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1. 发明申请

US20050192305A1 HIV inhibiting pyrimidine derivatives 审中-公开
公开(公告)号：US20050192305A1
公开(公告)日：2005-09-01
申请号：US11111400
申请日：2005-04-21
申请人： Koenraad Jozef Andries , Bart De Corte , Marc De Jonge , Jan Heeres , Chih Ho , Marcel Janssen , Paul Janssen , Lucien Koymans , Michael Kukla , Donald Ludovici , Koen Van Aken
发明人： Koenraad Jozef Andries , Bart De Corte , Marc De Jonge , Jan Heeres , Chih Ho , Marcel Janssen , Paul Janssen , Lucien Koymans , Michael Kukla , Donald Ludovici , Koen Van Aken
IPC分类号： C07D239/42 , C07D239/46 , C07D239/48 , C07D239/50 , C07D401/12 , A61K31/506 , C07D43/14
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted: or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl: or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical: for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

2. 发明申请

US20050197354A1 HIV inhibiting pyrimidine derivatives 有权
公开(公告)号：US20050197354A1
公开(公告)日：2005-09-08
申请号：US11111358
申请日：2005-04-21
申请人： Koenraad Jozef Andries , Bart De Corte , Marc De Jonge , Jan Heeres , Chih Ho , Marcel Janssen , Paul Janssen , Lucien Koymans , Michael Kukla , Donald Ludovici , Koen Van Aken
发明人： Koenraad Jozef Andries , Bart De Corte , Marc De Jonge , Jan Heeres , Chih Ho , Marcel Janssen , Paul Janssen , Lucien Koymans , Michael Kukla , Donald Ludovici , Koen Van Aken
IPC分类号： C07D239/42 , C07D239/46 , C07D239/48 , C07D239/50 , C07D401/12 , A61K31/506 , C07D43/02
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D239/49 , C07D239/50 , C07D401/12
摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl. C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

3. 发明申请

US20070021410A1 Respiratory syncytial virus replication inhibitors 失效
标题翻译：呼吸道合胞病毒复制抑制剂
公开(公告)号：US20070021410A1
公开(公告)日：2007-01-25
申请号：US11519719
申请日：2006-09-11
申请人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
发明人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
IPC分类号： A61K31/551 , A61K31/55 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , C07D235/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3 =a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
摘要翻译：本发明涉及式（I）化合物的用途，其中-a-1-a- 是式-CH-CH-CH-CH-，-N-CH-CH-CH-，-CH-N-CH-CH-，-CH-CH-N-CH-， - CH-CH-N-，其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7） -8）。 G是直链或C 1-10烷二基; R 1是任选取代的单环杂环; 用于制备用于治疗病毒感染，特别是RSV感染的药物。某些式（I）化合物是新的。

4. 发明申请

US20060058309A1 Respiratory syncytial virus replication inhibitors 失效
公开(公告)号：US20060058309A1
公开(公告)日：2006-03-16
申请号：US11247392
申请日：2005-10-11
申请人： Frans Janssens , Jean Fernand Lacrampe , Jerome Guillemont , Marc Venet , Koenraad Jozef Andries
发明人： Frans Janssens , Jean Fernand Lacrampe , Jerome Guillemont , Marc Venet , Koenraad Jozef Andries
IPC分类号： A61K31/498 , A61K31/4709 , A61K31/454 , C07D403/02
CPC分类号： C07D401/14 , C07D409/14 , C07D471/04 , Y02P20/55
摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of formula —CH═CH—CH═CH—; —N═CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; CH═CH—CH═N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4); X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3; provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the α position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, arylC1-6alkyl or arylC1-6alkyloxy, R4 is hydrogen, C1-6alkyl or arylC1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)S— wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

