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1. 发明专利

IL258553D0 N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use 未知
公开(公告)号：IL258553D0
公开(公告)日：2018-05-31
申请号：IL25855318
申请日：2018-04-08
申请人： GALAPAGOS NV , ABBVIE SARL , AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
发明人： AKKARI RHALID , ALVEY LUKE JONATHAN , BOCK XAVIER MARIE , BROWN BRIAN S , CLAES PIETER ISABELLE ROGER , COWART MARLON D , DE LEMOS ELSA , DESROY NICOLAS , DUTHION BERANGER , GFESSER GREGORY A , GOSMINI ROMAIN LUC MARIE , HOUSSEMAN CHRISTOPHER GAETAN , JANSEN KOEN KAREL , JI JIANGUO , KYM PHILIP R , LEFRANCOIS JEAN-MICHEL , MAMMOLITI OSCAR , MENET CHRISTEL JEANNE MARIE , MERAYO NURIA MERAYO , NEWSOME GREGORY JOHN ROBERT , PALISSE ADELINE MARIE ELISE , PATEL SACHIN V , PIZZONERO MATHIEU RAFAEL , SHRESTHA ANURUPA , SWIFT ELIZABETH C , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , DE BLIECK ANN
IPC分类号： C07D20060101
摘要： wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

2. 发明专利

IL273163D0 Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use 未知
公开(公告)号：IL273163D0
公开(公告)日：2020-04-30
申请号：IL27316320
申请日：2020-03-09
申请人： GALAPAGOS NV , ALTENBACH ROBERT J , BOGDAN ANDREW , LIU BO , MALAGU KARINE FABIENNE , SEARLE XENIA B , YEUNG MING C , DESROY NICOLAS , GFESSER GREGORY A , HOUSSEMAN CHRISTOPHER GAETAN , KYM PHILIP R , PIZZONERO MATHIEU RAFAEL , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , ABBVIE OVERSEAS SARL , COUTY SYLVAIN , MAI THI THU TRANG , MERAYO MERAYO NURIA , PICOLET OLIVIER LAURENT
发明人： ALTENBACH ROBERT J , BOGDAN ANDREW , LIU BO , MALAGU KARINE FABIENNE , SEARLE XENIA B , YEUNG MING C , DESROY NICOLAS , GFESSER GREGORY A , HOUSSEMAN CHRISTOPHER GAETAN , KYM PHILIP R , PIZZONERO MATHIEU RAFAEL , VAN DER PLAS STEVEN EMIEL , WANG XUEQING , COUTY SYLVAIN , MAI THI THU TRANG , MERAYO MERAYO NURIA , PICOLET OLIVIER LAURENT
IPC分类号： C07D20060101
摘要： The invention discloses compounds of Formula (I):wherein A 1 , R 1 , R 2 , R 3 , R 4 , and n are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis and pharmaceutical compositions comprising the same. Also disclosed are methods for their production and methods of treating cystic fibrosis by administering the compounds.

3. 发明申请

WO2008038136A2 NEW CHEMICAL INHIBITORS OF BACTERIAL HEPTOSE SYNTHESIS, METHODS FOR THEIR PREPARATION AND BIOLOGICAL APPLICATIONS OF SAID INHIBITORS 审中-公开
标题翻译：细菌肝素合成新化学抑制剂，其抑制剂的制备和生物应用方法
公开(公告)号：WO2008038136A2
公开(公告)日：2008-04-03
申请号：PCT/IB2007/003276
申请日：2007-09-25
申请人： MUTABILIS SA , ESCAICH, Sonia , DENIS, Alexis , MOREAU, François , GERUSZ, Vincent , DESROY, Nicolas
发明人： ESCAICH, Sonia , DENIS, Alexis , MOREAU, François , GERUSZ, Vincent , DESROY, Nicolas
CPC分类号： C07D417/14 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR 1 , C1-C10 alkyl-NR 1 R 1 , alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO 2 R 1 , NR 1 R 1 , NR 1 C(O)R 1 , C(O)NR 1 R 1 , NR 1 C(S)R 1 , C(S)NR 1 R 1 , SO 2 NR 1 R 1 , SO 2 R 1 , NR 1 SO 2 R 1 , NR 1 C(O)NR 1 R 1 , NR 1 C(O)OR 1 , NR 1 C(S)NR 1 R 1 , NR 1 C(S)OR 1 , R 1 C=NOR 1 , C(O)R 1 , aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B 1 , B 2 , B 3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B 4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
摘要翻译：本发明涉及具有式（I）的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药，其中A是芳基或杂环，任选被一个或多个相同或不同的R如H，C1 -C 10烷基，C 1 -C 10烷基-OR 1，C 1 -C 10烷基-NR 1 R 1，烷氧基，羟基，硫代烷基，芳基，杂环，卤素，硝基，氰基，CO 2 R 1，NR 1 R 1，NR N， C（O）R 1，C（O）NR 1 R 1，NR 1， C（S）R 1，C（S）NR 1 R 1，SO 2 NR 3， 2个1，1个，1个，1个，2个，1个，1个，1个，1个，1个，3个， NR 1，NR 1，NR 1，NR 1，NR 1， 1个C（O）OR 1，NR 1 C（S）NR 1 R 1，，NR 1 C（S）OR 1，R 1 C = NOR 1，C（O）R 芳氧基，硫代芳基，烯基，炔基R1相同或相同不同的是H或C 1 -C 10烷基B 1，B 2，B 3 3相同或不表示C，N，O，S以形成一个五元芳环，其中一至三个碳原子被选自任选被一个或多个相同或不同的R如上面定义的R 4取代的S，O，N的杂原子取代为C 或NY为H，任选被一个或几个相同或不同的R取代的C 1 -C 10烷基，烷氧基，硫代烷基，W如C，O或N，被一个或多个C 1 -C 10烷基取代或不被 D是任选被一个或多个相同或不同的R取代的杂环，如上所定义。

