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1. 发明申请

WO2009153569A2 CB1 RECEPTOR MODULATORS 审中-公开
标题翻译： CB1受体调节剂
公开(公告)号：WO2009153569A2
公开(公告)日：2009-12-23
申请号：PCT/GB2009/001539
申请日：2009-06-18
申请人： 7TM PHARMA A/S , MURRAY, Anthony , HOEGBERG, Thomas , COOPER, Martin , BJURLING, Emelie , RECEVEUR, Jean-Marie , NOERREGAARD, Pia, Karina
发明人： MURRAY, Anthony , HOEGBERG, Thomas , COOPER, Martin , BJURLING, Emelie , RECEVEUR, Jean-Marie , NOERREGAARD, Pia, Karina
IPC分类号： C07D401/06 , C07D403/06 , A61K31/4178 , A61P3/04
CPC分类号： C07D401/06 , C07D403/06
摘要： Compounds of formula (I) suppress the normal signalling activity of cannabinoid receptor CB1 and are therefore useful inter alia in the treatment of conditions directly or indirectly associated with obesity and overweight, Wherein A 1 is -COOH or tetrazolyl; R 2 , R 3 , R' 2 and R' 3 are independently selected from -R 9 , - CN, -F, -Cl, -Br, -OR 9 , or -SR 9 ; R 9 is hydrogen, C 1 -C 3 alkyl, cycloalkyl, or fully or partially fluorinated C 1 -C 3 alkyl; R 1 is (i) a bond, or (ii) -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, Or -CH 2 C(R 10 )(R 11 )-*, wherein the bond indicated by an asterisk is attached to Ring A ring; R 10 is hydrogen and R 11 is hydrogen, (C 1 -C 3 alkyl or -OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring; Ring A is an aromatic ring as specified ion the claims; Z 1 is a moncyclic group as specified in the claims.
摘要翻译：式（I）化合物抑制大麻素受体CB1的正常信号传导活性，因此特别可用于治疗与肥胖和超重直接或间接相关的病症，其中A1是-COOH或四唑基; R 2，R 3，R'2和R'3独立地选自-R 9，-CN，-F，-Cl，-Br，-OR 9或-SR 9; R9是氢，C1-C3烷基，环烷基或完全或部分氟化的C1-C3烷基; R 1是（i）键或（ii）-C（R 10）（R 11） - *，-C（R 10）（R 11）-O- *，-C（R 10）（R 11）CH 2 - CH2C（R10）（R11） - *，其中由星号表示的键连接到环A环上; R10是氢，R11是氢，（C1-C3烷基或-OH;或R10和R11都是（C1-C3）烷基;或R10和R11与它们所连接的碳原子一起形成（C3-C5 ）环烷基环;环A是权利要求书中规定的芳环; Z1是如权利要求中所指定的单环基团。

2. 发明申请

WO2009153569A3 CB1 RECEPTOR MODULATORS 审中-公开
标题翻译： CB1受体调节剂
公开(公告)号：WO2009153569A3
公开(公告)日：2010-02-04
申请号：PCT/GB2009001539
申请日：2009-06-18
申请人： 7TM PHARMA AS , MURRAY ANTHONY , HOEGBERG THOMAS , COOPER MARTIN , BJURLING EMELIE , RECEVEUR JEAN-MARIE , NOERREGAARD PIA KARINA
发明人： MURRAY ANTHONY , HOEGBERG THOMAS , COOPER MARTIN , BJURLING EMELIE , RECEVEUR JEAN-MARIE , NOERREGAARD PIA KARINA
IPC分类号： C07D401/06 , A61K31/4178 , A61P3/04 , C07D403/06
CPC分类号： C07D401/06 , C07D403/06
摘要： Compounds of formula (I) suppress the normal signalling activity of cannabinoid receptor CB1 and are therefore useful inter alia in the treatment of conditions directly or indirectly associated with obesity and overweight, Wherein A1 is -COOH or tetrazolyl; R2, R3, R'2 and R'3 are independently selected from -R9, - CN, -F1 -Cl, -Br, -OR9, or -SR9; R9 is hydrogen, C1-C3 alkyl, cycloalkyl, or fully or partially fluorinated C1-C3 alkyl; R1 is (i) a bond, or (H) -C(R10)(R11)-*. -C(R10)(R11)-O-*. -C(R10)(R11)CH2*, or -CH2C(R10)(R11)-*, wherein the bond indicated by an asterisk is attached to Ring A ring; R10 is hydrogen and R11 is hydrogen, (C1-C3)alkyl or -OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring; Ring A is an aromatic ring as specified in the claims; Z1 is a moncyclic group as specified in the claims.
摘要翻译：式（I）化合物抑制大麻素受体CB1的正常信号传导活性，因此特别可用于治疗与肥胖和超重直接或间接相关的病症，其中A1是-COOH或四唑基; R 2，R 3，R'2和R'3独立地选自-R 9，-CN，-F 1 -Cl，-Br，-OR 9或-SR 9; R9是氢，C1-C3烷基，环烷基或完全或部分氟化的C1-C3烷基; R1是（i）键或（H）-C（R10）（R11） - 。 -C（R 10）（R 11）-O- *。 -C（R 10）（R 11）CH 2 *或-CH 2 C（R 10）（R 11） - *，其中由星号表示的键连接到环A环上; R10为氢，R11为氢，（C1-C3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）环烷基环; 环A是如权利要求中所指定的芳环; Z1是如权利要求中所指定的单环基团。

