSA-N 0.000 claims description 24
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 23
- 125000006495 3-trifluoromethyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1[H])C([H])([H])*)C(F)(F)F 0.000 claims description 22
- 150000001408 amides Chemical class 0.000 claims description 21
- 125000003118 aryl group Chemical group 0.000 claims description 21
- 125000004432 carbon atom Chemical group C* 0.000 claims description 21
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims description 21
- WNQSDASWQZYDDP-UHFFFAOYSA-N 1-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid Chemical compound ClC1=C(OCCOC2=CC=C(C=C2)C23CNCC(C(=CC2)C(=O)O)N3)C(=CC(=C1)C)Cl WNQSDASWQZYDDP-UHFFFAOYSA-N 0.000 claims description 20
- 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 18
- 150000003839 salts Chemical class 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- WYQUCNZBUBLJHN-UHFFFAOYSA-N n-[(2-methylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC=C1CNC1CC1 WYQUCNZBUBLJHN-UHFFFAOYSA-N 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 14
- CRIMYHBFDHWKQY-UHFFFAOYSA-N n-[(2,3-dimethylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC(CNC2CC2)=C1C CRIMYHBFDHWKQY-UHFFFAOYSA-N 0.000 claims description 14
- UZYPFBRRGVZJNV-UHFFFAOYSA-N n-[(2-fluorophenyl)methyl]cyclopropanamine Chemical compound FC1=CC=CC=C1CNC1CC1 UZYPFBRRGVZJNV-UHFFFAOYSA-N 0.000 claims description 14
- USBAUXJPPHVCTF-UHFFFAOYSA-N n-benzylcyclopropanamine Chemical compound C=1C=CC=CC=1CNC1CC1 USBAUXJPPHVCTF-UHFFFAOYSA-N 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 13
- HWDVTQAXQJQROO-UHFFFAOYSA-N cyclopropylazanide Chemical compound [NH-]C1CC1 HWDVTQAXQJQROO-UHFFFAOYSA-N 0.000 claims description 13
- KJYVKUQRRKDPAX-UHFFFAOYSA-N n-[(2,3-dichlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC(CNC2CC2)=C1Cl KJYVKUQRRKDPAX-UHFFFAOYSA-N 0.000 claims description 13
- NJHZDGHFBLATGX-UHFFFAOYSA-N n-[2-(2-chlorophenyl)ethyl]cyclopropanamine Chemical compound ClC1=CC=CC=C1CCNC1CC1 NJHZDGHFBLATGX-UHFFFAOYSA-N 0.000 claims description 13
- 125000003070 2-(2-chlorophenyl)ethyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000003342 alkenyl group Chemical group 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 230000036454 renin-angiotensin system Effects 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
- 125000004494 ethyl ester group Chemical group 0.000 claims description 11
- 125000001072 heteroaryl group Chemical group 0.000 claims description 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- CEQDKNLDFWAMEL-UHFFFAOYSA-N n-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]cyclopropanamine Chemical compound FC(F)(F)C1=CC=CC(CNC2CC2)=C1Cl CEQDKNLDFWAMEL-UHFFFAOYSA-N 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 206010019280 Heart failures Diseases 0.000 claims description 9
- ILHIZUJWNGLALK-UHFFFAOYSA-N n-(2-phenylethyl)cyclopropanamine Chemical compound C1CC1NCCC1=CC=CC=C1 ILHIZUJWNGLALK-UHFFFAOYSA-N 0.000 claims description 9
- SBKDFWWYKALTKE-UHFFFAOYSA-N n-[(2-bromophenyl)methyl]cyclopropanamine Chemical compound BrC1=CC=CC=C1CNC1CC1 SBKDFWWYKALTKE-UHFFFAOYSA-N 0.000 claims description 9
- LJBFNXZKZYKGFY-UHFFFAOYSA-N n-[(3-methylphenyl)methyl]cyclopropanamine Chemical compound CC1=CC=CC(CNC2CC2)=C1 LJBFNXZKZYKGFY-UHFFFAOYSA-N 0.000 claims description 9
- XOJVVFBFDXDTEG-UHFFFAOYSA-N pristane Chemical compound CC(C)CCCC(C)CCCC(C)CCCC(C)C XOJVVFBFDXDTEG-UHFFFAOYSA-N 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 8
- 208000001647 Renal Insufficiency Diseases 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 201000006370 kidney failure Diseases 0.000 claims description 8
- 230000000877 morphologic effect Effects 0.000 claims description 8
