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1. 发明申请

WO2018206739A1 PYRAZOLE[1,5-A]PYRIMIDINE DERIVATIVES AS KINASE JAK INHIBITORS 审中-公开
公开(公告)号：WO2018206739A1
公开(公告)日：2018-11-15
申请号：PCT/EP2018/062164
申请日：2018-05-10
申请人： CELON PHARMA S.A.
发明人： MROCZKIEWICZ, Michal , STYPIK, Bartosz , BUJAK, Anna , SZYMCZAK, Krzysztof , GUNERKA, Pawel , DUBIEL, Krzysztof , WIECZOREK, Maciej , PIECZYKOLAN, Jerzy
IPC分类号： C07D487/04 , A61P29/00 , A61P37/00 , A61K31/519
摘要： A compound or its acid addition salt of the general formula (I), wherein R 1 represents phenyl substituted with one or two substituents selected from the group consisting of halogen and C1-C3 alkoxyl, or 6-membered heteroaryl with 1 or 2 nitrogen atoms, which is unsubstituted or substituted with a substituent selected from the group consisting of -NH 2 , halogen, alkyl C1-C4, alkoxyl C1-C3, and 6-membered heterocyclyl comprising 1 or 2 heteroatoms selected from the group consisting of N and O. The compound has the activity of kinase JAK1/JAK3 inhibitor and can find use in the treatment of chronic inflammatory and autoimmunological diseases.

2. 发明申请

WO2016157091A1 7-(MORPHOLIN-4-YL)PYRAZOLE[1,5-A]PYRIMIDINE DERIVATIVES WHICH ARE USEFUL FOR THE TREATMENT OF IMMUNE OR INFLAMMATORY DISEASES OR CANCER 审中-公开
标题翻译： 7-（MORPHOLIN-4-YL）吡唑[1,5-A]吡嗪衍生物，可用于治疗免疫或炎症性疾病或癌症
公开(公告)号：WO2016157091A1
公开(公告)日：2016-10-06
申请号：PCT/IB2016/051792
申请日：2016-03-30
申请人： CELON PHARMA S.A.
发明人： DYMEK, Barbara , ZAGOZDA, Marcin , WIECZOREK, Maciej , DUBIEL, Krzysztof , STANCZAK, Aleksandra , ZDZALIK, Daria , GUNERKA, Pawel , SEKULAR, Mariola , DZIACHAN, Maciej
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04 , A61P29/02 , A61P35/00 , A61P37/00 , C07D413/14 , C07D417/14 , C07D519/00
摘要： A compound of the general formula (I) wherein Y represents -CH 2 - or >C=0; R 1 is selected from the group consisting of A1, A2 and A3; R 2 represents dioxothiomorpholino moiety B1, piperazinyl moiety B2, azetidinyl moiety B3, or piperidinyl moiety B4; R 3 is selected from the group consisting of H, halogen, and C1 -C4 alkyl; R 4 is selected from the group consisting of C1 -C4 alkyl, C3-C4- cycloalkyl, C1 -C4 alkyl substituted with C1 -C4 alkoxy, and CHF 2 , and their pharmaceutically acceptable salts. Pharmaceutical compositions comprising said compounds and their use in the treatment of diseases of immune system, inflammatory diseases and cancer.
摘要翻译：通式（I）的化合物，其中Y表示-CH 2 - 或> C = 0; R1选自A1，A2和A3; R2表示二氧代硫代吗啉代部分B1，哌嗪基部分B2，氮杂环丁烷基部分B3或哌啶基部分B4; R 3选自H，卤素和C 1 -C 4烷基; R 4选自C 1 -C 4烷基，C 3 -C 4环烷基，被C 1 -C 4烷氧基取代的C 1 -C 4烷基和CHF 2，及其药学上可接受的盐。包含所述化合物的药物组合物及其在治疗免疫系统疾病，炎性疾病和癌症中的用途。