4. 发明申请

WO2010001220A1 NEW 1,2,4-TRIAZINE DERIVATIVES AND BIOLOGICAL APPLICATIONS THEREOF 审中-公开
标题翻译：新的1,2,4-三唑衍生物及其生物应用
公开(公告)号：WO2010001220A1
公开(公告)日：2010-01-07
申请号：PCT/IB2009/006101
申请日：2009-06-29
申请人： MUTABILIS SA , DESROY, Nicolas , DENIS, Alexis , GERUSZ, Vincent , OLIVEIRA, Chrystelle , VONGSOUTHI, Vanida , MOREAU, Françoise , ESCAICH, Sonia
发明人： DESROY, Nicolas , DENIS, Alexis , GERUSZ, Vincent , OLIVEIRA, Chrystelle , VONGSOUTHI, Vanida , MOREAU, Françoise , ESCAICH, Sonia
IPC分类号： C07D417/12 , A61K31/53 , A61P31/00
CPC分类号： C07D417/12 , C07D403/12 , C07D413/12 , C07D417/14 , C07D513/04
摘要： The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.
摘要翻译：本发明涉及式（I）的新的1,2,4-三嗪衍生物：其中A，B，R2和Y在本申请中的定义，它们的制备和中间体，它们作为药物和药物组合物的用途以及含有它们的缔合物。式（I）化合物能够抑制细菌性肝炎合成。

5. 发明申请

WO2008038136A3 SUBSTITUTED HETEROCYCLYLCARBONYLAMINO-ACETIC-ACID-DERIVATIVES AS INHIBITORS OF BACTERIAL HEPTOSE SYNTHESIS, METHODS FOR THEIR PREPARATION AND BIOLOGICAL APPLICATIONS OF SAID INHIBITORS 审中-公开
标题翻译：作为细菌肝素合成抑制剂的取代的杂环碳酰氨基 - 乙酸衍生物，其制备和抑制剂的生物应用的方法
公开(公告)号：WO2008038136A3
公开(公告)日：2008-08-14
申请号：PCT/IB2007003276
申请日：2007-09-25
申请人： MUTABILIS SA , ESCAICH SONIA , DENIS ALEXIS , MOREAU FRANCOIS , GERUSZ VINCENT , DESROY NICOLAS
发明人： ESCAICH SONIA , DENIS ALEXIS , MOREAU FRANCOIS , GERUSZ VINCENT , DESROY NICOLAS
IPC分类号： C07D401/12 , A61K31/4427 , A61P31/04 , C07D405/12 , C07D417/12 , C07D417/14
CPC分类号： C07D417/14 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR 1 , C1-C10 alkyl-NR 1 R 1 , alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO 2 R 1 , NR 1 R 1 , NR 1 C(O)R 1 , C(O)NR 1 R 1 , NR 1 C(S)R 1 , C(S)NR 1 R 1 , SO 2 NR 1 R 1 , SO 2 R 1 , NR 1 SO 2 R 1 , NR 1 C(O)NR 1 R 1 , NR 1 C(O)OR 1 , NR 1 C(S)NR 1 R 1 , NR 1 C(S)OR 1 , R 1 C=NOR 1 , C(O)R 1 , aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B 1 , B 2 , B 3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B 4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
摘要翻译：本发明涉及具有式（I）的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药，其中A是芳基或杂环，任选被一个或几个相同或不同的R如H，C1 -C 10烷基，C 1 -C 10烷基-OR 1，C 1 -C 10烷基-NR 1 R 1，烷氧基，羟基，硫代烷基，芳基，杂环，卤素，硝基，氰基，CO 2 R 1，NR 1 R 1，NR N， C（O）R 1，C（O）NR 1 R 1，NR 1， C（S）R 1，C（S）NR 1 R 1，SO 2 NR 2， 1个1，1个，1个，1个，1个，1个，2个，1个，1个，1个， NR 1，NR 1，NR 1，NR 1，NR 1， 1个C（O）或1个NR 1，NR 1 C（S）NR 1 R 1，，NR 1 C（S）OR 1，R 1 C = NOR 1，C（O）R 芳氧基，硫代芳基，烯基，炔基R1相同或相同不同的是H或C 1 -C 10烷基B 1，B 2，B 3 3相同或不表示C，N，O，S以形成一个五元芳环，其中一至三个碳原子被选自任选被一个或多个相同或不同的R如上面定义的R 4取代的S，O，N的杂原子取代为C 或NY为H，任选被一个或几个相同或不同的R取代的C 1 -C 10烷基，烷氧基，硫代烷基，W如C，O或N，被一个或多个C 1 -C 10烷基取代或不被 D是任选被一个或多个相同或不同的R取代的杂环，如上所定义。

