3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): 125-. (canceled)27. The method of wherein Ris —OH or —C(O)NH.28. The method of wherein Rand Rare each independently methyl or ethyl.29. The method of wherein Ris methyl.31. The method of wherein the compound of formula (I) is (S)-4-((2S claim 26 ,3S)-7-carbamoyl-1 claim 26 ,1-diethyl-3-methoxy-1 claim 26 ,2 claim 26 ,3 claim 26 ,4-tetrahydro-naphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid or a pharmaceutically-acceptable salt thereof.32. The method of wherein the medical condition is opioid-induced bowel dysfunction or post-operative ileus.33. The method of wherein the medical condition is opioid-induced bowel dysfunction or post-operative ileus.35. The method of wherein Ris —OH or —C(O)NH.36. The method of wherein Rand Rare each independently methyl or ethyl.37. The method of wherein Ris methyl.39. The method of wherein the compound of formula (I) is (S)-4-((2S claim 34 ,3S)-7-carbamoyl-1 claim 34 ,1-diethyl-3-methoxy-1 claim 34 ,2 claim 34 ,3 claim 34 ,4-tetrahydro-naphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid or a pharmaceutically-acceptable salt thereof.40. The method of wherein the opioid agent is selected from morphine claim 34 , pethidine claim 34 , codeine claim 34 , dihydrocodeine claim 34 , oxycontin claim 34 , oxycodone claim 34 , hydrocodone claim 34 , sufentanil claim 34 , fentanyl claim 34 , remifentanil claim 34 , buprenorphine claim 34 , methadone claim 34 , and heroin.41. The method of wherein the opioid agent is morphine.42. The method of wherein the opioid agent is oxycodone.43. The method of wherein the opioid agent is selected from morphine claim 39 , pethidine claim 39 , codeine claim 39 , dihydrocodeine claim 39 , oxycontin claim 39 , oxycodone claim 39 , hydrocodone claim 39 , sufentanil claim 39 , fentanyl claim 39 , remifentanil claim 39 , buprenorphine claim 39 , methadone claim 39 , and heroin.44. The method of wherein the opioid agent is morphine ...

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

AMINOTETRALIN COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

The invention provides aminotetralin compounds of formula (I): 120-. (canceled)22. The method of wherein Ris —C(O)NH.23. The method of wherein Rand Rare each independently selected from hydrogen claim 21 , benzyl claim 21 , and phenyl claim 21 , or Rand Rtogether with the carbon atom to which they are attached form a cyclohexyl ring.24. The method of wherein Ris —NRR.25. The method of wherein Rand Rare each independently selected from hydrogen claim 24 , Calkyl claim 24 , and benzyl or Rand Rtogether with the nitrogen atom to which they are attached form piperidinyl.26. The method of wherein Ris —OH or —C(O)NH; Rand Rare each methyl or Rand Rare each ethyl; Ris methyl; Rand Rare each hydrogen; and n is 0 and m is 0.27. The method of wherein the medical condition is opioid-induced bowel dysfunction.28. The method of wherein the medical condition is post-operative ileus.30. The method of wherein Rand Rare each independently selected from hydrogen claim 29 , benzyl claim 29 , and phenyl claim 29 , or Rand Rtogether with the carbon atom to which they are attached form a cyclohexyl ring.31. The method of wherein Ris —NRR.32. The method of wherein Rand Rare each independently selected from hydrogen claim 31 , Calkyl claim 31 , and benzyl or Rand Rtogether with the nitrogen atom to which they are attached form piperidinyl.33. The method of wherein Ris —OH or —C(O)NH; Rand Rare each methyl or Rand Rare each ethyl; Ris methyl; Rand Rare each hydrogen; and n is 0 and m is 0. This application claims the benefit of U.S. Provisional Application No. 61/007,127 filed on Dec. 11, 2007, the disclosure of which is incorporated herein by reference in its entirety.1. Field of the InventionThe invention is directed to aminotetralin compounds which are useful as mu opioid receptor antagonists. The invention is also directed to pharmaceutical compositions comprising such compounds, methods of using such compounds for treating or ameliorating medical conditions mediated by mu opioid ...

