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1. 发明授权

US06465486B1 Pyridyl/quinolinyl imidazoles 有权
标题翻译：吡啶基/喹啉基咪唑
公开(公告)号：US06465486B1
公开(公告)日：2002-10-15
申请号：US09524451
申请日：2000-03-10
申请人： Ellen W. Baxter , Robert E. Boyd , John R. Carson , Michele C. Jetter , Allen B. Reitz
发明人： Ellen W. Baxter , Robert E. Boyd , John R. Carson , Michele C. Jetter , Allen B. Reitz
IPC分类号： A61K3147
CPC分类号： C07D401/06 , A61K31/47
摘要： Certain imidazo pyridines/quinolines of the formula: where n is 0, 1, 2; X is independently selected from the group consisting of C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2, nitro, and two adjacent X may be fused to form the moiety: whereby a saturated, partially unsaturated or aromatic six-membered fused ring is formed; Y is independently selected from the group consisting of hydrogen, hydroxy, C1-4alkyl, C1-4alkoxy, trifluoromethyl and phenyl; and Z is independently selected from the group consisting of hydroxy, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2 and nitro; are &agr;2-adrenoceptor modulators which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, Parkinsonism, the need for anesthesia, cardiac arrythmia or the need for analgesia.
摘要翻译：某些具有下式的咪唑并吡啶/喹啉：其中n是0,1,2; X独立地选自C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基，-SO 2 NH 2，硝基和两个相邻 X可以稠合形成部分：由此形成饱和的，部分不饱和的或芳族的六元稠环; Y独立地选自氢，羟基，C 1-4烷基，C 1-4烷氧基，三氟甲基和苯基; 和Z独立地选自羟基，C 1-4烷基，溴，氯，碘，三氟甲基，C 1-4烷氧基，-SO 2 NH 2和硝基;是可用于治疗高血压，青光眼，性功能障碍的α2-肾上腺素能受体调节剂，抑郁症，注意力缺陷多动障碍，帕金森综合征，麻醉需要，心脏心律失常或需要镇痛。

2. 发明授权

US06436959B1 4-[aryl(piperidin-4-yl)]aminobenzamides 失效
标题翻译： 4- [芳基（哌啶-4-基）]氨基苯甲酰胺
公开(公告)号：US06436959B1
公开(公告)日：2002-08-20
申请号：US09220189
申请日：1998-12-23
申请人： John R. Carson , Richard J. Carmosin , Louis J. Fitzpatrick , Allen B. Reitz , Michele C. Jetter
发明人： John R. Carson , Richard J. Carmosin , Louis J. Fitzpatrick , Allen B. Reitz , Michele C. Jetter
IPC分类号： A61K314468
CPC分类号： C07D211/58
摘要： 4-[aryl(piperidin-4-yl)]aminobenzamides are delta-opioid receptor agonists/antagonists. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases.
摘要翻译： 4- [芳基（哌啶-4-基）]氨基苯甲酰胺是δ-阿片受体激动剂/拮抗剂。作为δ-阿片受体激动剂，这些化合物可用作镇痛药。取决于它们的激动剂/拮抗剂作用，这些化合物也可以是有用的免疫抑制剂，抗炎剂，用于治疗精神疾病的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，心血管药剂和用于治疗呼吸疾病。

3. 发明授权

US07358261B2 Heteroaryl alkylamide derivatives useful as bradykinin receptor modulators 有权
标题翻译：可用作缓激肽受体调节剂的杂芳基烷基酰胺衍生物
公开(公告)号：US07358261B2
公开(公告)日：2008-04-15
申请号：US11014471
申请日：2004-12-16
申请人： John R. Carson , Michele C. Jetter , Jung S. Lee , Mark A. Youngman
发明人： John R. Carson , Michele C. Jetter , Jung S. Lee , Mark A. Youngman
IPC分类号： A61K31/47 , C07D215/38
CPC分类号： C07D401/12 , A61K31/4709 , A61K31/4745 , C07D401/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D471/04
摘要： This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.
摘要翻译：本发明涉及作为缓激肽受体拮抗剂的新型烷基酰胺衍生物，其用于治疗缓激肽调节障碍如疼痛，炎症，哮喘和过敏。此外，本发明涉及作为可用于治疗缓激肽调节障碍如高血压等的缓激肽受体激动剂的新型烷基酰胺衍生物。

