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1. 发明申请

US20060014779A1 3-Aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norephinephrine reuptake 失效
公开(公告)号：US20060014779A1
公开(公告)日：2006-01-19
申请号：US10532657
申请日：2003-10-24
申请人： Serge Boulet , Ann Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawla , John Masters , Victor Matassa , Brian Mathes , Richard Rathmell , Maria Whatton , Chad Wolfe
发明人： Serge Boulet , Ann Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawla , John Masters , Victor Matassa , Brian Mathes , Richard Rathmell , Maria Whatton , Chad Wolfe
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4704 , A61K31/428 , A61K31/423
CPC分类号： C07C217/20 , C07C217/34 , C07D333/54
摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.

2. 发明申请

US20060058360A1 Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors 失效
公开(公告)号：US20060058360A1
公开(公告)日：2006-03-16
申请号：US10532765
申请日：2003-10-24
申请人： Serge Boulet , Sandra Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawala , John Masters , Brian Mathes , Richard Rathmell , Maria Whatton , Victor Matassa , Chad Wolfe
发明人： Serge Boulet , Sandra Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawala , John Masters , Brian Mathes , Richard Rathmell , Maria Whatton , Victor Matassa , Chad Wolfe
IPC分类号： A61K31/428 , A61K31/425 , C07D277/62 , C07D275/06
CPC分类号： C07D275/04 , C07D215/20 , C07D217/02 , C07D217/04 , C07D217/24 , C07D277/62 , C07D333/54 , C07D471/04 , C07D495/04
摘要： There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —)— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.

3. 发明申请

US20070093526A1 4-Amino-piperidine derivatives as monoamine uptake inhibitors 失效
标题翻译： 4-氨基 - 哌啶衍生物作为单胺吸收抑制剂
公开(公告)号：US20070093526A1
公开(公告)日：2007-04-26
申请号：US10597795
申请日：2005-02-11
申请人： Serge Boulet , Barry Clark , John Fairhurst , Peter Gallagher , Anette Johansson , Maria Whatton , Virginia Wood
发明人： Serge Boulet , Barry Clark , John Fairhurst , Peter Gallagher , Anette Johansson , Maria Whatton , Virginia Wood
IPC分类号： A61K31/4545 , A61K31/454 , C07D403/02 , C07D401/02
CPC分类号： C07D513/04 , A61K31/454 , A61K31/4545 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.
摘要翻译：本发明提供式（I）化合物，其中n，R 1，R 2，R 3，R 4，R 5和杂芳基如本文所定义。这些化合物是一种或多种选自5-羟色胺，去甲肾上腺素和多巴胺的单胺摄取的抑制剂，因此可用于治疗中枢和/或周围神经系统疾病。

4. 发明申请

US20070072859A1 Pharmaceutical compounds 审中-公开
公开(公告)号：US20070072859A1
公开(公告)日：2007-03-29
申请号：US10597835
申请日：2005-02-18
申请人： Serge Boulet , Anette Johansson , Sarah Smith
发明人： Serge Boulet , Anette Johansson , Sarah Smith
IPC分类号： A61K31/5375 , A61K31/445 , A61K31/40 , A61K31/137 , C07D211/06
CPC分类号： C07C217/20 , C07D295/125 , C07D295/13
摘要： The present invention relates to inhibitors of serotonin and/or norepinephrine reuptake and specifically provides compounds of formula (I): wherein A is selected from —O— and —S—; X is selected from C1-C8 alkyl, C2-C8 alkenyl, and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from phenyl, pyrrolidinyl, piperidinyl, morpholinyl, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from (a), (b), (c), (d), (e), (f) where R3, R4 and R5 are independently selected from hydrogen, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R6 and R7 are independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R8 is selected from chloro, bromo, iodo, C1-C4alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R1 and R2 are each independently hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; or compositions thereof and methods of using the same.

5. 发明授权

US06747156B2 Method of producing 6-substituted (s)-nicotine derivatives and intermediate compounds 失效
标题翻译：生产6-取代的烟碱衍生物和中间体化合物的方法
公开(公告)号：US06747156B2
公开(公告)日：2004-06-08
申请号：US10221175
申请日：2002-12-04
申请人： Anette Johansson , Torgny Svensson
发明人： Anette Johansson , Torgny Svensson
IPC分类号： C07D40104
CPC分类号： C07D401/04
摘要： A method of producing a 6-substituted (S)-nicotine derivative with the general formula (III), wherein R is an optionally substituted alkyl, alkenyl, alkynyl, amido or amino group, optionally coupled to a carrier protein, is disclosed. An intermediate compound useful in the method is also comprised by the invention. The formula of the compound is (A) in which A represents the cationic radical of an organic nitrogen base, Y represents an anion formed by an electrophilic compound.
摘要翻译：公开了一种制备具有通式（III）的6-取代的（S） - 烟碱衍生物的方法，其中R是可任意取代的烷基，烯基，炔基，酰胺基或氨基，任选与载体蛋白偶联。用于该方法的中间体化合物也包括在本发明中。化合物的式为（A），其中A表示有机氮碱的阳离子基团，Y表示由亲电子化合物形成的阴离子。

