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1. 发明申请

US20070129375A1 6-Substituted 2-quinolinones and 2-quinoxalinones as poly (adp-ribose) polymerase inhibitors 有权
标题翻译： 6-取代的2-喹啉酮和2-喹喔啉酮作为聚（adp-核糖）聚合酶抑制剂
公开(公告)号：US20070129375A1
公开(公告)日：2007-06-07
申请号：US10596086
申请日：2004-11-18
申请人： Dominique Mabire , Jerome Guillemont , Jacobus Alphonsus Van Dun , Maria Victorina Somers , Walter Boudewijn Wouters
发明人： Dominique Mabire , Jerome Guillemont , Jacobus Alphonsus Van Dun , Maria Victorina Somers , Walter Boudewijn Wouters
IPC分类号： A61K31/498 , A61K31/4709 , A61K31/473 , C07D241/36
CPC分类号： C04B35/632 , C07D241/44 , C07D401/12 , C07D407/06 , C07D409/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4 and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，R 1，R 2， >，R 3，R 4和X具有定义的含义。

2. 发明申请

US20070072842A1 6-Alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adpribose) polymerase inhibitors 有权
标题翻译： 6-烯基和6-苯基烷基取代的2-喹啉酮和2-喹喔啉酮作为聚（adpribose）聚合酶抑制剂
公开(公告)号：US20070072842A1
公开(公告)日：2007-03-29
申请号：US10595891
申请日：2004-11-18
申请人： Mabire Dominique , Jerome Guillemont , Jacobus Alphonsus Van Dun , Maria Victorina Somers , Walter Wouters
发明人： Mabire Dominique , Jerome Guillemont , Jacobus Alphonsus Van Dun , Maria Victorina Somers , Walter Wouters
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/498 , A61K31/4747 , A61K31/4709 , C07D403/02 , C07D413/02
CPC分类号： C07D215/227 , C07D241/44 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/12
摘要： The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
摘要翻译：本发明提供式（I）化合物和式（VII-a）化合物以及包含所述化合物的药物组合物及其作为PARP抑制剂的用途，其中n，R 1，R 2， 2，R 3，R 4，R 5，R 6，R 6， 7，R e，R d和X具有限定的含义。

3. 发明申请

US20070082895A1 Novel mycobacterial inhibitors 有权
标题翻译：新型分枝杆菌抑制剂
公开(公告)号：US20070082895A1
公开(公告)日：2007-04-12
申请号：US10596386
申请日：2005-01-21
申请人： Jerome Guillemont , Elisabeth Pasquier
发明人： Jerome Guillemont , Elisabeth Pasquier
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/14 , C07D413/14
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R8 is oxo; or R7 and R8 taken together form the radical CH═CH—N═; Z is CH2 or C(═O). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as M. tuberculosis, M. bovis, M. avium, M. smegmatis and M. marinum. Also claimed is a pharmaceutical composition containing a compound of the present invention, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或通式（Ib）的新的取代喹啉衍生物，其盐，季胺，立体化学异构形式，互变异构形式和N-氧化物形式，其中R 1，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，硫代，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式R 3的基团是烷基，Ar，Ar- 烷基，Het或Het-烷基; R 4是氢，烷基或苄基; R 5是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; 或两个邻位R 5个基团可以与它们所连接的苯环一起形成萘基; r为1,2,3,4或5; R 6是氢，烷基，Ar或Het; R 7是氢或烷基; R 8是氧代; 或R 7和R 8一起形成基团CH-CH-N-; Z是CH 2或C（-O）。所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌，耻垢分枝杆菌和马氏海马。还要求保护的是含有本发明化合物，所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途的药物组合物及其制备方法。

4. 发明申请

US20060252764A1 HIV inhibiting pyrimidines derivatives 有权
公开(公告)号：US20060252764A1
公开(公告)日：2006-11-09
申请号：US11474855
申请日：2006-06-26
申请人： Jerome Guillemont , Patrice Palandijian , Marc De Jonge , Lucien Koymans , Hendrik Vinkers , Frederik Daeyaert , Jan Heeres , Koen Van Aken , Paulus Lewi , Paul Janssen , Frank Xavier Arts
发明人： Jerome Guillemont , Patrice Palandijian , Marc De Jonge , Lucien Koymans , Hendrik Vinkers , Frederik Daeyaert , Jan Heeres , Koen Van Aken , Paulus Lewi , Paul Janssen , Frank Xavier Arts
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07C255/42 , C07C257/12 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N═N—, —O—, —C(═O)—, C1-4alkanediyl, —CHOH—, —S—, —S(═O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1-6alkyl substituted with hydroxy and a second substituent; —C(═N—O—R8)—C1-4alkyl; R7; or —X3—R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