- CUPDQCKBQJVOMC-UHFFFAOYSA-N n-[(2-fluoro-5-methoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC=C(F)C(CNC2CC2)=C1 CUPDQCKBQJVOMC-UHFFFAOYSA-N 0.000 claims description 8
- VALINFAZSMPKJJ-UHFFFAOYSA-N n-[(3-chlorophenyl)methyl]cyclopropanamine Chemical compound ClC1=CC=CC(CNC2CC2)=C1 VALINFAZSMPKJJ-UHFFFAOYSA-N 0.000 claims description 8
- UGRMITBWUVWUEB-UHFFFAOYSA-N 1-$l^{1}-oxidanyl-3-methylbenzene Chemical group CC1=CC=CC([O])=C1 UGRMITBWUVWUEB-UHFFFAOYSA-N 0.000 claims description 7
- DTJKAALGEAHUIV-UHFFFAOYSA-N 2-(2-chlorophenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC=C1Cl DTJKAALGEAHUIV-UHFFFAOYSA-N 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- 125000004450 alkenylene group Chemical group 0.000 claims description 7
- 125000000304 alkynyl group Chemical group 0.000 claims description 7
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- NUPAMNLYORQZRV-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]cyclopropanamine Chemical compound COC1=CC=CC(CNC2CC2)=C1 NUPAMNLYORQZRV-UHFFFAOYSA-N 0.000 claims description 7
- VRDMJNOXKZMLTF-UHFFFAOYSA-N n-[(6-chloro-1,3-benzodioxol-5-yl)methyl]cyclopropanamine Chemical compound ClC1=CC=2OCOC=2C=C1CNC1CC1 VRDMJNOXKZMLTF-UHFFFAOYSA-N 0.000 claims description 7
- 238000011321 prophylaxis Methods 0.000 claims description 7
- 239000005541 ACE inhibitor Substances 0.000 claims description 6
- 206010063897 Renal ischaemia Diseases 0.000 claims description 6
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 6
- 239000012876 carrier material Substances 0.000 claims description 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- 208000031225 myocardial ischemia Diseases 0.000 claims description 5
- ORZRHMRDNOCKDU-UHFFFAOYSA-N n-[(3,4-dimethoxyphenyl)methyl]cyclopropanamine Chemical compound C1=C(OC)C(OC)=CC=C1CNC1CC1 ORZRHMRDNOCKDU-UHFFFAOYSA-N 0.000 claims description 5
- 230000002378 acidificating effect Effects 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- WRRVCXHKEDNRNB-UHFFFAOYSA-N n-[(3,5-difluorophenyl)methyl]cyclopropanamine Chemical compound FC1=CC(F)=CC(CNC2CC2)=C1 WRRVCXHKEDNRNB-UHFFFAOYSA-N 0.000 claims description 4
- ANCFTHKEGKDXKD-UHFFFAOYSA-N n-[[3-(trifluoromethoxy)phenyl]methyl]cyclopropanamine Chemical compound FC(F)(F)OC1=CC=CC(CNC2CC2)=C1 ANCFTHKEGKDXKD-UHFFFAOYSA-N 0.000 claims description 4
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 4
- 208000037803 restenosis Diseases 0.000 claims description 4
- ZWEGOGARWMDMDR-UHFFFAOYSA-N 2,2-dimethyl-5-oxopentanoic acid Chemical compound OC(=O)C(C)(C)CCC=O ZWEGOGARWMDMDR-UHFFFAOYSA-N 0.000 claims description 3
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- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
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- 206010018364 Glomerulonephritis Diseases 0.000 claims description 3
- BHHGXPLMPWCGHP-UHFFFAOYSA-N Phenethylamine Chemical compound NCCC1=CC=CC=C1 BHHGXPLMPWCGHP-UHFFFAOYSA-N 0.000 claims description 3
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 3
- 206010038419 Renal colic Diseases 0.000 claims description 3
- 206010062237 Renal impairment Diseases 0.000 claims description 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 3
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- 238000007631 vascular surgery Methods 0.000 claims description 3
- UCAUHTUMXIYKFJ-UHFFFAOYSA-N 2-(2-methoxyphenyl)-n-methylethanamine Chemical compound CNCCC1=CC=CC=C1OC UCAUHTUMXIYKFJ-UHFFFAOYSA-N 0.000 claims description 2
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- VCSUCPDSYSXLEX-UHFFFAOYSA-N 2-(4-chlorophenyl)-n-methylethanamine Chemical compound CNCCC1=CC=C(Cl)C=C1 VCSUCPDSYSXLEX-UHFFFAOYSA-N 0.000 claims description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 2
