公开(公告)号：US09624152B2

公开(公告)日：2017-04-18

申请号：US14674028

申请日：2015-03-31

Applicant: Esperion Therapeutics, Inc.

Inventor： Jean-Louis H. Dasseux ,  Carmen D. Oniciu

IPC: A61K31/20 ,  C07C31/27 ,  C07C61/12 ,  C07C47/34 ,  C07C309/25 ,  C07F9/24 ,  C07D261/12 ,  C07C59/105 ,  C07C33/26 ,  C07C47/19 ,  C07C69/675 ,  C07C69/003 ,  C07C69/017 ,  C07C309/08 ,  C07F9/11 ,  C07C309/24 ,  C07F9/12 ,  C07D495/04 ,  C07C255/00 ,  C07D257/04 ,  C07D261/08 ,  C07D305/12 ,  C07D307/33 ,  C07C59/01 ,  C07D309/30 ,  A61K31/194 ,  A61K31/23 ,  A61K31/191 ,  C07C31/20 ,  C07C31/22 ,  C07C31/24 ,  C07C59/11 ,  C07C59/245 ,  C07C59/285 ,  C07C59/29 ,  C07C59/46 ,  C07C59/48 ,  C07C59/54 ,  C07C62/02 ,  C07C62/06 ,  C07C65/17 ,  C07C69/757 ,  C07D213/80 ,  C07D309/10 ,  C07D309/12 ,  C07D405/12 ,  C07F9/09 ,  C07F9/117 ,  C07F9/44

CPC classification number: C07C31/27 ,  A61K31/191 ,  A61K31/194 ,  A61K31/20 ,  A61K31/23 ,  C07C31/20 ,  C07C31/22 ,  C07C31/24 ,  C07C33/26 ,  C07C47/19 ,  C07C47/34 ,  C07C59/01 ,  C07C59/105 ,  C07C59/11 ,  C07C59/245 ,  C07C59/285 ,  C07C59/29 ,  C07C59/46 ,  C07C59/48 ,  C07C59/54 ,  C07C61/12 ,  C07C62/02 ,  C07C62/06 ,  C07C65/17 ,  C07C69/003 ,  C07C69/017 ,  C07C69/675 ,  C07C69/757 ,  C07C255/00 ,  C07C309/08 ,  C07C309/24 ,  C07C309/25 ,  C07C2101/02 ,  C07C2101/04 ,  C07C2101/08 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/80 ,  C07D257/04 ,  C07D261/08 ,  C07D261/12 ,  C07D305/12 ,  C07D307/33 ,  C07D309/10 ,  C07D309/12 ,  C07D309/30 ,  C07D405/12 ,  C07D495/04 ,  C07F9/093 ,  C07F9/094 ,  C07F9/11 ,  C07F9/117 ,  C07F9/12 ,  C07F9/2408 ,  C07F9/2416 ,  C07F9/242 ,  C07F9/2425 ,  C07F9/4423

Abstract: The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

公开(公告)号：US08748658B2

公开(公告)日：2014-06-10

申请号：US13052556

申请日：2011-03-21

Applicant: Uppuluri Venkata Mallavadhani ,  Banita Pattnaik

Inventor： Uppuluri Venkata Mallavadhani ,  Banita Pattnaik

IPC: C07C61/12 ,  C07C61/28

CPC classification number: C07J63/008

Abstract: The present invention relates to a process for the fast isolation of ursolic acid, a highly potent natural scaffold, from the leaves of Diospyros melanoxylon. The present invention also provides an improved and fast isolation process of the title compound, which is a pentacyclic triterpenic acid highly useful for the synthesis of a wide range of novel and potent bio-active molecules.

Abstract translation: 本发明涉及一种快速分离来自柿子黑色素的叶的熊果酸（一种高效天然支架）的方法。 本发明还提供了一种改进和快速的标题化合物的分离方法，该方法是对于广泛的新型和有效的生物活性分子的合成非常有用的五环三萜酸。

公开(公告)号：US20110142916A1

公开(公告)日：2011-06-16

申请号：US12988587

申请日：2009-04-22

Applicant: Mark Stephen Baird ,  Juma' a Raheem Najeem Al-Dulayymi ,  Cornelias Theunissen ,  Gani Koza ,  Seppe Vander Beken ,  Johan Adriann Marc Grooten

Inventor： Mark Stephen Baird ,  Juma' a Raheem Najeem Al-Dulayymi ,  Cornelias Theunissen ,  Gani Koza ,  Seppe Vander Beken ,  Johan Adriann Marc Grooten