3. 发明申请

WO03087044A3 NOVEL CARBOXAMIDE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS 审中-公开
标题翻译：新型羧酰胺化合物用于妇幼保健相关疾病
公开(公告)号：WO03087044A3
公开(公告)日：2004-11-04
申请号：PCT/DK0300232
申请日：2003-04-08
申请人： 7TM PHARMA AS , HOEGBERG THOMAS , BJURLING ANNA EMELIE , RECEVEUR JEAN-MARIE , ULVEN TROND , LITTLE PAUL BRIAN , ELLING CHRISTIAN E , NOERREGAARD PIA KARINA
发明人： HOEGBERG THOMAS , BJURLING ANNA EMELIE , RECEVEUR JEAN-MARIE , ULVEN TROND , LITTLE PAUL BRIAN , ELLING CHRISTIAN E , NOERREGAARD PIA KARINA
IPC分类号： A61P3/04 , A61P3/10 , C07C237/42 , C07C275/42 , C07D207/09 , C07D207/32 , C07D207/327 , C07D211/58 , C07D235/06 , C07D239/70 , C07D265/30 , C07D271/06 , C07D295/13 , C07D405/12 , C07D413/12 , C07D417/04 , C07C275/28 , A61K31/175 , A61K31/4245 , C07C237/40
CPC分类号： C07D207/327 , C07C237/42 , C07C275/42 , C07D207/09 , C07D211/58 , C07D235/06 , C07D239/70 , C07D265/30 , C07D271/06 , C07D295/13 , C07D405/12 , C07D413/12 , C07D417/04
摘要： Novel compounds of formula (I) which modulate MCH activity are disclosed, in which A is a linker; B is a connecting moiety; Ar1 and Ar2 are aryl or heteroaryl groups; R1 and R2 are hydrogen, halogen atoms, CF3, OCF3, SCF3, SCH3, nitrile, alkyl, alkenyl, alkynyl groups; R1 and R2 could be connected to each other; R5 and R6 are hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups, -CHO, nitrile, alkyl, alkenyl or alkynyl groups, -SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as -CH2CF3, -CF2CF3, -CF3, -OCF3, -SCF3; -SO2NH2, -SO2NHAlk, -SO2Nalk2, -SO2Alk; Q together with the carbonyl forms an amide group, which is further substituted with an amine group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.