6. 发明授权

US06258997B1 Liquid-pervious cover layer for an absorbent article 失效
标题翻译：用于吸收制品的透液性透液层
公开(公告)号：US06258997B1
公开(公告)日：2001-07-10
申请号：US09367814
申请日：1999-09-30
申请人： Anette Johansson , Nils Ljungqvist
发明人： Anette Johansson , Nils Ljungqvist
IPC分类号： A61F1315
CPC分类号： A61F13/15699 , A61F13/51121 , A61F2013/51007
摘要： A liquid-pervious cover layer for an absorbent article, such as a sanitary napkin, a panty-liner, a diaper, or the like, which comprises a liquid-pervious carrier layer against which individual hydrophobic fibers, detached from each other and each exhibiting two fiber ends, are attached with one fiber end against the carrier layer, with an attachment angle &agr; between the carrier layer and each individual fiber. The cover layer exhibits fiber-free regions for facilitating liquid transfer through the cover layer. The invention further includes an absorbent article provided with the cover layer, and a method of manufacturing the cover layer.
摘要翻译：用于吸收制品的透液性覆盖层，例如卫生巾，内裤衬里，尿布等，其包括透液性载体层，各个疏水性纤维彼此分离并且各自展现出两个纤维端部以一个纤维端部抵靠载体层附着，载体层和每个单独纤维之间具有连接角α。覆盖层表现出无纤维区域，以便于通过覆盖层的液体转移。本发明还包括设置有覆盖层的吸收性物品，以及制造覆盖层的方法。

7. 发明授权

US07005558B1 Apertured covering sheet for an absorbent article and a method of producing the covering sheet 失效
标题翻译：用于吸收性物品的开孔覆盖片及其制造方法
公开(公告)号：US07005558B1
公开(公告)日：2006-02-28
申请号：US09171520
申请日：1997-04-25
申请人： Anette Johansson , Agneta Thorén
发明人： Anette Johansson , Agneta Thorén
IPC分类号： A61F13/15
CPC分类号： A61F13/512
摘要： A liquid permeable covering sheet of an absorbent article such as a diaper, an incontinence protector, or a sanitary napkin which comprises an apertured textile material. The covering sheet has a plurality of holes, each of which is surrounded by an essentially liquid-type edge. The invention further comprises an absorbent article with a covering sheet according to the invention. A method of making the covering sheet by causing heated needles to penetrate a textile material layer comprising at one thermoplastic component is also covered by the invention.
摘要翻译：尿布，失禁保护器或卫生巾等吸收性物品的透液性覆盖片，其包含有孔纺织材料。覆盖片具有多个孔，每个孔被基本上液体的边缘包围。本发明还包括具有根据本发明的覆盖片的吸收制品。通过使加热的针穿透包含一种热塑性成分的织物材料层来制造覆盖片的方法也被本发明覆盖。

8. 发明授权

US06656469B1 Nicotine immunogen 失效
标题翻译：尼古丁免疫原
公开(公告)号：US06656469B1
公开(公告)日：2003-12-02
申请号：US09700718
申请日：2000-11-28
申请人： Torgny Svensson , Anette Johansson
发明人： Torgny Svensson , Anette Johansson
IPC分类号： A61K3900
CPC分类号： A61K39/0013 , A61K2039/6081 , A61K2039/627
摘要： A 5- or 6-nicotinyl-linker-carrier protein compound and immunogen having formula (a) wherein X is —NH—CO— or NH— or —C≡C— or —C═C— or CH2—; Y is —(CH2)k— or —(CH2)m—C6H10—(CH2)n— or (CH2)m—C6H4—(CH2)n— when Z is —NH—, with the proviso that X is not —NH—CO— when Y is (CH2)5 and Z is —NH—, and X is —NH—CO— or —C≡C— or —C═C— or CH2—, Y is —(CH2)m—C6H10—(CH2)n— or —(CH2)m—C6H4—(CH2)n—, when Z is —CO—, and X is —C≡C— or —C═C—, Z is —CO—, when Y is (CH2)k—, is disclosed. The compound may be used as a medicament, suitably in the form of a pharmaceutical composition. Additionally, a method of prophylactic and/or therapeutic immunological treatment of nicotine dependence from tobacco products to achieve harm reduction is described.
摘要翻译： 5-或6-烟酰基 - 接头 - 载体蛋白化合物和具有式（a）的免疫原，其中X是-NH-CO-或NH-或-C = C-或-C = C-或CH 2 - ; 当Z为-NH-时，Y为 - （CH 2）k - 或 - （CH 2）m -C 6 H 10 - （CH 2）n - 或（CH 2）m -C 6 H 4 - （CH 2）n-，条件是X不为 - 当Y为（CH 2）5且Z为-NH-，X为-NH-CO-或-C = C - 或-C = C-或CH 2 - 时，Y为 - （CH 2）m - 当Z为-CO-，且X为-C = C-或-C = C-，Z为-CO-时，C 6 H 10 - （CH 2）n - 或 - （CH 2）m -C 6 H 4 - （CH 2）n - 当Y是（CH 2）k - 时。该化合物可以用作药物，适合以药物组合物的形式。另外，描述了一种从烟草制品中预防和/或治疗免疫治疗尼古丁依赖以实现危害降低的方法。

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