公开(公告)号：US20240010615A1

公开(公告)日：2024-01-11

申请号：US18253137

申请日：2021-12-20

申请人： Kyowa Pharma Chemical Co., Ltd.

发明人： Yuto YABUUCHI ,  Yuki TAKEUCHI

IPC分类号： C07C405/00

CPC分类号： C07C405/00 ,  C07B2200/09 ,  C07C2601/08

摘要： The present invention provides a method for separating a compound represented by Formula (1) or (2) [in the formula, P1 is a hydrogen atom or a protective group of a hydroxyl group, R1 is a linear or branched C1-6 alkyl group that may be substituted with a phenyl group, A is an alkenylene group, and R2 is a hydroxyl group, a C1-3 alkoxy group, a mono(C1-3 alkyl)amino group, or a di(C1-3 alkyl)amino group] from a geometrical isomer thereof, in which the geometrical isomer is a geometrical isomer in a double bond included in A, the method including processing a mixture containing the compound and the geometrical isomer thereof by a chromatographic method using an acidic functional group-modified silica gel as a stationary phase.

公开(公告)号：US20210332011A1

公开(公告)日：2021-10-28

申请号：US17055970

申请日：2019-05-14

申请人： California Institute of Technology

发明人： Jiaming LI ,  Xu CHEN ,  Tonia S. AHMED ,  Brian STOLTZ ,  Robert H. GRUBBS

IPC分类号： C07C405/00 ,  B01J23/46

摘要： This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).

公开(公告)号：US10273206B2

公开(公告)日：2019-04-30

申请号：US14318402

申请日：2014-06-27

申请人： ALLERGAN, INC.

发明人： Thomas K. Karami ,  Scott W. Smith ,  Fiona Dubas-Fisher ,  Adrian St. Clair Brown

IPC分类号： A61K31/215 ,  C07C405/00 ,  C07C215/10

摘要： The present invention provides tromethamine salt of (Z)-7-[3,5-Dihydroxy-2-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline Form 1 and amorphous form. This compound is may also be referred to as “tromethamine salt of bimatoprost acid.” The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.

公开(公告)号：US10106499B1

公开(公告)日：2018-10-23

申请号：US15809002

申请日：2017-11-10

申请人： CHIROGATE INTERNATIONAL INC.

发明人： Shih-Yi Wei ,  Shih-Hsun Su

IPC分类号： C07C315/04 ,  C07C67/297 ,  C07C405/00 ,  C07C39/23 ,  A61K31/5575

摘要： Novel processes for preparing cyclopenta[b]naphthalenol derivatives of Formula 1 which are useful for the synthesis of corresponding benzindene prostaglandins are provided. The present invention also relates to novel intermediates prepared from the processes.

公开(公告)号：US09856213B2

公开(公告)日：2018-01-02

申请号：US14965515

申请日：2015-12-10

申请人： CHINOIN ZRT

发明人： Gábor Havasi ,  Tibor Kiss ,  Irén Hortobágyi ,  Zsuzsanna Kardos ,  István Lászlófi ,  Zoltán Bischof ,  Ádám Bódis

IPC分类号： C07C405/00 ,  C07D207/46 ,  C07D209/48 ,  C07D233/60 ,  C07D307/935 ,  C07D209/50

CPC分类号： C07C405/0041 ,  C07B2200/13 ,  C07C405/00 ,  C07C2601/08 ,  C07D207/46 ,  C07D209/48 ,  C07D209/50 ,  C07D233/60 ,  C07D307/935

摘要： The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.

公开(公告)号：US09828356B2

公开(公告)日：2017-11-28

申请号：US14802026

申请日：2015-07-17

申请人： CHIROGATE INTERNATIONAL INC.

发明人： Shih-Yi Wei ,  Yu-Chih Yeh ,  Min-Kuan Hsu ,  Li-Ta Kao

IPC分类号： C07D313/00 ,  C07C69/618 ,  C07C69/608 ,  C07F7/18 ,  C07D309/12 ,  C07C51/347 ,  C07D407/12 ,  C07D405/00 ,  C07C67/10 ,  C07C59/72 ,  C07C405/00 ,  C07C231/02 ,  C07D407/14

CPC分类号： C07D313/00 ,  C07C51/347 ,  C07C59/72 ,  C07C67/10 ,  C07C69/608 ,  C07C69/618 ,  C07C231/02 ,  C07C405/00 ,  C07C405/0016 ,  C07C405/0041 ,  C07C2601/08 ,  C07D309/12 ,  C07D407/12 ,  C07D407/14 ,  C07F7/1804 ,  C07F7/1864