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- 241001465754 Metazoa Species 0.000 claims description 2
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- 125000005248 alkyl aryloxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical class 0.000 claims description 2
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- HROUFMHZMXWOHI-UHFFFAOYSA-N n-(1,3-benzodioxol-5-ylmethyl)cyclopropanamine Chemical compound C=1C=C2OCOC2=CC=1CNC1CC1 HROUFMHZMXWOHI-UHFFFAOYSA-N 0.000 claims description 2
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- 208000035475 disorder Diseases 0.000 claims 2
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- 239000004480 active ingredient Substances 0.000 abstract 1
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- 238000007911 parenteral administration Methods 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 239000000816 peptidomimetic Substances 0.000 description 1
- KHIWWQKSHDUIBK-UHFFFAOYSA-N periodic acid Chemical compound OI(=O)(=O)=O KHIWWQKSHDUIBK-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- 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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0204705 | 2002-04-29 | ||
| PCT/EP2003/003721 WO2003093267A1 (en) | 2002-04-29 | 2003-04-08 | 7-aryl-3,9-diazabicyclo(3.3.1)non-6-ene derivatives and their use as renin inhibitors in the treatment of hypertension, cardiovascular or renal diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA04010608A true MXPA04010608A (es) | 2004-12-13 |
Family
ID=29286070
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA04010608A MXPA04010608A (es) | 2002-04-29 | 2003-04-08 | Derivados de 7-aril-3,9-diazabiciclo(3.3.1)non-6-eno y sus usos como inhibidores de renina en el tratamiento de enfermedades de hipertension, cardiovasculares o renales. |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7427613B2 (enExample) |
| EP (1) | EP1501830B1 (enExample) |
| JP (1) | JP4041123B2 (enExample) |
| KR (1) | KR100783863B1 (enExample) |
| CN (1) | CN1649870A (enExample) |
| AT (1) | ATE527261T1 (enExample) |
| AU (1) | AU2003233963B2 (enExample) |
| BR (1) | BR0309498A (enExample) |
| CA (1) | CA2483241C (enExample) |
| CL (1) | CL2003002042A1 (enExample) |
| CO (1) | CO5631443A2 (enExample) |
| EC (1) | ECSP045378A (enExample) |
| ES (1) | ES2372931T3 (enExample) |
| HR (1) | HRP20041132A2 (enExample) |
| IL (1) | IL164767A0 (enExample) |
| IS (1) | IS7545A (enExample) |
| MA (1) | MA27305A1 (enExample) |
| MX (1) | MXPA04010608A (enExample) |
| NO (1) | NO20045042L (enExample) |
| NZ (1) | NZ536750A (enExample) |
| PL (1) | PL372141A1 (enExample) |
| RU (1) | RU2343153C2 (enExample) |
| TW (1) | TW200514786A (enExample) |
| UA (1) | UA80821C2 (enExample) |
| WO (1) | WO2003093267A1 (enExample) |
| ZA (1) | ZA200408283B (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004234040A1 (en) * | 2003-04-28 | 2004-11-11 | Actelion Pharmaceuticals Ltd | Diazabicyclononene and tetrahydropyridine derivatives as renin inhibitors |
| RU2005137174A (ru) * | 2003-04-30 | 2006-03-27 | Актелион Фармасьютикалз Лтд. (Ch) | Азабициклононеновые производные |
| WO2004096799A1 (en) * | 2003-04-30 | 2004-11-11 | Actelion Pharmaceuticals Ltd | Tropane derivatives and their use as ace inhibitors |
| EP1622685A1 (en) * | 2003-04-30 | 2006-02-08 | Actelion Pharmaceuticals Ltd. | 9-azabicyclo[3.3.1]non-6-ene derivatives with a heteroatom at the 3-position as renin inhibitors |
| KR20060015573A (ko) * | 2003-05-02 | 2006-02-17 | 액테리온 파마슈티칼 리미티드 | 신규한 디아자비시클로노넨 유도체 |
| WO2004105762A1 (en) * | 2003-05-30 | 2004-12-09 | Actelion Pharmaceuticals Ltd | Medical use of diazabicyclononene derivatives as inhibitors of parasite aspartic proteases |
| WO2005040120A1 (en) * | 2003-10-09 | 2005-05-06 | Actelion Pharmaceuticals Ltd | Tetrahydropyridine derivatives |
| JP2007508262A (ja) * | 2003-10-13 | 2007-04-05 | アクテリオン ファマシューティカルズ リミテッド | 新規ジアザビシクロノネン誘導体およびその使用 |
| JP2007509099A (ja) * | 2003-10-23 | 2007-04-12 | アクテリオン ファマシューティカルズ リミテッド | 新規ジアザビシクロノネンおよび新規極性側鎖を有するテトラヒドロピリジン誘導体 |
| WO2005054243A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd | Diazabicyclononene derivatives and their use as renin inhibitors |
| AU2004295092A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd. | Azabicyclooctene and other tetrahydropyridine derivatives with a new side-chain |
| WO2006021403A1 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Bicyclononene derivatives |
| ATE462703T1 (de) * | 2004-08-25 | 2010-04-15 | Actelion Pharmaceuticals Ltd | Bicyclononen-derivate als renin-inhibitoren |
| WO2006021399A2 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Azabicyclononene derivatives as renin inhibitors |
| WO2006021401A2 (en) * | 2004-08-25 | 2006-03-02 | Actelion Pharmaceuticals Ltd | Bicylononene derivatives |
| AR052263A1 (es) * | 2004-12-08 | 2007-03-07 | Actelion Pharmaceuticals Ltd | Derivado de diazabiciclononeno |
| WO2006063610A1 (en) * | 2004-12-17 | 2006-06-22 | Actelion Pharmaceuticals Ltd | Heteroaryl substituted diazabicyclononene derivatives |
| GB0428526D0 (en) | 2004-12-30 | 2005-02-09 | Novartis Ag | Organic compounds |
| ATE514697T1 (de) * | 2005-01-28 | 2011-07-15 | Actelion Pharmaceuticals Ltd | 7-ä4-ä2-(2,6-dichloro-4- methylphenoxy)ethoxyüphenylü-3,9- diazabicycloä3.3.1ünon-6-ene-6-carbonsäure- cyclopropyl-(2,3-dimethylbenzyl)amid als renin- hemmer für die behandlung von bluthochdruck |
| BRPI0609890A2 (pt) * | 2005-05-27 | 2010-05-04 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica, e, uso de um composto |
| GB0514203D0 (en) | 2005-07-11 | 2005-08-17 | Novartis Ag | Organic compounds |
| PT2420491E (pt) | 2005-12-30 | 2013-10-14 | Novartis Ag | Compostos de piperidina 3,5-substituída como inibidores de renina |
| RU2425032C2 (ru) | 2006-02-02 | 2011-07-27 | Актелион Фармасьютикалз Лтд | Вторичные амины в качестве ингибиторов ренина |
| CL2007000595A1 (es) * | 2006-03-08 | 2008-01-04 | Actelion Pharmaceuticals Ltd | Compuestos derivados de piperidina; composicion farmaceutica y uso para el tratamiento y/o profilaxis de enfermedades seleccionadas entre hipertension, insuficiencia cardiaca congestiva e insuficiencia renal entre otras. |
| US8343968B2 (en) | 2007-05-24 | 2013-01-01 | Merck Canada Inc. | Case of renin inhibitors |
| WO2009000811A1 (en) | 2007-06-25 | 2008-12-31 | Novartis Ag | N5-(2-ethoxyethyl)-n3-(2-pyridinyl)-3,5-piperidinedicarboxamide derivatives for use as renin inhibitors |
| WO2009023964A1 (en) | 2007-08-20 | 2009-02-26 | Merck Frosst Canada Ltd. | Renin inhibitors |
| CA2722734C (en) | 2008-05-05 | 2013-11-05 | Merck Frosst Canada Ltd. | 3,4-substituted piperidine derivatives as renin inhibitors |
| CN109721613B (zh) * | 2017-10-27 | 2021-07-30 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的大环酰胺化合物及其药物组合物和用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US3509161A (en) | 1967-07-10 | 1970-04-28 | Boehringer & Soehne Gmbh | 3-phenyl-granatene-(2)-derivatives |
| GB9020927D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Pharmaceuticals |
| US5268361A (en) * | 1991-06-07 | 1993-12-07 | Sri International | Hydroxyazido derivatives and related compounds as renin inhibitors |
| US5374719A (en) * | 1993-06-04 | 1994-12-20 | Eli Lilly And Company | Process for converting loracarbef dihydrate to loracarbef monohydrate |
| KR100384979B1 (ko) | 1995-09-07 | 2003-10-17 | 에프. 호프만-라 로슈 아게 | 심부전증및신부전증치료용의신규한4-(옥시알콕시페닐)-3-옥시-피페리딘 |
