公开(公告)号：US20080275256A1

公开(公告)日：2008-11-06

申请号：US11722121

申请日：2005-12-20

Applicant: Fridtjof Schroder

Inventor： Fridtjof Schroder

IPC: C07D313/00 ,  C07C35/06 ,  C07C35/04 ,  C07C13/465 ,  C07C35/21

CPC classification number: C07C29/36 ,  C07C2/861 ,  C07C29/32 ,  C07C41/16 ,  C07C41/30 ,  C07C67/347 ,  C07C253/30 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2602/18 ,  C07D313/00 ,  C07C13/32 ,  C07C69/608 ,  C07C255/31 ,  C07C43/23 ,  C07C43/115 ,  C07C43/162 ,  C07C31/137 ,  C07C33/05 ,  C07C33/12 ,  C07C31/1333

Abstract: A process for the cyclopropanation of a substituted alkene, comprising the reaction of the alkene with a carbenoide, generated from dibromomethane and a tri-(C2-C8)-alkyl aluminium compound, in the presence of a catalytic amount of a metal compound selected from the group consisting of Lewis acids, metallocenes and metal carbonyl complexes. The process advantageously uses transition metal compounds as catalysts and the dibromomethane can be recovered.The process is especially useful for the preparation of ingredients for the flavour and fragrance industry.

Abstract translation: 一种取代烯烃的环丙烷化方法，其包括由二溴甲烷和三（C 1 -C 6）-C 8 - 烷基取代的烯烃与烯烃反应， 铝化合物，在催化量的选自路易斯酸，金属茂和金属羰基络合物的金属化合物存在下进行。 该方法有利地使用过渡金属化合物作为催化剂，并且可以回收二溴甲烷。 该方法对于制备风味和香料工业的成分特别有用。

公开(公告)号：US07368613B2

公开(公告)日：2008-05-06

申请号：US11422917

申请日：2006-06-08

Applicant: Marcus Eh

Inventor： Marcus Eh

IPC: C07C27/10 ,  C07C29/10 ,  C07C35/00 ,  C07C35/21

CPC classification number: C07C33/14 ,  C07C45/69 ,  C07C47/44 ,  C07C49/553 ,  C07D303/04 ,  C11B9/0034

Abstract: A compound of formula (Ia) or (Ib), wherein in each of formulae (Ia) and (Ib) R1 and R2, independently of one another, are H or CH3, and the use thereof as a sandalwood fragrance.

Abstract translation: 式（Ia）或（Ib）的化合物，其中在式（Ia）和（Ib）的每一个中，R 1和R 2彼此独立地为 H或CH 3 3，以及其作为檀香香料的用途。

公开(公告)号：US5801164A

公开(公告)日：1998-09-01

申请号：US480310

申请日：1995-06-07

Applicant: Joyce C. Knutson ,  Charles W. Bishop ,  Robert M. Moriarty

Inventor： Joyce C. Knutson ,  Charles W. Bishop ,  Robert M. Moriarty

IPC: A61K8/60 ,  A61K8/67 ,  A61K31/59 ,  A61Q19/00 ,  C07C35/21 ,  C07C401/00

CPC classification number: A61K31/592 ,  A61K31/59 ,  A61K8/606 ,  A61K8/67 ,  A61Q19/00 ,  C07C35/21 ,  C07C401/00

Abstract: Methods of treating osteoporosis prophylactically or therapeutically are disclosed. The method of treating osteoporosis includes administering to a patient suffering therefrom an effective amount to treat the osteoporosis of novel 1.alpha.-hydroxyvitamin D.sub.4 and novel analogues 1,25-dihydroxyvitamin D.sub.4 and 1,24-dihydroxyvitamin D.sub.4, the aforementioned compounds having lower toxicity as measured by an LD.sub.50 test in rats when compared to a corresponding vitamin D.sub.3 compound. The method of administering the compound is substantially without occurrence of hypercalcemia.