5. 发明授权

US5157133A Dihydropyran derivatives, processes for preparation and use 失效
标题翻译：二氢衍生物，制备和使用方法
公开(公告)号：US5157133A
公开(公告)日：1992-10-20
申请号：US620609
申请日：1990-12-03
申请人： Pierre F. Chabardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
发明人： Pierre F. Chabardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
IPC分类号： C07C45/60 , C07C403/14 , C07D309/30 , C07D311/72 , C07D403/14
CPC分类号： C07C403/14 , C07C45/60 , C07D309/30
摘要： The present invention relates to dihydropyran derivatives, processes for preparing, and processes of using the derivatives. The derivatives are prepared by condensation of lithium dienolate of prenal with an aldehyde or a ketone.The pyran derivative prepared from .beta.-ionylideneacetaldehyde when treated in the presence of a catalyst directly forms retinal.
摘要翻译：本发明涉及二氢吡喃衍生物，制备方法和使用衍生物的方法。衍生物通过将prenal的二烯酸锂与醛或酮的缩合来制备。由β-亚酰基乙醛制备的吡喃衍生物在催化剂存在下处理直接形成视网膜。

6. 发明申请

US20070208022A1 HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES 有权
公开(公告)号：US20070208022A1
公开(公告)日：2007-09-06
申请号：US11576068
申请日：2005-09-29
申请人： Jerome Guillemont , Jan Heeres , Paulus Lewi
发明人： Jerome Guillemont , Jan Heeres , Paulus Lewi
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/506 , C07D403/02 , C07D413/02
CPC分类号： C07D403/12 , C07D239/48 , C07D239/50 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylthio; —S(═O)rR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(═O)—, CH2, —CHOH—, —S—, —S(═O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X3—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is —Y—CqH2q-L or —CqH2q—Y—CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceutical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

7. 发明申请

US20070093478A1 Novel mycobacterial inhibitors 有权
标题翻译：新型分枝杆菌抑制剂
公开(公告)号：US20070093478A1
公开(公告)日：2007-04-26
申请号：US10596270
申请日：2005-01-21
申请人： Jerome Guillemont , Elisabeth Pasquier , David Lancois
发明人： Jerome Guillemont , Elisabeth Pasquier , David Lancois
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4709 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D215/14 , C07D215/227 , C07D215/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomers forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula is equal to 0 or 1 and R7 is hydrogen or Ar. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或通式（Ib）的其取代的喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其互变异构体形式的立体化学异构形式和 N-氧化物形式。所要求保护的化合物可用于治疗分枝杆菌病。特别地，要求保护的化合物，其中R 1彼此独立地为卤素; p = 1; R 2是任选取代的烷氧基，烷基，Ar，Het或式R 3的基团是任选取代的Ar或Het; q = 1，R 4和R 5各自独立地为烷基; R 6是氢或式的基团等于0或1，R 7是氢或Ar。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要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途以及制备方法要求保护的化合物。

8. 发明申请

US20070021449A1 Pyrimidine derivatives for the prevention of hiv infection 审中-公开
标题翻译：嘧啶衍生物用于预防HIV感染
公开(公告)号：US20070021449A1
公开(公告)日：2007-01-25
申请号：US10544735
申请日：2004-02-04
申请人： Jan Heeres , Paulus Lewi , Paul Janssen , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Hendrik Vinkers , Jerome Guillemont , Elisabeth Pasquier , Frank Xavier Arts
发明人： Jan Heeres , Paulus Lewi , Paul Janssen , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Hendrik Vinkers , Jerome Guillemont , Elisabeth Pasquier , Frank Xavier Arts
IPC分类号： A61K31/513 , C07D239/47
CPC分类号： A61K31/513 , C07D239/47 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及化合物在制备药物中的用途，所述药物通过性交和伴侣之间的相关紧密接触来预防HIV感染，其中所述化合物是式（I）的化合物，N-氧化物，药学上可接受的添加剂盐，季胺及其立体化学异构形式，其中含-a 1〜 > 4 - 和 - b 1 - b 2 - b 3 - b 4 - 表示苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基; 和包含它们的药物组合物。

9. 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。

10. 发明申请

US20060281741A1 Quinoline derivatives as antibacterial agents 有权
公开(公告)号：US20060281741A1
公开(公告)日：2006-12-14
申请号：US11296918
申请日：2005-12-08
申请人： Koenraad Jozef Marcel Andries , Anil Koul , Jerome Guillemont , Elisabeth Therese Pasquier
发明人： Koenraad Jozef Marcel Andries , Anil Koul , Jerome Guillemont , Elisabeth Therese Pasquier
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/53 , A61K31/4709 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D215/227 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D215/36 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , Y02A50/473
摘要： The present invention relates to the use of a compound for the manufacture of a medicament for the treatment of a bacterial infection, said compound being a compound of formula a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, Ar or Het; p is an integer equal to 1 or 2; R2 is C1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy or C1-6alkylthio; R3 is Ar, Het or Het1; R4 and R5 each independently are hydrogen, C1-6alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl, 2-pyrazolinyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1-6alkyl, C1-6alkyloxy, amino, mono- or di(C1-6alkyl)amino, C1-6alkylthio, C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl or pyrimidinyl; R6 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; r is an integer equal to 1 or 2; R7 is hydrogen, C1-6alkyl, Ar, Het or Het1; provided that the bacterial infection is other than a Mycobacterial infection.

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