HUP0100024A2 - Alzheimer-kór kezelésére szolgáló hatóanyagként karvedilolszármazékokat tartalmazó gyógyszerkészítmények - Google Patents
Alzheimer-kór kezelésére szolgáló hatóanyagként karvedilolszármazékokat tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0100024A2 HUP0100024A2 HU0100024A HUP0100024A HUP0100024A2 HU P0100024 A2 HUP0100024 A2 HU P0100024A2 HU 0100024 A HU0100024 A HU 0100024A HU P0100024 A HUP0100024 A HU P0100024A HU P0100024 A2 HUP0100024 A2 HU P0100024A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- carbon atoms
- hydrogen atom
- active ingredient
- hydroxy
- Prior art date
Links
- 239000004480 active ingredient Substances 0.000 title abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 title 1
- 229960004195 carvedilol Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 abstract 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 241000790917 Dioxys <bee> Species 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 239000002160 alpha blocker Substances 0.000 abstract 1
- 102000015007 alpha-adrenergic receptor activity proteins Human genes 0.000 abstract 1
- 108040006816 alpha-adrenergic receptor activity proteins Proteins 0.000 abstract 1
- 206010002022 amyloidosis Diseases 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- -1 benzyl- Chemical group 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000001038 naphthoyl group Chemical group C1(=CC=CC2=CC=CC=C12)C(=O)* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004344 phenylpropyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 abstract 1
- 125000004149 thio group Chemical group *S* 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Abstract
A találmány tárgya amiloid betegségek kezelésére szolgálógyógyszerkészítmények, amelyek hatóanyagként egy kettős nemszelektív<-adrenoceptor és a1-adrenoceptor antagonista vegyületet, előnyösenegy (I) általános képletű vegyületet - amelynek képletében R7-R13jelentése egymástól függetlenül hidrogénatom vagy hidroxicsoport; és Ajelentése hidrogénatom, hidroxicsoport vagy egy (II) általános képletűcsoport, amelyben R1 jelentése hidrogénatom, legfeljebb 6 szénatomosalkanoilcsoport vagy egy, a benzoil- és naftoilcsoport közülkiválasztott aril-karbonil-csoport, R2 jelentése hidrogénatom,legfeljebb 6 szénatomos alkanoilcsoport vagy egy, a benzil-, fenil-etil- és fenil-propil-csoport közül kiválasztott aril-alkil-csoport,R3 jelentése hidrogénatom vagy legfeljebb 6 szénatomos alkilcsoport,R4 jelentése hidrogénatom vagy legfeljebb 6 szénatomos alkilcsoport,vagy ha X jelentése oxicsoport, akkor R4 és R5 együtt -CH2-O- képletűcsoportot képezhet, X jelentése vegyértékkötés, metiléncsoport, oxi-vagy tiocsoport, Ar jelentése fenil-, naftil-, indanil- vagytetrahidronaftilcsoport, R5 és R6 jelentése egymástól függetlenül hidrogén-, fluor-, klór-,brómatom, hidroxicsoport, legfeljebb 6 szénatomos alkilcsoport,karbamoilcsoport, legfeljebb 6 szénatomos alkoxicsoport, benzil-oxi--csoport, legfeljebb 6 szénatomos alkil-tio-csoport, legfeljebb 6szénatomos alkil-szulfinil-csoport vagy legfeljebb 6 szénatomos alkil-szulfonil-csoport, vagy R5 és R6 együtt metil-dioxi-csoportot képez -vagy gyógyászatilag elfogadható sójának hatásos mennyiségéttartalmazzák. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US6236697P | 1997-10-15 | 1997-10-15 | |
PCT/US1998/021789 WO1999018794A1 (en) | 1997-10-15 | 1998-10-15 | Method for treating alzheimer's disease |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0100024A2 true HUP0100024A2 (hu) | 2001-07-30 |