3. 发明申请

WO2014016789A1 PYRAZOLO[3,4-D]PYRIMIDIN-4(5H)-ONE DERIVATIVES AS PDE9 INHIBITORS 审中-公开
标题翻译： PYRAZOLO [3,4-D] PYRIMIDIN-4（5H） - 酮衍生物作为PDE9抑制剂
公开(公告)号：WO2014016789A1
公开(公告)日：2014-01-30
申请号：PCT/IB2013/056086
申请日：2013-07-24
申请人： CELON PHARMA S.A.
发明人： MOSZCZYŃSKI-PĘTKOWSKI, Rafał , BOJARSKI, Łukasz , STEFANIAK, Filip , WIECZOREK, Maciej , DUBIEL, Krzysztof , LAMPARSKA-PRZYBYSZ, Monika
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00
CPC分类号： C07D487/04
摘要： A compound of the general formula (I) wherein R 1 is selected from the group consisting of phenyl unsubstituted or substituted with 1 to 3 substituents selected from F, Cl, Br, I, CN, -O-C1-C3-alkyl, fluorinated -O-C1-C3-alkyl, -(CH 2 ) m OH and 5-membered heterocyclic group with 1 or 2 heteroatoms selected from N, O and S; and 6- or 10-membered heteroaryl with 1 to 3 heteroatoms selected from O, N and S; R 2 and R 3 independently of each other represent H atom or straight or branched C1-C3 alkyl; R 4 is selected from the group consisting of 4- to 6- membered cycloalkyl, wherein one of carbon atoms can be replaced by O atom, and which is unsubstituted or substituted with one or two halogen atoms,and straight or branched C1-C4 alkyl; Q represents a bond or C1-C3-alkylene, which can be optionally substituted by one to three C1-C3-alkyls; X is selected from the group consisting of O, NR 5 , and S(O) p ; R 5 represents H atom or C1-C3alkyl; m is 1, 2 or 3; p is 0, 1 or 2; and salts thereof, for use as a medicament, in particular for treating cognitive function disorders and neurodegenerative diseases.
摘要翻译：通式（I）的化合物，其中R 1选自未取代的或被1至3个选自F，Cl，Br，I，CN，-O-C 1 -C 3 - 烷基，氟化 - O-C 1 -C 3 - 烷基， - （CH 2）m OH和具有1或2个选自N，O和S的杂原子的5元杂环基; 和具有1至3个选自O，N和S的杂原子的6-或10-元杂芳基; R2和R3彼此独立地表示H原子或直链或支链C1-C3烷基; R4选自4-至6-元环烷基，其中一个碳原子可以被O原子取代，并且是未取代的或被一个或两个卤素原子取代的直链或支链C 1 -C 4烷基; Q表示键或C1-C3-亚烷基，其可任选被一至三个C 1 -C 3 - 烷基取代; X选自O，NR 5和S（O）p; R5表示H原子或C1-C3烷基; m为1,2或3; p为0,1或2; 其盐，用作药物，特别是用于治疗认知功能障碍和神经变性疾病。

4. 发明申请

WO2022250555A1 HUMAN FIBROBLAST GROWTH FACTOR 1 (FGF-1) MUTEINS, THEIR DIMERS AND USES 审中-公开
公开(公告)号：WO2022250555A1
公开(公告)日：2022-12-01
申请号：PCT/PL2022/050032
申请日：2022-05-25
申请人： CELON PHARMA S.A. , UNIWERSYTET WROCŁAWSKI
发明人： OTLEWSKI, Jacek Józef , ZAKRZEWSKA, Małgorzata Urszula , KROWARSCH, Daniel Rafał , CZYREK, Aleksandra Anna , JANISZEWSKI, Michał Mieczysław , PIECZYKOLAN, Jerzy Szczepan , DRZAZGA, Ewa , BAZYDŁO-GUZENDA, Katarzyna , BUDA, Paweł , WIECZOREK, Maciej
IPC分类号： C07K14/50 , C07K14/71 , C07K14/501
摘要： The present invention relates to human fibroblast growth factor (FGF-1) muteins having decreased mitogenicity, dimers of human FGF-1 muteins, as well as such human FGF-1 muteins and dimers of such muteins for use in reducing blood glucose level, particularly for use in the treatment of diabetes.

5. 发明申请

WO2014141015A1 PYRAZOLYLBENZO[D]IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：吡唑并[D]咪唑衍生物
公开(公告)号：WO2014141015A1
公开(公告)日：2014-09-18
申请号：PCT/IB2014/059515
申请日：2014-03-07
申请人： CELON PHARMA S.A.
发明人： ZDZALIK, Daria , LIPNER, Joanna , WIECZOREK, Maciej , DZWONEK, Karolina , YAMANI, Abdellah , DUBIEL, Krzysztof , LAMPARSKA-PRZYBYSZ, Monika , GRYGIELEWICZ, Paulina , STANCZAK, Aleksandra
IPC分类号： C07D403/04 , C07D409/14 , A61K31/5377 , A61K31/496 , A61K31/454 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D409/14
摘要： A compound represented by the general Formula (I), whereinhydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R 1 represents -X-Q-P, wherein X is absent or represents –CH 2 -, –C(O)-, or –C(O)NH-(CH 2 ) k -, wherein k is 0, 1 or 2; Q is selected from the group consisting of Q1, Q2, Q3, Q4 and Q5; P is absent or represents straight-or branched-chain C1-C3 alkyl, –(CH 2 ) l -NR 2 R 3 , or–(CH 2 ) m -C(O)-NR 2 R 3 , wherein l and m independently of each other represent 0, 1 or 2, with the proviso that when B in Q1 represents oxygen atom, then P is absent;and R 2 and R 3 independently represent C1 or C2 alkyl, or R 2 and R 3 together with nitrogen atom to which they are both attached form a 6- membered saturated heterocyclicring, wherein one of carbon atoms can be replaced with oxygen, -NH-or –N(C1-C2)alkyl-; and acid addition salts thereof. The compound can be useful in the treatment of cancer diseases. (I)
摘要翻译：由通式（I）表示的化合物，其中与吡唑和苯并咪唑环连接的氢原子分别连接到吡唑或苯并咪唑环的氮原子之一; R 1表示-X-Q-P，其中X不存在或表示-CH 2 - ， - C（O） - 或-C（O）NH-（CH 2）k - ，其中k为0,1或2; Q选自Q1，Q2，Q3，Q4和Q5; P不存在或表示直链或支链C 1 -C 3烷基， - （CH 2）1 -NR 2 R 3或 - （CH 2）m C（O）-NR 2 R 3，其中l和m彼此独立地表示0,1或2 条件是当Q1中的B表示氧原子时，则P不存在; R 2和R 3独立地表示C 1或C 2烷基，或者R 2和R 3与它们所连接的氮原子一起形成6-元饱和杂环，其中一个碳原子可以被氧，-NH-或-N（C1-C2）烷基 - 取代; 及其酸加成盐。该化合物可用于治疗癌症疾病。（一世）

6. 发明申请

WO2014024125A1 PYRAZOLO[4,3-D]PYRIMIDIN-7(6H)-ONE DERIVATIVES AS PDE9 INHIBITORS 审中-公开
标题翻译： PYRAZOLO [4,3-D] PYRIMIDIN-7（6H） - 酮衍生物作为PDE9抑制剂
公开(公告)号：WO2014024125A1
公开(公告)日：2014-02-13
申请号：PCT/IB2013/056423
申请日：2013-08-06
申请人： CELON PHARMA S.A.
发明人： MOSZCZYNSKI-PETKOWSKI, Rafal , BOJARSKI, Lukasz , MAJER, Jakub , WIECZOREK, Maciej , DUBIEL, Krzysztof , LAMPARSKA-PRZYBYSZ, Monika
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04
摘要： Pyrazolo[4,3-d]pyrimidin-7(6H)-one derivatives represented by the general formula (I), wherein R 1 represents hydrogen atom or methyl; when R 1 represents hydrogen atom, then R 2 represents cyclopentyl, tetrahydropyranyl, cyclohexyl, or cyclohexyl substituted with 1 or 2 halogen atoms; when R 1 represents methyl, then R 2 represents cyclopentyl; R 3 is selected from the group consisting of phenyl unsubstituted or substituted with 1 to 3 substituents selected from F, CI, Br, I, and OCH 3 ; and 6- to 10-membered heteroaryl with 1 to 3 heteroatoms selected independently form O, N and S; and Q represents C1 -C3-alkylene group, which is unsubstituted or substituted with 1 to 3 C1 -C3-alkyl groups; and their salts. The compounds are PDE9A inhibitors useful as medicaments, in particular for treatment of cognitive function disorders and neurodegenerative diseases.
摘要翻译：由通式（I）表示的吡唑并[4,3-d]嘧啶-7（6H） - 酮衍生物，其中R1表示氢原子或甲基; 当R 1表示氢原子时，R 2表示被1或2个卤素原子取代的环戊基，四氢吡喃基，环己基或环己基; 当R 1表示甲基时，R 2表示环戊基; R3选自未取代的或被1至3个选自F，Cl，Br，I和OCH 3的取代基取代的苯基; 和具有1至3个独立选自O，N和S的杂原子的6-至10-元杂芳基; 且Q表示未被取代或被1至3个C 1 -C 3 - 烷基取代的C 1 -C 3 - 亚烷基; 和它们的盐。该化合物是用作药物的PDE9A抑制剂，特别是用于治疗认知功能障碍和神经变性疾病。

