JP2005527523A5 - - Google Patents
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- JP2005527523A5 JP2005527523A5 JP2003575945A JP2003575945A JP2005527523A5 JP 2005527523 A5 JP2005527523 A5 JP 2005527523A5 JP 2003575945 A JP2003575945 A JP 2003575945A JP 2003575945 A JP2003575945 A JP 2003575945A JP 2005527523 A5 JP2005527523 A5 JP 2005527523A5
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- JP
- Japan
- Prior art keywords
- angiotensin
- medicament according
- hypertrophy
- active ingredient
- induced
- 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.)
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- 239000003814 drug Substances 0.000 claims description 18
- 206010020772 Hypertension Diseases 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- -1 4-pyrazinyl Chemical group 0.000 claims description 13
- 206010020880 Hypertrophy Diseases 0.000 claims description 13
- 239000004480 active ingredient Substances 0.000 claims description 12
- 102000005862 Angiotensin II Human genes 0.000 claims description 11
- 101800000733 Angiotensin-2 Proteins 0.000 claims description 11
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 claims description 11
- 125000000217 alkyl group Chemical group 0.000 claims description 11
- 229950006323 angiotensin ii Drugs 0.000 claims description 11
- 230000001404 mediated effect Effects 0.000 claims description 11
- 238000007634 remodeling Methods 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 7
- 230000002526 effect on cardiovascular system Effects 0.000 claims description 7
- 239000002253 acid Substances 0.000 claims description 6
- 125000002723 alicyclic group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 210000000748 cardiovascular system Anatomy 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- 125000000623 heterocyclic group Chemical group 0.000 claims description 3
- 230000001969 hypertrophic effect Effects 0.000 claims description 3
- 208000017169 kidney disease Diseases 0.000 claims description 3
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 108010055723 PDGF receptor tyrosine kinase Proteins 0.000 claims description 2
- 125000003277 amino group Chemical group 0.000 claims description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 230000006378 damage Effects 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 239000001301 oxygen Substances 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 206010019280 Heart failures Diseases 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 2
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- ZPBWCRDSRKPIDG-UHFFFAOYSA-N amlodipine benzenesulfonate Chemical compound OS(=O)(=O)C1=CC=CC=C1.CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl ZPBWCRDSRKPIDG-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229960002003 hydrochlorothiazide Drugs 0.000 claims 2
- 206010020871 hypertrophic cardiomyopathy Diseases 0.000 claims 2
- 201000009925 nephrosclerosis Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims 2
- 229960004699 valsartan Drugs 0.000 claims 2
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims 1
- CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 claims 1
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 claims 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 claims 1
- 102000015427 Angiotensins Human genes 0.000 claims 1
- 108010064733 Angiotensins Proteins 0.000 claims 1
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010056370 Congestive cardiomyopathy Diseases 0.000 claims 1
- 201000010046 Dilated cardiomyopathy Diseases 0.000 claims 1
- 108010061435 Enalapril Proteins 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 206010037368 Pulmonary congestion Diseases 0.000 claims 1
- 208000000924 Right ventricular hypertrophy Diseases 0.000 claims 1
- 229960002478 aldosterone Drugs 0.000 claims 1
- 239000002170 aldosterone antagonist Substances 0.000 claims 1
- 229940083712 aldosterone antagonist Drugs 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000005277 alkyl imino group Chemical group 0.000 claims 1
- 229960000528 amlodipine Drugs 0.000 claims 1
- 229960004005 amlodipine besylate Drugs 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 210000001367 artery Anatomy 0.000 claims 1
- 229960005370 atorvastatin Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 claims 1
- 229960000873 enalapril Drugs 0.000 claims 1
- 230000008753 endothelial function Effects 0.000 claims 1
- 229960001208 eplerenone Drugs 0.000 claims 1
- JUKPWJGBANNWMW-VWBFHTRKSA-N eplerenone Chemical compound C([C@@H]1[C@]2(C)C[C@H]3O[C@]33[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)C(=O)OC)C[C@@]21CCC(=O)O1 JUKPWJGBANNWMW-VWBFHTRKSA-N 0.000 claims 1
- 229950011548 fadrozole Drugs 0.000 claims 1
- 229960003765 fluvastatin Drugs 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001631 hypertensive effect Effects 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
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- 230000003647 oxidation Effects 0.000 claims 1
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- 229960002797 pitavastatin Drugs 0.000 claims 1
- VGYFMXBACGZSIL-MCBHFWOFSA-N pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical class 0.000 claims 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical class NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 1
