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1. 发明申请

WO2007062797A1 AMINO-SUBSTITUTED AZO-HETEROCYCLIC COMPOUNDS FOR TREATING INFLAMMATORY CONDITIONS 审中-公开
标题翻译：用于处理炎症条件的氨基取代的AZO-杂环化合物
公开(公告)号：WO2007062797A1
公开(公告)日：2007-06-07
申请号：PCT/EP2006/011384
申请日：2006-11-23
申请人： 7TM PHARMA A/S , GRIMSTRUP, Marie , RIST, Øystein , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , FRIMURER, Thomas, Michael
发明人： GRIMSTRUP, Marie , RIST, Øystein , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , FRIMURER, Thomas, Michael
IPC分类号： C07D277/42 , C07D417/12 , A61K31/426 , A61K31/4436 , A61P29/00
CPC分类号： C07D277/42 , C07D417/12
摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein X 1 is -S-, -O-, -N=N-. -NR 5 -, -CR 5 =CR 6 -, -CR 5 =N-, wherein R 5 and R 6 are independently hydrogen or C 1 -C 3 alkyl; R 1 is hydrogen or C 1 -C 3 alkyl or cyclopropyl; R 2 is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring; R 3 is an optionally substituted carbocyclic ring of 3 to 7 ring atoms, or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; R 4 is a group other than hydrogen, methyl or ethyl of formula Q-[Alk 1 ] m -[X] n -[Alk 2 ] p -[Z} s - wherein m, n p, and s are independently 0 or 1 ; Q is hydrogen or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; Alk 1 and Alk 2 are independently optionally substituted C 1 -C 3 alkylene radicals; X is -O-, -S-, -C(=O)-, - S(=O)-, -S(=O) 2 -, -CH(R 7 )-, -N(R 7 )-, or, in either orientation -SO 2 N(R 7 )- or - C(=O)N(R 7 )-, wherein R 7 is hydrogen, or R 7 represents a C 2 -C 4 bridge between the C or N atom of X to which it is attached and a carbon atom of Alk 2 and Z is -CH 2 , - C(=O) or -S(=O) 2 .
摘要翻译：式（I）化合物是可用于治疗炎性，自身免疫，呼吸或过敏疾病的CRTH2拮抗剂：其中X 1 -S-，-O-，-N = N-。 -NR 5 - ，-CR 5 = CR 6 - ，-CR 5 N = N-，其中R R 5和R 6独立地是氢或C 1 -C 3烷基; R 1是氢或C 1 -C 3烷基或环丙基; R 2是任选取代的苯基或5-或6-元单环杂芳基环; R 3是任选取代的3至7个环原子的碳环，或任选取代的4-，5-或6-元单环杂环; R 4是除了氢，甲基或式Q-的基团之外的基团 - [Alk 1] m - [X] n 其中m，np和s独立地为0或1; - 其中m，np和s独立地为0或1; - 其中m，np和s独立地为0或1; Q是氢或任选取代的4-，5-或6-元单环杂环; Alk＆lt; 1＆gt;和Alk 2独立地是任选取代的C 1 -C 3亚烷基; X是-O - ， - S - ， - C（= O） - ， - S（= O） - ， - S（= O）2 - ， - CH -N（R 7） - ，或者以任一取向-SO 2 N（R 7） - ， - （R 7）或-C（= O）N（R 7） - ，其中R 7为氢，或R 7为C 1 -C 6烷基，其连接的X的C或N原子与Alk 2的碳原子之间的2个或更多的桥是-CH _。

