- NITROXY DERIVATIVES OF SOFT STEROIDS
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A compound of formula (I) or a pharmaceutically acceptable salt thereof, and an ophthalmic composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to the use of the ophthalmic compositions for treating inflammatory conditions of the palpebral or bulbar conjunctiva, cornea and anterior segment of the globe, and to ameliorate inflammation associated with corneal injury.
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Page/Page column 17; 18
(2013/09/26)
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- NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0384; 0386
(2014/01/07)
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- Synthesis and biological evaluation of nitric oxide-donating thalidomide analogues as anticancer agents
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In search of more potent anticancer agents, 15 nitric oxide (NO)-donating thalidomide analogues, 6a, 6b, 8a-8e, and 13a-13h, were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against three human tumor cell lines (HepG2, A549, and PC-3). The results indicated that 13a-13d exhibited notable anticancer activities comparable to or stronger than that of 5-fluorouracil (5-FU). Structure-activity relationships were also discussed, based on the experimental data obtained. Generally, the cytotoxic activity of target compounds is closely related to the type of NO donors, and the length of the spacers connecting to NO donors also appears important for the bioactivities.
- Wang, Tao,Zhang, Yi-Hua,Kong, Xiang-Wen,Lai, Yi-Sheng,Ji, Hui,Chen, Yan-Ping,Peng, Si-Xun
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experimental part
p. 466 - 474
(2010/04/23)
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- PHENOL DERIVATIVES
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The present invention relates to the use of a compound of the general formula (I): wherein: n is an integer from 1 to 20; R is H, an halogen atom, a linear or branched (C1-C10)- alkoxy group, an hydroxy group, -CF3, -NHR' wherein R' is H or a linear or branched (C1-C10)-alkyl; or a salt thereof for treating inflammatory disease states or disorders, cardiovascular and/or peripheral vascular diseases.
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Page/Page column 8
(2008/06/13)
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- New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: Design, synthesis, and biopharmacological properties
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In a preliminary work, we reported two NO-sartans, possessing the characteristics of an AT1 antagonist and a "slow NO donor", obtained by adding NO-donor side chains to losartan 1. The NO release from an NO-sartan should be modulated in order to strengthen the antihypertensive activity of the native drug and to ensure additional effects, such as the antiplatelet and anti-ischemic ones. To obtain a collection of proto-typical NO-sartans, showing different rates of NO release, new NO-donor moieties have been linked to 1 or its active metabolite 2 (EXP 3174). Almost all the synthesized compounds exhibited both AT1-antagonist and NO-mediated vasorelaxing properties, with a wide range of NO-releasing rates. Further pharmacological investigation on compound 4a showed that it possessed antihypertensive and cardiac antihypertrophic effects similar to those of the reference AT1-blocking or ACE-inhibiting drugs. Furthermore, the additional anti-ischemic cardio-protective properties and antiplatelet effects of 4a have been preliminarily investigated.
- Breschi, Maria C.,Calderone, Vincenzo,Digiacomo, Maria,Macchia, Marco,Martelli, Alma,Martinotti, Enrica,Minutolo, Filippo,Rapposelli, Simona,Rossello, Armando,Testai, Lara,Balsamo, Aldo
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p. 2628 - 2639
(2007/10/03)
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- PROSTAGLANDIN NITROOXYDERIVATIVES
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Prostaglandin nitrooxyderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
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Page/Page column 40-41
(2008/06/13)
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- NITRIC OXIDE RELEASING PRODRUGS OF DIARYL-2-(5H)-FURANONES AS CYCLOOXYGENASE-2 INHIBITORS
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The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while simultaneously reducing the risk of thrombotic cardiovascular events.
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