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公开(公告)号：US20220378793A1
公开(公告)日：2022-12-01
申请号：US17811914
申请日：2022-07-12
IPC分类号： A61K31/519 , A61P11/00 , A61K31/505 , A61K31/496
摘要： The application refers to a novel combination treatment/combination medicament for PF-ILD treatment, comprising as a first combination partner a therapeutically effective amount of Nintedanib or a pharmaceutically acceptable salt thereof and as a second combination partner a therapeutically effective amount of a PDE4B-inhibitor of formula I wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center or a pharmaceutically acceptable salt thereof. Hereby the second combination partner is preferably a therapeutically effective amount of the PDE4B-inhibitior of formula III or a pharmaceutically acceptable salt thereof.
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2.发明申请公开(公告)号：US20190134043A1
公开(公告)日：2019-05-09
申请号：US16166239
申请日：2018-10-22
IPC分类号： A61K31/519 , A61K31/496 , A61P11/00
摘要： The application refers to a novel combination treatment/combination medicament for PF-ILD treatment, comprising as a first combination partner a therapeutically effective amount of Nintedanib or a pharmaceutically acceptable salt thereof and as a second combination partner a therapeutically effective amount of a PDE4B-inhibitor of formula I wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center or a pharmaceutically acceptable salt thereof. Hereby the second combination partner is preferably a therapeutically effective amount of the PDE4B-inhibitor of formula III or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20240142467A1
公开(公告)日：2024-05-02
申请号：US18474419
申请日：2023-09-26
IPC分类号： G01N33/68 , C07D409/14
CPC分类号： G01N33/6893 , C07D409/14 , G01N2800/12 , G01N2800/52
摘要： The PDE4-inhibitor of formula A′
for use in a method for the treatment of a progressive fibrosing interstitial lung disease (PF-ILD), preferably IPF, in a patient comprising the following steps:
a) measuring or having measured the concentration, expression level or activity of one or more biomarkers selected from the group consisting of Krebs von den Lungen protein (KL-6), Pulmonary Surfactant Protein D (SP-D), Matrilysin (MMP7), CA-125 (also named MUC-16), CA19-9, E-selectin, sICAM-1, Stromelysin (MMP3), osteopontin (OPN), connective tissue growth factor (CTGF), Cartilage oligomeric matrix protein (COMP), prostasin, von-Willebrand-Faktor (vWF), and C-reactive protein (CRP) in the serum or plasma of a blood sample obtained from said patient,
b) comparing or having compared the concentration, expression level or activity of the one or more biomarkers as listed in step a) in said patient's blood serum or blood plasma sample to a reference concentration, expression level or activity of the respective one or more biomarkers,
c) determining or having determined that the concentration, expression level or activity of the respective one or more biomarkers as listed in step a) is modified compared to a respective reference concentration, expression or activity of that respective one or more biomarker,
d) administering to said patient a therapeutically efficient amount of the PDE4-inhibitor of formula A′.-
4.发明公开公开(公告)号：US20230181590A1
公开(公告)日：2023-06-15
申请号：US18063190
申请日：2022-12-08
发明人： Christian HESSLINGER , Verena BAUER , Sebastian Martin BOSSERT , Susan KOBER , Yi LIU , Peter NICKOLAUS , Maria SARNO , Florian VOSS
IPC分类号： A61K31/519 , A61K9/28 , A61K9/00 , A61P11/00
CPC分类号： A61K31/519 , A61K9/28 , A61K9/0053 , A61P11/00
摘要： The invention concerns an oral pharmaceutical composition consisting essentially of
the PDE4B-inhibitor of formula III
in the dose of 18 mg or 9 mg and
optionally of one or more pharmaceutically acceptable carriers or excipients
for use in the treatment of a patient suffering from one or more progressive fibrosing interstitial lung diseases (PF-ILD), wherein this oral pharmaceutical composition is to be administered to the patient twice daily.
The invention further concerns oral pharmaceutical compositions comprising the PDE4B-inhibitor of formula III in the dose of 18 mg or 9 mg and a therapeutically effective dose of a second active ingredient selected from nintedanib or pirfenidone, wherein these oral pharmaceutical compositions are administered to the patient twice daily.-
5.发明公开公开(公告)号：US20230405010A1
公开(公告)日：2023-12-21
申请号：US18343792
申请日：2023-06-29
IPC分类号： A61K31/519 , A61P11/00 , A61K31/505 , A61K31/496
CPC分类号： A61K31/519 , A61P11/00 , A61K31/505 , A61K31/496
摘要： The application refers to a novel combination treatment/combination medicament for PF-ILD treatment, comprising as a first combination partner a therapeutically effective amount of Nintedanib or a pharmaceutically acceptable salt thereof and as a second combination partner a therapeutically effective amount of a PDE4B-inhibitor of formula I
wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and
wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A,
wherein S* is a sulphur atom that represents a chiral center
or a pharmaceutically acceptable salt thereof.