HUP0100024A3 HUP0100024A3 (en) | 2002-12-28 |
Family
ID=22042015
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0100024A HUP0100024A3 (en) | 1997-10-15 | 1998-10-15 | Pharmaceutical compositions for treating alzheimer's disease containing carvedilol as active ingredient |
Country Status (16)
Country | Link |
---|---|
US (1) | US6358990B1 (hu) |
EP (1) | EP1024697A4 (hu) |
JP (1) | JP2001519364A (hu) |
KR (1) | KR100573352B1 (hu) |
CN (1) | CN1281334A (hu) |
AU (1) | AU751526B2 (hu) |
BR (1) | BR9814075A (hu) |
CA (1) | CA2305262A1 (hu) |
HU (1) | HUP0100024A3 (hu) |
IL (1) | IL135584A (hu) |
NO (1) | NO20001869L (hu) |
NZ (1) | NZ504419A (hu) |
PL (1) | PL339910A1 (hu) |
TR (1) | TR200001018T2 (hu) |
WO (1) | WO1999018794A1 (hu) |
ZA (1) | ZA989365B (hu) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE10142175A1 (de) * | 2001-10-09 | 2003-03-27 | Eucro Europe Contract Res Gmbh | Verwendung von ß-Adrenozeptor-Agonisten zur Behandlung von neurodegenerativen Erkrankungen |
US8101209B2 (en) * | 2001-10-09 | 2012-01-24 | Flamel Technologies | Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles |
EP1499310A4 (en) * | 2002-04-30 | 2005-12-07 | Sb Pharmco Inc | MONOCITRATE MONOHYDRATE OF CARVEDILOL |
CN103254114A (zh) * | 2002-06-27 | 2013-08-21 | 史密斯克莱.比奇曼(科克)有限公司 | 卡维地洛磷酸盐和/或其溶剂合物相应的组合物和/或治疗方法 |
JP2005533822A (ja) * | 2002-06-27 | 2005-11-10 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | 臭化水素酸カルベジロール |
JP2007512350A (ja) * | 2003-11-25 | 2007-05-17 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | カルベジロール組成物の治療および送達方法 |
US8734850B2 (en) * | 2003-11-25 | 2014-05-27 | Flamel Technologies | Oral medicinal product with modified release of at least one active principle in multimicrocapsular form |
JP2007512372A (ja) * | 2003-11-25 | 2007-05-17 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | カルベジロール塩、対応する組成物、送達および/または治療方法 |
CN1991364A (zh) | 2005-12-26 | 2007-07-04 | 中国科学院上海生命科学研究院 | 预防和治疗阿尔兹海默症的g蛋白偶联受体拮抗剂 |
EP2007385A4 (en) * | 2006-03-23 | 2010-08-18 | Sinai School Medicine | CARDIOVASCULAR COMPOSITION AND ITS USE FOR THE TREATMENT OF MORBUS ALZHEIMER |
WO2008021552A2 (en) * | 2006-08-18 | 2008-02-21 | Duke University | Biased ligands and methods of identifying same |
US20090076116A1 (en) * | 2007-09-13 | 2009-03-19 | Protia, Llc | Deuterium-enriched carvediolo |
PL2247558T3 (pl) | 2008-02-14 | 2022-05-02 | Eli Lilly And Company | Nowe środki obrazujące do wykrywania czynnościowych zaburzeń neurologicznych |
US8932557B2 (en) | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
CN103172643B (zh) * | 2011-12-26 | 2016-03-02 | 中国医学科学院药物研究所 | 黄皮咔唑生物碱及其制备方法和其药物组合物与用途 |
CN102816107B (zh) * | 2012-08-20 | 2015-06-03 | 东南大学 | 咔唑衍生物及其制备方法与用途 |
KR20160026897A (ko) * | 2013-06-27 | 2016-03-09 | 세다르스-신나이 메디칼 센터 | 신경퇴행성 질환의 예방 및 치료를 위한 아드레날린 수용체 길항제 |
EP4213836A1 (en) * | 2020-09-17 | 2023-07-26 | UTI Limited Partnership | Methods of treating and/or preventing alzheimer's disease with r-carvedilol |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2815926A1 (de) * | 1978-04-13 | 1979-10-18 | Boehringer Mannheim Gmbh | Neue carbazolyl-(4)-oxy-propanolamin-derivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
DE3319027A1 (de) * | 1983-05-26 | 1984-11-29 | Boehringer Mannheim Gmbh, 6800 Mannheim | Verfahren zur herstellung von optisch aktiven carbazol-derivaten, neue r- und s-carbazol-derivate, sowie arzneimittel, die diese verbindungen enthalten |
