AR031364A1 - Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose - Google Patents
Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que poseInfo
- Publication number
- AR031364A1 AR031364A1 ARP990102698A ARP990102698A AR031364A1 AR 031364 A1 AR031364 A1 AR 031364A1 AR P990102698 A ARP990102698 A AR P990102698A AR P990102698 A ARP990102698 A AR P990102698A AR 031364 A1 AR031364 A1 AR 031364A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- group
- multimeric
- ligand
- alkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 9
- 239000000556 agonist Substances 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000001800 adrenalinergic effect Effects 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 239000003446 ligand Substances 0.000 abstract 11
- 239000011230 binding agent Substances 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000002947 alkylene group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 239000000048 adrenergic agonist Substances 0.000 abstract 2
- 229940126157 adrenergic receptor agonist Drugs 0.000 abstract 2
- 125000004450 alkenylene group Chemical group 0.000 abstract 2
- 125000004419 alkynylene group Chemical group 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000005156 substituted alkylene group Chemical group 0.000 abstract 2
- -1 2-hydroxyethylamino Chemical group 0.000 abstract 1
- 208000001738 Nervous System Trauma Diseases 0.000 abstract 1
- 206010036595 Premature delivery Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 1
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 1
Classifications
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- 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
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
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- C07C215/56—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
- C07C215/58—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
- C07C215/60—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
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- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/08—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
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- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
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Abstract
Agonistas del receptor adrenérgico b, que comprenden un compuesto de enlace multiple de la formula (1): (L)p (X)q, en la cual p es un numero entero desde 2 hasta 10; q es un numero entero desde 1 hasta 20; L es un ligando en el cual: Uno de los ligando, L, es un compuesto de la formula (2), en la cual Ar1 es seleccionado del grupo que consiste de arilo, heteroarilo, cicloalquilo, cicloalquilo sustituido, y heterociclilo donde cada uno de los sustituyentes mencionados Ar1 y Ar2 opcionalmente forma el enlace entre el ligando y un agente de union; R1 es seleccionado del grupo que consiste de hidrogeno, alquilo y alquilo sustituido, o R1 es una union covalente que une el ligando con un agente de union; R2 y R3 independientemente son seleccionados del grupo que consiste de hidrogeno, alquilo, acilo y alquilo sustituido, o R2 y R3 son uniones covalentes uniendo el ligando con un agente de union; y los otros ligandos son seleccionados independientemente de un compuesto de la formula -Q-Ar2, donde Ar2 es seleccionado del grupo que consiste de arilo, heteroarilo, cicloalquilo, cicloalquilo sustituido y heterociclilo; Q es una union covalente, o un grupo de alquileno sustituido donde uno o más átomos de carbono en dicho grupo de alquileno sustituido son opcionalmente reemplazados por un sustituyente seleccionado entre ûNRa- (donde Ra es hidrogeno, alquilo, acilo, o una union covalente que une el ligando con un agente de union), -O-, -S(O)n (donde n es un numero entero desde 0 hasta 2), -CO-, -PRb- (donde Rb es alquilo), -P(O)2-, y -O-P(O)O- y une el ligando con un agente de union. Cada agente de union, X, en el compuesto de enlaces multiples de la Formula (1), independientemente tiene la formula: -Xa-Z-(Ya-Z)m-Xa-, donde m es un numero entero desde 0 hasta 20; Xa en cada ocurrencia separada es seleccionado del grupo que consiste de -O-, -S-, -NR-, -C(O)-, -C(O)O-, -C(O)NR-, -NRC(O)-, -C(S)=, -C(S)NR-, -NRC(S)-, o una union covalente donde R es definido como sigue: Z en cada ocurrencia separada es seleccionada del grupo que consiste de alquileno, alquileno sustituido, alquenileno, alquenileno sustituido, alquinileno, alquinileno sustituido, o una union covalente; cada Ya en cada ocurrencia separada es seleccionado del grupo que consiste de -O-, C(O)-, -OC(O)-, -NR-, -S(O)n, -C(O)NR' -NR'C(O)-, -NR'C(O)NR', -NR'C(S)NR'-, -C(=NR')-NR'-, -NR'-C(=NR')-, -OC(O)-NR'-, -NR'-C(O)-O-, -N=C(Xa)-NR'-, -NR'-C(Xa)=N-, -P(O)(OR')-O-, -O-P(O)(OR')-, -S(O)nCR'R''-, -S(O)n-NR'-, -NR'-S(O)n-, y una union covalente; donde n es 0, 1 o 2; y R, R', y R'' en cada ocurrencia separada es seleccionado del grupo que consiste de hidrogeno, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, alquenilo, alquenilo sustituido, cicloalquenilo, cicloalquenilo sustituido, alquinilo, alquinilo sustituido, arilo, heteroarilo, y heterocíclico a condicion de que Xa, Xa, y Z no son uniones covalentes al mismo tiempo; y sales farmacéuticamente aceptables de éstos a condicion de que: i) cuando Q es un grupo de 2-hidroxietilamino entonces el agente de union no es alquileno o -C(O)-alquileno-C(O)-; ii) cuando Q, Xa y Ya son uniones covalentes entonces Z no puede ser alquileno y por lo tanto son utiles en el tratamiento y prevencion de enfermedades respiratorias como por ejemplo asma, bronquitis, y otras similares. Estos compuestos también son utiles en el tratamiento de lesiones del sistema nervioso y parto prematuro. Además se describe agonistas del receptor adrenérgico b-2, una composicion farmacéutica, uso de dichos agonistas para la manufactura de un medicamento, un método para identificar compuestos de ligando multimérico que poseen propiedades de enlace multimérico, un centro de compuestos de ligando multimérico que posee propiedades multivalentes y un método iterativo para identificar los compuestos de ligando multimérico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8846698P | 1998-06-08 | 1998-06-08 | |
| US9293898P | 1998-07-15 | 1998-07-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR031364A1 true AR031364A1 (es) | 2003-09-24 |
Family
ID=26778693
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102699A AR031973A1 (es) | 1998-06-08 | 1999-06-08 | Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, y uso de dichos agonistas para la manufactura de un medicamento |
| ARP990102702A AR019628A1 (es) | 1998-06-08 | 1999-06-08 | Metodo para identificar nuevos agentes multimericos que modulan receptores. |
| ARP990102706A AR019630A1 (es) | 1998-06-08 | 1999-06-08 | Agentes multiaglutinantes que modulan receptores ppar gama y rxr |
| ARP990102698A AR031364A1 (es) | 1998-06-08 | 1999-06-08 | Agonistas del receptor adrenergico beta-2, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para identificar compuestos de ligando multimerico que poseen propiedades de enlace multimerico, y un centro de compuestos de ligando multimerico que pose |
| ARP990102697A AR030142A1 (es) | 1998-06-08 | 1999-06-08 | Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para la identificacion de compuestos con ligandos multimericos que poseen propiedades de multiple ligamiento, una biblioteca de compuestos con ligand |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102699A AR031973A1 (es) | 1998-06-08 | 1999-06-08 | Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, y uso de dichos agonistas para la manufactura de un medicamento |
| ARP990102702A AR019628A1 (es) | 1998-06-08 | 1999-06-08 | Metodo para identificar nuevos agentes multimericos que modulan receptores. |
| ARP990102706A AR019630A1 (es) | 1998-06-08 | 1999-06-08 | Agentes multiaglutinantes que modulan receptores ppar gama y rxr |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102697A AR030142A1 (es) | 1998-06-08 | 1999-06-08 | Agonistas de los receptores beta2-adrenergicos, una composicion farmaceutica, uso de dichos agonistas para la manufactura de un medicamento, un metodo para la identificacion de compuestos con ligandos multimericos que poseen propiedades de multiple ligamiento, una biblioteca de compuestos con ligand |
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- 1999-06-08 WO PCT/US1999/012994 patent/WO1999064055A1/en not_active Ceased
- 1999-06-08 CA CA002319497A patent/CA2319497A1/en not_active Abandoned
- 1999-06-08 WO PCT/US1999/012907 patent/WO1999064053A1/en not_active Ceased
- 1999-06-08 AU AU43368/99A patent/AU4336899A/en not_active Abandoned
- 1999-06-08 WO PCT/US1999/012989 patent/WO1999066944A1/en not_active Ceased
- 1999-06-08 PE PE1999000493A patent/PE20000878A1/es not_active Application Discontinuation
- 1999-06-09 AU AU46776/99A patent/AU4677699A/en not_active Abandoned
-
2000
- 2000-02-07 US US09/499,476 patent/US6288055B1/en not_active Expired - Lifetime
- 2000-12-07 NO NO20006220A patent/NO20006220L/no not_active Application Discontinuation
-
2001
- 2001-12-13 US US10/015,534 patent/US20030087306A1/en not_active Abandoned
-
2009
- 2009-07-13 JP JP2009165173A patent/JP2009280590A/ja active Pending
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