公开(公告)号：US20210322413A1

公开(公告)日：2021-10-21

申请号：US17265134

申请日：2019-07-31

Applicant: NICOX S.A.

Inventor： Nicoletta ALMIRANTE ,  Stefania BRAMBILLA ,  Laura STORONI ,  Francesco IMPAGNATIELLO ,  Elena BASTIA

IPC: A61K31/506 ,  A61K31/197 ,  A61K45/06 ,  A61P27/06 ,  A61K31/519 ,  C07D403/14 ,  C07D487/04

Abstract: The invention relates to nitric oxide releasing phosphodiesterase type 5 (PDE5) inhibitors of formula (I) or (Ib) or (II) or a stereoisomer or a pharmaceutically acceptable salt thereof: useful for the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies. The invention further relates to 3-[(2S)-2,3-bis(nitrooxy)propoxy]propanoic acid and 6-(nitrooxy)hexanoic acid for use in the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies.

公开(公告)号：US20170354634A1

公开(公告)日：2017-12-14

申请号：US15527129

申请日：2015-11-17

Applicant: NICOX S.A.

Inventor： Nicoletta ALMIRANTE ,  Laura STORONI ,  Elena BASTIA ,  Francesco IMPAGNATIELLO

IPC: A61K31/34 ,  A61K31/5575 ,  A61K9/00

CPC classification number: A61K31/34 ,  A61K9/0048 ,  A61K31/164 ,  A61K31/191 ,  A61K31/343 ,  A61K31/5575 ,  A61K2300/00

Abstract: The present invention relates to compositions for treating glaucoma and elevated ocular pressure. The compositions comprise a nitric oxide releasing isomannide derivative and a prostaglandin F2α analog.

公开(公告)号：US20230414621A1

公开(公告)日：2023-12-28

申请号：US18251283

申请日：2021-10-28

Applicant: Nicox S.A.

Inventor： Tomas NAVRATIL ,  Francesco IMPAGNATIELLO ,  Nicoletta ALMIRANTE

IPC: A61K31/519 ,  A61K31/506

CPC classification number: A61K31/519 ,  A61K31/506

Abstract: The invention relates to the use of nitric oxide releasing cyclic guanosine 3′,5′ monophosphate (cGMP) phosphodiesterase type 5 inhibitors (NO-PDES inhibitors) in a method for the treatment of dry age-related macular degeneration and geographic atrophy. This invention also relates to the use of such compounds to provide neuroprotection to the eye in a patient suffering from glaucoma or retinal neuropathies.

公开(公告)号：US20180118677A1

公开(公告)日：2018-05-03

申请号：US15561885

申请日：2016-01-28

Applicant: NICOX S.A.

Inventor： Nicoletta ALMIRANTE ,  Laura STORONI ,  Elena BASTIA ,  Stefania BRAMBILLA ,  Francesco IMPAGNATIELLO

IPC: C07C405/00 ,  A61K31/5575 ,  A61P27/06

CPC classification number: C07C405/0016 ,  A61K31/5575 ,  A61P27/06 ,  C07C2601/08

Abstract: The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxy derivatives of fluprostenol.

公开(公告)号：US20230069076A1

公开(公告)日：2023-03-02

申请号：US17760012

申请日：2021-02-03

Applicant: Nicox S.A.

Inventor： Nicoletta ALMIRANTE ,  Stefania BRAMBILLA ,  Francesco IMPAGNATIELLO ,  Elena BASTIA ,  Corinna GALLI

IPC: A61K31/519 ,  A61K31/5575 ,  A61K31/5578 ,  A61K9/00

Abstract: The invention relates to ophthalmic compositions comprising a nitric oxide releasing phosphodiesterase type 5 inhibitor (NO-PDE5 inhibitor) and a prostaglandin analog, and to the use of these ophthalmic compositions for the treatment of all forms of glaucoma or ocular hypertension as well as eyes diseases or conditions associated with elevated intraocular pressure. The NO-PDE5 inhibitor is selected from the following compounds: [(2S)-1-(4-{[(3-chloro-4-methoxyphenyl)methyl]amino}-5-{[(pyrimidin-2-yl)methyl]carbamoyl}pyrimidin-2-yl)pyrrolidin-2-yl]methyl 6-(nitrooxy) hexanoate (Compound (1)), [(2S)-1-(4-{[(3-chloro-4-methoxyphenyl)methyl]amino}-5-{[(pyrimidin-2-yl)methyl]carbamoyl}pyrimidin-2-yl)pyrrolidin-2-yl]methyl 3-[(2S)-2,3-bis(nitrooxy)propoxy]propanoate (Compound (1A)) or 2-{4-[3-(5-Ethyl-4-oxo-7-propyl-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidin-2-yl)-4-propoxybenzene-1-sulfonyl]piperazin-1-yl}ethyl 3-[(2S)-2,3-bis(nitrooxy) propoxy]propanoate (Compound (2)). The prostaglandin analog is selected from latanoprost, bimatoprost, travoprost or tafluprost.

公开(公告)号：US20180118676A1

公开(公告)日：2018-05-03

申请号：US15561919

申请日：2016-03-22

Applicant: Nicox S.A.

Inventor： Nicoletta ALMIRANTE ,  Laura STORONI ,  Elena BASTIA ,  Stefania BRAMBILLA ,  Francesco IMPAGNATIELLO

IPC: C07C405/00 ,  A61P27/02 ,  A61P27/06 ,  A61K9/00 ,  A61K31/5575 ,  A61K45/06

CPC classification number: C07C405/00 ,  A61K9/0048 ,  A61K31/5575 ,  A61K45/06 ,  A61P27/02 ,  A61P27/06 ,  C07C2601/08 ,  A61K2300/00

Abstract: The present invention relates to 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid.