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1. 发明授权

US09127010B2 Preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid 有权
标题翻译：制备13-环己基-3-甲氧基-6- [甲基 - （2- {2- [甲基 - （氨磺酰基） - 氨基] - 乙氧基} - 乙基） - 氨基甲酰基] -7H-吲哚并[2,1-a ] - [2] - 苯并氮杂-10-羧酸
公开(公告)号：US09127010B2
公开(公告)日：2015-09-08
申请号：US13805607
申请日：2011-06-24
申请人： Tom Cornelis Hortense Govaerts , Jean-Pierre-Andre Marc Bongartz , Patrick Hubert J. Nieste
发明人： Tom Cornelis Hortense Govaerts , Jean-Pierre-Andre Marc Bongartz , Patrick Hubert J. Nieste
IPC分类号： C07D487/04 , C07D223/14 , C07C307/06
CPC分类号： C07C307/06 , C07D223/14 , C07D487/04
摘要： The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.
摘要翻译：本发明涉及一种制备13-环己基-3-甲氧基-6- [甲基 - （2- {2- [甲基 - （氨磺酰基） - 氨基] - 乙氧基} - 乙基） - 氨基甲酰基] - 7H-吲哚并[2,1-a] - [2] - 苯并氮杂-10-羧酸。本发明还涉及一种新的化合物，即在该改进方法中使用的（甲基 - {2- [2-（甲基氨基） - 乙氧基] - 乙基} - 氨磺酰基） - 氨基甲酸叔丁酯。

2. 发明申请

US20100184776A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
公开(公告)号：US20100184776A1
公开(公告)日：2010-07-22
申请号：US12663007
申请日：2008-06-05
申请人： Jean-Pierre Andre Marc Bongartz , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Christophe Francis Robert Nestor Buyck
发明人： Jean-Pierre Andre Marc Bongartz , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Christophe Francis Robert Nestor Buyck
IPC分类号： A61K31/496 , C07D241/04 , A61K31/495 , C07D403/12 , A61P3/04 , A61P3/06 , A61P1/16
CPC分类号： C07D295/215 , C07D231/12
摘要： The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; —NRx—C(═O)—; —C(═O)—NRx—; —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—; —NRx—C(═O)—Z—NRy—C(═O)—O—; —NRx—C(═O)—Z—O—; —NRx—C(═O)—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—; —NRx—C(═O)—Z—C(═O)—O—; —NRx—C(═O)—O—Z—C(═O)—; —NRx—C(═O)—O—Z—C(═O)—O—; —NRx—C(═O)—O—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—Z—; —C(═O)—Z—O—; —C(═O)—NRx—Z—; —C(═O)—NRx—Z—O—; —C(═O)—NRx—Z—C(═O)—O—; —C(═O)—NRx—Z—O—C(═O)—; —C(═O)—NRx—O—Z—; —C(═O)—NRx—Z—NRy—; —C(═O)—NRx—Z—NRy—C(═O)—; —C(═O)—NRx—Z—NRy—C(═O)—O—; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy; —NRx—C(═O)—Z—C(═O)—NRy—; —C(═O)—Z—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—NRx—Z—; —C(═O)—NRx—O—Z—; or —C(═O)—NRx—Z—NRy—; then R1 may also represent hydrogen; R2 and R3 each independently represent hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; C1-6alkyloxyoptionally substituted with C1-4alkyloxy; C1-6alkylthio; polyhaloC1-6alkyloxy; C1-6alkyloxycarbonyl; cyano; aminocarbonyl; mono- or di(C1-4alkyl)aminocarbonyl; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; —S(═O)p-C1-4alkyl; R4 represents hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; C1-6alkylthio; polyhalo-C1-6alkyloxy; C1-6alkyloxycarbonyl wherein C1-6alkyl may optionally be substituted; cyano; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; C1-4alkylcarbonylamino; —S(═O)p-C1-4alkyl; R6R5N—C(═O)—; R6R5N—C1-6alkyl; C3-6cycloalkyl aryl; aryloxy; arylC1-4alkyl; aryl-C(═O)—C1-4alkyl; aryl-C(═O)—; Het; HetC1-4alkyl; Het-C(═O)—C1-4alkyl; Het-C(═O)—; Het-O—; R9 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

3. 发明申请

US20130102777A1 PREPARATION OF 13-CYCLOHEXYL-3-METHOXY-6-[METHYL-(2--ETHYL)-CARBAMOYL]-7H-INDOLO-[2,1-a]-[2]-BENZAZEPINE-10-CARBOXYLIC ACID 有权
标题翻译： 13-环己基-3-甲氧基-6- [甲基 - （2-乙基） - 氨基] -7H-吲哚并[2,1-a] - [2] - 苯甲腈-10-羧酸的制备
公开(公告)号：US20130102777A1
公开(公告)日：2013-04-25
申请号：US13805607
申请日：2011-06-24
申请人： Tom Cornelis Hortense Govaerts , Jean-Pierre-Andre Marc Bongartz , Patrick Hubert J. Nieste
发明人： Tom Cornelis Hortense Govaerts , Jean-Pierre-Andre Marc Bongartz , Patrick Hubert J. Nieste
IPC分类号： C07D487/04 , C07C307/06
CPC分类号： C07C307/06 , C07D223/14 , C07D487/04
摘要： The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.
摘要翻译：本发明涉及一种制备13-环己基-3-甲氧基-6- [甲基 - （2- {2- [甲基 - （氨磺酰基） - 氨基] - 乙氧基} - 乙基） - 氨基甲酰基] - 7H-吲哚并[2,1-a] - [2] - 苯并氮杂-10-羧酸。本发明还涉及一种新的化合物，即在该改进方法中使用的（甲基 - {2- [2-（甲基氨基） - 乙氧基] - 乙基} - 氨磺酰基） - 氨基甲酸叔丁酯。

