HUP0203438A2 - Foszfodiészteráz gátló hatású 5-(2-helyettesített-5-heterociklilszulfonilpirid-3-il)-dihidropirazolo[4,3-d]-pirimidin-7-on-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Foszfodiészteráz gátló hatású 5-(2-helyettesített-5-heterociklilszulfonilpirid-3-il)-dihidropirazolo[4,3-d]-pirimidin-7-on-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0203438A2 HUP0203438A2 HU0203438A HUP0203438A HUP0203438A2 HU P0203438 A2 HUP0203438 A2 HU P0203438A2 HU 0203438 A HU0203438 A HU 0203438A HU P0203438 A HUP0203438 A HU P0203438A HU P0203438 A2 HUP0203438 A2 HU P0203438A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- het
- group
- substituents
- optionally substituted
- Prior art date
Links
- 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 title 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 abstract 1
- 101150085511 PEDS1 gene Proteins 0.000 abstract 1
- 102100037592 Plasmanylethanolamine desaturase Human genes 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- -1 cyano- Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 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
- 229920003199 poly(diethylsiloxane) Polymers 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
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
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Reproductive Health (AREA)
- General Health & Medical Sciences (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
A találmány az (I) általános képletű vegyületre, továbbá ennek humánvagy állatorvosi gyógyászatban elfogadható sójára és/vagy szolvátjáravonatkozik. Az (I) általános képletben X jelentése oxigénatom vagy -NR5- általános képletű csoport , R1 jelentése hidrogénatom, kisszénatomszámú alkil-, Het-, alkil-Het-, aril- vagy alkilarilcsoport,amely utóbbi öt csoport mindegyike adott esetben egy vagy többhelyettesítővel helyettesített, R2 jelentése hidrogénatom,halogénatom, ciano- vagy nitrocsoport, -OR6, -OC(O)R7, -C(O)R8, -C(O)OR9, - C(O)NR10R11, -NR12R13 és/vagy -SO2NR14R15 altalános képletűcsoport, kis szénatomszámú alkil-, Het-, alkil-Het-, aril- vagyalkilarilcsoport, amely utóbbi öt csoport adott esetben egy vagy többhelyettesítővel helyettesített. R3 jelentése hidrogénatom, kisszénatomszámú alkil-, alkil-Het- vagy alkilarilcsoport, amely utóbbihárom csoport mindegyike adott esetben egy vagy több helyettesítővelhelyettesített; R4 jelentése hidrogénatom, halogénatom, ciano-, nitro-vagy halogén-(kis szénatomszámú alkil)-csoport, -OR6, -OC(O)R7, -C(O)R8, -C(O)OR9, - C(O)NR10R11, -NR12R13, -NR16Y(O)R17, -N[Y(O)R17]2,-SOR18, -SO2R19, -C(O)AZ általános képletű csoport, kis szénatomszámúalkil-, kis szénatomszámú alkenil-, kis szénatomszámú alkinil-, Het-,alkil-Het-, aril-, alkilarilcsoport, amely utóbbi hét csoportmindegyike adott esetben egy vagy több helyettesítővel helyettesített.A találmány kiterjed a fenti vegyületek előállítására, az ezekettartalmazó gyógyászati készítményekre, valamint ezek olyan betegségekkezelésére történő alkalmazására, ahol cGMP PDES gátlására vanszükség. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9924041.8A GB9924041D0 (en) | 1999-10-11 | 1999-10-11 | Pharmaceutically active compounds |
GB0018660A GB0018660D0 (en) | 2000-07-28 | 2000-07-28 | Pharmaceutically active compounds |
PCT/IB2000/001430 WO2001027112A1 (en) | 1999-10-11 | 2000-10-04 | 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)-dihydropyrazolo[4,3-d]pyrimidin-7-ones as phosphodiesterase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0203438A2 true HUP0203438A2 (hu) | 2003-01-28 |
HUP0203438A3 HUP0203438A3 (en) | 2003-05-28 |
Family
ID=26244758
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0203438A HUP0203438A3 (en) | 1999-10-11 | 2000-10-04 | 5-(2-substituted-5-heterocyclysulphonylpyrid-3-yl)-dihydropyrazolo[4,3-d]pyrimidin-7-ones as phosphodiesterase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Country Status (34)
Country | Link |
---|---|
US (1) | US6756373B1 (hu) |
EP (1) | EP1222190A1 (hu) |
JP (1) | JP2003511452A (hu) |
KR (1) | KR20020038941A (hu) |
CN (1) | CN1378547A (hu) |
AP (1) | AP2002002455A0 (hu) |
AR (1) | AR022665A1 (hu) |
AU (1) | AU7547900A (hu) |
BG (1) | BG106568A (hu) |
BR (1) | BR0014695A (hu) |
CA (1) | CA2387353A1 (hu) |
CO (1) | CO5261539A1 (hu) |
CZ (1) | CZ20021151A3 (hu) |
DZ (1) | DZ3218A1 (hu) |
EA (1) | EA200200240A1 (hu) |
EE (1) | EE200200192A (hu) |
GT (1) | GT200000168A (hu) |
HK (1) | HK1049834A1 (hu) |
HU (1) | HUP0203438A3 (hu) |
IL (1) | IL149025A0 (hu) |
IS (1) | IS6288A (hu) |
MA (1) | MA26824A1 (hu) |
NO (1) | NO20021695L (hu) |
NZ (1) | NZ517324A (hu) |
OA (1) | OA12058A (hu) |
PA (1) | PA8504401A1 (hu) |
PE (1) | PE20010736A1 (hu) |
PL (1) | PL357522A1 (hu) |
SK (1) | SK4562002A3 (hu) |
SV (1) | SV2002000192A (hu) |
TN (1) | TNSN00198A1 (hu) |
TR (1) | TR200200954T2 (hu) |
UY (1) | UY26383A1 (hu) |
WO (1) | WO2001027112A1 (hu) |
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JP2022543155A (ja) | 2019-08-06 | 2022-10-07 | インサイト・コーポレイション | Hpk1阻害剤の固体形態 |
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- 2000-10-04 WO PCT/IB2000/001430 patent/WO2001027112A1/en not_active Application Discontinuation
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- 2000-10-04 EP EP00964557A patent/EP1222190A1/en not_active Withdrawn
- 2000-10-04 DZ DZ003218A patent/DZ3218A1/fr active
- 2000-10-04 CN CN00814083A patent/CN1378547A/zh active Pending
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