4. 发明申请

WO2009074782A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：WO2009074782A1
公开(公告)日：2009-06-18
申请号：PCT/GB2008/004051
申请日：2008-12-08
申请人： 7TM PHARMA A/S , RECEVEUR, Jean Marie , BJURLING, Emelie , MURRAY, Anthony , HOEGBERG, Thomas , NEILSEN, Peter, Aadal , LINGET, Jean-Michel , NOERREGAARD, Pia, Karina , ALMHOLT, Dorthe
发明人： RECEVEUR, Jean Marie , BJURLING, Emelie , MURRAY, Anthony , HOEGBERG, Thomas , NEILSEN, Peter, Aadal , LINGET, Jean-Michel , NOERREGAARD, Pia, Karina , ALMHOLT, Dorthe
IPC分类号： C07D231/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/06 , A61K31/415 , A61K31/4155 , A61P3/04
CPC分类号： C07D413/06 , C07D231/14 , C07D401/12 , C07D401/14 , C07D403/04
摘要： Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein:X is a bond, or a divalent radical selected from -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, -C(R 10 )(R 11 )CH 2 -O-*, -CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 ) -O-*. and -CH 2 -O-C(R 10 )(R 11 )-*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R 3 is hydrogen, (C 1 -C)aIkyI or (C 1 C 3 )fluoroalkyl; R 4 is a radical of formula -(AIk 1 ) P -(Q 1 ) r (L) s -Q 2 wherein p, r, s, AIk 1 , L, Q 1 and Q 2 are as specified; or R 3 and R 4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L) s -Q 2 wherein s, L and Q 2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, -NH 2 -, or mono- or di-(C 1 C 3 )alkylamino; R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen -F, -Cl, -Br, -CN, (C 1 -C 3 )alkyl, (C 1 C 3 )fluoroalkyl, cyclopropyl, and -OR 9 ; R 10 is hydrogen, (C 1 C 3 )alkyl, hydroxyl or NH 2 , and R 11 is hydrogen or (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring.
摘要翻译：式（I）化合物是大麻素受体CB1的调节剂，尤其用于治疗肥胖症：式（I）。其中X为键或选自-C（R 10）（R 11） - *，-C（R 10）（R 11）-O- *，-C（R 10）（R 11）CH 2 - C（R10）（R11）CH2-O- *，-CH2C（R10）（R11） - *，-CH2C（R10）（R11）-O- *。和-CH 2 -O-C（R 10）（R 11） - *，其中由星号表示的键连接到吡唑环上; Z是选自指定组的羧基等价基团; R3是氢，（C1-C）aI1I或（C1C3）氟代烷基; R4是式 - （AIk1）P-（Q1）r（L）s -Q2的基团，其中p，r，s，Alk1，L，Q1和Q2如所规定; 或者R 3和R 4与它们所连接的氮原子一起形成4至7个环原子的环状氨基环，其任选被式 - （L）s-Q 2的基团取代，其中s，L和Q2如上定义或选自羟基，甲氧基，-NH 2 - 或单 - 或二 - （C 1 -C 3）烷基氨基的任选取代基; R5，R6，R7和R8各自独立地选自-F，-Cl，-Br，-CN，（C1-C3）烷基，（C1C3）氟烷基，环丙基和-OR9; R 10是氢，（C 1 -C 3）烷基，羟基或NH 2，R 11是氢或（C 1 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）环烷基环。

