HRP20150305T1 - Postupak za pripravu intermedijera spojeva korisnih kao modulatori opioid receptora - Google Patents
Postupak za pripravu intermedijera spojeva korisnih kao modulatori opioid receptora Download PDFInfo
- Publication number
- HRP20150305T1 HRP20150305T1 HRP20150305TT HRP20150305T HRP20150305T1 HR P20150305 T1 HRP20150305 T1 HR P20150305T1 HR P20150305T T HRP20150305T T HR P20150305TT HR P20150305 T HRP20150305 T HR P20150305T HR P20150305 T1 HRP20150305 T1 HR P20150305T1
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- Prior art keywords
- alkyl
- aryl
- aminocarbonyl
- hydrogen
- group
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims 3
- 238000004519 manufacturing process Methods 0.000 title claims 2
- 102000003840 Opioid Receptors Human genes 0.000 title 1
- 108090000137 Opioid Receptors Proteins 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- -1 formylamino Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Classifications
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- 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
- C07D233/64—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 substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- 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
-
- 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
-
- 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
- A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
-
- 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
- A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
Claims (9)
1. Postupak za proizvodnju spoja formule D-9 iz spoja formule D-1, koji obuhvaća korake:
[image]
naznačen time što
R41a predstavlja aminokarbonil, C1-6 alkilaminokarbonil, ili (C1-6 alkil)2 aminokarbonil;
RD1 = H, C1-6 alkil, ili aril (C1-6) alkil;
R41 je izabran između: (C1-6)alkil, (C1-6)alkoksi, aril(C1-6)alkoksi, aril(C1-6)alkilkarboniloksi, heteroaril(C1-6) alkilkarboniloksi, heteroaril, hidroksi, halogen, aminosulfonil, formilamino, aminokarbonil, C1-6 alkilaminokarbonil, (C1-6alkil)2 aminokarbonil, heterociklilkarbonil, karboksi, ili cijano; i gdje je C1-6 alkil po izboru supstituiran sa amino, C1-6 alkilamino, ili (C1-6alkil)2 amino; i gdje je arilni dio aril(C1-6) alkilkarboniloksi po izboru supstituiran sa jednim do četiri supstituenata nezavisno izabrana iz grupe koju čine: (C1-6)alkil, (C1-6)alkoksi, halogen, cijano, amino, i hidroksi;
R6 je izabran iz grupe koju čine vodik i C1-6 alkil;
Ra i Rb su nezavisno izabrani iz grupe koju čine vodik, C1-6 alkil, i C1-6 alkoksikarbonil;
ili kada Ra i Rb nisu vodik, Ra i Rb su proizvoljno uzeti zajedno sa dušikom za koji su oba vezani da formiraju peto- do osmo-člani monociklični prsten; i
L je izabran iz grupe koju čine O, S i N (Rd); gdje Rd predstavlja vodik, C1-6 alkil, ili aril.