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- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims 1
- 230000036454 renin-angiotensin system Effects 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
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- 229920006395 saturated elastomer Polymers 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 229910052717 sulfur Chemical group 0.000 description 1
- 239000011593 sulfur Chemical group 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
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| GB0206216A GB0206216D0 (en) | 2002-03-15 | 2002-03-15 | Organic compounds |
| GB0206217A GB0206217D0 (en) | 2002-03-15 | 2002-03-15 | Organic compounds |
| GB0217505A GB0217505D0 (en) | 2002-07-29 | 2002-07-29 | Organic compounds |
| PCT/EP2003/002709 WO2003077892A2 (en) | 2002-03-15 | 2003-03-14 | 4-(4-methylpiperazin-1-ylmethyl)-n-[4-methyl-3(4-pyridin-3-yl)pyrimidin-2-yl-amino)phenyl]-benzamide for treating ang ii-mediated diseases |
Publications (2)
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| JP2005527523A JP2005527523A (ja) | 2005-09-15 |
| JP2005527523A5 true JP2005527523A5 (https=) | 2006-08-03 |
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| Country | Link |
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| US (1) | US20050124624A1 (https=) |
| EP (1) | EP1487424B1 (https=) |
| JP (1) | JP2005527523A (https=) |
| AT (1) | ATE339197T1 (https=) |
| AU (1) | AU2003233946A1 (https=) |
| CY (1) | CY1105839T1 (https=) |
| DE (1) | DE60308337T2 (https=) |
| DK (1) | DK1487424T3 (https=) |
| ES (1) | ES2274234T3 (https=) |
| PT (1) | PT1487424E (https=) |
| WO (1) | WO2003077892A2 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US20060154936A1 (en) * | 2002-10-25 | 2006-07-13 | Lasky Joseph A | Use of n-'5-'4-(4-methylpiperaziomethyl)-benzoylamido!-2-methylphenyl!-4-(3-pyridyl)2-pyridine-amine for the treatment of pulmonary hypertension |
| US20050192314A1 (en) | 2003-11-13 | 2005-09-01 | Ambit Biosciences Corporation | Urea derivatives as C-kit modulators |
| CA2552759A1 (en) * | 2004-01-22 | 2005-08-04 | Novartis Ag | Combination of organic compounds |
| GB0401761D0 (en) * | 2004-01-27 | 2004-03-03 | Novartis Ag | Organic compounds |
| AR047530A1 (es) * | 2004-02-04 | 2006-01-25 | Novartis Ag | Formas de sal de 4-(4-metilpiperazin-1-ilmetil)-n-(4-metil-3-(4-piridin-3-il)pirimidin-2-ilamino)fenil)-benzamida |
| MY148074A (en) * | 2005-05-10 | 2013-02-28 | Novartis Ag | Pharmaceutical compositions comprising imatinib and a release retardant |
| EP1741432A1 (de) * | 2005-07-07 | 2007-01-10 | Universitätsklinikum Freiburg | Tyrosinkinase-Inhibitor Imatinib zur Behandlung von Bluthochdruck |
| DE102005042544A1 (de) * | 2005-09-07 | 2007-03-08 | Ernst-Moritz-Arndt-Universität | Beeinflussung des kardialen Fc-Rezeptors zur Behandlung der dilatativen Kardiomyopathie |
| US20090304625A1 (en) * | 2006-01-18 | 2009-12-10 | Ahsan Husain | Modulators of cardiac cell hypertrophy and hyperplasia |
| EP1996582A2 (en) * | 2006-03-13 | 2008-12-03 | Encysive Pharmaceuticals, Inc | Polymorphs of n-(4-chloro-3-methyl-5-isoxazolyl)2-ý2-methyl-4,5-(methylenedioxy) phenylacetyl¨thiophene-3-sulfonamide, sodium salt |
| MX2008011842A (es) * | 2006-03-13 | 2008-10-02 | Encysive Pharmaceuticals Inc | Procedimientos y composiciones para el tratamiento de insuficiencia cardiaca diastolica. |
| CA2662265A1 (en) * | 2006-09-01 | 2008-03-06 | Teva Pharmaceutical Industries Ltd. | Imatinib compositions |
| TW201006823A (en) * | 2008-07-14 | 2010-02-16 | Novartis Ag | Use of pyrimidylaminobenzamide derivatives for the treatment of fibrosis |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2020245208A1 (en) | 2019-06-04 | 2020-12-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN121712504A (zh) * | 2023-07-27 | 2026-03-20 | 矿物疗法公司 | 用洛伦司他及两种或更多种降压药的组合治疗高血压的方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| US20010051631A1 (en) * | 1994-07-15 | 2001-12-13 | Muneo Takatani | Tricyclic compounds, their production and use |
| DK0831910T3 (da) * | 1995-06-07 | 2002-05-21 | Searle & Co | Kombinationsterapi med epoxy-steroid aldosteronantagonist og angiotensin II-receptorantagonist til behandling af kongestivt hjertesvigt |
| CO4940418A1 (es) * | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
-
2003
- 2003-03-14 AU AU2003233946A patent/AU2003233946A1/en not_active Abandoned
- 2003-03-14 US US10/507,642 patent/US20050124624A1/en not_active Abandoned
- 2003-03-14 EP EP03727265A patent/EP1487424B1/en not_active Expired - Lifetime
- 2003-03-14 DE DE60308337T patent/DE60308337T2/de not_active Expired - Lifetime
- 2003-03-14 PT PT03727265T patent/PT1487424E/pt unknown
- 2003-03-14 WO PCT/EP2003/002709 patent/WO2003077892A2/en not_active Ceased
- 2003-03-14 AT AT03727265T patent/ATE339197T1/de active
- 2003-03-14 JP JP2003575945A patent/JP2005527523A/ja active Pending
- 2003-03-14 DK DK03727265T patent/DK1487424T3/da active
- 2003-03-14 ES ES03727265T patent/ES2274234T3/es not_active Expired - Lifetime
-
2006
- 2006-12-11 CY CY20061101774T patent/CY1105839T1/el unknown
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