7. 发明申请

WO2019097282A1 ISOINDOLINE DERIVATIVES FOR THE TREATMENT OF CNS DISEASES 审中-公开
公开(公告)号：WO2019097282A1
公开(公告)日：2019-05-23
申请号：PCT/IB2017/057247
申请日：2017-11-20
申请人： CELON PHARMA S.A. , UNIWERSYTET JAGIELLONSKI , INSTYTUT FARMAKOLOGII POLSKIEJ AKADEMII NAUK
发明人： KAMINSKI, Krzysztof , GRYCHOWSKA, Katarzyna , CANALE, Vittorio , BOJARSKI, Andrzej J. , SATALA, Grzegorz , LENDA, Tomasz , POPIK, Piotr , MATLOKA, Mikolaj , DUBIEL, Krzysztof , MOSZCZYNSKI-PETKOWSKI, Rafal , PIECZYKOLAN, Jerzy , WIECZOREK, Maciej , ZAJDEL, Pawel
IPC分类号： C07D403/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D487/08 , C07D209/44 , A61P25/28 , A61K31/4035
CPC分类号： C07D209/44 , A61K31/4035 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5513 , A61K31/554 , A61P25/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/04 , C07D487/08
摘要： A compound of the formula (I) wherein R 1 represents hydrogen atom and R 2 represents moiety of the formula G1, or R 1 and R 2 are connected with each other to form with nitrogen atom to which they are attached a moiety of the formula G2; A is selected from the group consisting of phenyl substituted with one or two substituents selected from the group consisting of halogen atom, straight or branched C1- C4 alkyl, C1-C2 alkoxyl, CF 3 , CN, and -OCF 3 , naphthyl, quinolinyl, thienyl, thienyl substituted with halogen atom, and pyridyl; X is selected from the group consisting of -NR 4 , -0-, and -CHN(R 5 ) 2 ; R 3 is selected from the group consisting of hydrogen atom, methyl, ethyl, and cyclopropyl; R 4 is selected from the group consisting of hydrogen atom, straight or branched C1-C4 alkyl, straight or branched C1-C4 alkyl substituted with one or two halogen atoms, cyclopropyl and methylcyclopropyl; R 5 represents C1-C2 alkyl; k is an integer equal 1 or 2; I is an integer equal 1 or 2; m is an integer equal 0, 1 or 2; n is an integer 0 or 1 when X represents -NR4"or -CHN(R5) 2, wherein n is 1 only when m is 1; and n is 0 when X represents -0-; and acid addition salts thereof, can be useful as selective inhibitors of 5HT6 in the treatment of CNS diseases.

8. 发明申请

WO2014020531A1 IMIDAZO[1,2-B]PYRIDAZIN-6-AMINE DERIVATIVES AS KINASE JAK-2 INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-B]吡嗪-6-胺衍生物作为激酶JAK-2抑制剂
公开(公告)号：WO2014020531A1
公开(公告)日：2014-02-06
申请号：PCT/IB2013/056241
申请日：2013-07-30
申请人： CELON PHARMA S.A.
发明人： DZWONEK, Karolina , MROCZKIEWICZ, Michal , STEFANIAK, Filip , WIECZOREK, Maciej , DUBIEL, Krzysztof , LAMPARSKA-PRZYBYSZ, Monika
IPC分类号： C07D487/04 , A61P35/00 , A61K31/5025 , A61K31/506
CPC分类号： C07D487/04
摘要： A compound represented by the general formula (I) wherein R 1 represents H or C 1 -C 4 alkyl; R 2 represents phenyl substituted with one or two substituents selected from the group consisting of halogen atom and OC 1 -C 4 alkyl;R 3 represents phenyl or 5 to 10-membered monocyclic or bicyclic heteroaryl having from 1 to 4 ring heteroatoms selected from the group consisting of N, S, and O, which can be unsubstituted or substituted with a substituent selected from halogen atom, C 1 -C 4 -alkyl, and -C(O)O-C 1 -C 4 -alkyl; and X represents –CH 2 -group or carbonyl-C(O)-group;and their acid addition salts;with the exclusion of 3-(4-chloro-2-fluorobenzyl)-2-methyl- N -(5-methyl-1 H -pyrazol-3-yl)-8-(morpholinomethyl)-imidazo[1,2- b ]pyridazine-6-amine and its salts. The compounds are JAK2 inhibitors and are useful as medicaments, especially for treating proliferative disorders and cancer diseases
摘要翻译：由通式（I）表示的化合物，其中R 1表示H或C 1 -C 4烷基; R 2表示被一个或两个选自卤素原子和OC 1 -C 4烷基的取代基取代的苯基; R 3表示苯基或具有1至4个选自下组的环状杂原子的5至10元单环或双环杂芳基，S和O，其可以是未取代的或被选自卤素原子，C 1 -C 4 - 烷基和-C（O）O-C 1 -C 4 - 烷基的取代基取代; 并且X代表-CH2-基或羰基-C（O） - 基团;及其酸加成盐;除了3-（4-氯-2-氟苄基）-2-甲基-N-（5-甲基 - -8-（吗啉代甲基） - 咪唑并[1,2-b]哒嗪-6-胺及其盐。这些化合物是JAK2抑制剂，可用作药物，特别是用于治疗增殖性疾病和癌症疾病

