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91. 发明申请

US20110124924A1 Cyclopropanation Process 有权
标题翻译：环丙烷化方法
公开(公告)号：US20110124924A1
公开(公告)日：2011-05-26
申请号：US12673901
申请日：2008-08-19
申请人： Fridtjof Schroder
发明人： Fridtjof Schroder
IPC分类号： C07C35/18 , C07C35/20 , C07C29/36 , C07C35/04 , C07C35/23 , C07C35/44
CPC分类号： C07C27/00 , A23L27/203 , C07C29/44 , C07C31/1333 , C07C31/137 , C07C35/27 , C07C35/37 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2602/18 , C07C2602/20 , C07C2602/50 , C07C2603/64 , C07C2603/94 , C07C2603/96 , C11B9/003 , C11B9/0042 , C11B9/0049 , C11B9/0057 , C11B9/0061 , C07C33/12 , C07C33/05 , C07C31/13 , C07C35/28 , C07C33/34 , C07C35/23
摘要： A method for the preparation of cyclopropyl carbinols by cyclopropanation of unsaturated alcoholates, utilising a reagent system selected from (A) magnesium metal and dibromomethane, and (B) dibromomethane and a tertiary Grignard reagent, the reaction being carried out in the presence of an ether solvent.The process is useful, for example, for the preparation of ingredients for the flavour and fragrance industry.
摘要翻译：通过使用选自（A）镁金属和二溴甲烷的试剂系统和（B）二溴甲烷和叔格氏试剂，通过不饱和醇的环丙烷化制备环丙基甲醇的方法，该反应在醚的存在下进行溶剂。该方法例如用于制备风味和香料工业的成分是有用的。

92. 发明申请

US20110065934A1 METHOD OF PRODUCING BICYCLO[3.1.0] HEXANE DERIVATIVE USING ENZYME 失效
标题翻译：使用酶的双氰胺衍生物[3.1.0] HEXANE衍生物的制备方法
公开(公告)号：US20110065934A1
公开(公告)日：2011-03-17
申请号：US12950609
申请日：2010-11-19
申请人： Mitsuaki HIROTSUKA , Joji SASAKI , Hiroaki KAMIYAMA , Motoko OSHIDA , Takaaki ISHII
发明人： Mitsuaki HIROTSUKA , Joji SASAKI , Hiroaki KAMIYAMA , Motoko OSHIDA , Takaaki ISHII
IPC分类号： C07C67/00 , C07D317/72 , C07C67/26 , C12P7/62 , C12P17/04
CPC分类号： C12P7/62 , C07C67/31 , C07C67/313 , C07C67/32 , C07C67/327 , C07C67/343 , C07C2602/18 , C07D317/72 , C07C69/757 , C07C69/732
摘要： Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.
摘要翻译：作为代谢型谷氨酸受体调节剂有用的双环[3.1.0]己烷衍生物的制备可以通过以下制备方法来实现：包括将由式（II）表示的化合物转化成由式（III）表示的化合物与在不使用昂贵的光学活性羟基羟基酯作为起始原料的情况下，在微生物衍生的酶的存在下，不需要超低温反应的氟化反应。此外，由于不对称合成可以在更接近最终产物的阶段进行，所以制造方法可用作可大量生产双环[3.1.0]己烷衍生物的制备方法。

93. 发明申请

US20080096869A1 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 有权
公开(公告)号：US20080096869A1
公开(公告)日：2008-04-24
申请号：US11958593
申请日：2007-12-18
申请人： Joannes Linders , Gustaaf Willemsens , Ronaldus Arnodus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
发明人： Joannes Linders , Gustaaf Willemsens , Ronaldus Arnodus Gilissen , Christophe Francis Buyck , Greta Vanhoof , Louis Van Der Veken , Libuse Jaroskova
IPC分类号： A61K31/551 , A61K31/165 , A61K31/357 , A61K31/47 , C07D217/04 , C07D243/08 , C07D317/28 , C07D265/30 , C07D241/04 , C07C233/03 , A61K31/495 , A61K31/535
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R7 and R8 each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl or indenyl.