4. 发明授权

US06958349B2 Heteroaryl alkylamide derivatives useful as bradykinin receptor modulators 有权
标题翻译：可用作缓激肽受体调节剂的杂芳基烷基酰胺衍生物
公开(公告)号：US06958349B2
公开(公告)日：2005-10-25
申请号：US10403186
申请日：2003-03-31
申请人： John R. Carson , Michele C. Jetter , Jung S. Lee , Mark A. Youngman
发明人： John R. Carson , Michele C. Jetter , Jung S. Lee , Mark A. Youngman
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/4745 , A61P1/04 , A61P1/18 , A61P11/06 , A61P17/02 , A61P19/02 , A61P25/04 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D471/04 , A61K31/47 , C07D215/12 , C07D215/16
CPC分类号： C07D401/12 , A61K31/4709 , A61K31/4745 , C07D401/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D471/04
摘要： This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.
摘要翻译：本发明涉及作为缓激肽受体拮抗剂的新型烷基酰胺衍生物，其用于治疗缓激肽调节障碍如疼痛，炎症，哮喘和过敏。此外，本发明涉及作为可用于治疗缓激肽调节障碍如高血压等的缓激肽受体激动剂的新型烷基酰胺衍生物。

5. 发明授权

US06201025B1 N-aralkylaminotetralins as ligands for the neuropeptide Y Y5 receptor 有权
标题翻译： N-芳烷基氨基螺环素作为神经肽Y Y5受体的配体
公开(公告)号：US06201025B1
公开(公告)日：2001-03-13
申请号：US09413292
申请日：1999-10-06
申请人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
发明人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
IPC分类号： A61K31135
CPC分类号： C07C217/74 , C07B2200/07 , C07C217/58 , C07C2602/10 , C07D209/16 , C07D213/38
摘要： &bgr;-Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a &bgr;-aminotetralin derivative as the active ingredient are described. The 62 -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
摘要翻译：描述了作为神经肽Y Y5（NPY5）受体的配体的制备方法和含有β-氨基四氢卟吩衍生物作为活性成分的药物组合物的下式的β-氨基四氢萘衍生物。 62-氨基四氢叶酸可用于治疗与NPY受体亚型Y5相关的疾病和疾病。

6. 发明授权

US06552036B2 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives 有权
标题翻译： 3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物
公开(公告)号：US06552036B2
公开(公告)日：2003-04-22
申请号：US09791246
申请日：2001-02-22
申请人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
发明人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
IPC分类号： C07D45102
CPC分类号： C07D451/02 , A61K31/439
摘要： This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
摘要翻译：本发明涉及可用作δ-阿片样物质或μ-阿片受体调节剂的3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物。根据其激动剂或拮抗剂的作用，化合物是有用的止痛剂，免疫抑制剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，用于治疗的心血管药剂和药剂的呼吸系统疾病。

7. 发明授权

US06306876B1 4-[aryl(8-azabicyclo[3.2.1]octan-3-yl)]aminobenzoic acid derivatives 有权
标题翻译： 4- [芳基（8-氮杂双环[3.2.1]辛-3-基）]氨基苯甲酸衍生物
公开(公告)号：US06306876B1
公开(公告)日：2001-10-23
申请号：US09728972
申请日：2000-12-04
申请人： John R. Carson , Robert E. Boyd , Lou Anne Neilson
发明人： John R. Carson , Robert E. Boyd , Lou Anne Neilson
IPC分类号： A61K3146
CPC分类号： C07D451/04
摘要： 4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
摘要翻译： 4- [芳基（8-氮杂双环[3.2.1]辛-3-基）]氨基苯甲酸衍生物是δ-阿片受体调节剂。作为δ-阿片受体激动剂，这些化合物可用作镇痛药。根据它们的拮抗作用，这些化合物也可以是有用的免疫抑制剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，用于治疗呼吸的心血管药剂和药剂疾病