3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): 125-. (canceled)27. The method of wherein Ris —OH or —C(O)NH.28. The method of wherein Rand Rare each independently methyl or ethyl.29. The method of wherein Ris methyl.31. The method of wherein the compound of formula (I) is (S)-4-((2S claim 26 ,3S)-7-carbamoyl-1 claim 26 ,1-diethyl-3-methoxy-1 claim 26 ,2 claim 26 ,3 claim 26 ,4-tetrahydro-naphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid or a pharmaceutically-acceptable salt thereof.32. The method of wherein the opioid agent is selected from morphine claim 26 , pethidine claim 26 , codeine claim 26 , dihydrocodeine claim 26 , oxycontin claim 26 , oxycodone claim 26 , hydrocodone claim 26 , sufentanil claim 26 , fentanyl claim 26 , remifentanil claim 26 , buprenorphine claim 26 , methadone claim 26 , and heroin.33. The method of wherein the opioid agent is morphine.34. The method of wherein the opioid agent is oxycodone.35. The method of wherein the opioid agent is selected from morphine claim 30 , pethidine claim 30 , codeine claim 30 , dihydrocodeine claim 30 , oxycontin claim 30 , oxycodone claim 30 , hydrocodone claim 30 , sufentanil claim 30 , fentanyl claim 30 , remifentanil claim 30 , buprenorphine claim 30 , methadone claim 30 , and heroin.36. The method of wherein the opioid agent is morphine.37. The method of wherein the opioid agent is oxycodone.40. The method of wherein the compound of formula (I) is (S)-4-((2S claim 38 ,3S)-7-carbamoyl-1 claim 38 ,1-diethyl-3-methoxy-1 claim 38 ,2 claim 38 ,3 claim 38 ,4-tetrahydro-naphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid or a pharmaceutically-acceptable salt thereof.43. The method of wherein the compound of formula (I) is (S)-4-((2S claim 41 ,3S)-7-carbamoyl-1 claim 41 ,1-diethyl-3-methoxy-1 claim 41 ,2 claim 41 ,3 claim 41 ,4-tetrahydro-naphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid or a pharmaceutically-acceptable salt thereof. This application claims the benefit ...

3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): 125-. (canceled)27. A pharmaceutical composition comprising the compound of and a pharmaceutically-acceptable carrier.28. A method of treating opioid-induced bowel dysfunction or post-operative ileus in a mammal claim 26 , the method comprising administering to the mammal a therapeutically effective amount of a pharmaceutical composition comprising a pharmaceutically-acceptable carrier and the compound of .29. A method of reducing a gastrointestinal side effect associated with use of an opioid agent in a mammal claim 26 , the method comprising administering to the mammal an opioid agent and the compound of .30. The method of wherein the opioid agent is selected from morphine claim 29 , pethidine claim 29 , codeine claim 29 , dihydrocodeine claim 29 , oxycontin claim 29 , oxycodone claim 29 , hydrocodone claim 29 , sufentanil claim 29 , fentanyl claim 29 , remifentanil claim 29 , buprenorphine claim 29 , methadone claim 29 , and heroin.31. The method of wherein the opioid agent is morphine.32. The method of wherein the opioid agent is oxycodone or hydrocodone.33. A method of enhancing motility of the gastrointestinal tract in a mammal claim 26 , the method comprising administering to the mammal a pharmaceutical composition comprising a pharmaceutically-acceptable carrier and a compound of .35. A pharmaceutical composition comprising the compound of and a pharmaceutically-acceptable carrier.36. A method of treating opioid-induced bowel dysfunction or post-operative ileus in a mammal claim 34 , the method comprising administering to the mammal a therapeutically effective amount of a pharmaceutical composition comprising a pharmaceutically-acceptable carrier and the compound of .37. A method of reducing a gastrointestinal side effect associated with use of an opioid agent in a mammal claim 34 , the method comprising administering to the mammal an opioid agent and the compound of .38. The ...

By amidino group substituted heterocyclic derivatives and their use as anticoagulants

The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Compounds and compositions as anticoagulants

The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Substituted amidinoaryl derivatives and their use as anticoagulants

The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Cross-linked glycopeptide-cephalosporin antibiotics