5. 发明申请

WO2008059207A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：WO2008059207A1
公开(公告)日：2008-05-22
申请号：PCT/GB2007/004225
申请日：2007-11-07
申请人： 7TM PHARMA A/S , RECEVEUR, Jean-Marie , NIELSEN, Peter, Aadal , HOEGBERG, Thomas , LINGET, Jean-Michel , COOPER, Martin , NOERREGAARD, Pia, Karina
发明人： RECEVEUR, Jean-Marie , NIELSEN, Peter, Aadal , HOEGBERG, Thomas , LINGET, Jean-Michel , COOPER, Martin , NOERREGAARD, Pia, Karina
IPC分类号： C07D231/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/4155 , A61P3/04
CPC分类号： C07D231/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful for the treatment of obesity and diseases for which obesity is a risk factor: (I) wherein: X is a bond, Or-C(R 10 )(R 11 )-*. -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2- *, -C(R 10 )(R 11 )CH 2 -O-*, -CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 )-O-*, or -CH 2 -O-C(R 10 )(R 11 )-*; Y is =O, =N(R 9 ), =N(OR 9 ), =CH(CN), =C(CN) 2 or =N(CN); Z is a bond, -O- or -NH-; R 1 and R 2 are hydrogen, (CrC3)alkyl, (C3-C6)cycloalkyl or monocyclic heterocyclic; or R1 and R2 taken together with the nitrogen to which they are attached form a cyclic amino ring; R 3 is hydrogen or a radical of formula -(O)a- AIk 3 wherein a and AIk 3 are as defined in the claims; R 4 is a radical of formula -(O) b -(Alk 1 ) p -(Q) r -(L) s -Q 2 wherein b, p, r, s AIk 1 , L, Q1 and Q2 are as defined in the claims; or R 3 and R 4 taken together with the nitrogen to which they are attached form a cyclic amino ring; R 5 is hydrogen -F, -Cl, -Br, -CN, (C 1 -C 3 )alkyl, (C 1 -C 3 )fluoroalkyl, cyclopropyl, -COOH, tetrazole or -OR 9 ; R 6 , R 7 and R 8 are hydrogen -F, -Cl, -Br, -CN, (C 1 -C 3 )alkyl, (C 1 -C 3 )fluoroalkyl, cyclopropyl, or -OR 9 ; and R 9 R 10 and R 11 are as defined in the claims.
摘要翻译：式（I）化合物是大麻素受体CB1的调节剂，其可用于治疗肥胖症和肥胖症是其中的危险因素的疾病：（I）其中：X是一个键，Or-C（R 10） SUB>）（R _{11 ） - *。 -C（R 10）（R 11） - O- *， - C（R 11）（R 11） CH 2 - ， - C（R 10）（R 11）CH 2 -O-O - *，-CH 2 C（R 10）（R 11） - *，-CH 2 C （R 10）（R 11） - O- *或-CH 2 -O-C（R 10））（R _{11 ） - *; Y是= O，= N（R 9），= N（OR 9），= CH（CN），= C（CN）2 < SUB>或= N（CN）; Z是键，-O-或-NH-; R 1和R 2是氢，（C 1 -C 3）烷基，（C 3 -C 6）环烷基或单环杂环; 或者R 1和R 2与它们所连接的氮一起形成环状氨基环; R 3是氢或式 - （O）a -Alk 3的基团，其中a和i个3如权利要求中所定义; R 4是式 - （O）b - （Q 1）的基团 - （Q）其中b，p，r，s，i，1，...，L， Q1和Q2如权利要求中所定义; 或R 3和R 4与它们所连接的氮一起形成环状氨基环; R 5是氢-F，-Cl，-Br，-CN，（C 1 -C 3）烷基，（C _{; 并且R 9 R 10和R 11如权利要求中所定义。}}}

6. 发明申请

WO2004052371A3 CYCLIC QUINOLINE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS 审中-公开
标题翻译：周期性喹啉化合物用于妇幼保健相关疾病
公开(公告)号：WO2004052371A3
公开(公告)日：2004-08-19
申请号：PCT/DK0300858
申请日：2003-12-11
申请人： 7TM PHARMA AS , FRIMURER THOMAS MICHAEL , ULVEN TROND , HOEGBERG THOMAS , NOERREGAARD PIA KARINA , LITTLE PAUL BRIAN , RECEVEUR JEAN-MARIE
发明人： FRIMURER THOMAS MICHAEL , ULVEN TROND , HOEGBERG THOMAS , NOERREGAARD PIA KARINA , LITTLE PAUL BRIAN , RECEVEUR JEAN-MARIE
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519 , C07D401/04 , A61K31/4709
CPC分类号： C07D401/04 , A61K31/435 , A61K31/4375 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519
摘要： The present invention relates to the use of cyclic quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel cyclic quinoline compounds per se . The cyclic quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonisitic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia etc. or in the treatment or prevention of depression.
摘要翻译：本发明涉及环喹啉化合物在制备用于治疗，预防和/或诊断由黑色素浓缩激素引起或涉及的病症的药物和/或化妆品组合物中的用途。本发明还涉及新的环状喹啉化合物本身。已经发现环状喹啉化合物与黑色素浓缩激素受体MCH受体相互作用。这些化合物对MCH受体具有调节活性，例如。拮抗，激动或变构活性，并且可用于药物或化妆品目的，例如，用于治疗或预防肥胖，代谢综合征，II型糖尿病，食欲过盛等进食障碍或治疗或预防抑郁症。

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