HRP20030003B1 - N-oksidi kao predlijekovi antagonista nk1 receptora iz skupine derivata 4-fenil-piridina - Google Patents
N-oksidi kao predlijekovi antagonista nk1 receptora iz skupine derivata 4-fenil-piridinaInfo
- Publication number
- HRP20030003B1 HRP20030003B1 HR20030003A HRP20030003A HRP20030003B1 HR P20030003 B1 HRP20030003 B1 HR P20030003B1 HR 20030003 A HR20030003 A HR 20030003A HR P20030003 A HRP20030003 A HR P20030003A HR P20030003 B1 HRP20030003 B1 HR P20030003B1
- Authority
- HR
- Croatia
- Prior art keywords
- lower alkyl
- hydrogen
- phenyl
- halogen
- mutually independent
- Prior art date
Links
- 150000005362 4-phenylpyridines Chemical class 0.000 title 1
- 150000001204 N-oxides Chemical class 0.000 title 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 title 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 title 1
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- -1 cyclic tertiary amine Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 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
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Addiction (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Spoj, naznacen time, da se bira iz skupine spojeva prikazanih opcom formulom: u kojoj jeR vodik, nizi alkil, nizi alkoksi, halogen ili trifluorometil; R1 vodik ili halogen; iliR i R1 mogu isto tako biti prstenasti atomi ugljika na koje su vezani -CH=CH-CH=CH-;R2 i R2' su uzajamno neovisni vodik, halogen, trifluorometil, nizi alkoksi ili cijano,; iliR2 i R2' mogu isto tako biti -CH=CH-CH=CH-, po izboru supstituirani s jednim ili vise supstituenata odabranih izmedu nizeg alkila ili nizeg alkoksi; R3, R3' su uzajamno neovisni vodik, nizi alkil ili cikloalkil; R4, R4' su uzajamno neovisni -(CH2)mOR6 ili nizi alkil; iliR4 i R4' tvore zajedno s N-atomom na koji su vezani ciklicni tercijarni amin skupineR5 vodik, hidroksi, nizi alkil, -nizi alkoksi, -(CH2)mOH, -COOR3, -CON(R3)2, -N(R3)CO-nizi alkil ili -C(O)R3;R6 vodik, nizi alkil ili fenil; X predstavlja -C(O)N(R6)-, -N(R6)C(O)-, -(CH2)mO- ili -O(CH2)m-;n predstavlja 0, 1, 2, 3 ili 4; im predstavlja 1, 2 ili 3; i njihove farmaceutski prihvatljive kiselinske adicijske soli. Patent sadrzi jos 11 patentnih zahtjeva.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00115287 | 2000-07-14 | ||
PCT/EP2001/007850 WO2002006236A1 (en) | 2000-07-14 | 2001-07-09 | N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20030003A2 HRP20030003A2 (en) | 2003-02-28 |
HRP20030003B1 true HRP20030003B1 (hr) | 2011-01-31 |
Family
ID=8169262
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20030003A HRP20030003B1 (hr) | 2000-07-14 | 2003-01-02 | N-oksidi kao predlijekovi antagonista nk1 receptora iz skupine derivata 4-fenil-piridina |
Country Status (39)
Country | Link |
---|---|
US (4) | US6593472B2 (hr) |
EP (1) | EP1303490B1 (hr) |
JP (1) | JP3950044B2 (hr) |
KR (1) | KR100501608B1 (hr) |
CN (1) | CN1178917C (hr) |
AR (1) | AR029717A1 (hr) |
AT (1) | ATE400556T1 (hr) |
AU (1) | AU7061901A (hr) |
BR (1) | BRPI0112475B8 (hr) |
CA (1) | CA2415890C (hr) |
CY (1) | CY1108557T1 (hr) |
CZ (1) | CZ303639B6 (hr) |
DE (1) | DE60134749D1 (hr) |
DK (1) | DK1303490T3 (hr) |
EC (1) | ECSP034431A (hr) |
EG (1) | EG24968A (hr) |
ES (1) | ES2309075T3 (hr) |
GT (1) | GT200100137A (hr) |
HK (1) | HK1058198A1 (hr) |
HR (1) | HRP20030003B1 (hr) |
HU (1) | HU230316B1 (hr) |
IL (2) | IL153834A0 (hr) |
JO (1) | JO2372B1 (hr) |
MA (1) | MA26929A1 (hr) |
ME (1) | ME01311B (hr) |
MX (1) | MXPA03000366A (hr) |
MY (1) | MY154976A (hr) |
NO (1) | NO324700B1 (hr) |
NZ (1) | NZ523273A (hr) |
PA (1) | PA8522001A1 (hr) |
PE (1) | PE20020272A1 (hr) |
PL (1) | PL205207B1 (hr) |
PT (1) | PT1303490E (hr) |
RS (1) | RS50932B (hr) |
RU (1) | RU2266284C2 (hr) |
SI (1) | SI1303490T1 (hr) |
UY (1) | UY26839A1 (hr) |
WO (1) | WO2002006236A1 (hr) |
ZA (1) | ZA200210207B (hr) |
Families Citing this family (42)
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PT1103545E (pt) * | 1999-11-29 | 2004-03-31 | Hoffmann La Roche | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-o-totil-piridin-3-il)-isobutiramida |
KR100501608B1 (ko) * | 2000-07-14 | 2005-07-18 | 에프. 호프만-라 로슈 아게 | 4-페닐-피리딘 유도체의 nk1 수용체의 길항성선구약물로서의 n-산화물 |
TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
KR100599134B1 (ko) * | 2001-04-23 | 2006-07-12 | 에프. 호프만-라 로슈 아게 | 양성 전립선 비대증에 대한 nk-1 수용체 길항물질의 용도 |
NZ544244A (en) * | 2003-07-03 | 2008-10-31 | Hoffmann La Roche | Dual NK1/NK3 antagonists for treating schizophrenia |
CN1984891B (zh) | 2004-07-06 | 2012-08-08 | 弗·哈夫曼-拉罗切有限公司 | 用作合成nk-1受体拮抗剂的中间体的甲酰胺吡啶衍生物的制备方法 |
US20060030600A1 (en) * | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
BRPI0606187A2 (pt) | 2005-02-25 | 2009-06-09 | Hoffmann La Roche | comprimidos com capacidade de dispersão da substáncia do fármaco melhorada |
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EP1035115A1 (en) * | 1999-02-24 | 2000-09-13 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
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EP1035115A1 (en) * | 1999-02-24 | 2000-09-13 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
EP1103545A1 (en) * | 1999-11-29 | 2001-05-30 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide |
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