Hereby the second combination partner is preferably a therapeutically effective amount of the PDE4B-inhibitior of formula III
or a pharmaceutically acceptable salt thereof.-
6.发明申请公开(公告)号：US20180072754A1
公开(公告)日：2018-03-15
申请号：US15698859
申请日：2017-09-08
发明人： Pascale Arielle Jane-Josee POUZET , Peter NICKOLAUS , Ulrike WERTHMANN , Rogelio P. FRUTOS , Bing-Shiou YANG , Soojin KIM , Jason Alan MULDER , Nitinchandra D. PATEL , Chris Hugh SENANAYAKE , Thomas Gabriel TAMPONE , Xudong WEI
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
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7.发明申请NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA 审中-公开新型哌啶二氢吲哚尼酮硫代磷酸酯及其用于治疗COPD和ASTHMA的用途公开(公告)号：US20170008903A9
公开(公告)日：2017-01-12
申请号：US13963513
申请日：2013-08-09
发明人： Pascale A.J. POUZET , Peter NICKOLAUS , Ulrike WERTHMANN , Rogelio P. FRUTOS , Bing-Shiou YANG , Soojin KIM , Jason Alan MULDER , Nitinchandra D. PATEL , Chris Hugh SENANAYAKE , Thomas Gabriel TAMPONE , Xudong WEI
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
摘要翻译： 式I的哌啶子基 - 二氢噻吩并嘧啶亚砜其中：环A是任选地包含一个或两个氮原子并且R是Cl并且位于环A的对位，间位或邻位的6元芳香环，S * 是表示手性中心的硫原子及其所有药学上可接受的盐，对映异构体和外消旋体，水合物和溶剂合物，以及这些化合物用于治疗呼吸道炎症或过敏性疾病如COPD或哮喘的用途。
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8.发明公开公开(公告)号：US20230190754A1
公开(公告)日：2023-06-22
申请号：US18063196
申请日：2022-12-08
发明人： Christian HESSLINGER , Verena BAUER , Sebastian Martin BOSSERT , Susan KOBER , Yi LIU , Peter NICKOLAUS , Maria SARNO , Florian VOSS
IPC分类号： A61K31/519 , A61K31/4418 , A61K31/496 , A61P11/00
CPC分类号： A61K31/519 , A61K31/4418 , A61K31/496 , A61P11/00 , A61K9/0053
摘要： The invention concerns an oral pharmaceutical composition comprising
either 18 mg or 9 mg of the PDE4B-inhibitor of formula III
a therapeutically effective dose of a second active agent selected from the group consisting of nintedanib or pirfenidone and
optionally, one or more pharmaceutically acceptable carriers or excipients for the treatment of a patient suffering from a progressive fibrosing interstitial lung disease (PF-ILD), wherein this oral pharmaceutical composition is to be administered to said patient twice daily.
The invention further concerns the use of the PDE4B-inhibitor of formula III for preparing an oral pharmaceutical composition comprising either 18 mg or 9 mg of the PDE4B-inhibitor of formula III for use in a method of treating a patient suffering from one or more Progressive Fibrosing Interstitial Lung Diseases (PF-ILDs), wherein said oral pharmaceutical composition is to be orally administered twice daily to said patient in combination with a therapeutically effective amount of a therapeutically effective dose of a second active agent selected from the group consisting of nintdanib and pirfenidone.-
9.发明申请公开(公告)号：US20200048278A1
公开(公告)日：2020-02-13
申请号：US16599209
申请日：2019-10-11
发明人： Pascale Arielle Jane-Josee POUZET , Peter NICKOLAUS , Ulrike WERTHMANN , Rogelio P. FRUTOS , Bing-Shiou YANG , Soojin KIM , Jason Alan MULDER , Nitinchandra D. PATEL , Chris Hugh SENANAYAKE , Thomas Gabriel TAMPONE , Xudong WEI
IPC分类号： C07D495/04
摘要： Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
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