BR9810360A - Polymorphic form of compound 2- (r) - (1- (r) - (3,5-bis (tri-fluoromethyl) phenyl) ethoxy) -3- (s) - (4-fluoro) phenyl-4 (3- (5-oxo-1h, 4h-1,2,4-triazolo) methylmorpholine, process for preparing form 1 thereof, pharmaceutical composition, process for antagonizing the effect of substance p on its receptor site or for blocking the receptors of neurokinin-1 in a mammal, processes to treat or prevent a selected condition, emesis, a central nervous system disorder, depression, anxiety, and schizophrenia in a mammal, and product - Google Patents
Polymorphic form of compound 2- (r) - (1- (r) - (3,5-bis (tri-fluoromethyl) phenyl) ethoxy) -3- (s) - (4-fluoro) phenyl-4 (3- (5-oxo-1h, 4h-1,2,4-triazolo) methylmorpholine, process for preparing form 1 thereof, pharmaceutical composition, process for antagonizing the effect of substance p on its receptor site or for blocking the receptors of neurokinin-1 in a mammal, processes to treat or prevent a selected condition, emesis, a central nervous system disorder, depression, anxiety, and schizophrenia in a mammal, and productInfo
- Publication number
- BR9810360A BR9810360A BR9810360-1A BR9810360A BR9810360A BR 9810360 A BR9810360 A BR 9810360A BR 9810360 A BR9810360 A BR 9810360A BR 9810360 A BR9810360 A BR 9810360A
- Authority
- BR
- Brazil
- Prior art keywords
- phenyl
- mammal
- methylmorpholine
- oxo
- bis
- Prior art date
Links
- -1 1- (r) - (3,5-bis (tri-fluoromethyl) phenyl) ethoxy Chemical group 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 4
- 206010047700 Vomiting Diseases 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 208000019901 Anxiety disease Diseases 0.000 title abstract 2
- 230000003042 antagnostic effect Effects 0.000 title abstract 2
- 230000036506 anxiety Effects 0.000 title abstract 2
- 230000000903 blocking effect Effects 0.000 title abstract 2
- 208000015114 central nervous system disease Diseases 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 241000124008 Mammalia Species 0.000 title 2
- ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 title 2
- 101000831616 Homo sapiens Protachykinin-1 Proteins 0.000 title 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 title 1
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 102100024304 Protachykinin-1 Human genes 0.000 title 1
- 201000000980 schizophrenia Diseases 0.000 title 1
- 206010065390 Inflammatory pain Diseases 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 239000002462 tachykinin receptor antagonist Substances 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
''FORMA POLIMóRFICA DO COMPOSTO 2-(R)-(1-(R)-(3,5-BIS(TRI-FLUOROMETIL)FENIL)ETOXI)-3-(S)-(4-FL UORO)FENIL-4-(3-(5-OXO-1H,4H-1,2,4-TRIAZOLO) METILMORFOLINO, PROCESSO PARA PREPARAçãO DA FORMA 1 DO MESMO, COMPOSIçãO FARMACêUTICA, PROCESSO PARA ANTAGONIZAR O EFEITO DA SUBSTâNCIA P EM SEU SìTIO RECEPTOR OU PARA O BLOQUEIO DOS RECEPTORES DA NEUROCININA-1 EM UM MAMìFERO, PROCESSOS PARA TRATAR OU PREVENIR UMA CONDIçãO SELECIONADA, A êMESE, UM DISTúRBIO DO SISTEMA NERVOSO CENTRAL, A DEPRESSãO, A ANSIEDADE, E A ESQUIZOFRENIA EM UM MAMìFERO, E, PRODUTO" Esta invenção diz respeito a uma nova forma polimórfica do composto 2-(R)-(1-(R)-(3,5-bis( trifluorometil)fenil)etoxi)-3-(S)-(4-fluoro)fenil-4-(3-(5-oxo-1H,4H-1,2,4-tr iazolo)metilmorfolino, que é um antagonista receptor da taquicinina útil no tratamento ou na prevenção de distúrbios do sistema nervoso central, de doenças inflamatórias, dor ou enxaqueca, asma e êmese. A forma polimórfica presente tem vantagens sobre as outras formas conhecidas de 2-(R)-(1-(R)-(3,5-bis(trifluorometil)fenil)etoxi)-3-(S)-(4-fluoro) fenil-4-(3-5(-oxo-1H,4H-1,2,4-triazolo)metilmorfolino, em termos de estabilidade termodinâmica e adequabilidade para inclusão em formulações farmacêuticas.'' POLYMORPHIC FORM OF THE COMPOUND 2- (R) - (1- (R) - (3,5-BIS (TRI-FLUOROMETHYL) PHENYL) ETOXI) -3- (S) - (4-FL UORO) PHENYL-4 - (3- (5-OXO-1H, 4H-1,2,4-TRIAZOLE) METHYLMORPHOLINE, PROCESS FOR PREPARING FORM 1 OF THE SAME, PHARMACEUTICAL COMPOSITION, PROCESS FOR ANTAGONIZING THE EFFECT OF THE P SUBSTANCE ON ITS RECEIVER SITE OR THE RECEIVER SITE BLOCKING THE NEUROCININ-1 RECEPTORS IN A MAMMALIAN, PROCESSES TO TREAT OR PREVENT A SELECTED CONDITION, THE EMESIS, A DISTURBANCE OF THE CENTRAL NERVOUS SYSTEM, THE DEPRESSION, THE ANXIETY, AND THE SQUAFFEIN, EMPHASIS, MISCELLANEOUS, EMPHASIZES A MISCELLANEOUS ", with respect to a new polymorphic form of the compound 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phenyl) ethoxy) -3- (S) - (4-fluoro) phenyl-4- (3- (5-oxo-1H, 4H-1,2,4-triazole) methylmorpholine, which is a tachykinin receptor antagonist useful in the treatment or prevention of central nervous system disorders, inflammatory diseases, pain or migraine , asthma and emesis.The polymorphic form present has advantages over other known forms of 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phenyl) ethoxy) -3- (S) - (4-fluoro) phenyl-4- (3-5 (-oxo-1H, 4H-1,2,4-triazole) methylmorpholine, in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5160097P | 1997-07-02 | 1997-07-02 | |
| US80021698A | 1998-01-07 | 1998-01-07 | |
| PCT/US1998/013766 WO1999001444A1 (en) | 1997-07-02 | 1998-07-01 | Polymorphic form of the tachykinin receptor antagonist 2-(r)-(1-(r) -(3,5-bis(trifluoromethyl) phenyl)ethoxy)-3-(s)-(4-fluoro) phenyl-4-(3-5 (-oxo-1h,4h-1,2,4,-triazolo) methylmorpholine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9810360A true BR9810360A (en) | 2001-01-30 |
Family
ID=26729614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9810360-1A BR9810360A (en) | 1997-07-02 | 1998-07-01 | Polymorphic form of compound 2- (r) - (1- (r) - (3,5-bis (tri-fluoromethyl) phenyl) ethoxy) -3- (s) - (4-fluoro) phenyl-4 (3- (5-oxo-1h, 4h-1,2,4-triazolo) methylmorpholine, process for preparing form 1 thereof, pharmaceutical composition, process for antagonizing the effect of substance p on its receptor site or for blocking the receptors of neurokinin-1 in a mammal, processes to treat or prevent a selected condition, emesis, a central nervous system disorder, depression, anxiety, and schizophrenia in a mammal, and product |
Country Status (1)
| Country | Link |
|---|---|
| BR (1) | BR9810360A (en) |
-
1998
- 1998-07-01 BR BR9810360-1A patent/BR9810360A/en not_active Application Discontinuation
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| B09B | Patent application refused [chapter 9.2 patent gazette] |
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| B12B | Appeal against refusal [chapter 12.2 patent gazette] | ||
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