HUP0100836A2 - Oxamides as impdh inhibitors - Google Patents
Oxamides as impdh inhibitorsInfo
- Publication number
- HUP0100836A2 HUP0100836A2 HU0100836A HUP0100836A HUP0100836A2 HU P0100836 A2 HUP0100836 A2 HU P0100836A2 HU 0100836 A HU0100836 A HU 0100836A HU P0100836 A HUP0100836 A HU P0100836A HU P0100836 A2 HUP0100836 A2 HU P0100836A2
- Authority
- HU
- Hungary
- Prior art keywords
- hydrogen
- heterocyclyl
- lower alkyl
- impd
- halo
- Prior art date
Links
- 101150088003 IMPDH gene Proteins 0.000 title 1
- YIKSCQDJHCMVMK-UHFFFAOYSA-N Oxamide Chemical class NC(=O)C(N)=O YIKSCQDJHCMVMK-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- KWKRTNFTBCZAGB-UHFFFAOYSA-N n'-phenyloxamide Chemical class NC(=O)C(=O)NC1=CC=CC=C1 KWKRTNFTBCZAGB-UHFFFAOYSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 1
- 101710088194 Dehydrogenase Proteins 0.000 abstract 1
- GRSZFWQUAKGDAV-KQYNXXCUSA-N IMP Chemical compound O[C@@H]1[C@H](O)[C@@H](COP(O)(O)=O)O[C@H]1N1C(NC=NC2=O)=C2N=C1 GRSZFWQUAKGDAV-KQYNXXCUSA-N 0.000 abstract 1
- 239000002671 adjuvant Substances 0.000 abstract 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 230000001088 anti-asthma Effects 0.000 abstract 1
- 230000000844 anti-bacterial effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000002141 anti-parasite Effects 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- 239000000924 antiasthmatic agent Substances 0.000 abstract 1
- 239000003096 antiparasitic agent Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical class O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 abstract 1
- 229960003444 immunosuppressant agent Drugs 0.000 abstract 1
- 230000001861 immunosuppressant effect Effects 0.000 abstract 1
- 239000003018 immunosuppressive agent Substances 0.000 abstract 1
- 235000013902 inosinic acid Nutrition 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000003431 oxalo group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 238000009790 rate-determining step (RDS) Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
N-Phenyl-oxalamide derivatives (I) and their pharmaceutically acceptable salts. N-Phenyl-oxalamide derivatives of formula (I) and their pharmaceutically acceptable salts are new. [Image] R1>heterocyclyl; R2>hydrogen, lower alkyl or alkoxy, halo, hydroxy or cyano; R3>, R5> and R6>hydrogen, lower alkyl or alkoxy, halo or cyano; R4>hydrogen, lower (cyclo)alkyl, aryl or heterocyclyl; and R7> and R8>hydrogen or lower alkyl; or R4> and R8> together : heterocyclyl. Independent claims are also included for the following: (1) method for preparing (I); (2) intermediates (IV), similar to (I) but with NR4>R8> replaced by hydroxy; and (3) pharmaceutical composition containing (I), a carrier, diluent or adjuvant, optionally also additional therapeutic agents. ACTIVITY : Immunosuppressant; antiviral; antibacterial; antiparasitic; anti-inflammatory; anti-asthma; antiproliferative; cardiovascular; antitumor. MECHANISM OF ACTION : Inhibition of inosine monophosphate dehydrogenase (IMPD), which catalyzes the rate-determining step in de novo synthesis of guanine nucleotides. The compound tert-butyl [3-[[[3-methoxy-4-(5-oxazolyl)anilino]oxalyl]amino]benzyl] carbamate had ID50 for inhibition of IMPD of 0.036 MicroM.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0004392A GB0004392D0 (en) | 2000-02-24 | 2000-02-24 | Oxamide derivatives |
| GB0020322A GB0020322D0 (en) | 2000-08-17 | 2000-08-17 | Oxamide derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HU0100836D0 HU0100836D0 (en) | 2001-04-28 |
| HUP0100836A2 true HUP0100836A2 (en) | 2001-10-28 |
Family
ID=26243721
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0100836A HUP0100836A2 (en) | 2000-02-24 | 2001-02-21 | Oxamides as impdh inhibitors |
Country Status (9)
| Country | Link |
|---|---|
| CO (1) | CO5300390A1 (en) |
| CZ (1) | CZ2001667A3 (en) |
| HR (1) | HRP20010127A2 (en) |
| HU (1) | HUP0100836A2 (en) |
| ID (1) | ID29372A (en) |
| IL (1) | IL141543A0 (en) |
| MA (1) | MA26755A1 (en) |
| NO (1) | NO20010900L (en) |
| PL (1) | PL346098A1 (en) |
-
2001
- 2001-02-21 HR HRP20010127 patent/HRP20010127A2/en not_active Application Discontinuation
- 2001-02-21 CZ CZ2001667A patent/CZ2001667A3/en unknown
- 2001-02-21 HU HU0100836A patent/HUP0100836A2/en unknown
- 2001-02-21 IL IL14154301A patent/IL141543A0/en unknown
- 2001-02-22 ID IDP20010157D patent/ID29372A/en unknown
- 2001-02-22 MA MA26144A patent/MA26755A1/en unknown
- 2001-02-22 NO NO20010900A patent/NO20010900L/en not_active Application Discontinuation
- 2001-02-22 CO CO01014294A patent/CO5300390A1/en not_active Application Discontinuation
- 2001-02-23 PL PL34609801A patent/PL346098A1/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| HU0100836D0 (en) | 2001-04-28 |
| CO5300390A1 (en) | 2003-07-31 |
| HRP20010127A2 (en) | 2001-12-31 |
| PL346098A1 (en) | 2001-08-27 |
| CZ2001667A3 (en) | 2001-10-17 |
| MA26755A1 (en) | 2004-12-20 |
| NO20010900L (en) | 2001-08-27 |
| IL141543A0 (en) | 2002-03-10 |
| NO20010900D0 (en) | 2001-02-22 |
| ID29372A (en) | 2001-08-30 |
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