PH25025A (en) * | 1986-12-17 | 1991-01-28 | Glaxo Group Ltd | A method of treating dementia and other cognitive disorders using 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1h-imidazol-1-yl)methyl)-4h-carbazol-4-one |
US4868190A (en) * | 1988-12-27 | 1989-09-19 | Hoechst-Roussel Pharmaceuticals, Inc. | N-pyridinyl-9H-carbazol-9-amines |
US4983608A (en) | 1989-09-05 | 1991-01-08 | Hoechst-Roussell Pharmaceuticals, Inc. | N-substituted-4-pyrimidinamines and pyrimidinediamines |
JPH0558998A (ja) * | 1991-09-06 | 1993-03-09 | Taisho Pharmaceut Co Ltd | カルバゾール誘導体 |
CA2196046A1 (en) * | 1994-07-27 | 1996-02-08 | Nigel Birdsall | Heterocyclic compounds, useful as allosteric effectors at muscarinic receptors |
FR2724933A1 (fr) * | 1994-09-22 | 1996-03-29 | Pf Medicament | Nouveaux ethers aromatiques derives d'indoles utiles comme medicaments |
US5760069A (en) * | 1995-02-08 | 1998-06-02 | Boehringer Mannheim Pharmaceuticals Corporation-Smithkline Beecham Corporation Limited Partnership #1 | Method of treatment for decreasing mortality resulting from congestive heart failure |
FR2731222A1 (fr) * | 1995-03-02 | 1996-09-06 | Pf Medicament | Nouveaux derives de piperazine aminoindoles cycliques, leur procede de preparation et leur utilisation a titre de medicaments |
EP1110945A3 (en) * | 1995-05-01 | 2003-05-07 | University Of Pittsburgh | Azocompounds for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
-
1998
- 1998-10-14 ZA ZA989365A patent/ZA989365B/xx unknown
- 1998-10-15 WO PCT/US1998/021789 patent/WO1999018794A1/en not_active Application Discontinuation
- 1998-10-15 BR BR9814075-2A patent/BR9814075A/pt not_active IP Right Cessation
- 1998-10-15 TR TR2000/01018T patent/TR200001018T2/xx unknown
- 1998-10-15 IL IL13558498A patent/IL135584A/en not_active IP Right Cessation
- 1998-10-15 KR KR1020007003990A patent/KR100573352B1/ko not_active IP Right Cessation
- 1998-10-15 EP EP98953558A patent/EP1024697A4/en not_active Withdrawn
- 1998-10-15 HU HU0100024A patent/HUP0100024A3/hu unknown
- 1998-10-15 JP JP2000515438A patent/JP2001519364A/ja active Pending
- 1998-10-15 PL PL98339910A patent/PL339910A1/xx unknown
- 1998-10-15 CN CN98812171A patent/CN1281334A/zh active Pending
- 1998-10-15 US US09/529,526 patent/US6358990B1/en not_active Expired - Fee Related
- 1998-10-15 CA CA002305262A patent/CA2305262A1/en not_active Abandoned
- 1998-10-15 AU AU10897/99A patent/AU751526B2/en not_active Ceased
- 1998-10-15 NZ NZ504419A patent/NZ504419A/xx unknown
-
2000
- 2000-04-11 NO NO20001869A patent/NO20001869L/no unknown
Also Published As
Publication number | Publication date |
---|---|
HUP0100024A3 (en) | 2002-12-28 |
US6358990B1 (en) | 2002-03-19 |
CA2305262A1 (en) | 1999-04-22 |
CN1281334A (zh) | 2001-01-24 |
EP1024697A1 (en) | 2000-08-09 |
EP1024697A4 (en) | 2007-05-02 |
NO20001869D0 (no) | 2000-04-11 |
BR9814075A (pt) | 2000-09-26 |
WO1999018794A1 (en) | 1999-04-22 |
AU751526B2 (en) | 2002-08-22 |
TR200001018T2 (tr) | 2000-08-21 |
ZA989365B (en) | 1999-04-15 |
KR20010031108A (ko) | 2001-04-16 |
IL135584A0 (en) | 2001-05-20 |
NO20001869L (no) | 2000-06-14 |
PL339910A1 (en) | 2001-01-15 |
IL135584A (en) | 2005-12-18 |
AU1089799A (en) | 1999-05-03 |
JP2001519364A (ja) | 2001-10-23 |
NZ504419A (en) | 2002-11-26 |
KR100573352B1 (ko) | 2006-04-25 |
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