摘要： Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

公开(公告)号：US09382272B2

公开(公告)日：2016-07-05

申请号：US13145999

申请日：2010-01-22

申请人： Kiran Kumar Kothakonda ,  Fan Wang ,  Bhaskar Reddy Guntoori ,  Minh T. N. Nguyen ,  Alfredo Paul Ceccarelli ,  Yajun Zhao ,  Uma Kotipalli ,  Sammy Chris Duncan ,  Kaarina K. Milnes ,  Kevin Wade Kells ,  Laura Kaye Montemayor

发明人： Kiran Kumar Kothakonda ,  Fan Wang ,  Bhaskar Reddy Guntoori ,  Minh T. N. Nguyen ,  Alfredo Paul Ceccarelli ,  Yajun Zhao ,  Uma Kotipalli ,  Sammy Chris Duncan ,  Kaarina K. Milnes ,  Kevin Wade Kells ,  Laura Kaye Montemayor

IPC分类号： C07D323/04 ,  C07D311/00 ,  C07D315/00 ,  C07D307/93 ,  C07C61/06 ,  C07C69/74 ,  C07F7/18 ,  C07C69/734 ,  C07C69/738 ,  C07C405/00 ,  C07D307/935

CPC分类号： C07F7/1892 ,  C07C69/734 ,  C07C69/738 ,  C07C405/00 ,  C07C2601/08 ,  C07D307/935

摘要： There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)

摘要翻译： 提供了用于制备卢比克石及其中间体的方法。 还提供了化合物，包括用于制备柳替罗石的中间体以及包含卢比石和其它化合物的组合物，包括用于制备柳普罗石和其它化合物的中间体。 （一世）

公开(公告)号：US09353055B2

公开(公告)日：2016-05-31

申请号：US14594668

申请日：2015-01-12

申请人： Johnson Matthey Public Limited Company

发明人： Robert R. Hogan ,  Ronald Rossi

IPC分类号： C07C69/74 ,  C07C405/00 ,  C07D307/93 ,  C07D307/937 ,  C07C69/732 ,  C07C323/56

CPC分类号： C07C405/00 ,  C07C69/732 ,  C07C323/56 ,  C07C2601/08 ,  C07C2603/14 ,  C07D307/93 ,  C07D307/937 ,  Y02P20/544

摘要： The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.

公开(公告)号：US20160137602A1

公开(公告)日：2016-05-19

申请号：US14965489

申请日：2015-12-10

申请人： CHINOIN ZRT

发明人： Gábor HAVASI ,  Tibor KISS ,  Irén HORTOBÁGYI ,  Zsuzsanna KARDOS ,  István LÁSZLÓFI ,  Zoltán BISCHOF ,  Ádám BÓDIS

IPC分类号： C07D209/50 ,  C07C405/00 ,  C07D207/46

CPC分类号： C07C405/0041 ,  C07B2200/13 ,  C07C405/00 ,  C07C2601/08 ,  C07D207/46 ,  C07D209/48 ,  C07D209/50 ,  C07D233/60 ,  C07D307/935

摘要： The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula, the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5, 6 and 13, 14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.

摘要翻译： 本发明的主题是制备通式I的前列腺素酰胺的方法，其中在该式中，用虚线标记的键可以是单键或双键，在5,6位的双重界限的情况下， 13,14可以是顺式或反向取代，Q表示羟基，Z表示羟基或氧代基，R1和R2独立地表示氢原子或直链或支链C1-10烷基或 任选被-ONO 2基团取代的芳烷基，或含有杂原子的芳烷基 - 或芳基，R 3表示直链或支链，饱和或不饱和的C 4-6烃基或C 4-10烷基环烷基 - 或环烷基 - 基团或任选具有烷基或卤素原子取代的苯基 - ，C7-10烷基芳基或杂芳基，Y表示（CH 2）n基团或O原子或S原子，并且其中n = 0-3。

公开(公告)号：US09089579B2

公开(公告)日：2015-07-28

申请号：US13980179

申请日：2012-01-18

申请人： Murat V. Kalayoglu

发明人： Murat V. Kalayoglu

IPC分类号： A61K31/5575 ,  C07C405/00 ,  A61P3/10 ,  A61K31/5585 ,  C07C69/732 ,  C07C235/30 ,  C07D307/20

CPC分类号： A61K31/5575 ,  A61K9/0014 ,  A61K31/133 ,  A61K31/5585 ,  C07C69/732 ,  C07C235/30 ,  C07D307/20

摘要： Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein, L, R1; R2, Z, X, A and B are defined herein.

摘要翻译： 提供了用于治疗代谢综合征或与代谢综合征相关的病症（例如肥胖，血脂异常和/或糖尿病）的方法，组合物，系统和试剂盒，其包括向受试者全身施用一种或多种式（I ）和/或（II）：或其药学上可接受的盐，水合物，溶剂合物，立体异构体，多晶型物，互变异构体，同位素富集的衍生物或前药。 R2，Z，X，A和B在本文中定义。