4. 发明申请

US20100210618A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
公开(公告)号：US20100210618A1
公开(公告)日：2010-08-19
申请号：US12663011
申请日：2008-06-06
申请人： Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Mieerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M. De Waepenaret , Peter Walter Maria Roevens , Petr Vladimirivich Davidenko
发明人： Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Mieerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M. De Waepenaret , Peter Walter Maria Roevens , Petr Vladimirivich Davidenko
IPC分类号： A61K31/397 , C07D401/12 , C07D417/12 , A61K31/497 , A61K31/454 , C07D405/12 , C07D241/04 , A61K31/4965 , C07D211/78 , A61K31/451 , C07D403/12 , C07D413/12 , A61K31/5377 , C07D279/02 , A61K31/541 , C07D279/12 , A61P3/04 , A61P3/06 , A61P3/10 , A61P1/16
CPC分类号： A61K31/4523 , A61K31/451 , A61K31/454 , A61K31/495 , A61K31/496 , C07D207/277 , C07D207/323 , C07D211/26 , C07D211/60 , C07D231/12 , C07D233/54 , C07D233/64 , C07D235/18 , C07D249/08 , C07D257/04 , C07D263/34 , C07D277/56 , C07D279/02 , C07D279/12 , C07D295/20 , C07D295/205 , C07D295/21 , C07D295/215 , C07D307/54 , C07D319/18 , C07D401/12 , C07D417/12 , C07D417/14
摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(═O)—; —C(═O)—C(═O)—; —NRX—C(═O)—; —Z—C(═O)—; —Z—NRX—C(═O)—; —C(═O)—Z—; —NRX—C(═O)—Z—; —C(═S)—; —NRX—C(═S)—; —Z—C(═S)—; —Z—NRX—C(═S)—; —C(═S)—Z—; —NRX—C(═S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(═O)—NRX— or —NRX—C(═O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

5. 发明申请

US20100190789A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
公开(公告)号：US20100190789A1
公开(公告)日：2010-07-29
申请号：US12663013
申请日：2008-06-06
申请人： Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Meerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M De Waepenaert , Peter Walter Maria Roevens , Gustaaf Maria Boeckx , Peter Vladimirivich Davidenko
发明人： Jean-Pierre Andre Marc Bongartz , Joannes Theodorus Maria Linders , Lieven Meerpoel , Guy Rosalia Eugeen Van Lommen , Erwin Coesemans , Mirielle Braeken , Christophe Francis Robert Nestor Buyck , Monique Jenny Marie Berwaer , Katharina Antonia Germania J.M De Waepenaert , Peter Walter Maria Roevens , Gustaaf Maria Boeckx , Peter Vladimirivich Davidenko
IPC分类号： A61K31/5377 , C07D241/04 , A61K31/495 , C07D401/12 , A61K31/496 , C07D403/10 , C07D405/12 , C07D403/12 , C07D413/12 , C07D211/34 , A61K31/451 , A61P3/04 , A61P3/06 , A61P3/10 , A61P1/16
CPC分类号： C07D295/205 , C07D207/09 , C07D211/26 , C07D211/38 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/18 , C07D295/192 , C07D295/21 , C07D295/215 , C07D295/24 , C07D295/26 , C07D307/52 , C07D307/79 , C07D309/04 , C07D317/58 , C07D333/24
摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z 2—NRy—C(=0)—; —NRx—C(=0)-Z2—NRy—C(=0)-; O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)—NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRx—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)—NRy—; —C(═O)—NR—Z2—; —C(═O)—NR—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 O represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

6. 发明申请

US20090030039A1 Piperidine Derivatives as Cxcr3 Receptor Antagonists 审中-公开
标题翻译：哌啶衍生物作为Cxcr3受体拮抗剂
公开(公告)号：US20090030039A1
公开(公告)日：2009-01-29
申请号：US12278719
申请日：2007-02-06
申请人： Erwin Coesemans , Jean-Pierre Andre Marc Bongartz , Guy Rosali Eugeen Van Lommen , Jean Pierre Frans Van Wauwe , Mieke Buntinx
发明人： Erwin Coesemans , Jean-Pierre Andre Marc Bongartz , Guy Rosali Eugeen Van Lommen , Jean Pierre Frans Van Wauwe , Mieke Buntinx
IPC分类号： A61K31/4545 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(═O) or CH2 provided that at least one of Y and Z represents C(═O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的化合物，其N-氧化物，其药学上可接受的盐，其立体化学异构形式或其溶剂合物，其中X表示N或CH; Y和Z各自独立地表示C（-O）或CH 2，条件是Y和Z中的至少一个表示C（-O）; R 1表示CH（R 4） - 芳基或CH（R 4） - 杂芳基; R 2表示芳基2或杂芳基; R3表示氢; C 1-4烷基羰基; 任选被C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基; 条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 4表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代的苯基或与一个或两个C 1 -4-烷基，则R1定义中的芳基不同于被一个卤素或一个或两个C 1-4烷基取代的苯基; 并且条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代或与一个或两个C 1-4烷基取代的苯基，那么R1的定义中的杂芳基不是未取代的噻吩基或未取代的吡啶基。本发明还涉及式（I）化合物在制备用于预防或治疗通过活化CXCR3受体介导的疾病的药物中的用途; 制备式（I）化合物的方法和包含它们的药物组合物。

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