2. Postupak prema zahtjevu 1 naznačen time što R41 predstavlja (C1-6) alkil.
3. Postupak prema zahtjevu 1 naznačen time što L predstavlja kisik.
4. Postupak prema zahtjevu 1 naznačen time što R41a predstavlja aminokarbonil.
5. Postupak prema zahtjevu 1 naznačen time što RD1 predstavlja (C1-6) alkil.
6. Postupak prema zahtjevu 1 naznačen time što R6 predstavlja vodik.
7. Postupak prema zahtjevu 1 naznačen time što Ra predstavlja vodik.
8. Postupak prema zahtjevu 1 naznačen time što Rb predstavlja C1-6 alkoksikarbonil.
9. Postupak prema zahtjevu 1 koji obuhvaća slijedeće korake:
[image]
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55334204P | 2004-03-15 | 2004-03-15 | |
| EP12194058.9A EP2573068B9 (en) | 2004-03-15 | 2005-03-14 | Process for preparing intermediates of compounds useful as opioid receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20150305T1 true HRP20150305T1 (hr) | 2015-04-24 |
Family
ID=34962827
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110694T HRP20110694T1 (hr) | 2004-03-15 | 2011-09-28 | Novi spojevi kao modulatori opioidnog receptora |
| HRP20130800TT HRP20130800T1 (en) | 2004-03-15 | 2013-08-22 | Opioid receptor modulators |
| HRP20150305TT HRP20150305T1 (hr) | 2004-03-15 | 2015-03-18 | Postupak za pripravu intermedijera spojeva korisnih kao modulatori opioid receptora |
| HRP20161331TT HRP20161331T1 (hr) | 2004-03-15 | 2016-10-12 | Modulatori opioidnih receptora |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110694T HRP20110694T1 (hr) | 2004-03-15 | 2011-09-28 | Novi spojevi kao modulatori opioidnog receptora |
| HRP20130800TT HRP20130800T1 (en) | 2004-03-15 | 2013-08-22 | Opioid receptor modulators |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161331TT HRP20161331T1 (hr) | 2004-03-15 | 2016-10-12 | Modulatori opioidnih receptora |
Country Status (36)
| Country | Link |
|---|---|
| US (8) | US7741356B2 (hr) |
| EP (5) | EP2573068B9 (hr) |
| JP (1) | JP4778954B2 (hr) |
| KR (1) | KR101166342B1 (hr) |
| CN (2) | CN1950342B (hr) |
| AR (2) | AR048269A1 (hr) |
| AT (1) | ATE516274T1 (hr) |
| AU (1) | AU2005224091B2 (hr) |
| BR (1) | BRPI0508820B8 (hr) |
| CA (1) | CA2560047C (hr) |
| CR (1) | CR8655A (hr) |
| CY (3) | CY1111927T1 (hr) |
| DK (5) | DK3112352T3 (hr) |
| EC (1) | ECSP066856A (hr) |
| ES (5) | ES2533176T3 (hr) |
| HK (4) | HK1099016A1 (hr) |
| HR (4) | HRP20110694T1 (hr) |
| HU (2) | HUE029852T2 (hr) |
| IL (3) | IL178040A (hr) |
| LT (2) | LT2653465T (hr) |
| LU (1) | LUC00007I2 (hr) |
| ME (3) | ME02221B (hr) |
| MX (1) | MXPA06010642A (hr) |
| MY (1) | MY146972A (hr) |
| NL (1) | NL300865I2 (hr) |
| NO (3) | NO338203B1 (hr) |
| NZ (1) | NZ549842A (hr) |
| PH (1) | PH12012501640B1 (hr) |
| PL (4) | PL2573068T3 (hr) |
| PT (4) | PT2573068E (hr) |
| RS (4) | RS52933B (hr) |
| SI (4) | SI1725537T1 (hr) |
| TW (1) | TWI361069B (hr) |
| UA (1) | UA86053C2 (hr) |
| WO (1) | WO2005090315A1 (hr) |
| ZA (1) | ZA200608587B (hr) |
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| EP2573068B9 (en) | 2004-03-15 | 2015-08-26 | Janssen Pharmaceutica NV | Process for preparing intermediates of compounds useful as opioid receptor modulators |
| EA013261B1 (ru) | 2004-05-14 | 2010-04-30 | Янссен Фармацевтика, Н.В. | Опиоидные соединения, замещенные карбоксамидогруппой |
| PE20061329A1 (es) | 2004-12-15 | 2006-12-08 | Neuralab Ltd | Anticuerpos ab humanizados para mejorar la cognicion |
| US7629488B2 (en) * | 2005-03-14 | 2009-12-08 | Janssen Pharmaceutica N.V. | Process for the preparation of opioid modulators |
| JP5225098B2 (ja) * | 2005-12-14 | 2013-07-03 | ブリストル−マイヤーズ スクイブ カンパニー | 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ |
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