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41. 发明授权

US08173672B2 Quinolizidinone M1 receptor positive allosteric modulators 有权
公开(公告)号：US08173672B2
公开(公告)日：2012-05-08
申请号：US12933799
申请日：2009-03-11
申请人： Scott D. Kuduk , Ronald K. Chang , Christina Ng Di Marco
发明人： Scott D. Kuduk , Ronald K. Chang , Christina Ng Di Marco
IPC分类号： A61K31/44
CPC分类号： C07D455/02 , C07D519/00
摘要： The present invention is directed to compounds of 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.

42. 发明申请

US20120040978A1 Heterocyclic Fused Cinnoline M1 Receptor Positive Allosteric Modulators 有权
标题翻译：杂环Cin啉M1受体正变构调节剂
公开(公告)号：US20120040978A1
公开(公告)日：2012-02-16
申请号：US13264267
申请日：2010-04-13
申请人： Scott D. Kuduk , Douglas C. Beshore
发明人： Scott D. Kuduk , Douglas C. Beshore
IPC分类号： A61K31/5377 , C07D495/14 , A61P25/00 , A61P25/28 , A61P25/18 , C07D471/14 , A61K31/5025
CPC分类号： C07D471/14 , C07D495/14
摘要： The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in 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：本发明涉及式（I）的杂环稠合噌啉化合物，其为M1受体阳性变构调节剂，可用于治疗阿尔茨海默病，精神分裂症，疼痛或睡眠障碍中的疾病。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。

43. 发明申请

US20110301167A1 PYRAZOLO [4,3-c] CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS 有权
标题翻译：吡唑并[4,3-c] CINNOLIN-3-ONE M1受体阳性全调制剂
公开(公告)号：US20110301167A1
公开(公告)日：2011-12-08
申请号：US13201575
申请日：2010-02-12
申请人： Douglas C. Beshore , Scott D. Kuduk
发明人： Douglas C. Beshore , Scott D. Kuduk
IPC分类号： A61K31/5025 , A61P25/00 , A61P25/20 , A61P25/28 , C07D487/04 , A61P25/18
CPC分类号： A61K31/495 , C07D487/04
摘要： The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of 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：本发明涉及作为M1受体阳性变构调节剂的式（I）的吡唑并[4,3-c]噌啉-3-酮化合物，其可用于治疗涉及M1受体的疾病，例如如阿尔茨海默病，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。

44. 发明申请

US20110136863A1 N-Heterocyclic M1 Receptor Positive Allosteric Modulators 有权
标题翻译： N-杂环M1受体阳性变构调节剂
公开(公告)号：US20110136863A1
公开(公告)日：2011-06-09
申请号：US13057079
申请日：2009-07-31
申请人： Scott D. Kuduk , Christina Ng Di Marco
发明人： Scott D. Kuduk , Christina Ng Di Marco
IPC分类号： A61K31/4709 , C07D401/10 , C07D215/58 , A61K31/47 , A61P25/28 , A61P25/18 , A61P25/04
CPC分类号： A61K31/47 , C07D215/56 , C07D401/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要： The present invention is directed to compounds of formula (I) (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：本发明涉及作为M1受体阳性变构调节剂的式（I）（I）化合物，其可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，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。

45. 发明申请

US20100222355A1 QUINOLIZIDINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS 有权
标题翻译：喹诺啶酮M1受体阳性单调性调节剂
公开(公告)号：US20100222355A1
公开(公告)日：2010-09-02
申请号：US12738208
申请日：2008-10-15
申请人： Ronald K. Chang , Scott D. Kuduk
发明人： Ronald K. Chang , Scott D. Kuduk
IPC分类号： A61K31/498 , C07D455/02 , A61K31/4545 , C07D241/42 , A61P25/00 , A61P29/00
CPC分类号： C07D455/02
摘要： The present invention is directed to spiropiperidine compounds of 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：本发明涉及作为M1受体阳性变构调节剂的式（I）的哌啶哌啶化合物，其可用于治疗涉及M1受体的疾病，例如阿尔茨海默氏病，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。

46. 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;

47. 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。

48. 发明授权

US06670348B1 Methods and compositions for destruction of selected proteins 失效
标题翻译：用于破坏所选蛋白质的方法和组合物
公开(公告)号：US06670348B1
公开(公告)日：2003-12-30
申请号：US09403434
申请日：1999-10-20
申请人： Neal Rosen , Samuel Danishefsky , Ouathek Ouerfelli , Scott D. Kuduk , Laura Sepp-Lorenzino
发明人： Neal Rosen , Samuel Danishefsky , Ouathek Ouerfelli , Scott D. Kuduk , Laura Sepp-Lorenzino
IPC分类号： A61K3131
CPC分类号： C07D225/06 , A61K47/554 , C07J17/00 , C07J43/00
摘要： Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease. Exemplary targeting moieties which may be employed in compounds of the invention include testosterone, estradiol, tamoxifen and wortmannin.
摘要翻译：具有安莎霉素无抗生素或与hsp90结合的其它部分的化合物偶联到特异性结合蛋白质，受体或标记的靶向部分可以提供安莎霉素抗生素的有效靶向递送，导致蛋白质的降解和靶细胞的死亡。这些组合物可以具有与单独的安莎霉素不同的特异性，允许治疗更具体的靶向，并且在单独使用安沙霉素没有作用的情况下可以是有效的。因此，根据靶向部分的性质，这些化合物提供了一类全新的靶向化学疗法，可用于治疗多种不同形式的癌症。此类试剂可进一步用于促进与其他疾病发病相关的蛋白质的选择性降解，所述疾病包括与自身免疫疾病相关的抗原和与阿尔茨海默病有关的病原性蛋白质。可用于本发明化合物的示例性靶向部分包括睾酮，雌二醇，他莫昔芬和渥曼青霉素。

49. 发明申请

US20170355692A1 ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS 有权
公开(公告)号：US20170355692A1
公开(公告)日：2017-12-14
申请号：US15532602
申请日：2015-12-14
申请人： Ronald M. Kim , Scott D. Kuduk , Nigel Liverton , Gang Zhou
发明人： Ronald M. Kim , Scott D. Kuduk , Nigel Liverton , Gang Zhou
IPC分类号： C07D413/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D401/12 , C07D403/14 , C07D213/84 , C07D239/42
CPC分类号： C07D413/12 , C07D213/84 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12
摘要： The present invention is directed to ethyldiamne 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.

50. 发明申请

US20170320856A1 AMIDOETHYL AZOLE OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：US20170320856A1
公开(公告)日：2017-11-09
申请号：US15535271
申请日：2015-12-18
申请人： Scott D. Kuduk , Nigel Liverton , Yunfu Luo
发明人： Scott D. Kuduk , Nigel Liverton , Yunfu Luo
IPC分类号： C07D403/14 , C07D401/14 , C07D401/12 , C07D403/12 , C07D249/04
CPC分类号： C07D403/14 , A61K31/4192 , A61K45/06 , C07D249/04 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12
摘要： The present invention is directed to amidoethyl azole 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.

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