2. 发明申请

WO2007062773A1 OXADIAZOLE DERIVATIVES WITH CRTH2 RECEPTOR ACTIVITY 审中-公开
标题翻译：具有CRTH2受体活性的OXADIAZOLE衍生物
公开(公告)号：WO2007062773A1
公开(公告)日：2007-06-07
申请号：PCT/EP2006/011216
申请日：2006-11-22
申请人： 7TM PHARMA A/S , RECEVEUR, Jean-Marie , CHRISTENSEN, Ann , GRIMSTRUP, Marie , HOEGBERG, Thomas
发明人： RECEVEUR, Jean-Marie , CHRISTENSEN, Ann , GRIMSTRUP, Marie , HOEGBERG, Thomas
IPC分类号： C07D271/06 , C07D413/04 , A61K31/4245 , A61P11/00
CPC分类号： C07D271/06 , C07D413/04
摘要： Compounds of formula (I) are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R 1 is hydrogen or methyl and R 2 is optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having 4 to 6 ring atoms; or R 1 and R 2 , taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl ring having 4 to 6 ring atoms; R is hydrogen or an optional substituent; the phenyl ring containing the substituent R is optionally substituted by 1 , 2 or 3 optional substituents; A is hydrogen or C 1 -C 3 alkyl; and ring Ar is an optionally substituted phenyl or 5- or 6- membered monocyclic heteroaryl ring.
摘要翻译：式（I）化合物是CRTH2配体，可用于治疗炎症，自身免疫，呼吸或过敏疾病：其中R 1是氢或甲基，R 2 2是任选取代的环烷基或任选取代的具有4-6个环原子的非芳族杂环基; 或R 1和R 2与它们所连接的碳原子一起形成任选取代的环烷基，或任选取代的具有4-6个碳原子的非芳族杂环基环原子; R是氢或任选的取代基; 含有取代基R的苯环任选被1,2或3个任选的取代基取代; A是氢或C 1 -C 3烷基; 并且环Ar是任选取代的苯基或5-或6-元单环杂芳基环。

