AR041589A1 - PERIPHERALLY SELECTIVE DOPAMINE-BETA-HYDROXYLASE INHIBITORS AND METHOD FOR PREPARATION - Google Patents
PERIPHERALLY SELECTIVE DOPAMINE-BETA-HYDROXYLASE INHIBITORS AND METHOD FOR PREPARATIONInfo
- Publication number
- AR041589A1 AR041589A1 ARP030103711A ARP030103711A AR041589A1 AR 041589 A1 AR041589 A1 AR 041589A1 AR P030103711 A ARP030103711 A AR P030103711A AR P030103711 A ARP030103711 A AR P030103711A AR 041589 A1 AR041589 A1 AR 041589A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- term
- preparation
- alkyloxy
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 108010015720 Dopamine beta-Hydroxylase Proteins 0.000 title 1
- 102100033156 Dopamine beta-hydroxylase Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 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 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- -1 hydroxy, nitro, amino Chemical group 0.000 abstract 2
- 206010007558 Cardiac failure chronic Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition 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
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D487/22—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 four or more hetero rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/409—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 having four such rings, e.g. porphine derivatives, bilirubin, biliverdine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
- C07D233/84—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos con propiedades farmacéuticas potencialmente valiosas para el tratamiento de trastornos cardiovasculares tales como la hipertensión y la insuficiencia cardíaca crónica. También reivindica, composición farmacéutica, uso para preparación de medicamentos, procesos e intermediarios. Reivindicación 1: Un compuesto de fórmula (1) donde R1, R2, y R3 son iguales o diferentes y significan hidrógenos, halógenos, grupo alquilo, alquiloxi, hidroxi, nitro, amino, alquilcarbonilamino, alquilamino o dialquilamino; R4 significa H, grupo alquilo o alquilarilo; X significa CH2, átomo de O o átomo de S; n es 1, 2 o 3, con la condición de que cuando n es 1, X no es CH2; y los enantiómeros ( R )y (S) individuales o mezclas de enantiómeros y sus sales farmacéuticamente aceptables; donde el término alquilo significa cadenas de hidrocarburos, rectas o ramificadas que contienen entre 1 y 6 átomos de C, opcionalmente sustituidas con grupos arilo, alcoxi, halógeno, alcoxicarbonilo o hidroxicarbonilo; el término arilo significa un grupo fenilo o naftilo, opcionalmente sustituido con un grupo alquiloxi, halógeno o nitro; el término halógeno significa F, Cl, Br, o I .Compounds with potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure. It also claims, pharmaceutical composition, use for preparation of medicines, processes and intermediaries. Claim 1: A compound of formula (1) wherein R1, R2, and R3 are the same or different and mean hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino groups; R4 means H, alkyl or alkylaryl group; X means CH2, O atom or S atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R) and (S) enantiomers or mixtures of enantiomers and their pharmaceutically acceptable salts; where the term "alkyl" means straight or branched hydrocarbon chains containing between 1 and 6 C atoms, optionally substituted with aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term "aryl" means a phenyl or naphthyl group, optionally substituted with an alkyloxy, halogen or nitro group; the term halogen means F, Cl, Br, or I.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0223719A GB2393958A (en) | 2002-10-11 | 2002-10-11 | Peripherally-selective imidazole inhibitors of dopamine-beta-hydroxylase |
GB0224306A GB2394223B (en) | 2002-10-11 | 2002-10-18 | Peripherally-selective inhibitors of dopamine-beta-hydroxylase and method of their preparation |
Publications (1)
Publication Number | Publication Date |
---|---|
AR041589A1 true AR041589A1 (en) | 2005-05-26 |
Family
ID=9945777
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030103711A AR041589A1 (en) | 2002-10-11 | 2003-10-10 | PERIPHERALLY SELECTIVE DOPAMINE-BETA-HYDROXYLASE INHIBITORS AND METHOD FOR PREPARATION |
ARP140101283A AR095674A2 (en) | 2002-10-11 | 2014-03-18 | PERIPHERALLY SELECTIVE DOPAMINE-B-HYDROXYLASE INHIBITORS AND METHOD FOR PREPARATION |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP140101283A AR095674A2 (en) | 2002-10-11 | 2014-03-18 | PERIPHERALLY SELECTIVE DOPAMINE-B-HYDROXYLASE INHIBITORS AND METHOD FOR PREPARATION |
