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1. 发明申请

US20140336405A1 Process for preparing spiro[2.5]octane-5,7-dione 审中-公开
标题翻译：制备螺[2.5]辛烷-5,7-二酮的方法
公开(公告)号：US20140336405A1
公开(公告)日：2014-11-13
申请号：US14445371
申请日：2014-07-29
申请人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
发明人： Torsten BUSCH , Sven ANKLAM , Joerg JUNG , Markus OSTERMEIER
IPC分类号： C07C45/65 , C07C69/608 , C07C259/06 , C07C69/635 , C07C69/716 , C07C59/205
CPC分类号： C07C45/65 , C07C45/455 , C07C49/443 , C07C51/08 , C07C51/083 , C07C59/205 , C07C67/08 , C07C67/30 , C07C67/343 , C07C69/608 , C07C69/635 , C07C69/716 , C07C259/06 , C07C2601/02 , C07C2602/50 , C07D311/96 , C07C55/28
摘要： Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.
摘要翻译：公开了用于合成制备药物活性成分的螺[2.5]辛烷-5,7-二酮作为中间体的方法。还公开了用于合成该化合物的新型中间体。

2. 发明申请

US20140256782A1 Opsin-Binding Ligands, Compositions and Methods of Use 有权
标题翻译：组合物和使用方法
公开(公告)号：US20140256782A1
公开(公告)日：2014-09-11
申请号：US14352178
申请日：2012-10-19
申请人： David S. Garvey , Gregory J. Larosa , Jeremy R. Greenwood , Leah L. Frye , Tan Quach , Jamie B. Cote , Judd Berman
发明人： David S. Garvey , Gregory J. Larosa , Jeremy R. Greenwood , Leah L. Frye , Tan Quach , Jamie B. Cote , Judd Berman
IPC分类号： C07C49/443 , C07C233/58 , C07C69/75 , C07C35/32 , C07D307/83 , C07D209/34
CPC分类号： C07D307/83 , C07C35/32 , C07C49/443 , C07C49/553 , C07C69/75 , C07C233/58 , C07C251/44 , C07C2102/24 , C07D209/34 , C07D209/46
摘要： Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
摘要翻译：公开的化合物可用于治疗由生产有毒的视觉循环产物引起的或与生物相关的眼部疾病，其是积聚在眼睛中的视觉循环产物，例如干性成年黄斑变性，以及由突变视蛋白质蛋白质错误折叠引起或与之相关的病症和/或视蛋白蛋白质的错误定位。还描述了这些化合物单独或与其它治疗剂组合的组合物，以及使用这些化合物和/或组合物的治疗方法。还公开了合成这些试剂的方法。

3. 发明申请

US20090281340A1 1ALPHA-HYDROXY-2-(3'-HYDROXYPROPYLIDENE)-19-NOR-VITAMIN D COMPOUNDS AND METHODS OF MAKING AND TREATMENT THEREOF 审中-公开
标题翻译： 1ALPHA-羟基-2-（3'-羟基丙烯酰基）-19-异维生素D化合物及其制备和处理方法
公开(公告)号：US20090281340A1
公开(公告)日：2009-11-12
申请号：US12437892
申请日：2009-05-08
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
IPC分类号： C07C401/00 , C07C45/00
CPC分类号： C07C401/00 , C07C45/29 , C07C2602/24 , C07C49/443
摘要： Disclosed are 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3′-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
摘要翻译：公开了1α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物，药物组合物及其制备和处理方法。化合物通常指向生物活性的2-亚烷基-19-去甲维生素D化合物及其类似物，其特征在于在C-2存在3'-羟基亚丙基部分，并且存在没有任何的缩写的烷基侧链羟基部分。

4. 发明授权

US07482313B2 Bicyclo(3.3.1)nonanes and bicyclo(3.3.1)nonenes and their use as flavor or fragrance ingredient 失效
标题翻译：双酚（3.3.1）壬烷和双环（3.3.1）壬烯及其作为香料或香料成分的用途
公开(公告)号：US07482313B2
公开(公告)日：2009-01-27
申请号：US10597289
申请日：2005-01-14
申请人： Thierry Granier , Andreas Hanhart , Jerzy A. Bajgrowicz
发明人： Thierry Granier , Andreas Hanhart , Jerzy A. Bajgrowicz
IPC分类号： C11D3/50
CPC分类号： C07C49/443 , C07C35/23 , C07C43/188 , C07C43/305 , C07C49/647 , C07C49/753 , C07C2602/46 , C07D317/72
摘要： The present invention relates to substituted bicyclo[3.3.1]nonanes and bicyclo[3.3.1]nonenes of formula (I) wherein R, and R1 to R5 have the same meaning as described in the specification.
摘要翻译：本发明涉及式（I）的取代的双环[3.3.1]壬烷和双环[3.3.1]壬烯，其中R 1和R 1至R 5具有与说明书中所述相同的含义。

5. 发明申请

US20080274927A1 Bicyclo(3.3.1)Nonanes and Bicyclo(3.3.1)Nonenes and Their Use as Flavor or Fragrance Ingredient 失效
标题翻译：双酚（3.3.1）壬烷和双环（3.3.1）壬烯及其作为香料或香料成分的用途
公开(公告)号：US20080274927A1
公开(公告)日：2008-11-06
申请号：US10597289
申请日：2005-01-14
申请人： Thierry Granier , Andreas Hanhart , Jerzy A. Bajgrowicz
发明人： Thierry Granier , Andreas Hanhart , Jerzy A. Bajgrowicz
IPC分类号： C11D3/50 , C07C49/323 , C07C35/23 , A61K8/34 , C11D9/44 , A61K8/35 , A61Q13/00
CPC分类号： C07C49/443 , C07C35/23 , C07C43/188 , C07C43/305 , C07C49/647 , C07C49/753 , C07C2602/46 , C07D317/72
摘要： The present invention relates to substituted bicyclo[3.3.1]nonanes and bicyclo[3.3.1]nonenes of formula (I) wherein R, and R1 to R5 have the same meaning as described in the specification.
摘要翻译：本发明涉及式（I）的取代的双环[3.3.1]壬烷和双环[3.3.1]壬烯，其中R 1和R 1至R 5具有与说明书中描述的含义相同。