9. 发明申请

WO2020239244A1 AN INHALER FOR ELECTRONICALLY SUPERVISED PARENTERAL ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION 审中-公开
公开(公告)号：WO2020239244A1
公开(公告)日：2020-12-03
申请号：PCT/EP2019/064244
申请日：2019-05-31
申请人： CELON PHARMA S.A.
发明人： WIECZOREK, Maciej , WIECZOREK, Artur , TRATKIEWICZ, Ewa , MAJSTRUK, Maciej
IPC分类号： A61M15/00 , A61B5/00 , A61K9/00
摘要： An inhaler (400) for electronically supervised parenteral administration of a dry powder pharmaceutical composition comprising: storage means (410) for the pharmaceutical composition in a form of a dry powder; administration means (411) for administration of the pharmaceutical composition; memory (404) and processing means (402); communication means (401); controlled blocking means (403) for blocking administration of the pharmaceutical composition, wherein the inhaler (400) is adapted to receive data corresponding to an administration scheme (11), to determine whether a mobile device (300) with an authorisation token assigned thereto is present, and to control the controlled blocking means (403) so as to allow administration of the pharmaceutical composition only with compliance with the administration scheme (11) in the presence of the mobile device (300) with the authorisation token (12) assigned thereto.

10. 发明申请

WO2020239243A1 ELECTRONICALLY SUPERVISED ADMINISTRATION OF A PHARMACEUTICAL COMPOSITION 审中-公开
公开(公告)号：WO2020239243A1
公开(公告)日：2020-12-03
申请号：PCT/EP2019/064243
申请日：2019-05-31
申请人： CELON PHARMA S.A.
发明人： WIECZOREK, Maciej , WIECZOREK, Artur , TRATKIEWICZ, Ewa , MAJSTRUK, Maciej
IPC分类号： G16H20/10 , G16H20/17
摘要： A system for electronically supervised administration of a pharmaceutical composition, that comprises an authorised entity node (100, 200) for an authorised entity, a mobile device (300) of a patient, and a medical device (400) adapted to administer the pharmaceutical composition, wherein the authorised entity node (100, 200) is adapted, when operated by the authorised entity, to generate data corresponding to an administration scheme (11) and an authorisation token (12) for assigning to a patient's mobile device (300), and to send the data corresponding to an administration scheme (11) and authorisation token (12) to the patient's mobile device (300). The mobile device (300) is adapted to send to the authorised entity node (100, 200) the data corresponding to the mobile device (300) and medical device (400), and to receive the authorisation token (12) assigned to a patient's mobile device (300) and send to the medical device (400) the data corresponding to the administration scheme (11) in response to receiving the authorisation token (12) assigned to a patient's mobile device (300). The medical device (400) is provided with a controlled blocking means (403) for blocking administration of the pharmaceutical composition, is adapted to determine whether the mobile device (300) with the authorisation token assigned thereto is present and is adapted to control the controlled blocking means (403) so as to allow administration of the pharmaceutical composition only with compliance with the administration scheme (11) received from the mobile device (300) in the presence of the mobile device (300) with the authorisation token (12) assigned thereto.

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