Aminotetralin compounds as mu opioid receptor antagonists

The invention provides aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

2 -aminotetralin derivatives as mu opioid receptor antagonists

Aminotetralin compounds as opioid receptor antagonists mu

Un compuesto de la fórmula (I): en la que: R1 es -Un compuesto de la fórmula (I): en la que: R1 es -ORa o -C(O)NRbRc; R2, R3 y R4 son con independenciORa o -C(O)NRbRc; R2, R3 y R4 son con independencia entre sí alquilo C1-3; R5 y R6 se eligen con inda entre sí alquilo C1-3; R5 y R6 se eligen con independencia entre sí entre hidrógeno, bencilo y fenependencia entre sí entre hidrógeno, bencilo y fenilo, dicho fenilo está opcionalmentesustituido porilo, dicho fenilo está opcionalmentesustituido por halógeno, o R5 y R6 junto con el átomo de carbono halógeno, o R5 y R6 junto con el átomo de carbono al que están unidos forman un anillo ciclopentilo al que están unidos forman un anillo ciclopentilo ociclohexilo, R7 se elige entre hidroxi, alcoxi C ociclohexilo, R7 se elige entre hidroxi, alcoxi C1-3 y -NR8R9; R8 y R9 se eligen con independencia 1-3 y -NR8R9; R8 y R9 se eligen con independencia entre sí entre hidrógeno, alquilo C1-6, ciclohexilentre sí entre hidrógeno, alquilo C1-6, ciclohexilo y bencilo, o R8 y R9 junto con elátomo de nitrógo y bencilo, o R8 y R9 junto con elátomo de nitrógeno al que están unidos forman un piperidinilo o peno al que están unidos forman un piperidinilo o piperazinilo, dichos piperidinilo y piperazinilo esiperazinilo, dichos piperidinilo y piperazinilo estánopcionalmente sustituidos por metilo; Ra, Rb y tánopcionalmente sustituidos por metilo; Ra, Rb y Rc son con independencia entre sí hidrógeno o alquRc son con independencia entre sí hidrógeno o alquilo C1-3; n es el número 0, 1, 2, 3 ó 4; y m es elilo C1-3; n es el número 0, 1, 2, 3 ó 4; y m es el número 0 ó 1; en la que los sustituyentes de los número 0 ó 1; en la que los sustituyentes de los centros quirales marcados con un asterisco están ecentros quirales marcados con un asterisco están en la configuración trans; con la condición de que n la configuración trans; con la condición de que si n + m >= 1 y R7 es hidroxi o alcoxi C1-3, entonsi n + m >= 1 y R7 es hidroxi o alcoxi C1-3, ...

3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): (I) wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Substituted amidinoaryl derivatives and their use as anticoagulants

Aryl aniline derivatives as β2 adrenergic receptor agonists

The invention provides novel β 2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β 2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): (I) wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Novel antiviral compounds

Novel compounds are disclosed, useful as antiviral agents.

3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVE AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

DERIVADOS DE 3-CARBOXIPROPIL-AMINOTETRALINA E COMPOSTOS RELACIONADOS COMO ANTAGONISTAS DO RECEPTOR OPIÓIDE MU. A invenção fornece compostos de 3-carboxipropilaminotetralina de fórmula (I): em que R1, R2, R3, R4, R5 e R6 são definidos na especificação, ou um sal farmaceuticamente aceitável deste, que são antagonistas no receptor opióide mu. A invenção também fornece composições farmacêuticas que compreendem estes compostos, métodos de utilização destes compostos para tratar condições associadas à atividade do receptor opióide mu, e processos e intermediários úteis para a preparação destes compostos. 3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS. The invention provides 3-carboxypropylaminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are defined in the specification, or a pharmaceutically acceptable salt thereof, which are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising these compounds, methods of using these compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing these compounds.

Compounds derived from 3-carbopropyl-aminotetralin; preparation procedure; pharmaceutical composition comprising them; and its uses to treat opioid-induced intestinal dysfunctions.

FORMULA (I):<br /> A UNA DE SUS SALES FARMACEUTICAMENTE ACEPTABLES, DONDE R1•RE SE DEFINEN TAL COMO EN EL PLIEGO DE REIVINDICACIONES. LA INVENCIÓN<br /> TAMBIÉN PROVEE COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN DICHOS COMPUESTOS Y UN PORTADOR FARMACEUTICAMENTE ACEPTABLE; UN PROCEDIMIENTO PARA ELABORAR LOS COMPUESTOS; Y SUS USOS PARA TRATAR AFECCIONES TALES COMO DISFUNCION INTESTINAL INDUCIDA POR<br /> OPIOIDES O ILEO POSTOPERATORIO, Y TRASTORNO DE MOTILIDAD REDUCIDA DEL TRACTO GASTROINTESTINAL, ASL COMO TAMBIEN, PARA REDUCIR O PREVENIR UN EFECTO COLATERAL ASOCIADO CON EL EMPLEO DE UN AGENTE OPIOIDE .<br />  

ARYL ANILINE beta2 ADRENERGIC RECEPTOR AGONIST

【課題】特性を改良したさらなるβ ２ アドレナリン作用性レセプタアゴニストを提供する。 【解決手段】例えば下式で例示されるアドレナリン作用性レセプタアゴニスト化合物であり 、このような化合物を含有する製薬組成物、このような化合物を使用してβ ２ アドレナリン作用性レセプター活性に関連した疾患を治療する方法、ならびにこのような化合物を調製するのに有用な方法および中間体。 【選択図】なし

Aryl aniline β 2 adrenergic receptor agonists

Arylanilinderivate als agonisten des beta2- adrenergen rezeptors

Aryl aniline beta-2 adrenergic receptor agonists

Cross-linked glycopeptide-cephalosporin antibiotics

This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Combinations of an aryl aniline beta-2 adrenergic receptor agonist and a corticosteroid

The invention provides novel beta2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with beta2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Combinations of an aryl aniline beta-2 adrenergic receptor agonist and a corticosteroid

The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1 - R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Combinations of an aryl aniline beta-2 adrenergic receptor agonist and a corticosteroid

The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1 - R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.