6. 发明授权

US07205286B2 (20S)-1α-hydroxy-2α-methyl and 2β-methyl-19-nor-vitamin D3 and their uses 有权
标题翻译：（20S）-1α-羟基-2α-甲基和2b-甲基-19-维生素D3及其用途
公开(公告)号：US07205286B2
公开(公告)日：2007-04-17
申请号：US10762911
申请日：2004-01-22
申请人： Hector F. DeLuca , Rafal R. Sicinski , Pawel K. Grzywacz
发明人： Hector F. DeLuca , Rafal R. Sicinski , Pawel K. Grzywacz
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
摘要翻译：本发明公开了（20S）-1α-羟基-2α-甲基-19-去甲维生素D 3和（20S）-1α-羟基-2β-甲基-19-去甲维生素D _{3 及其制药用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。这些化合物还具有非常显着的钙血活性，因此可用于治疗人类的免疫疾病以及代谢性骨疾病如骨质疏松症。}

7. 发明申请

US20040152678A1 (20S)-1alpha-hydroxy-2alpha-methyl and 2beta-methyl-19-nor-vitamin D3 and their uses 有权
公开(公告)号：US20040152678A1
公开(公告)日：2004-08-05
申请号：US10762911
申请日：2004-01-22
申请人： Wisconsin Alumni Research Foundation
发明人： Hector F. DeLuca , Rafal R. Sicinski , Pawel K. Grzywacz
IPC分类号： A61K031/59
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.

8. 发明申请

US20040152677A1 (20S)-1alpha-hydroxy-2alpha-methl and 2beta-methyl-19-nor-vitamin D3 and their uses 有权
标题翻译：（20S）-1α-羟基-2α-甲基和2beta-甲基-19-维生素D3及其用途
公开(公告)号：US20040152677A1
公开(公告)日：2004-08-05
申请号：US10762906
申请日：2004-01-22
申请人： Wisconsin Alumni Research Foundation
发明人： Hector F. DeLuca , Rafal R. Sicinski , Pawel K. Grzywacz
IPC分类号： A61K031/59
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
摘要翻译：本发明公开了（20S）-1α-羟基-2α-甲基-19-去甲维生素D3和（20S）-1α-羟基-2β-甲基-19-去甲维生素D3及其药物用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。这些化合物还具有非常显着的钙血活性，因此可用于治疗人类的免疫疾病以及代谢性骨疾病如骨质疏松症。

9. 发明申请

US20030203882A1 (20S) 1alpha-hydroxy-2alpha-methyl and 2beta-methyl-19-nor-vitamin D3 and their uses 有权
标题翻译：（20S）1α-羟基-2α-甲基和2β-甲基-19-维生素D3及其用途
公开(公告)号：US20030203882A1
公开(公告)日：2003-10-30
申请号：US10127180
申请日：2002-04-22
发明人： Hector F. DeLuca , Rafal R. Sicinski , Pawel K. Grzywacz
IPC分类号： A61K031/59
CPC分类号： C07C49/433 , A61K31/593 , C07C49/443
摘要： This invention discloses (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and (20S)-1null-hydroxy-2null-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
摘要翻译：本发明公开了（20S）-1α-羟基-2α-甲基-19-去甲维生素D3和（20S）-1α-羟基-2β-甲基-19-去甲维生素D3及其药物用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。这些化合物还具有非常显着的钙血活性，因此可用于治疗人类的免疫疾病以及代谢性骨疾病如骨质疏松症。

10. 发明授权

US4206089A 5-Alkylbicyclo[4.3.0]non-1-en-3-one and 5-alkylbicyclo[4.3.0]nonane-3-one perfume compositions 失效
标题翻译： 5-烷基双环[4.3.0]壬-1-烯-3-酮和5-烷基双环[4.3.0]壬烷-3-酮香料组合物
公开(公告)号：US4206089A
公开(公告)日：1980-06-03
申请号：US888778
申请日：1978-03-21
申请人： Brian J. Willis , Robert G. Eilerman
发明人： Brian J. Willis , Robert G. Eilerman
IPC分类号： C07C45/62 , C07C45/67 , C07C49/443 , C07C49/633 , C11B9/00 , A61K7/46
CPC分类号： C11B9/0049 , C07C45/62 , C07C45/673 , C07C49/443 , C07C49/633
摘要： Novel bicyclic ketones having the structure: ##STR1## wherein R is a C.sub.1 -C.sub.5 alkyl group, either straight-chain or branched, and saturated analogs have been prepared. These compounds exhibit floral and woody odors and/or desirable flavor properties, and are useful as fragrance and/or flavor materials. The compounds are conveniently prepared from alkylidene cyclopentanones by Michael addition with alkyl metalloacetoacetates and subsequent decarboxylative cyclization of the adducts. The saturated analogs may then be prepared by hydrogenation.
摘要翻译：具有以下结构的新型双环酮：其中R是直链或支链的C 1 -C 5烷基和饱和类似物。这些化合物表现出花香和木质气味和/或期望的风味特性，并且可用作香料和/或香料材料。通过与烷基金属乙酰乙酸酯进行迈克尔加成，随后加成的脱羧环化，方便地由亚烷基环戊酮制备化合物。然后可以通过氢化制备饱和类似物。

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