公开(公告)号：US20080269166A2

公开(公告)日：2008-10-30

申请号：US10720134

申请日：2003-11-25

Applicant: Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

Inventor： Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

IPC: A61K31/724 ,  A61K31/277

CPC classification number: C07D295/192 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4866 ,  A61K31/135 ,  C07C215/64 ,  C07C217/74 ,  C07C233/18 ,  C07C255/36 ,  C07C255/37 ,  C07C2601/14

Abstract: Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract translation: 公开了制备方法和包含文拉法辛衍生物的组合物。 还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和 体重增加，失禁，痴呆和相关疾病。

公开(公告)号：US20060199860A1

公开(公告)日：2006-09-07

申请号：US11418137

申请日：2006-05-05

Applicant: Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

Inventor： Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

IPC: A61K31/277

CPC classification number: C07C217/74 ,  A61K31/137 ,  A61K31/277 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/02 ,  C07C215/64 ,  C07C2601/14

Abstract: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract translation: 公开了制备方法和包含（ - ） - 文拉法辛的衍生物的组合物。 还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和 体重增加，失禁，痴呆和相关疾病。

公开(公告)号：US5639875A

公开(公告)日：1997-06-17

申请号：US430437

申请日：1995-04-28

Applicant: Nandkumar Bhongle

Inventor： Nandkumar Bhongle

IPC: C07H19/10 ,  C07H21/00 ,  C07H1/02

CPC classification number: C07H19/10 ,  C07H21/00

Abstract: New methods of synthesizing mono- and oligo-nucleoside H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphorous acid and triphosgene to yield the corresponding mononucleoside H-phosphonate. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of triphosgene, a mononucleoside or oligonucleotide having a free 5' hydroxyl with a mononucleoside having a 3' hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).

Abstract translation: 公开了合成单 - 和寡 - 核苷H - 膦酸酯的新方法。 所述方法包括使单核苷与亚磷酸和三光气接触以产生相应的单核苷酸H-膦酸酯。 可以使用类似的方法将第一单核苷连接到第二单核苷或寡核苷酸，所述方法包括在三光气存在下使具有游离5'羟基的单核苷或寡核苷酸与具有3'羟基 - 带有磷部分（优选H-膦酸酯）。

公开(公告)号：US5554744A

公开(公告)日：1996-09-10

申请号：US311156

申请日：1994-09-23

Applicant: Nandkumar Bhongle ,  Jin-Yan Tang

Inventor： Nandkumar Bhongle ,  Jin-Yan Tang

IPC: C07H21/00

CPC classification number: C07H21/00

Abstract: New methods of loading solid supports for oligonucleotide synthesis are presented. The new methods comprise coupling a succinylated nucleoside to a solid support using diisopropylcarbodiimide (DIC) as an activator and N-hydroxybenzotriazole (HOBT) as an acid catalyst. DIC is substantially cheaper than the currently used activating agent, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (DEC). Furthermore, in the preferred embodiment, when it is used in combination with HOBT, coupling is more efficient, requiring less nucleoside to achieve the same loading densities as in the prior art. The loading process is faster than prior art methods and the overall cost savings of about 43% are realized.

Abstract translation: 提出了加载寡核苷酸合成固体载体的新方法。 新方法包括使用二异丙基碳二亚胺（DIC）作为活化剂和作为酸催化剂的N-羟基苯并三唑（HOBT）将琥珀酰化的核苷偶联到固体支持物上。 DIC比目前使用的活化剂，1-（3-二甲基氨基丙基）-3-乙基碳二亚胺（DEC）便宜得多。 此外，在优选实施方案中，当与HOBT组合使用时，耦合更有效，需要更少的核苷以实现与现有技术相同的装载密度。 加载过程比现有技术方法更快，并且实现了约43％的总体成本节约。

公开(公告)号：US20060199861A1

公开(公告)日：2006-09-07

申请号：US11418138

申请日：2006-05-05

Applicant: Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

Inventor： Thomas Jerussi ,  Chrisantha Senanayake ,  Nandkumar Bhongle

IPC: A61K31/277

CPC classification number: C07C217/74 ,  A61K31/137 ,  A61K31/277 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/02 ,  C07C215/64 ,  C07C2601/14

Abstract: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract translation: 公开了制备方法和包含（ - ） - 文拉法辛的衍生物的组合物。 还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和 体重增加，失禁，痴呆和相关疾病。

公开(公告)号：US5705629A

公开(公告)日：1998-01-06

申请号：US546318

申请日：1995-10-20

Applicant: Nandkumar Bhongle

Inventor： Nandkumar Bhongle

IPC: C07H1/02 ,  C07H21/04

CPC classification number: C07H1/02

Abstract: New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anyhydride to yield the corresponding mononucleoside H-phosphonate. Preferrably a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferrably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5' hydroxyl with a mononucleoside having a 3' hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).

Abstract translation: 公开了合成单核苷酸和寡核苷酸H-膦酸酯的新方法。 所述方法包括使单核苷与膦酸和苯甲酰酐接触，得到相应的单核苷酸H - 膦酸酯。 也可以使用催化量的三光气。 可以使用类似的方法将第一单核苷连接到第二单核苷或寡核苷酸，所述方法包括在苯甲酸酐存在下，优选催化量的三光气，具有游离的5'末端的单核苷酸或寡核苷酸， 羟基与具有3'含羟基的磷部分（优选H-膦酸酯）的单核苷。