| WO1998039328A1 (en) | 1997-03-03 | 1998-09-11 | F.Hoffmann-La Roche Ag | Substituted 2,4-diaminopyrimidines |
| US20060223795A1 (en) * | 2003-05-02 | 2006-10-05 | Oliver Bezencon | Novel diazabicyclononene derivatives |
| WO2005054243A1 (en) * | 2003-12-05 | 2005-06-16 | Actelion Pharmaceuticals Ltd | Diazabicyclononene derivatives and their use as renin inhibitors |
-
2003
- 2003-04-08 AU AU2003233963A patent/AU2003233963B2/en not_active Ceased
- 2003-04-08 RU RU2004134320/04A patent/RU2343153C2/ru not_active IP Right Cessation
- 2003-04-08 AT AT03727287T patent/ATE527261T1/de not_active IP Right Cessation
- 2003-04-08 ES ES03727287T patent/ES2372931T3/es not_active Expired - Lifetime
- 2003-04-08 US US10/513,103 patent/US7427613B2/en not_active Expired - Fee Related
- 2003-04-08 MX MXPA04010608A patent/MXPA04010608A/es not_active Application Discontinuation
- 2003-04-08 CA CA2483241A patent/CA2483241C/en not_active Expired - Fee Related
- 2003-04-08 EP EP03727287A patent/EP1501830B1/en not_active Expired - Lifetime
- 2003-04-08 WO PCT/EP2003/003721 patent/WO2003093267A1/en not_active Ceased
- 2003-04-08 HR HR20041132A patent/HRP20041132A2/xx not_active Application Discontinuation
- 2003-04-08 PL PL03372141A patent/PL372141A1/xx not_active Application Discontinuation
- 2003-04-08 JP JP2004501406A patent/JP4041123B2/ja not_active Expired - Fee Related
- 2003-04-08 KR KR1020047016845A patent/KR100783863B1/ko not_active Expired - Fee Related
- 2003-04-08 NZ NZ536750A patent/NZ536750A/xx unknown
- 2003-04-08 IL IL16476703A patent/IL164767A0/xx unknown
- 2003-04-08 BR BR0309498-7A patent/BR0309498A/pt not_active IP Right Cessation
- 2003-04-08 CN CNA038097664A patent/CN1649870A/zh active Pending
- 2003-08-04 UA UA20041109469A patent/UA80821C2/uk unknown
- 2003-10-10 CL CL200302042A patent/CL2003002042A1/es unknown
- 2003-10-23 TW TW092129421A patent/TW200514786A/zh unknown
-
2004
- 2004-10-13 ZA ZA200408283A patent/ZA200408283B/xx unknown
- 2004-10-22 MA MA27914A patent/MA27305A1/fr unknown
- 2004-10-22 CO CO04106347A patent/CO5631443A2/es not_active Application Discontinuation
- 2004-10-22 EC EC2004005378A patent/ECSP045378A/es unknown
- 2004-11-19 NO NO20045042A patent/NO20045042L/no not_active Application Discontinuation
- 2004-11-22 IS IS7545A patent/IS7545A/is unknown
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2008
- 2008-07-07 US US12/168,666 patent/US20080312242A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1501830A1 (en) | 2005-02-02 |
| CA2483241A1 (en) | 2003-11-13 |
| TW200514786A (en) | 2005-05-01 |
| ES2372931T3 (es) | 2012-01-27 |
| JP2005527602A (ja) | 2005-09-15 |
| ECSP045378A (es) | 2004-11-26 |
| KR20040101546A (ko) | 2004-12-02 |
| NZ536750A (en) | 2007-02-23 |
| BR0309498A (pt) | 2005-02-15 |
| AU2003233963B2 (en) | 2008-09-11 |
| US20080312242A1 (en) | 2008-12-18 |
| PL372141A1 (en) | 2005-07-11 |
| CO5631443A2 (es) | 2006-04-28 |
| HRP20041132A2 (en) | 2006-07-31 |
| ATE527261T1 (de) | 2011-10-15 |
| RU2004134320A (ru) | 2005-08-27 |
| CA2483241C (en) | 2011-05-31 |
| IL164767A0 (en) | 2005-12-18 |
| ZA200408283B (en) | 2006-05-31 |
| UA80821C2 (en) | 2007-11-12 |
| RU2343153C2 (ru) | 2009-01-10 |
| CN1649870A (zh) | 2005-08-03 |
| WO2003093267A1 (en) | 2003-11-13 |
| JP4041123B2 (ja) | 2008-01-30 |
| NO20045042L (no) | 2004-11-19 |
| CL2003002042A1 (es) | 2005-02-04 |
| EP1501830B1 (en) | 2011-10-05 |
| AU2003233963A1 (en) | 2003-11-17 |
| US20050176700A1 (en) | 2005-08-11 |
| MA27305A1 (fr) | 2005-05-02 |
| KR100783863B1 (ko) | 2007-12-10 |
| IS7545A (is) | 2004-11-22 |
| US7427613B2 (en) | 2008-09-23 |
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| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |