公开(公告)号：US20190071379A1

公开(公告)日：2019-03-07

申请号：US16082737

申请日：2017-03-07

Applicant: HANMI PHARM. CO., LTD.

Inventor： Dae Jin KIM ,  Jong Soo LEE ,  Sung Min BAE ,  Se Chang KWON

IPC: C07C47/198 ,  C07D213/71 ,  A61K47/60 ,  C07C323/12 ,  C07C233/18 ,  C07C323/22 ,  A61K39/395

Abstract: The present invention relates to polyethylene glycol derivatives and use thereof.

公开(公告)号：US20170275230A1

公开(公告)日：2017-09-28

申请号：US15620493

申请日：2017-06-12

Applicant: P2 SCIENCE, INC.

Inventor： Patrick FOLEY ,  Yonghua YANG ,  Robert BEDOUKIAN ,  Thomas KILLINGER

IPC: C07C67/08 ,  C07C45/40 ,  C07C45/85 ,  C07C51/34 ,  C07C69/533 ,  C07C69/708 ,  C11B9/00 ,  C07C51/285 ,  C07C47/198 ,  A23L27/20 ,  C07C59/125

CPC classification number: C07C67/08 ,  A23L27/202 ,  A23V2002/00 ,  C07C45/40 ,  C07C45/85 ,  C07C51/285 ,  C07C51/34 ,  C07C59/125 ,  C07C69/708 ,  C11B9/0019 ,  C07C47/198 ,  C07C69/533

Abstract: The invention relates to terpene-derived acids and esters thereof as well as to processes for synthesizing them.

公开(公告)号：US09756872B2

公开(公告)日：2017-09-12

申请号：US14714010

申请日：2015-05-15

Applicant: TAKASAGO INTERNATIONAL CORPORATION

Inventor： Frank Derosa ,  Michael E. Lankin ,  Andrew T. Lupo

IPC: C11B9/00 ,  A61Q13/00 ,  A23L1/226 ,  A61K8/33 ,  A61K8/37 ,  A61K8/39 ,  A61Q5/02 ,  A61Q11/00 ,  A61Q19/10 ,  A61K47/08 ,  A61K47/14 ,  C07C69/003 ,  C07C69/708 ,  C07C69/96 ,  C07C43/11 ,  C07C43/15 ,  C07C47/198 ,  C11D3/50 ,  A23L2/56 ,  C11D3/20 ,  A23L27/20

CPC classification number: A23L27/2028 ,  A23L2/56 ,  A23L27/20 ,  A23V2002/00 ,  A61K8/33 ,  A61K8/37 ,  A61K8/39 ,  A61K47/08 ,  A61K47/14 ,  A61Q5/02 ,  A61Q11/00 ,  A61Q13/00 ,  A61Q19/10 ,  C07C43/11 ,  C07C43/15 ,  C07C47/198 ,  C07C69/003 ,  C07C69/708 ,  C07C69/96 ,  C11B9/0015 ,  C11B9/0019 ,  C11D3/2068 ,  C11D3/2072 ,  C11D3/2093 ,  C11D3/50

Abstract: The present invention is related to substituted butanol derivatives of the formula: wherein R is an unsubstituted or substituted C1-6 straight chain alkyl, an unsubstituted or substituted C3-6 branched chain alkyl, an unsubstituted or substituted C3-6 straight chain alkenyl, an unsubstituted or substituted C3-6 branched chain alkenyl, an unsubstituted or substituted C3-6 cycloalkyl, an unsubstituted or substituted C1-6 alkoxy, nitrile, halo, amino, an unsubstituted or substituted C1-6 alkylamino, an unsubstituted or substituted C1-6 dialkylamino, carboxy-C1-6 alkylamino, carboxy-C1-6 dialkylamino, an unsubstituted or substituted acetoxy, carboxy, an unsubstituted or substituted carboxyethyl, an unsubstituted or substituted C1-6 alkylcarbonyl, an unsubstituted or substituted C1-6 alkylcarboxy, an unsubstituted or substituted C1-6 alkylthio, an unsubstituted or substituted C1-6 alkyloxy, carboxamido, an unsubstituted or substituted C1-6 alkylcarboxamido or an unsubstituted or substituted C1-6 dialkylcarboxamido. Such compounds are useful in flavor or flavor compositions.

公开(公告)号：US09327034B2

公开(公告)日：2016-05-03

申请号：US14363884

申请日：2012-12-13

Applicant: University of Tsukuba

Inventor： Yukio Nagasaki ,  Yutaka Ikeda ,  Hiromichi Kawasaki ,  Jinya Katamachi

IPC: A61K8/72 ,  A61K47/48 ,  C08G65/32 ,  C07C47/198 ,  C07D211/40 ,  C08G65/324 ,  C08G65/333 ,  C08G65/338 ,  A61K8/86 ,  A61K8/84

CPC classification number: A61K47/48215 ,  A61K47/50 ,  A61K47/51 ,  A61K47/56 ,  A61K47/59 ,  A61K47/60 ,  C07C47/198 ,  C07D211/40 ,  C08G65/2609 ,  C08G65/321 ,  C08G65/322 ,  C08G65/323 ,  C08G65/324 ,  C08G65/33303 ,  C08G65/338 ,  C08G2650/30 ,  C08L2203/02

Abstract: The present invention allows formation of covalent bonds in a bioactive compound having at least one amino group so as to efficiently provide the compound modified with PEG. The present invention thus provides a functionalized polyethylene glycol having a structure that allows reaction of two aldehyde groups with one amino group to form two covalent bonds.

Abstract translation: 本发明允许在具有至少一个氨基的生物活性化合物中形成共价键，以有效提供用PEG修饰的化合物。 因此，本发明提供具有允许两个醛基与一个氨基反应形成两个共价键的结构的官能化聚乙二醇。

公开(公告)号：US6043250A

公开(公告)日：2000-03-28

申请号：US472296

申请日：1995-06-07

Applicant: J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar ,  Glenn C. Rice

Inventor： J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar ,  Glenn C. Rice

IPC: C07D239/54 ,  A61K31/42 ,  A61K31/421 ,  A61K31/496 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P9/10 ,  A61P9/14 ,  A61P11/16 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/04 ,  A61P37/08 ,  A61P43/00 ,  C07C47/198 ,  C07C47/277 ,  C07C49/175 ,  C07C49/255 ,  C07C57/46 ,  C07C59/64 ,  C07C65/21 ,  C07C69/06 ,  C07C69/14 ,  C07C69/24 ,  C07C69/608 ,  C07C69/612 ,  C07C225/06 ,  C07C233/01 ,  C07D239/56 ,  C07D241/18 ,  C07D263/30 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D487/04 ,  C07D513/04 ,  C07D521/00 ,  A61K3/52

CPC classification number: C07D487/04 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D513/04

Abstract: Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C(.sub.1-10) alkyl, C(.sub.2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C(.sub.1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyalkyl; --A(R.sub.5).sub.m, A being N or 0, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.

Abstract translation: 具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。 核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中： 或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的 或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟烷基; -A（R5）m，A为N或0，m为一个或两个，R5为氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基 或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。 这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

公开(公告)号：US5807862A

公开(公告)日：1998-09-15

申请号：US478112

申请日：1995-06-07

Applicant: J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar

Inventor： J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar

IPC: C07D239/54 ,  A61K31/42 ,  A61K31/421 ,  A61K31/496 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P9/10 ,  A61P9/14 ,  A61P11/16 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/04 ,  A61P37/08 ,  A61P43/00 ,  C07C47/198 ,  C07C47/277 ,  C07C49/175 ,  C07C49/255 ,  C07C57/46 ,  C07C59/64 ,  C07C65/21 ,  C07C69/06 ,  C07C69/14 ,  C07C69/24 ,  C07C69/608 ,  C07C69/612 ,  C07C225/06 ,  C07C233/01 ,  C07D239/56 ,  C07D241/18 ,  C07D263/30 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D487/04 ,  C07D513/04 ,  C07D521/00

CPC classification number: C07D487/04 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D513/04

Abstract: Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula: CORE MOIETY--(R).sub.j wherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyalkyl; --A(R.sub.5).sub.m, A being N or O, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.

Abstract translation: 具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：其中j是1至3的整数。 核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I： I其中：一个或两个p是整数一个，否则p是两个; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的 或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟烷基; -A（R5）m，A是N或O，m是一个或两个，R5是氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基 或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。 这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

公开(公告)号：US4986885A

公开(公告)日：1991-01-22

申请号：US329942

申请日：1989-03-29

Applicant: Robert K. Driscoll ,  Ingo Leupold ,  Karl-Heinz Schonwalder

Inventor： Robert K. Driscoll ,  Ingo Leupold ,  Karl-Heinz Schonwalder

IPC: C07C27/28 ,  C07C27/00 ,  C07C29/80 ,  C07C31/12 ,  C07C45/00 ,  C07C45/82 ,  C07C45/84 ,  C07C47/198 ,  C07C67/00

CPC classification number: C07C45/82 ,  C07C29/80 ,  C07C45/84

Abstract: A process for the separation of butanol and butoxyacetaldehyde which involves subjecting a composition which contains these two compounds to a distillation at a pressure of at most 660 mbar. According to a special embodiment the composition to be distilled contains as essential components water, butanol, butoxyacetaldehyde, butylglycol and, if desired, also butyraldehyde.

Abstract translation: 一种用于分离丁醇和丁氧基乙醛的方法，其包括使含有这两种化合物的组合物在至多660毫巴的压力下进行蒸馏。 根据一个特殊的实施方案，待蒸馏的组合物含有水，丁醇，丁氧基乙醛，丁二醇以及如果需要也含有丁醛作为必要组分。

公开(公告)号：US4960946A

公开(公告)日：1990-10-02

申请号：US421266

申请日：1989-10-13

Applicant: Robert Eilerman ,  Philip Christenson ,  John Yurecko, Jr. ,  Thomas Zebovitz

Inventor： Robert Eilerman ,  Philip Christenson ,  John Yurecko, Jr. ,  Thomas Zebovitz

IPC: C07C43/13 ,  C07C43/15 ,  C07C43/178 ,  C07C43/315 ,  C07C45/40 ,  C07C45/49 ,  C07C45/51 ,  C07C45/62 ,  C07C45/67 ,  C07C45/72 ,  C07C47/198 ,  C07C47/21 ,  C07C49/517 ,  C07C49/753 ,  C11B9/00

CPC classification number: C11B9/0034 ,  C07C43/13 ,  C07C43/15 ,  C07C43/1781 ,  C07C43/315 ,  C07C45/40 ,  C07C45/49 ,  C07C45/513 ,  C07C45/515 ,  C07C45/62 ,  C07C45/673 ,  C07C45/72 ,  C07C47/198 ,  C07C47/21 ,  C07C49/517 ,  C07C49/753 ,  C07C2101/14 ,  C07C2101/16

Abstract: The present invention relates to novel substituted cyclohexanol compounds possessing a sandalwood aroma which are useful as fragrance materials. The invention also provides methods for synthesis thereof through a novel aldehyde intermediate. The compounds of the invention have the formula: ##STR1## wherein A is ##STR2## and wherein R.sub.1 is methyl or ethyl, R.sub.2 -R.sub.7 are independently hydrogen or methyl with the proviso that a maximum of two of the substituents R.sub.2 -R.sub.7 are methyl, and R.sub.8 is hydrogen, lower alkyl (C.sub.1 to C.sub.5) or acyl. The invention also provides fragrance compositions which utilize the compounds of the invention to impart a sandalwood aroma to perfume compositions, colognes and perfumed articles.

Abstract translation: 本发明涉及具有檀香香味的新型取代的环己醇化合物，其可用作香料。 本发明还提供了通过新的醛中间体合成它们的方法。 本发明的化合物具有下式：其中A为，其中R1为甲基或乙基，R2-R7独立地为氢或甲基，条件是最多两个取代基R2-R7为甲基 ，R8为氢，低级烷基（C1〜C5）或酰基。 本发明还提供了使用本发明化合物赋予香薰组合物，古龙水和香料制品的檀香香气的香料组合物。

公开(公告)号：US4691048A

公开(公告)日：1987-09-01

申请号：US732487

申请日：1985-05-10

Applicant: Francois Hugues ,  Dominique Commereuc ,  Yves Chauvin

Inventor： Francois Hugues ,  Dominique Commereuc ,  Yves Chauvin

IPC: C07C43/13 ,  B01J31/00 ,  C07B61/00 ,  C07C27/00 ,  C07C41/00 ,  C07C41/30 ,  C07C45/00 ,  C07C45/49 ,  C07C47/198 ,  C07C67/00 ,  C07C69/14 ,  C07C67/24

CPC classification number: C07C41/30 ,  C07C45/49

Abstract: The invention concerns a process for reducing carbonylation of an aldehyde wherein the aldehyde is used as hemiacetalester, the reaction being conducted in the presence of a catalyst consisting of a cobalt carbonyl complex.The hemiacetal-ester may be formed in situ by reacting an acetal with an anhydride of acid.The process preferentially yields alkylene-glycol mono-esters, free of esterified, for a ratio H.sub.2 /CO ranging from 1:1 to 3:1 and preferentially 2-alkoxy aldehydes, for a ratio H.sub.2 /CO ranging from 0.1:1 to 0.5:1.

Abstract translation: 本发明涉及一种还原醛的羰基化方法，其中醛用作半缩醛，该反应是在由羰基钴络合物组成的催化剂存在下进行的。 半缩醛酯可以通过使缩醛与酸酐反应而原位形成。 该方法优选产生不含酯化的亚烷基二醇单酯，比例为1:1至3:1的H 2 / CO 2，优选为2-烷氧基醛，比例为H 2 / CO为0.1:1至0.5:1 ：1。

公开(公告)号：US4608443A

公开(公告)日：1986-08-26

申请号：US694372

申请日：1985-01-24

Applicant: Juan Andrade ,  Gunter Prescher ,  Marc Samson

Inventor： Juan Andrade ,  Gunter Prescher ,  Marc Samson

IPC: C07C45/42 ,  B01J31/00 ,  B01J31/24 ,  C07B61/00 ,  C07C41/56 ,  C07C45/00 ,  C07C45/49 ,  C07C45/50 ,  C07C45/51 ,  C07C47/12 ,  C07C47/198 ,  C07C67/00

CPC classification number: C07C45/49 ,  C07C41/56 ,  C07C45/515

Abstract: The preparation of 1,4-butandial (succindialdehyde) is obtained using acrolein. The acrolein is first converted with an alkanol into 3,3-dialkoxy-1-propene and this is then hydroformylated in the presence of hydridotristriphenylphosphine-rhodiumcarbonyl mixed with triphenylphosphine or triphenylphosphite as the catalyst. The thereby obtained 4,4-dialkoxy-butanal is removed from the hydroformylation product by means of distillation and is then hydrolyzed to 1,4-butandial.

Abstract translation: 使用丙烯醛获得1,4-丁二醛（琥珀醛）的制备。 丙烯醛首先用链烷醇转化为3,3-二烷氧基-1-丙烯，然后在与三苯基膦或亚磷酸三苯酯作为催化剂混合的氢三溴三苯基膦 - 铑羰基存在下加氢甲酰化。 由此得到的4,4-二烷氧基 - 丁醛通过蒸馏从加氢甲酰化产物中除去，然后水解成1,4-丁二醛。