IPC: A61K9/127 ,  A61K39/00 ,  C07C59/01 ,  C07C61/12 ,  C07C61/04 ,  C07C59/90 ,  C07D303/38 ,  A61P31/00

CPC classification number: A61K39/39 ,  A61K2039/55555

Abstract: A compound of formula (I) for use as an adjuvant in vaccination; wherein R is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 50 carbon atoms; R1 is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 40 carbon atoms; each of R2, R3 and R4 is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, arylalkylene or alkylarylene moiety having from 1 to 40 carbon atoms; each of X, Y and Z is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, alkylarylene or cycloalkylene, ketone, ester, amide, imide, imine, thioether, ether, thioester, thioketone; and P is selected from hydrogen, an alkyl group, a sugar residue, or a metal, phosphonium or ammonium species; wherein at least one of X, Y and Z includes a moiety selected from cyclopropyl, C=A, C-AH and C—OR5; wherein R5 is alkyl or haloalkyl, and A is S, O or NR6, wherein R6 maybe H or 20 alkyl.

Abstract translation: 用作疫苗接种佐剂的式（I）化合物; 其中R是具有1至50个碳原子的任选取代的烷基，烯基，炔基，芳基，芳基烷基或烷芳基部分; R1是具有1至40个碳原子的任选取代的烷基，烯基，炔基，芳基，芳基烷基或烷芳基部分; R 2，R 3和R 4各自独立地选自具有1至40个碳原子的任选取代的亚烷基，亚烯基，亚炔基，亚芳基，芳基亚烷基或烷基亚芳基; X，Y和Z各自独立地选自任选取代的亚烷基，亚烯基，亚炔基，亚芳基，亚烷基亚芳基或亚环烷基，酮，酯，酰胺，酰亚胺，亚胺，硫醚，醚，硫酯，硫酮; 并且P选自氢，烷基，糖残基或金属，鏻或铵物质; 其中X，Y和Z中的至少一个包括选自环丙基，C = A，C-AH和C-OR 5的部分; 其中R 5是烷基或卤代烷基，A是S，O或NR 6，其中R 6可以是H或20烷基。

公开(公告)号：US20100190985A1

公开(公告)日：2010-07-29

申请号：US12637621

申请日：2009-12-14

Applicant: Shenggao Liu ,  Robert M. Carlson ,  Jeremy E. Dahl

Inventor： Shenggao Liu ,  Robert M. Carlson ,  Jeremy E. Dahl

IPC: C07C13/615 ,  C07D221/18 ,  C07D311/02 ,  C07C203/00 ,  C07C69/74 ,  C07C61/12 ,  C07C233/10 ,  C07C211/16 ,  C07C49/313 ,  C07C43/18 ,  C07C23/18

CPC classification number: C07C49/617 ,  C07C23/20 ,  C07C49/423 ,  C07C49/613 ,  C07C61/29 ,  C07D221/22 ,  C07D311/96 ,  C07D313/06 ,  C07D335/04 ,  C07D471/10 ,  C07F9/65683

Abstract: This invention is related to heteroatom containing diamondoids (i.e., “heterodiamondoids”) which are compounds having a diamondoid nucleus in which one or more of the diamondoid nucleus carbons has been substitutionally replaced with a noncarbon atom. These heteroatom substituents impart desirable properties to the diamondoid. In addition, the heterodiamondoids are functionalized affording compounds carrying one or more functional groups covalently pendant therefrom. This invention is further related to polymerizable functionalized heterodiamondoids. In a preferred aspect of this invention the diamondoid nuclei are triamantane and higher diamondoid nuclei. In another preferred aspect, the heteroatoms are selected to give rise to diamondoid materials which can serve as n- and p-type materials in electronic devices can serve as optically active materials.

Abstract translation: 本发明涉及含杂原子的类金刚石（即“异二亚类”），它们是具有金刚石核的化合物，其中一个或多个金刚石核碳原子被替代为非碳原子。 这些杂原子取代基赋予金刚石所需的性质。 此外，异二亚甲基二羧酸被官能化，从而提供携带一个或多个共价悬挂的官能团的化合物。 本发明进一步涉及可聚合的官能化异二聚体。 在本发明的优选方面，金刚石核是三金刚烷和更高的金刚石核。 在另一个优选的方面，选择这些杂原子以产生可用作电子器件中的n-型和p-型材料的类金刚石材料，可用作光学活性材料。

公开(公告)号：US20090288768A1

公开(公告)日：2009-11-26

申请号：US12421616

申请日：2009-04-09

Applicant: Stephen M. Dershem

Inventor： Stephen M. Dershem

IPC: B41J2/16 ,  C07C237/00 ,  C07C61/12 ,  C07F7/10 ,  C07F7/00 ,  C09J1/00 ,  C09J4/00

CPC classification number: C07C49/223 ,  C07C233/41 ,  C08F222/40 ,  C09J4/06

Abstract: The invention generally relates to di-cinnamyl compounds useful in a variety of adhesive applications. More specifically, the invention provides chain-extended bismaleimides and methods for generating them by reaction with di-cinnamyl compounds, including particular di-cinnamyl compounds disclosed herein. Invention di-cinnamyl compounds can also be used as co-monomers in a Diels-Alder type cure, and can act as a co-monomer in a thermoset composition with a maleimide monomer.

