公开(公告)号：US20100204321A1

公开(公告)日：2010-08-12

申请号：US12662364

申请日：2010-04-13

Applicant: Ahmed Z. El-Hashim ,  Ivan O. Edafiogho ,  Samuel B. Kombian ,  Mariam H. Yousif

Inventor： Ahmed Z. El-Hashim ,  Ivan O. Edafiogho ,  Samuel B. Kombian ,  Mariam H. Yousif

IPC: A61K31/216 ,  A61P11/14 ,  A61P11/08

CPC classification number: A61K31/24 ,  A61K9/0019 ,  A61K9/0073

Abstract: The antitussive and bronchodilator use for an enaminone ester relates to the use of ethyl 4-[(4-chlorophenyl)amino]-6-methyl-2-oxocyclohex-3-en-1-oate (also referred to as “enaminone E121”) for treatment of respiratory conditions, and particularly to use of the ester as the active ingredient in a cough suppressant for nonproductive cough. The ester may be used to achieve an antitussive effect, a bronchodilator effect, or both in a patient in need thereof. The ester may be formulated in any desired delivery form (such as a tablet, a capsule, a time-release capsule, a syrup, a liquid, an injection, a spray, or an inhalant), and be combined with any suitable pharmaceutical carrier, vehicles, binders, fillers, disintegrators, lubricants, solubilizers, emulsifiers, surfactants, and other excipients.

Abstract translation: 用于烯胺酯的镇咳药和支气管扩张剂涉及使用4 - [（4-氯苯基）氨基] -6-甲基-2-氧代环己-3-烯-1-酸乙酯（也称为“烯胺E121” ），特别是在用于非生产性咳嗽的止咳剂中使用酯作为活性成分。 该酯可以用于在有需要的患者中实现止咳作用，支气管扩张剂作用或两者。 酯可以以任何期望的递送形式（例如片剂，胶囊，时间释放胶囊，糖浆，液体，注射剂，喷雾剂或吸入剂）配制，并与任何合适的药物载体组合 ，载体，粘合剂，填充剂，崩解剂，润滑剂，增溶剂，乳化剂，表面活性剂和其它赋形剂。

公开(公告)号：US5468775A

公开(公告)日：1995-11-21

申请号：US024970

申请日：1993-03-02

Applicant: Kenneth R. Scott ,  Jesse M. Nicholson ,  Ivan O. Edafiogho

Inventor： Kenneth R. Scott ,  Jesse M. Nicholson ,  Ivan O. Edafiogho

IPC: C07C45/51 ,  C07C225/20 ,  C07C229/48 ,  C07C237/24 ,  C07C243/22 ,  C07D295/30 ,  A61K31/24

CPC classification number: C07D295/30 ,  C07C225/20 ,  C07C229/48 ,  C07C237/24 ,  C07C243/22 ,  C07C45/512 ,  C07C2101/16

Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is from the group consisting of COOCH.sub.3 and COOC.sub.2 H.sub.5 ; R.sup.1 is from the group consisting of H and CH.sub.3 ; R.sup.2 is from the group consisting of H when R.sup.1 is CH.sub.3 and CH.sub.3 when R.sup.1 is H; and R.sup.3 is from the group of first radicals consisting of benzyl, phenethyl, disubstituted phenyl and trisubstituted phenyl. The substituted species are second radicals having positive lipophilicity selected from the group consisting of F, Cl, Br, and I.

Abstract translation: 本发明涉及具有下式的烯胺基酮：其中R为COOCH 3和COOC 2 H 5; R1来自H和CH3组成的组; 当R1为CH3时，R2为H，当R1为H时为CH3; 并且R 3是由苄基，苯乙基，二取代的苯基和三取代的苯基组成的一组基团。 取代的物质是具有选自F，Cl，Br和I的正亲油性的第二基团。

公开(公告)号：US08324422B2

公开(公告)日：2012-12-04

申请号：US12662780

申请日：2010-05-03

Applicant: Charles I. Ezeamuzie ,  Ivan O. Edafiogho

Inventor： Charles I. Ezeamuzie ,  Ivan O. Edafiogho

IPC: C07C229/48

CPC classification number: A61K31/24 ,  C07C243/22 ,  C07C2601/16

Abstract: The enhydrazone esters for treating asthma, allergy, and inflammation relate to the use of two cyclohexenone derivatives and pharmaceutically acceptable salts thereof in the treatment of asthma, allergies, and inflammation. The esters have the formula: wherein R is ethyl or methyl. Administration of the esters inhibits the degranulation of eosinophils, the degranulation of mast cells, and the release or expression of tumor necrosis factor-α, thereby alleviating the debilitating symptoms of asthma, allergic reactions, and inflammatory responses.

Abstract translation: 用于治疗哮喘，变态反应和炎症的腙酯涉及使用两种环己烯酮衍生物及其药学上可接受的盐在治疗哮喘，过敏和炎症中的用途。 所述酯具有下式：其中R是乙基或甲基。 酯的施用抑制嗜酸性粒细胞的脱粒，肥大细胞的脱粒，以及肿瘤坏死因子-α的释放或表达，从而减轻哮喘，过敏反应和炎性反应的衰弱症状。

公开(公告)号：US5616615A

公开(公告)日：1997-04-01

申请号：US487341

申请日：1995-06-07

Applicant: Kenneth R. Scott ,  Jesse M. Nicholson ,  Ivan O. Edafiogho

Inventor： Kenneth R. Scott ,  Jesse M. Nicholson ,  Ivan O. Edafiogho

IPC: C07C45/51 ,  C07C225/20 ,  C07C229/48 ,  C07C237/24 ,  C07C243/22 ,  C07D295/30 ,  A61K31/24

CPC classification number: C07D295/30 ,  C07C225/20 ,  C07C229/48 ,  C07C237/24 ,  C07C243/22 ,  C07C45/512 ,  C07C2101/16

Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is COOCH.sub.3 ; R.sup.1 is CH.sub.3 ; R.sup.2 is H; and R.sup.3 is selected from the group consisting of C.sub.6 H.sub.4 (p-Cl) and CH.sub.2 C.sub.6 H.sub.5.