94. 发明申请

US20050119345A1 6-Fluorobicyclo[3.1.0]hexane derivatives 有权
标题翻译： 6-氟二环[3.1.0]己烷衍生物
公开(公告)号：US20050119345A1
公开(公告)日：2005-06-02
申请号：US10500101
申请日：2002-12-26
申请人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
发明人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
IPC分类号： A61K45/00 , A61K31/00 , A61K31/196 , A61K31/198 , A61K31/381 , A61P25/18 , A61P43/00 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07D333/16 , A61K31/195 , C07C229/32
CPC分类号： A61K31/381 , A61K31/00 , A61K31/196 , A61K31/198 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07C2601/08 , C07C2602/18 , C07D333/16
摘要： An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：作为活性成分的抗抑郁药，其具有对II型代谢型谷氨酸受体具有拮抗作用的化合物，以及2-氨基-3-烷氧基-6-氟 - 双环[3.1.0]己烷-2,6-二式[I]的二羧酸衍生物：其中R 1和R 2可以相同或不同，各自表示羟基，C 1〜 1-10个烷氧基等; R 3表示C 1-10烷基酰基，C 1-6烷氧基-C 1-6烷基，酰基等; 和R 4和R 5可以相同或不同，各自表示氢原子，C 1-10烷基，等]或其药学上可接受的盐或水合物。

95. 发明授权

US06835751B2 Bicyclic amino acids as pharmaceutical agents 失效
公开(公告)号：US06835751B2
公开(公告)日：2004-12-28
申请号：US10762026
申请日：2004-01-21
申请人： Justin Stephen Bryans , David Clive Blakemore , Simon Andrew Osborne , Jean-Marie Receveur
发明人： Justin Stephen Bryans , David Clive Blakemore , Simon Andrew Osborne , Jean-Marie Receveur
IPC分类号： A01N3712
CPC分类号： A61K31/195 , C07C229/28 , C07C2602/18 , C07C2602/20 , C07C2602/22 , C07C2602/24 , C07C2602/28
摘要： The compounds of the instant invention are bicyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, and sleep disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.

96. 发明授权

US06809207B2 Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US06809207B2
公开(公告)日：2004-10-26
申请号：US10202137
申请日：2002-07-24
申请人： Sekar Alla , Seung-Yong Choi , Dale Dhanoa , Elso DiFranco , Galina Krokhina , Keqiang Li , Balasubramanian Thiagarajan , Wen-Chun Zhang
发明人： Sekar Alla , Seung-Yong Choi , Dale Dhanoa , Elso DiFranco , Galina Krokhina , Keqiang Li , Balasubramanian Thiagarajan , Wen-Chun Zhang
IPC分类号： C07D33502
CPC分类号： C07C229/36 , C07C229/28 , C07C271/22 , C07C2602/18 , C07C2603/18 , C07D211/34 , C07D213/55 , C07D309/04 , C07D333/24 , C07D335/02
摘要： The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.
摘要翻译：本发明提供某些α-氨基酸及其衍生物，例如但不限于酯，酰胺和盐。这些衍生物可以包括如苯基，吡啶基，哌啶基，四氢吡喃基，四氢噻喃基或噻吩基这样的代表性的侧基。本发明还提供了使用醛，甲酸铵和C 1 -C 5烷基异氰酸酯通过改性的Ugi型反应合成α-氨基酸及其衍生物的方法。通过该方法提供的化合物可用于开发用于治疗人类疾病的新药物。

97. 发明申请

US20040121962A1 Prodrugs of excitatory amino acids 失效
标题翻译：兴奋性氨基酸的前药
公开(公告)号：US20040121962A1
公开(公告)日：2004-06-24
申请号：US10250448
申请日：2003-11-12
发明人： David Scott Coffey , James Allen Monn , Concepcion Pedregal-Tercero
IPC分类号： A61K038/04 , C07K005/04
CPC分类号： C07C237/12 , C07C271/22 , C07C2602/18 , Y02P20/55
摘要： This invention relates to synthetic excitatory amino acid prodrugs according to formula (I) and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders. 1
摘要翻译：本发明涉及式（I）的合成兴奋性氨基酸前药及其制备方法。本发明进一步涉及使用和药物组合物的方法，其包含用于治疗神经障碍和精神障碍的化合物。