Abstract translation: 本发明一般涉及可用于各种粘合剂应用的二肉桂基化合物。 更具体地说，本发明提供了链延伸的双马来酰亚胺和通过与二肉桂基化合物反应生成它们的方法，包括本文公开的具体的二肉桂酰化合物。 本发明的二肉桂基化合物也可以以Diels-Alder型固化的形式用作共聚单体，并且可以作为马来酰亚胺单体的热固性组合物中的共聚单体。

公开(公告)号：US20060270870A1

公开(公告)日：2006-11-30

申请号：US11139624

申请日：2005-05-31

Applicant: Mathias Berner ,  Reijo Partanen ,  Auli Salakka ,  Pekka Somersalo

Inventor： Mathias Berner ,  Reijo Partanen ,  Auli Salakka ,  Pekka Somersalo

IPC: C07C61/12 ,  C07C61/28

CPC classification number: C07C51/285 ,  C07C2603/74 ,  C07C59/215

Abstract: The invention relates to a process for the preparation of 3-hydroxyadamantaneglyoxylic acid of the general formula (1) or a derivative or salt thereof. In the process, an 1-acyl derivative of adamantane having the formula (2): wherein R is a C1-C5 hydrocarbyl; CH2OH; CHO; COOH, is contacted with an oxidant under oxidizing conditions leading to the 3-hydroxyadamantaneglyoxylic acid (1) or the derivative or salt thereof.

Abstract translation: 本发明涉及制备通式（1）的3-羟基金刚烷乙醛酸或其衍生物或盐的方法。 在该方法中，具有式（2）的金刚烷的1-酰基衍生物：其中R是C 1 -C 5烃基; CH 2 OH; CHO; COOH在导致3-羟基金刚烷乙醛酸（1）或其衍生物或盐的氧化条件下与氧化剂接触。

公开(公告)号：US07034180B2

公开(公告)日：2006-04-25

申请号：US10362460

申请日：2001-09-07

Applicant: Masafumi Fukae ,  Yoshiro Hiraishi

Inventor： Masafumi Fukae ,  Yoshiro Hiraishi

IPC: C07C61/12

CPC classification number: C07C51/02 ,  C07C51/43 ,  C07C2602/28 ,  C07C59/46

Abstract: The invention aims at producing high-purity crystals of a hydroxycarboxylic acid represented by the following formula (1): in high yield. Provided are a method for crystallization of a compound (1) which comprises acidifying a mixture of a solution of an alkali salt of the compound (1) and an organic solvent, and a method for crystallization of compound (1) by mixing a solution of the compound (1) in a water-miscible good solvent with water, in which a slurry with a necessary suspension amount of the compound (1) for inhibiting oil formation and scaling is prepared in advance and then a main crystallization is carried out in the presence of said slurry.

Abstract translation: 本发明旨在以高产率制备由下式（1）表示的羟基羧酸的高纯度晶体。 提供化合物（1）的结晶方法，其包括酸化化合物（1）的碱金属盐和有机溶剂的溶液的混合物，以及通过将化合物（1）的溶液 将与化合物（1）在水混溶性好的溶剂中与水一起预先制备具有用于抑制油形成和结垢的化合物（1）所需悬浮液量的浆料，然后进行主结晶 所述浆料的存在。

公开(公告)号：US06930128B2

公开(公告)日：2005-08-16

申请号：US10617150

申请日：2003-07-10

Applicant: Robert John D'Amato ,  Moses Judah Folkman

Inventor： Robert John D'Amato ,  Moses Judah Folkman

IPC: A61K31/05 ,  A61K31/473 ,  A61K31/56 ,  A61K31/565 ,  A61K31/567 ,  A61K31/59 ,  C07J1/00 ,  C07J63/00 ,  A61K31/00 ,  C07C35/22 ,  C07C61/12 ,  C07C69/74 ,  C07C211/00