3. 发明申请

WO2008092681A1 GHRELIN RECEPTOR MODULATORS 审中-公开
标题翻译： GHRELIN受体调节剂
公开(公告)号：WO2008092681A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/000758
申请日：2008-01-29
申请人： 7TM PHARMA A/S , LINNANEN, Tero , RIST, Øystein , GRIMSTRUP, Marie , FRIMURER, Thomas , HOEGBERG, Thomas , NIELSEN, Flemming, Elmelund , GERLACH, Lars-Ole
发明人： LINNANEN, Tero , RIST, Øystein , GRIMSTRUP, Marie , FRIMURER, Thomas , HOEGBERG, Thomas , NIELSEN, Flemming, Elmelund , GERLACH, Lars-Ole
IPC分类号： C07D307/00 , C07D491/08 , A61K31/075 , A61K31/34 , A61K31/407 , C07D209/56 , C07D307/93 , C07D491/18 , C07D491/153 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/02 , A61P43/00
CPC分类号： C07D491/18 , A61K31/075 , A61K31/34 , A61K31/407
摘要： Compounds of Formula (IA) or (IB) modulate ghrelin receptor activity, and are useful in the treatment of, for example, obesity and eating disorders: wherein W is, in either orientation, -C(=O)N(R 3 )-, or -C(=O)O-; R is hydrogen or C 1 -C 4 alkyl; R 1 is selected from hydrogen, (C 1 -C 4 )alkyl, cycloalkyl, fully or partially fluorinated (C 1 -C 4 )alkyl, or -OR 10 ; and R 2 is selected from (i) hydrogen and (ii) (C 1 -C 4 )alkyl, cycloalkyl, cycloalkenyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, C 1 -C 4 alkyl, cyclopropyl, -NR 7 COR 0 , -NR 7 SO 2 R 0 , -COR 0 , -COOH, -SOR 9 , -SO 2 R 0 , -OR 10 , -NR 7 R 8 , or -NR 7 COOR 8 ; and (iii) aryl, aryl-(C 1 -C 2 )alkyl-, heteroaryl and heteroaryl-(C 1 -C 2 alkyl)- each optionally substituted in the ring part or R 1 and R 2 , together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; R 3 is selected from hydrogen, (C 1 -C 4 )alkyl, cycloalkyl, fully or partially fluorinated (C 1 -C 4 )aIkyl, or -OR 10 ; and R 4 is selected from (iv) hydrogen and (v) (C 1 -C 4 )alkyl, cycloalkyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, -NR 7 COR 0 , -NR 7 SO 2 R 0 , -COR 0 , - COOH, -SOR 9 , -SO 2 R 0 , -OR 10 , -NR 7 R 8 , or -NR 7 COOR 8 ; and (vi) aryl, aryl-(C 1 -C 2 )alkyl-, heteroaryl and heteroaryl-(C 1 -C 2 alkyl)- each optionally substituted in the ring part thereof; or R 3 and R 4 , together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; L is a linker radical of formula -(CR 11 R 13 ) a B(CR 12 R 14 )b- as defined in the specification; R 0 , R 7 , R 8 , R 9 and R 10 are as defined in the specification.
摘要翻译：式（IA）或（IB）的化合物调节生长素释放肽受体活性，并且可用于治疗例如肥胖症和进食障碍：其中W为任一取向-C（= O）N（R _{或-C（= O）O-; R是氢或C 1 -C 4烷基; R 1选自氢，（C 1 -C 4 -C 4）烷基，环烷基，完全或部分氟化（C 1 -C 4）烷基，烷基或-OR 10; 和R 2选自（i）氢和（ii）（C 1 -C 4 -C 4）烷基，环烷基，环烯基和非环烷基芳基杂环基，各自任选被-F，-CN，C 1 -C 4烷基，环丙基，-NR 7 - 0，-NR 7，SO 2，-SO 2，-COOH， - SOR 9，-SO 2 R 0，-OR 10，-NR 7，/ SO 2， R 8，或-NR 7 COOR 8; 和（iii）芳基，芳基 - （C 1 -C 2 -C 2）烷基 - ，杂芳基和杂芳基 - （C 1 -C 3 > - >烷基） - 各自任选在环部分或R 1和R 2中被取代，与它们所连接的氮一起形成任选地取代的环状氨基; R 3选自氢，（C 1 -C 4 - ）烷基，环烷基，完全或部分氟化（C 1 -C 4）烷基， C 1 -C 4烷基或-OR 10; 和R 4选自（iv）氢和（v）（C 1 -C 4 -C 4）烷基，环烷基和非芳族杂环基，各自任选被-F，-CN，-NR 7 COR 0，-NR 7 SO 2取代， R 0 0，-COR 0，-COOH，-SOR 9，-SO 2 R 0 -OR 10，-NR 7 R 8或-NR 7 COOR _{> 8 ; 和（vi）芳基，芳基 - （C 1 -C 2 -C 2）烷基 - ，杂芳基和杂芳基 - （C 1 -C 3 > - >烷基） - 各自任选在其环部分取代; 或R 3和R 4与它们所连接的氮一起形成任选取代的环状氨基; L是式 - （CR 11 R 13）a B的连接基团（CR 12 R 12） > 14 b-如说明书中所定义; R 0，R 7，R 8，R 9和R 10是如说明书中所定义。}}

4. 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。

5. 发明申请

WO2008075019A1 MODULATORS OF CB1 RECEPTORS 审中-公开
标题翻译： CB1受体的调节剂
公开(公告)号：WO2008075019A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004842
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D409/14 , C07D417/14 , C07D231/12 , A61K31/4725 , A61K31/497 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A 1 is hydrogen, -COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; R 4 and R 5 are independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , -NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , or -SO 2 R 6 ; R 6 is C 1 -C 4 alkyl, cycloalkyl, -CF 3 or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl or cycloalkyl; R 9 is hydrogen, C 1 -C 4 alkyl, C 1 - C 4 alkoxy, C 1 -C 4 alkoxy(C 1 -C 4 alkyl)-, cycloalkyl, or fully or partially fluorinated C 1 -C 4 alkyl; R 1 (i) a bond; (ii) a divalent radical of formula -(CH 2 ) a B 1 (CH 2 ) b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B 1 is -CO-, -0-, -S-, -SO-, - SO 2 -, -CH 2 -, -CHCH 3 -, -CHOH- or -NR 7 -; or (iii) 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-*, -CH 2 -O-C(R 10 )(R 11 )-* and -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R 10 is hydrogen and R 11 is (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.
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和直接或间接与肥胖和超重相关的病症：其中A 1是氢，-COOH或四唑基; p和q独立地为0或1; A3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; R 4和R 5独立地是-R 9，-CN，-F，-Cl，-Br，-OR 9 -NR 7 R 8，-NR 7 COR 6，-NR N R 8， 7个SO 2，6个6， - 6个，-SR 9，-SOR， - SUB > 9 或-SO 2 R 6; R 6是C 1 -C 4烷基，环烷基，-CF 3或-NR 7 - [R _{8 ; R 7和R 8独立地是氢，C 1 -C 4烷基或环烷基; R 9是氢，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷氧基，C 1 -C 4烷氧基（C 1 -C 4烷基） - ，环烷基，或全部或部分氟化的C 1 -C 4烷基; R 1（i）键; （ii）式 - （CH 2）2的二价基团a（CH 2）2 N（CH 2）2 其中a和b独立地是0,1,2或3，条件是a + b是1,2或3，并且B 1是-CO - ， - O-， -S - ， - SO - ， - SO 2 - ， - CH 2 - ， - CHCH 3 - ， - CHOH-或-NR _{7 - ; 或（iii）选自-C（R 10）（R 11） - *， - C（R 10）（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 10）（R 11） - O *， - CH 2 - （R 10） - （R 11） - *和 -C（R 10）（R 11）-O-CH 2 - *，其中由星号表示的键连接到吡唑环 Z如规范中所定义; R 10是氢，R 11是（C 1 -C 3 -C 3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -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）烷基， / SUB）环烷基环。}}

6. 发明申请

WO2006010446A3 MEDICINAL USE OF RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2006010446A3
公开(公告)日：2006-02-02
申请号：PCT/EP2005/007318
申请日：2005-07-05
申请人： 7TM PHARMA A/S , RECEVEUR, Jean-Marie , BJURLING, Emelie , CHRISTENSEN, Ann , HOEGBERG, Thomas
发明人： RECEVEUR, Jean-Marie , BJURLING, Emelie , CHRISTENSEN, Ann , HOEGBERG, Thomas
IPC分类号： C07D401/12
摘要： Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH 3 ; X is =CH- or =N-; L, is -CH 2 - or -CH 2 CH 2 - ; L 2 is a bond, -CH 2 - or -CO-; R2 is H or C,-C 3 alkyl, or -N(R 2 ) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.

