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1. 发明授权

US06919343B2 N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives 有权
标题翻译： N-联苯（取代甲基）氨基环烷基 - 甲酰胺衍生物
公开(公告)号：US06919343B2
公开(公告)日：2005-07-19
申请号：US10354674
申请日：2003-01-30
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
IPC分类号： A61K31/166 , A61K31/24 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/505 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , C07C237/24 , C07D213/82 , C07D239/28 , C07D257/04 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12 , A61K31/165
CPC分类号： C07D257/04 , C07D213/82 , C07D239/28 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

2. 发明授权

US07091380B2 N-biphenylmethyl aminocycloalkanecarboxamide derivatives 有权
标题翻译： N-联苯甲基氨基环烷烃甲酰胺衍生物
公开(公告)号：US07091380B2
公开(公告)日：2006-08-15
申请号：US10503502
申请日：2003-02-04
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
IPC分类号： C07C233/05 , C07C233/65 , A61K31/165
CPC分类号： C07C237/24 , C07C237/22 , C07C2601/02 , C07D209/48 , C07D213/81 , C07D213/82 , C07D231/12 , C07D237/24 , C07D239/28 , C07D241/44 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/18 , C07D263/34 , C07D271/06 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

3. 发明申请

US20080318976A1 Alpha-Hydroxy Amides as Bradykinin Antagonists or Inverse Agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反激动剂
公开(公告)号：US20080318976A1
公开(公告)日：2008-12-25
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10 , C07C229/36 , A61K31/505 , A61P25/00 , C07D239/24 , A61K31/24
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2)(CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd. (4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra. and (7)(CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl;
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra（5）（CH2）k-杂环，任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）具有选自NO和S的环杂原子并且任选具有至多3个另外的环氮原子的5元杂芳环，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基;

4. 发明授权

US07790754B2 Alpha-hydroxy amides as bradykinin antagonists or inverse agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反向激动剂
公开(公告)号：US07790754B2
公开(公告)日：2010-09-07
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl.
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra。（5）（CH2）k-杂环，其任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）5元杂芳族环，其具有选自NO和S的环杂原子，并且任选地具有至多3个另外的环氮原子，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基。

5. 发明授权

US07163951B2 N-biarylmethyl aminocycloalkanecarboxamide derivatives 失效
标题翻译： N-二芳基甲基氨基环烷甲酰胺衍生物
公开(公告)号：US07163951B2
公开(公告)日：2007-01-16
申请号：US10523911
申请日：2003-08-25
申请人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
发明人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
IPC分类号： A61K31/4427 , C07D401/12
CPC分类号： C07D417/12 , C07D213/40 , C07D213/61 , C07D239/28 , C07D239/42 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/12
摘要： N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-二芳基甲基氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

6. 发明授权

US07816380B2 1-hydroxycycloalkanecarboxamide derivatives 有权
标题翻译： 1-羟基环烷烃甲酰胺衍生物
公开(公告)号：US07816380B2
公开(公告)日：2010-10-19
申请号：US11920306
申请日：2006-05-30
申请人： Scott D. Kuduk , Michael R. Wood
发明人： Scott D. Kuduk , Michael R. Wood
IPC分类号： A61K31/24 , C07D419/00 , C07D413/00
CPC分类号： C07D213/61 , C07D401/10 , C07D413/10
摘要： α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C1-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译：式（I）的α-羟基环烷甲酰胺衍生物或其药学上可接受的盐，其中式（a）是单键或双键; R 1，R 2和R 3各自独立地选自H，卤素和OH; 或连接在同一碳原子上的R1和R2一起代表氧代; R4是H或甲基; R5是Cl或I2; R 6选自-CO 2 -C 1-4烷基，-O-C 1-4烷基，-O-C 1-4卤代烷基，2-甲基四唑-5-基，5-甲基-1,2,4-恶二唑-3-基，3 - 甲基-1,2,4-恶二唑-5-基，5-卤代甲基-1,2,4-恶二唑-3-基，3-卤代甲基-1,2,4-恶二唑-5-基，四唑-5 - 5-氯甲基-1,2,3-三唑基和5-甲基-1,2,3-三唑基; R 7和R 8各自独立地为Cl或I 2; 和n为0或1是缓激肽B1拮抗剂或反激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