Abstract translation: 本发明涉及具有下式的烯胺基酮：其中R是COOCH 3; R1是CH3; R2为H; 并且R 3选自C 6 H 4（p-Cl）和CH 2 C 6 H 5。

公开(公告)号：US09238019B2

公开(公告)日：2016-01-19

申请号：US12662364

申请日：2010-04-13

Applicant: Ahmed Z. El-Hashim ,  Ivan O. Edafiogho ,  Samuel B. Kombian ,  Mariam H. Yousif

Inventor： Ahmed Z. El-Hashim ,  Ivan O. Edafiogho ,  Samuel B. Kombian ,  Mariam H. Yousif

IPC: A61K31/24 ,  A61K9/00

CPC classification number: A61K31/24 ,  A61K9/0019 ,  A61K9/0073

Abstract: The antitussive and bronchodilator use for an enaminone ester relates to the use of ethyl 4-[(4-chlorophenyl)amino]-6-methyl-2-oxocyclohex-3-en-1-oate (also referred to as “enaminone E121”) for treatment of respiratory conditions, and particularly to use of the ester as the active ingredient in a cough suppressant for nonproductive cough. The ester may be used to achieve an antitussive effect, a bronchodilator effect, or both in a patient in need thereof. The ester may be formulated in any desired delivery form (such as a tablet, a capsule, a time-release capsule, a syrup, a liquid, an injection, a spray, or an inhalant), and be combined with any suitable pharmaceutical carrier, vehicles, binders, fillers, disintegrators, lubricants, solubilizers, emulsifiers, surfactants, and other excipients.

Abstract translation: 用于烯胺酯的镇咳药和支气管扩张剂涉及使用4 - [（4-氯苯基）氨基] -6-甲基-2-氧代环己-3-烯-1-酸乙酯（也称为“烯胺E121” ），特别是在用于非生产性咳嗽的止咳剂中使用酯作为活性成分。 该酯可以用于在有需要的患者中实现止咳作用，支气管扩张剂作用或两者。 酯可以以任何期望的递送形式（例如片剂，胶囊，时间释放胶囊，糖浆，液体，注射剂，喷雾剂或吸入剂）配制，并与任何合适的药物载体组合 ，载体，粘合剂，填充剂，崩解剂，润滑剂，增溶剂，乳化剂，表面活性剂和其它赋形剂。

公开(公告)号：US20100216881A1

公开(公告)日：2010-08-26

申请号：US12662780

申请日：2010-05-03

Applicant: Charles I. Ezeamuzie ,  Ivan O. Edafiogho

Inventor： Charles I. Ezeamuzie ,  Ivan O. Edafiogho

IPC: A61K31/24 ,  C07C229/48 ,  A61P11/06 ,  A61P11/00

CPC classification number: A61K31/24 ,  C07C243/22 ,  C07C2601/16

Abstract: The enhydrazone esters for treating asthma, allergy, and inflammation relate to the use of two cyclohexenone derivatives and pharmaceutically acceptable salts thereof in the treatment of asthma, allergies, and inflammation. The esters have the formula: wherein R is ethyl or methyl. Administration of the esters inhibits the degranulation of eosinophils, the degranulation of mast cells, and the release or expression of tumor necrosis factor-α, thereby alleviating the debilitating symptoms of asthma, allergic reactions, and inflammatory responses.

Abstract translation: 用于治疗哮喘，变态反应和炎症的腙酯涉及使用两种环己烯酮衍生物及其药学上可接受的盐在治疗哮喘，过敏和炎症中的用途。 所述酯具有下式：其中R是乙基或甲基。 酯的施用抑制嗜酸性粒细胞的脱粒，肥大细胞的脱粒，以及肿瘤坏死因子-α的释放或表达，从而减轻哮喘，过敏反应和炎性反应的衰弱症状。

公开(公告)号：US5580894A

公开(公告)日：1996-12-03

申请号：US585329

申请日：1996-01-11

Applicant: Kenneth R. Scott ,  Ivan O. Edafiogho ,  Ralph R. Roberts

Inventor： Kenneth R. Scott ,  Ivan O. Edafiogho ,  Ralph R. Roberts

IPC: C07D261/14 ,  A61K31/41 ,  C07D261/10

CPC classification number: C07D261/14

Abstract: An oxazolyl enaminone is provided having the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of a branched or unbranched alkyl groups containing from 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of a branched or unbranched alkyl group containing from 1 to 4 carbon atoms, a chloro group, a trifluoromethyl group and a trifluoromethoxy group. Also provided are pharmaceutically accepatable salts and isomers of the above, and pharmaceutical compositions containing the same.

Abstract translation: 提供具有下式的恶唑基烯胺酮：其中R 1选自含有1至4个碳原子的支链或非支链烷基，R2选自支链或非支链烷基 1至4个碳原子，氯基，三氟甲基和三氟甲氧基。 还提供了上述药学上可接受的盐和异构体，以及含有它们的药物组合物。