98. 发明申请

US20040082806A1 Process for producing bicyclocarboxylic acid derivative 审中-公开
标题翻译：双酚羧酸衍生物的制备方法
公开(公告)号：US20040082806A1
公开(公告)日：2004-04-29
申请号：US10471537
申请日：2003-09-11
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami
IPC分类号： C07C069/74 , C07C061/12
CPC分类号： C07C51/377 , C07C67/327 , C07C2602/18 , Y02P20/55 , C07C62/24 , C07C69/757
摘要： A process for producing a 2-oxobicyclonull3.1.0nullhex-3-ene-6-carboxylic acid derivative represented by a formula: 1 (wherein R1 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C3-6 cycloalkyl C1-6 alkyl group, a C1-6 alkyl group substituted with a substituted or unsubstituted phenyl group, a C1-6 alkoxy C1-6 alkyl group, a C1-6 hydroxyalkyl group, a C1-6 alkylthio C1-6 alkyl group, a C1-6 mercaptoalkyl group, or a substituted or unsubstituted phenyl group) characterized by reacting a 4-hydroxy-2-oxobicyclonull3.1.0nullhexane-6-carboxylic acid derivative represented by a formula: 2 (wherein R1 has the same meaning as described above, and R2 represents a hydrogen atom or a protective group of a hydroxyl group) in the presence of an acid or a base. A process for producing the compounds which are useful for efficient syntheses of 2-amino-3-fluorobicyclonull3.1.0nullhexane-2,6-dicarboxylic acids is provided.
摘要翻译：一种制备由下式表示的2-氧代双环[3.1.0]己-3-烯-6-羧酸衍生物的方法：其中R 1表示氢原子，C1-6烷基，C3- 6环烷基，C3-6环烷基C1-6烷基，被取代或未取代的苯基取代的C1-6烷基，C1-6烷氧基C1-6烷基，C1-6羟基烷基，C1 -6烷硫基C 1-6烷基，C 1-6巯基烷基或取代或未取代的苯基），其特征在于使由4-羟基-2-氧代双环[3.1.0]己烷-6-羧酸衍生物式（式中，R 1具有与上述相同的含义，R 2表示氢原子或羟基的保护基）在酸或碱的存在下进行。提供了可用于高效合成2-氨基-3-氟双环[3.1.0]己烷-2,6-二羧酸的化合物的方法。

99. 发明申请

US20030171431A1 Intermediate and process for producing fluorinated carboxylic acid derivative from the same 失效
标题翻译：从其制备氟化羧酸衍生物的中间体和方法
公开(公告)号：US20030171431A1
公开(公告)日：2003-09-11
申请号：US10311230
申请日：2002-12-17
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Takeo Taguchi
IPC分类号： C07C069/74 , C07D307/02 , A61K031/215
CPC分类号： C07C69/716 , C07C67/317 , C07C2601/08 , C07C2602/18 , C07C69/757
摘要： The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): 1 The compound according to the present invention is useful for efficient syntheses of 2-amino-6-fluorobicyclonull3.1.0nullhexane-2,6-dicarboxylic acids.
摘要翻译：本发明涉及由式（1）表示的2-氟-2-（3-氧代环戊基）乙酸酯衍生物：本发明化合物可用于2-氨基-6-氟双环[3.1。 0]己烷-2,6-二羧酸。

100. 发明授权

US06506908B2 Process for preparing 3-hydroxymethyl-4-(aryl or heterocyclic)-cyclopentanones 有权
公开(公告)号：US06506908B2
公开(公告)日：2003-01-14
申请号：US09838989
申请日：2001-04-20
申请人： Nobuyoshi Yasuda , Michael Palucki , Joann M. Um , David Alan Conlon , Barry M. Trost
发明人： Nobuyoshi Yasuda , Michael Palucki , Joann M. Um , David Alan Conlon , Barry M. Trost
IPC分类号： C07D33302
CPC分类号： C07D213/81 , C07C45/673 , C07C49/747 , C07C51/09 , C07C57/60 , C07C67/317 , C07C67/343 , C07C69/65 , C07C69/738 , C07C69/757 , C07C245/18 , C07C2601/08 , C07C2602/18 , C07D239/28 , C07D263/16
摘要： Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.

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