6. 发明申请

WO2012172043A1 PURINE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS FOR PREVENTION OR TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译：嘌呤衍生物及其作为预防或治疗细菌感染的药物
公开(公告)号：WO2012172043A1
公开(公告)日：2012-12-20
申请号：PCT/EP2012/061428
申请日：2012-06-15
申请人： LABORATOIRE BIODIM , ATAMANYUK, Dmytro , DENIS, Alexis , GERUSZ, Vincent , LEDOUSSAL, Benoît , BONVIN, Yannick , DESROY, Nicolas , GOLD, Johan , MOREAU, François , OXOBY, Mayalen
发明人： ATAMANYUK, Dmytro , DENIS, Alexis , GERUSZ, Vincent , LEDOUSSAL, Benoît , BONVIN, Yannick , DESROY, Nicolas , GOLD, Johan , MOREAU, François , OXOBY, Mayalen
IPC分类号： C07D473/32 , A61K31/52 , A61P31/04
CPC分类号： C07D473/32
摘要： The invention relates to the compounds of general formula (I) and their addition salts thereof with acids and bases: wherein A is phenyl, naphthyl and 5-10 membered monocyclic or bicyclic unsaturated heterocycle, optionally substituted by a group R1 which is as defined in the application and is itself optionally substitutes by a group R2 which is as defined in the application and is itself optionally substituted by a group R3 which is defined in the application, Y and W, identical or different, are H, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, (C 2 -C 6 ) alkynyl, phenyl or 4-10 monocyclic or bicyclic saturated or unsaturated heterocycle, optionally substituted by R1, or Y and/or W form a 4-10 membered cycle with R1, or Y and W form with N a saturated or unsaturated nitrogenous 4-10 membered mono, bi or tricyclic system, fused, bridged or spiro system, said system being optionally substituted by R1, said system being different from morpholine, with the proviso that when Y and A are phenyl or heterocycle, W is not H, a process and intermediates for their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.
摘要翻译：本发明涉及通式（I）的化合物及其与酸和碱的加成盐：其中A是苯基，萘基和5-10元单环或双环不饱和杂环，任选地被如下定义的基团R 1所取代：本申请本身可以任选地被如申请中定义的基团R2取代，并且本身任选被在应用中定义的基团R 3取代，Y和W相同或不同，为H，（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基，苯基或4-10单环或双环饱和或不饱和杂环，任选被R 1取代，或Y和/或W与R 1形成4-10元环，或Y和W与N形成饱和或不饱和的含氮4-10元单，双或三环系统，稠合，桥连或螺环系统，所述系统任选被R 1取代，所述系统不同于吗啉，条件是当 Y和A是苯基或杂环 W不是H，它们的制备方法和中间体以及它们在抗菌预防和治疗中的用途，其单独使用或与抗菌剂，抗毒素剂或增强宿主先天免疫力的药物联合使用，以及含有它们的药物组合物和组合物。

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