5. 发明申请

US20060154913A1 Respiratory syncytial virus replication inhibitors 失效
标题翻译：呼吸道合胞病毒复制抑制剂
公开(公告)号：US20060154913A1
公开(公告)日：2006-07-13
申请号：US11332557
申请日：2006-01-12
申请人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
发明人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
IPC分类号： A61K31/551 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , C07D235/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
摘要翻译：本发明涉及式（I）化合物的用途，其中-a-1-a- 是式-CH-CH-CH-CH-，-N-CH-CH-CH-，-CH-N-CH-CH-，-CH-CH-N-CH-， - CH-CH-CH-，其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7） -8）。 G是直链或C 1-10烷二基; R 1是任选取代的单环杂环; 用于制备用于治疗病毒感染，特别是RSV感染的药物。某些式（I）化合物是新的。

6. 发明申请

US20070249667A1 Use of Substituted Quinoline Derivatives for the Treatment of Drug Resistant Mycobacterial Diseases 审中-公开
标题翻译：使用取代的喹啉衍生物治疗耐药性分枝杆菌病
公开(公告)号：US20070249667A1
公开(公告)日：2007-10-25
申请号：US11569681
申请日：2005-05-24
申请人： Koenraad Jozef Andries , Jozef Van Gestel
发明人： Koenraad Jozef Andries , Jozef Van Gestel
IPC分类号： A61K31/44 , A61P43/00
CPC分类号： A61K31/47 , A61K2300/00
摘要： The present invention relates to the use of a substituted quinoline derivative for the preparation of a medicament for the treatment of an infection with a drug resistant Mycobacterium strain wherein the substituted quinoline derivative is a compound according to Formula (Ia) or Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the above compounds and one or more other antimycobacterial agents.
摘要翻译：本发明涉及取代喹啉衍生物在制备用于治疗耐药性分枝杆菌菌株感染的药物中的用途，其中取代的喹啉衍生物是根据式（Ia）或式（Ib）的化合物其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式及其N-氧化物形式。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的上述化合物和一种或多种其它抗分枝杆菌药物的组合物。

7. 发明申请

US20070015747A1 RESPIRATORY SYNCYTIAL VIRUS REPLICATION INHIBITORS 失效
标题翻译：呼吸道同种病毒复制抑制剂
公开(公告)号：US20070015747A1
公开(公告)日：2007-01-18
申请号：US10817472
申请日：2004-04-02
申请人： Frans Janssens , Kathleen Petrus Meersman , Francois Sommen , Koenraad Jozef Andries
发明人： Frans Janssens , Kathleen Petrus Meersman , Francois Sommen , Koenraad Jozef Andries
IPC分类号： A61K31/551 , A61K31/454 , A61K31/4439 , C07D403/02
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , Y02P20/55
摘要： This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.
摘要翻译：本发明涉及用作呼吸道合胞病毒复制抑制剂等的式（I）化合物前药，加成盐或立体化学异构体形式; 它们的制备方法，含有它们的组合物和它们用于治疗呼吸道合胞病毒感染的方法。

8. 发明申请

US20050239771A1 Respiratory syncytial virus replication inhibitors 失效
标题翻译：呼吸道合胞病毒复制抑制剂
公开(公告)号：US20050239771A1
公开(公告)日：2005-10-27
申请号：US11144126
申请日：2005-06-03
申请人： Frans Janssens , Kathleen Meersman , François Sommen , Jérôme Guillemont , Jean Lacrampe , Koenraad Jozef Andries
发明人： Frans Janssens , Kathleen Meersman , François Sommen , Jérôme Guillemont , Jean Lacrampe , Koenraad Jozef Andries
IPC分类号： A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/443 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/55 , A61K31/551 , A61P31/12 , A61P31/14 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , C07D235/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the use of compounds of formula (I) wherein -a1=a2−a3=a4- is a radical of for CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
摘要翻译：本发明涉及式（I）化合物的用途，其中-a-1-a- 是式-CH = CH-CH = CH，-N-CH-CH-CH-，-CH-N-CH-CH-，-CH-CH-N-CH-，-CH -CH-CH-N-，其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7） -8）。 G是直链或C 1-10烷二基; R 1是任选取代的单环杂环; 用于制备用于治疗病毒感染，特别是RSV感染的药物。某些式（I）化合物是新的。

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