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公开(公告)号：US20230321053A1
公开(公告)日：2023-10-12
申请号：US18040508
申请日：2021-08-20
Applicant: PALOBIOFARMA, S.L.
Inventor： Julio CASTRO-PALOMINO LARIA , Juan CAMACHO GÓMEZ , Nahomi CASTROPALOMINO LARIA , Alina ARIOSA ÁLVAREZ
IPC: A61K45/06 , A61P11/06 , A61K31/426
CPC classification number: A61K31/426 , A61K45/06 , A61P11/06
Abstract: The present invention relates to (1R,3S)-3-((5-cyano-4-phenylthiazol-2-yl)carbamoyl)cyclopentane-1-carboxylic acid, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compound for use in the treatment of airway diseases, such as allergic asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), obstructive sleep apnea, allergic rhinitis, among others, in subjects having elevated levels of eosinophils in peripheral blood to the use of said compound for the manufacture of a medicament for the treatment of airway diseases, such as allergic asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), obstructive sleep apnea, allergic rhinitis, among others, in subjects having elevated levels of eosinophils in peripheral blood and to a method the treatment of airway diseases, such as allergic asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), obstructive sleep apnea, allergic rhinitis, among others, in subjects having elevated levels of eosinophils in peripheral blood by administering said compound.
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2.发明申请公开(公告)号：US20180037569A1
公开(公告)日：2018-02-08
申请号：US15552039
申请日：2016-02-19
Applicant: PALOBIOFARMA, S.L.
IPC: C07D401/14 , A61K31/506 , A61K31/444 , A61K45/06
CPC classification number: C07D401/14 , A61K31/444 , A61K31/506 , A61K45/06
Abstract: The present invention relates to novel pyridine derivatives of formula (I): as A2B adenosine receptor antagonists and ligands of MT3 melatonin receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by antagonizing the adenosine A2B receptor and by inhibition of MT3 melatonin receptor, such as respiratory disease, metabolic disorders, neurological disorders and cancer.
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3.发明申请公开(公告)号：US20200030300A1
公开(公告)日：2020-01-30
申请号：US16491185
申请日：2018-03-06
Applicant: PALOBIOFARMA, S.L.
Inventor： Julio CASTRO PALOMINO LARIA , Juan CAMACHO GÓMEZ
IPC: A61K31/426 , C07D277/56
Abstract: The present invention relates to the tromethamine salt of (1R,3S)-3-(5-cyano-4-phenyl-1,3-thiazol-2-ylcarbamoyl)cyclopentane carboxylic acid, a process for obtaining said salt, combination products and pharmaceutical compositions comprising said salts and their medical uses, in particular for the treatment or prevention of diseases known to ameliorate by A1 adenosine receptor antagonism.
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4.发明申请NEW PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS (PDE-10) 有权新型吡啶衍生物作为磷酸二酯酶10抑制剂（PDE-10）公开(公告)号：US20150336953A1
公开(公告)日：2015-11-26
申请号：US14762655
申请日：2014-01-23
Applicant: PALOBIOFARMA S.L
Inventor： Juan CAMACHO GÓMEZ , Julio CASTRO PALOMINO LARIA
IPC: C07D471/04 , A61K31/506 , A61K45/06 , C07D405/14 , A61K31/5377 , C07D403/04 , C07D417/14
CPC classification number: C07D471/04 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14
Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) as inhibitors of the enzyme phosphodiesterase 10 (PDE-10), pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition of the enzyme Phosphodiesterase 10 such as neurological, psychiatric, respiratory or metabolic diseases.
Abstract translation: 本发明涉及作为酶磷酸二酯酶10（PDE-10）的抑制剂的式（I）的新型嘧啶衍生物，包含有效量的这些化合物的药物组合物以及用于制备用于治疗病理学的药物的化合物的用途 可通过抑制酶Phosphodiesterase 10，如神经，精神，呼吸或代谢疾病而改善的病症或疾病。
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公开(公告)号：US20210145831A1
公开(公告)日：2021-05-20
申请号：US17156785
申请日：2021-01-25
Applicant: Novartis AG , Palobiofarma S.L.
Inventor： Kai CUI , Julio Cesar CASTRO-PALOMINO LARIA , Weiyong KONG
IPC: A61K31/506 , A61K39/395 , A61K45/06 , C07D403/14 , C07K16/28
Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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Patent Agency Ranking
公开(公告)号：US10744125B2
公开(公告)日：2020-08-18
申请号：US16479448
申请日：2018-01-19
Applicant: Palobiofarma, S.L.
IPC: A61K31/4545 , A61K31/167 , A61K31/352 , A61K31/366 , A61K31/40 , A61K31/47 , A61K31/505 , A61K31/519 , A61K31/549 , C07D417/14
Abstract: Modulators of the adenosine A3 receptors of formula (I): and process for preparing said compounds. Other aspects of the present invention are pharmaceutical compositions comprising an effective amount of said compounds and the use of said compounds in the preparation of a medicament for treating pathological conditions or diseases that can be improved by modulation of adenosine A3 receptors.
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公开(公告)号：US20200163963A1
公开(公告)日：2020-05-28
申请号：US16616844
申请日：2018-05-30
Applicant: Novartis AG , Palobiofarma S.L.
Inventor： Kai CUI , Julio Cesar CASTRO-PALOMINO LARIA , Weiyong KONG
IPC: A61K31/506 , A61K39/395 , C07K16/28 , C07D403/14 , A61K45/06
Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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公开(公告)号：US20180228802A1
公开(公告)日：2018-08-16
申请号：US15751140
申请日：2016-08-10
Applicant: NOVARTIS AG , PALOBIOFARMA, S.L.
Inventor： Sanela BILIC , Juan Alberto CAMACHO GOMEZ , John Scott CAMERON , Julio Cesar CASTRO-PALOMINO LARIA , Danny Roland HOWARD, Jr.
IPC: A61K31/506 , A61P35/00
Abstract: The present invention relates to 5-bromo-2,6-di-(1H-pyrazol-1-yl)pyrimidin-4-amine, its pharmaceutically acceptable salts and co-crystals thereof and to pharmaceutical compositions comprising said compounds for use in the treatment of cancer.
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公开(公告)号：US11078191B2
公开(公告)日：2021-08-03
申请号：US16484183
申请日：2018-02-08
Applicant: Novartis AG , Palobiofarma S.L.
Inventor： Sanela Bilic , Juan Alberto Camacho Gomez , John Scott Cameron , Julio Cesar Castro-Palomino Laria , Danny Roland Howard, Jr.
IPC: C07D403/14 , C07K16/28 , A61K31/506 , A61P35/00
Abstract: This invention relates to an active metabolite of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimindin-4-amine that modulates the activity of adenosine A2a receptor. In particular, the present invention relates to pharmaceutical compositions comprising 1-(4-amino-5-bromo-6-(1H-pyrazol-1-yl)-pyrimidin-2-yl)-1H-pyrazol-4-ol, as well as processes for its preparation and its use in the treatment of cancer alone of in combination with one or more immunotherapeutic agents.
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公开(公告)号：US10933064B2
公开(公告)日：2021-03-02
申请号：US16616844
申请日：2018-05-30
Applicant: Novartis AG , Palobiofarma S.L.
Inventor： Kai Cui , Julio Cesar Castro-Palomino Laria , Weiyong Kong
IPC: A61K31/506 , A61K39/395 , A61K45/06 , C07D403/14 , C07K16/28 , A61K39/00
Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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