8. 发明申请

US20100204284A1 HETERO-SUBSTITUTED ACETANILIDE DERIVATIVES AS ANALGESIC AGENTS 有权
标题翻译：替代替代的乙酰胺衍生物作为有效代谢物
公开(公告)号：US20100204284A1
公开(公告)日：2010-08-12
申请号：US12751382
申请日：2010-03-31
申请人： John R. Carson , James J. McNally
发明人： John R. Carson , James J. McNally
IPC分类号： A61K31/44 , C07D213/56 , C07D231/56 , A61K31/4184 , A61P43/00
CPC分类号： A61K31/4402 , A61K31/16 , A61K31/40 , A61K31/415 , A61K31/416 , A61K31/417 , A61K31/44 , A61K31/495 , A61K31/537 , A61K31/54 , C07D207/16 , C07D207/34 , C07D213/81 , C07D231/14 , C07D231/56 , C07D233/90
摘要： Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.
摘要翻译：杂芳取代的乙酰苯胺衍生物被公开为止痛剂。本发明的化合物可用于治疗以疼痛和/或发烧为特征的哺乳动物的疾病或病症的方法。

9. 发明授权

US06897319B2 Useful aroyl pyrrole heteroaryl methanones and methanols 有权
公开(公告)号：US06897319B2
公开(公告)日：2005-05-24
申请号：US10315585
申请日：2002-12-10
申请人： John R. Carson , Ellen E. Codd , Philip M. Pitis
发明人： John R. Carson , Ellen E. Codd , Philip M. Pitis
IPC分类号： A61K31/4178 , A61K31/4439 , A61P1/06 , A61P1/08 , A61P1/12 , A61P1/14 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/00 , A61P17/02 , A61P17/04 , A61P19/02 , A61P19/08 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/18 , A61P35/00 , A61P43/00 , C07D401/06 , C07D403/06 , C07D409/14 , C07D401/14
CPC分类号： C07D401/06 , C07D403/06 , C07D409/14
摘要： This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.

10. 发明授权

US5565456A Anxiolytic aroyl piperidinyl and piperazinylacyl pyrroles 失效
标题翻译：溶血性芳酰基哌啶基和哌嗪基酰基吡咯
公开(公告)号：US5565456A
公开(公告)日：1996-10-15
申请号：US403966
申请日：1995-03-15
申请人： Richard J. Carmosin , John R. Carson , Philip Pitis
发明人： Richard J. Carmosin , John R. Carson , Philip Pitis
IPC分类号： C07D207/32 , C07D207/335 , C07D401/06 , C07D403/12 , A61K31/445 , A61K31/505 , C07D401/14
CPC分类号： C07D207/335 , C07D401/06 , C07D403/12
摘要： Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5; R1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.
摘要翻译：下式的芳酰基（哌啶基和哌嗪基）酰基吡咯具有抗焦虑活性：p由N，CH或COH组成; A1选自 + TR ，n是1至5的整数; R 1选自H和C 1-4烷基; R2和R3选自H和C1-4烷基; R 4选自卤素，C 1-4烷基，羟基，C 1-4烷氧基，硝基，氨基，C 1-4酰氨基，氰基，三卤代C 1-4烷基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基和C 1-4酰基; R 5选自卤素，C 1-4烷基，羟基，C 1-4烷氧基，硝基，氨基，C 1-4酰氨基，氰基，三卤代C 1-4烷基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基和C 1-4酰基; 及其酸加成盐。

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