7. 发明申请

US20090062349A1 1-Hydroxycycloalkanecarboxamide derivatives 有权
标题翻译： 1-羟基环烷甲酰胺衍生物
公开(公告)号：US20090062349A1
公开(公告)日：2009-03-05
申请号：US11920306
申请日：2006-05-30
申请人： Scott D. Kuduk , Michael R. Wood
发明人： Scott D. Kuduk , Michael R. Wood
IPC分类号： C07D401/10 , C07D413/10 , A61K31/44 , A61K31/4439 , A61P29/00
CPC分类号： C07D213/61 , C07D401/10 , C07D413/10
摘要： α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C3-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译：式（I）的α-羟基环烷甲酰胺衍生物或其药学上可接受的盐，其中式（a）是单键或双键; R 1，R 2和R 3各自独立地选自H，卤素和OH; 或连接在同一碳原子上的R1和R2一起代表氧代; R4是H或甲基; R5是Cl或I2; R6选自-CO 2 -C 3-4烷基，-O-C 1-4烷基，-O-C 1-4卤代烷基，2-甲基四唑-5-基，5-甲基-1,2,4-恶二唑-3-基，3 - 甲基-1,2,4-恶二唑-5-基，5-卤代甲基-1,2,4-恶二唑-3-基，3-卤代甲基-1,2,4-恶二唑-5-基，四唑-5 - 5-氯甲基-1,2,3-三唑基和5-甲基-1,2,3-三唑基; R 7和R 8各自独立地为Cl或I 2; 和n为0或1是缓激肽B1拮抗剂或反激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

8. 发明申请

US20170260136A1 HETEROARYL OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：US20170260136A1
公开(公告)日：2017-09-14
申请号：US15531887
申请日：2015-12-14
申请人： Scott D. Kuduk , Nigel Liverton , Yunfu Luo
发明人： Scott D. Kuduk , Nigel Liverton , Yunfu Luo
IPC分类号： C07D213/40 , C07D403/12 , C07D401/14 , C07D401/12 , C07D213/82
CPC分类号： C07D213/40 , C07D213/82 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

9. 发明授权

US09586950B2 2-pyridyloxy-3-ester-4-nitrile orexin receptor antagonists 有权
标题翻译： 2-吡啶氧基-3-酯-4-腈食欲素受体拮抗剂
公开(公告)号：US09586950B2
公开(公告)日：2017-03-07
申请号：US14436380
申请日：2013-10-14
申请人： MERCK SHARP & DOHME CORP. , Scott D. Kuduk , Jason W. Skudlarek
发明人： Scott D. Kuduk , Jason W. Skudlarek
IPC分类号： C07D401/14 , A61K31/4545 , C07D413/14 , C07D401/12
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲肽受体拮抗剂的2-吡啶氧基-3-酯-4-腈化合物。本发明还涉及本文所述的2-吡啶氧基-3-酯-4-腈化合物在治疗或预防涉及食欲肽受体的神经和精神病症和疾病中的用途。本发明还涉及包含这些化合物的药物组合物。本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

10. 发明授权

US09206200B2 N-linked lactam M1 receptor positive allosteric mogulators 有权
标题翻译： N-连接内酰胺M1受体阳性变构调节剂
公开(公告)号：US09206200B2
公开(公告)日：2015-12-08
申请号：US14117341
申请日：2012-05-11
申请人： Scott D. Kuduk , Douglas C. Beshore , Zhi-Qiang Yang , Youheng Shu , Daniel Pitts
发明人： Scott D. Kuduk , Douglas C. Beshore , Zhi-Qiang Yang , Youheng Shu , Daniel Pitts
IPC分类号： C07D519/00 , C07D417/04 , C07D471/08 , C07D401/14 , C07D405/14 , C07D401/06 , C07D401/08 , C07D403/06 , C07D403/08 , C07D417/08 , C07D471/04 , C07D487/08 , C07D491/10 , C07D209/64
CPC分类号： C07D519/00 , C07D209/64 , C07D401/06 , C07D401/08 , C07D401/14 , C07D403/06 , C07D403/08 , C07D405/14 , C07D417/08 , C07D471/04 , C07D471/08 , C07D487/08 , C07D491/10
摘要： The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
摘要翻译：本发明涉及通式（I）的N-连接的内酰胺类化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默病，精神分裂症，疼痛或睡眠障碍本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。

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