7. 发明申请

WO2008075013A1 MODULATORS OF CANNABINOID RECEPTOR 审中-公开
标题翻译： CANNABINOID受体的调节剂
公开(公告)号：WO2008075013A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004835
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D231/18 , A61K31/415 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: Wherein A 1 is hydrogen, -COOH, or tetrazolyl, and A 2 is hydrogen, -COOH, or tetrazolyl, provided that one of A 1 and A 2 is either -COOH or tetrazolyl; p is O or 1; A 3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; q is O or 1; R 3 is hydrogen, C 1 C 4 alkyl, cycloalkyl, -CF 3 , or -OR 9 ; R 4 and R 5 independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , -NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , Or -SO2R 6 , R 6 is C 1 -C4 alkyl, cycloalkyl, -CF 3 Or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl or cycloalkyl; R 9 is hydrogen, C 1 -C 4 alkyl, cycloalkyl, fully or partially fluorinated C 1 -C 4 alkyl; R 1 is 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-*, -CH 2 -O-C(R 10 )(R 11 )-* and -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring, and R 10 is hydrogen and R 11 is (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; and R 2 is a bond, -(CH 2 ) a B 1 (CH 2 ) b - or -[(CH 2 ) a B 1 (CH 2 )b] n -A 4 - [(CH 2 ) c B 2 (CH 2 ) d ] m - wherein a and b are independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and B 1 and B 2 are independently is -CO-, -0-, -S-, -SO-, -SO 2 -, -CH 2 -, - CHOH- or -NR 7 -; c and d are independently 0,1, 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently 0 or 1 and A 4 is (i) a monocyclic carbocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF 3 , C 1 -C 4 alkyl, cycloalkyl, -OR 9 , oxo or -NR 7 R 8 ; or (ii) a monocyclic heterocyclic ring, having 4 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF 3 , C 1 -C 4 alkyl, cycloalkyl, -OR 9 , oxo or -NR 7 R 8 .
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和直接或间接与肥胖和超重相关的病症：其中A 1是氢，-COOH或四唑基，并且A 2 H 2是氢，-COOH或四唑基，提供 A 1和A 2之一是-COOH或四唑基; p是O或1; A 3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; q是O或1; R 3是氢，C 1 -C 4烷基，环烷基，-CF 3 - 或-OR _{9 ; R 4和R 5独立地-R 9，-CN，-F，-Cl，-Br，-OR 9， NR 7，-NR 7 R 6，-NR 7，-NR 7，-NR 7 R 8，-NR 7， SO 2，-SOR 9，-SOR 9，-SOR 9，-SOR 9，-SOR 9， 9或-SO 2 R 6，R 6是C 1 -C 4烷基，环烷基，-CF 3，或-NR 7 R 8 8; R 7和R 8独立地是氢，C 1 -C 4烷基或环烷基; R 9是氢，C 1 -C 4烷基，环烷基，完全或部分氟化的C 1 -C 烷基; R 1是选自-C（R 10） - （R 11） - ， - C（R 10）的二价基团（R 11） - O - ， - C（R 10）（R 11）CH 2 -C（R 10）（R 11）CH 2 -O - ， - CH- （R 10） - （CH 2） - ， - CH 2 C（R 10）（R 11） - O - ， - CH 2 -OC（R 10）（R 11）（R 11） - 和-C（R 10）（R 11）-O-CH 2 - *，其中由一个星号连接到吡唑环上，R 10是氢，R 11是（C 1 -C 3）烷基，烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -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）烷基， / SUB）环烷基环; 和R 2是（CH 2）2 - （CH 2）2 - ， - b） - 或 - - （（CH 2）2）B 1（CH 2） b）N - - - - - - - （（CH 2））C b - 2其中a和b独立地为0,1,2或3，条件是a + b不大于4，并且B 1和B 2个独立地是-CO - ， - O - ， - S - ， - SO - ， - SO 2 -CH 2 - ， - CH 2 - ， - CH 2 - ， - NR 2 - ， - CH 2 - 或-NR 7 - 。 c和d独立地为0,1,2或3; 条件是a + b + c + d不大于6，n和m独立地为0或1，并且A 4是（i）具有3至8个环原子的单环碳环，任选被-F，-Cl，-Br，-CN，-CF 3 N，C 1 -C 4中的一个或多个取代。烷基，环烷基，-OR 9，氧代或-NR 7 R 8; 或（ii）具有4至8个环原子的单环杂环，任选被-F，-Cl，-Br，-CN，-CF 3， C 1 -C 4烷基，环烷基，-OR 9，氧代或-NR 7 R 8 >。}