Country Status (11)
Country | Link |
---|---|
KR (1) | KR101350741B1 (en) |
CN (1) | CN100393715C (en) |
AR (2) | AR041589A1 (en) |
AT (5) | ATE500248T1 (en) |
CY (2) | CY1108452T1 (en) |
DE (4) | DE60336772D1 (en) |
DK (2) | DK1408038T3 (en) |
ES (5) | ES2384118T3 (en) |
GB (2) | GB2393958A (en) |
HK (1) | HK1116188A1 (en) |
SI (2) | SI1408038T1 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0708818D0 (en) * | 2007-05-08 | 2007-06-13 | Portela & Ca Sa | Compounds |
CN103380128B (en) * | 2010-12-22 | 2017-03-01 | 拜欧波尔特拉及正大有限公司 | Crystal formation and preparation method thereof |
GB201316410D0 (en) * | 2013-09-13 | 2013-10-30 | Bial Portela & Ca Sa | Processes for preparing peripherally-selective inhibitors of dopamine-?-hydroxylase and intermediates for use therein |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL82401A0 (en) * | 1986-05-06 | 1987-11-30 | Merrell Dow Pharma | Dopamine beta hydroxy-lase inhibiting imidazole derivatives and pharmaceutical compositions containing them |
US4868210A (en) | 1988-03-30 | 1989-09-19 | Warner-Lambert Company | Antihyperlipidemic and antiatherosclerotic compounds and compositions |
EP0757677B1 (en) * | 1994-04-26 | 2003-06-18 | Syntex (U.S.A.) LLC | Benzocyclohexylimidazolethione derivatives |
-
2002
- 2002-10-11 GB GB0223719A patent/GB2393958A/en not_active Withdrawn
- 2002-10-18 GB GB0224306A patent/GB2394223B/en not_active Expired - Lifetime
-
2003
- 2003-10-10 ES ES07076123T patent/ES2384118T3/en not_active Expired - Lifetime
- 2003-10-10 DE DE60336772T patent/DE60336772D1/en not_active Expired - Lifetime
- 2003-10-10 DE DE60336275T patent/DE60336275D1/en not_active Expired - Lifetime
- 2003-10-10 DE DE60322642T patent/DE60322642D1/en not_active Expired - Lifetime
- 2003-10-10 AT AT07076122T patent/ATE500248T1/en not_active IP Right Cessation
- 2003-10-10 AT AT03256420T patent/ATE403652T1/en active
- 2003-10-10 SI SI200331309T patent/SI1408038T1/en unknown
- 2003-10-10 AR ARP030103711A patent/AR041589A1/en active IP Right Grant
- 2003-10-10 DK DK03256420T patent/DK1408038T3/en active
- 2003-10-10 DK DK07076125.9T patent/DK1908760T3/en active
- 2003-10-10 AT AT07076125T patent/ATE505465T1/en active
- 2003-10-10 AT AT07076124T patent/ATE500247T1/en not_active IP Right Cessation
- 2003-10-10 AT AT07076123T patent/ATE550335T1/en active
- 2003-10-10 ES ES07076122T patent/ES2361938T3/en not_active Expired - Lifetime
- 2003-10-10 ES ES07076125T patent/ES2364919T3/en not_active Expired - Lifetime
- 2003-10-10 DE DE60336276T patent/DE60336276D1/en not_active Expired - Lifetime
- 2003-10-10 ES ES07076124T patent/ES2361939T3/en not_active Expired - Lifetime
- 2003-10-10 SI SI200331986T patent/SI1908760T1/en unknown
- 2003-10-10 ES ES03256420T patent/ES2309279T3/en not_active Expired - Lifetime
- 2003-10-10 CN CNB2003801059426A patent/CN100393715C/en not_active Expired - Fee Related
- 2003-10-10 KR KR1020127005102A patent/KR101350741B1/en active IP Right Grant
-
2008
- 2008-10-09 HK HK08111214.9A patent/HK1116188A1/en not_active IP Right Cessation
- 2008-10-24 CY CY20081101204T patent/CY1108452T1/en unknown
-
2011
- 2011-07-01 CY CY20111100639T patent/CY1112457T1/en unknown
-
2014
- 2014-03-18 AR ARP140101283A patent/AR095674A2/en unknown
Also Published As
Publication number | Publication date |
---|---|
AR095674A2 (en) | 2015-11-04 |
DE60336275D1 (en) | 2011-04-14 |
ES2364919T3 (en) | 2011-09-16 |
ATE500248T1 (en) | 2011-03-15 |
ATE550335T1 (en) | 2012-04-15 |
SI1908760T1 (en) | 2011-05-31 |
CY1112457T1 (en) | 2015-12-09 |
GB0223719D0 (en) | 2002-11-20 |
ES2384118T3 (en) | 2012-06-29 |
CY1108452T1 (en) | 2014-04-09 |
DK1408038T3 (en) | 2008-11-24 |
GB2394223A (en) | 2004-04-21 |
GB2393958A (en) | 2004-04-14 |
DK1908760T3 (en) | 2011-07-25 |
GB2394223B (en) | 2007-05-16 |
DE60336772D1 (en) | 2011-05-26 |
ATE500247T1 (en) | 2011-03-15 |
DE60336276D1 (en) | 2011-04-14 |
ATE505465T1 (en) | 2011-04-15 |
CN100393715C (en) | 2008-06-11 |
ES2309279T3 (en) | 2008-12-16 |
KR20120038014A (en) | 2012-04-20 |
ES2361938T3 (en) | 2011-06-24 |
ATE403652T1 (en) | 2008-08-15 |
ES2361939T3 (en) | 2011-06-24 |
KR101350741B1 (en) | 2014-01-10 |
SI1408038T1 (en) | 2008-10-31 |
CN1726211A (en) | 2006-01-25 |
HK1116188A1 (en) | 2008-12-19 |
GB0224306D0 (en) | 2002-11-27 |
DE60322642D1 (en) | 2008-09-18 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant, registration |