CPC classification number: A61K31/566 ,  A61K9/0019 ,  A61K9/0024 ,  A61K31/05 ,  A61K31/21 ,  A61K31/473 ,  A61K31/56 ,  A61K31/565 ,  A61K31/567 ,  A61K31/59 ,  C07J1/0059 ,  C07J1/007 ,  C07J1/0096 ,  C07J63/00 ,  Y10S514/912

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

公开(公告)号：US06927306B2

公开(公告)日：2005-08-09

申请号：US10329510

申请日：2002-12-27

Applicant: Fumiya Zaima

Inventor： Fumiya Zaima

IPC: C07D493/04 ,  C07B61/00 ,  C07C51/347 ,  C07C51/36 ,  C07C51/42 ,  C07C51/56 ,  C07C61/00 ,  C07C61/08 ,  C07C61/09 ,  C07C61/12 ,  C07C61/125 ,  C07C61/24 ,  C07D307/77

CPC classification number: C07C51/36 ,  C07D307/89 ,  C07C61/08

Abstract: Disclosed are processes for industrially advantageously producing at a good yield respectively, a hydrogenated aromatic polycarboxylic acid and an acid anhydride thereof each having a high purity. The present invention provides processes for producing a hydrogenated aromatic polycarboxylic acid by (1) hydrogenating an aromatic polycarboxylic acid at a hydrogen partial pressure of 1 MPa or more by a batch system in the presence of a catalyst containing rhodium and palladium in a proportion of 0.5 to 10 parts by weight per 100 parts by weight of the aromatic polycarboxylic acid and by (2) feeding an aromatic polycarboxylic acid to a filling bed of a catalyst containing rhodium and palladium at a WHSV of 1 to 100 h−1 to hydrogenate it at a hydrogen partial pressure of 1 MPa or more by a continuous flow system, and a process for producing a hydrogenated aromatic polycarboxylic anhydride by subjecting the hydrogenated aromatic polycarboxylic acid obtained by the processes described above to dehydration reaction with acetic anhydride of 0.64 to 5.7 times mole based on a carboxyl group of the hydrogenated aromatic polycarboxylic acid.

Abstract translation: 公开了工业上有利地以良好产率生产各自具有高纯度的氢化芳族多元羧酸和其酸酐的方法。 本发明提供了通过以下方式制备氢化芳族多元羧酸的方法：（1）在含有铑和钯的催化剂存在下，以0.5的比例，通过间歇系统在1MPa或更高的氢分压下氢化芳族多元羧酸 至10重量份/ 100重量份的芳族多元羧酸，并且通过（2）将芳族多元羧酸以1小时-100小时-1的WHSV加入含有铑和钯的催化剂的填充床中， 通过连续流动体系在1MPa以上的氢分压下氢化其氢化，以及通过使由上述方法得到的氢化芳香族多元羧酸与乙酸脱水反应来制造氢化芳香族多元羧酸酐的方法 酸酐为0.64〜5.7倍摩尔，基于氢化芳香族多元羧酸的羧基。

公开(公告)号：US4760175A

公开(公告)日：1988-07-26

申请号：US730967

申请日：1985-05-06

Applicant: Paul R. Zanno ,  Ronald E. Barnett ,  Glenn M. Roy

Inventor： Paul R. Zanno ,  Ronald E. Barnett ,  Glenn M. Roy

IPC: A23L27/30 ,  C07C61/12

CPC classification number: A23L27/30

Abstract: This invention relates to novel sweeteners of the formula: ##STR1## wherein A is hydroxyalkyl containing 1-3 carbon atomsA' is hydrogen or alkyl containing 1-3 carbon atoms;Y is --(CHR.sub.2).sub.n --R.sub.1 or --CHR.sub.3 R.sub.4 ;R.sub.1 is cycloalkyl, cycloalkenyl, bicycloalkyl or bicycloalkenyl containing up to 7 ring carbon atoms and up to a total of 12 carbon atoms;R.sub.2 is H or alkyl containing 1-4 carbon atoms;R.sub.3 and R.sub.4 are each cycloalkyl containing 3-4 ring carbon atoms;n=0 or 1; andm=0 or 1;and food-acceptable salts thereof.

Abstract translation: 本发明涉及下式的新型甜味剂：其中A是含1-3个碳原子的羟烷基，A'是氢或含有1-3个碳原子的烷基; Y是 - （CHR 2）n -R 1或-CHR 3 R 4; R 1是含有至多7个环碳原子并且总共12个碳原子的环烷基，环烯基，双环烷基或双环烯基; R2是H或含1-4个碳原子的烷基; R3和R4分别是含有3-4个环碳原子的环烷基; n = 0或1; m = 0或1; 及其食品可接受的盐。