8. 发明申请

WO2008075012A1 CB1 RECEPTOR MODULATORS 审中-公开
标题翻译： CB1受体调节剂
公开(公告)号：WO2008075012A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004831
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D231/12 , C07D231/18 , C07D401/12 , C07D403/06 , A61K31/415 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A 1 is hydrogen, -COOH, or tetrazolyl, and A 2 is hydrogen, -COOH, or tetrazolyl, provided that one of A 1 and A 2 is either -COOH or tetrazolyl; p is O or 1 and A 3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; q is O or 1; R 3 is hydrogen, C 1 -C 4 alkyl, cycloalkyi, -CF 3 , or -OR 9 ; R 4 and R 5 independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , - NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , or -SO 2 R 6 ; R 6 is C 1 -C 4 alkyl, cycloalkyl, -CF 3 or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl, -CF 3 , or cycloaikyL R 9 is hydrogen, C 1 -C 4 alkyl, cycloalkyl, fully or partially fluorinated C 1 -C 4 alkyl; R 1 is (i) a bond, or (ii) -(CH 2 ) a B 1 (CH 2 ) b - wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) -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-*, -CH 2 -O-C(R 10 )(R 11 )-* or -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q 1 A 4 -[Q 2 ]w- wherein Q 1 , A 4 , Q 2 and w are as defined in the specification; and R 10 is hydrogen and R 11 is (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.
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和与肥胖和超重直接或间接相关的病症：其中A 1是氢，-COOH或四唑基，并且A 2 H 2是氢，-COOH或四唑基，提供 A 1和A 2之一是-COOH或四唑基; p是0或1，并且A 3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; q是O或1; R 3是氢，C 1 -C 4烷基，环烷基，-CF 3或-OR 3， SUB> 9 ; R 4和R 5独立地-R 9，-CN，-F，-Cl，-Br，-OR 9， NR 7，-NR 7 R 6，-NR 7，-NR 7 R 6，-NR 7， SO 2，-SOR 9，-SOR 9，-SOR 9，-SOR 9，-SOR 9， 9或-SO 2 R 6; R 6是C 1 -C 4烷基，环烷基，-CF 3或-NR 7 - [R _{8 ; R 7和R 8独立地是氢，C 1 -C 4烷基，-CF 3 或R 3为氢，C 1 -C 4烷基，环烷基，完全或部分氟化的C 1 -C 6烷基， C 1 -C 4烷基; R 1是（i）键，或（ii） - （CH 2）2 - （CH 2）其中a和b独立地为O，1,2或3，条件是a + b为1,2或3; 或（iii）-C（R 10）（R 11） - *， - C（R 10）（R 11）） - O- *。 -C（R 10）（R 11）CH 2 - ， - （R 10）（R 10） R 11（CH 2）2 CH 2 -O - ， - CH 2 C（R 10）（R 11） - *，-CH 2 C（R 10）（R 11）-O - ， - CH （R 10） - *或-C（R 10）（R 10） - （R 10） O-CH 2 - *，其中由星号表示的键连接到吡唑环上; R 2是式-Q 1的二价基团，其中Q 1，R 2，R 2， A 4，Q 2和W如说明书中所定义; 并且R 10是氢，R 11是（C 1 -C 3 -C 3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -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）烷基， / SUB）环烷基环。}

9. 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。

10. 发明申请

WO2008074982A1 PYRAZOLE DERIVATIVES AS MODULATORS OF CANNABINOID RECEPTOR 审中-公开
标题翻译：作为CANNABINOID受体调节剂的吡唑衍生物
公开(公告)号：WO2008074982A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004703
申请日：2007-12-10
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina
IPC分类号： A61K31/4155 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , A61P3/04
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04
摘要： Compounds of formula (I) suppress the normal signalling activity of CB1 receptors, and are useful in the treatment of, for example obesity or overweight formula (I): wherein A 1 , A 2 , A 5 , A 6 , R 1 , R 2 , R 3 , and X are as defined in the claims.
摘要翻译：式（I）化合物抑制CB1受体的正常信号传导活性，并且可用于治疗例如肥胖或超重配方（I）：其中A 1，A 2， A 5，A 6，R 1，R 2，R 3， / SUB，和X如权利要求中所定义。

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