Abstract translation: 公开了预防或治疗骨质疏松症的方法。 治疗骨质疏松症的方法包括向患有其的患者施用有效量的治疗新型1α-羟基维生素D4和新型类似物1,25-二羟基维生素D4和1,24-二羟基维生素D4的骨质疏松症，上述具有较低毒性的化合物 与相应的维生素D3化合物相比，通过LD50测试在大鼠中测量。 施用化合物的方法基本上不发生高钙血症。

公开(公告)号：US5763428A

公开(公告)日：1998-06-09

申请号：US484342

申请日：1995-06-07

Applicant: Joyce C. Knutson ,  Charles W. Bishop

Inventor： Joyce C. Knutson ,  Charles W. Bishop

IPC: A61K31/59 ,  A61K8/60 ,  A61K8/67 ,  A61P17/00 ,  A61P35/00 ,  A61Q19/00 ,  C07C35/21 ,  C07C401/00 ,  C07J9/00

CPC classification number: A61K8/606 ,  A61K31/59 ,  A61K31/592 ,  A61K8/67 ,  A61Q19/00 ,  C07C35/21 ,  C07C401/00 ,  C07J9/00

Abstract: The disclosure is of methods of treating various skin disorders, including skin cancer, with compounds of novel 1.alpha.-hydroxy vitamin D.sub.4 and novel analogues, thereof, including 1,25 dihydroxy vitamin D.sub.4 and 1,24 dihydroxy vitamin D.sub.4. Novel 1.alpha.-hydroxy vitamin D.sub.4 compounds and compounds of novel analogues suitable for use in the treatment of such disorders are also disclosed herein.

Abstract translation: 本公开是用新的1α-羟基维生素D4及其新型类似物，包括1,25二羟基维生素D4和1,24二羟基维生素D4的化合物治疗各种皮肤疾病（包括皮肤癌）的方法。 本文还公开了新的1α-羟基维生素D 4化合物和适合用于治疗这种病症的新型类似物的化合物。

公开(公告)号：US5709911A

公开(公告)日：1998-01-20

申请号：US804753

申请日：1997-02-21

Applicant: Noriaki Onishi ,  Nobuaki Yamada ,  Masahiko Yoshida ,  Hoyo Mizobe ,  Kenji Suzuki

Inventor： Noriaki Onishi ,  Nobuaki Yamada ,  Masahiko Yoshida ,  Hoyo Mizobe ,  Kenji Suzuki

IPC: G02F1/13 ,  C07C33/50 ,  C07C35/21 ,  C07C35/50 ,  C07C69/54 ,  C07C69/653 ,  C09K19/30 ,  C09K19/38

CPC classification number: C09K19/3003 ,  C09K19/3852 ,  C09K2019/0444 ,  C09K2019/0448 ,  Y10T428/1005

Abstract: A polymerizable compound represented by Formula (I): ##STR1## where X is a hydrogen atom or a methyl group; Y and Z are independently a hydrogen atom or a fluorine atom; l is an integer of 0 to 14; m and n are independently an integer of 0 or 1; R is represented by Formula (II), (III), or (IV); and when m=1, l.gtoreq.1; ##STR2##

Abstract translation: 由式（I）表示的可聚合化合物：其中X是氢原子或甲基; Y和Z独立地为氢原子或氟原子; l为0〜14的整数; m和n独立地为0或1的整数; R由式（II），（III）或（IV）表示; 当m = 1时，l> / = 1; （二）（III）（IV）

公开(公告)号：US5488120A

公开(公告)日：1996-01-30

申请号：US296084

申请日：1994-08-24

Applicant: Joyce C. Knutson ,  Charles W. Bishop ,  Robert M. Moriarty

Inventor： Joyce C. Knutson ,  Charles W. Bishop ,  Robert M. Moriarty

IPC: A61K31/59 ,  C07C35/21 ,  C07C401/00

CPC classification number: A61K31/592 ,  C07C35/21 ,  C07C401/00

Abstract: Novel 1.alpha.-hydroxy Vitamin D.sub.4 and novel analogues, 1,25 dihydroxy Vitamin D.sub.4 and 1,24 dihydroxy Vitamin D.sub.4 which are useful for the treatment of disorders of calcium metabolism. Preparation of the novel 1.alpha.-hydroxy Vitamin D.sub.4 starts from ergosterol which is converted in six steps to 22,23-dihydroergosterol. 22,23-dihydroergosterol was irradiated to yield Vitamin D.sub.4 which was converted in four steps to 1.alpha.-hydroxy Vitamin D.sub.4 using a cyclovitamin procedure which produced the novel intermediates, Vitamin D.sub.4 tosylate, 3,5 cyclovitamin D.sub.4 and 1.alpha.-hydroxy cyclovitamin D.sub.4. 1,25 dihydroxy Vitamin D.sub.4 and 1,24 dihydroxy Vitamin D.sub.4 are isolated as biological products of the metabolism of novel 1.alpha.-hydroxy Vitamin D.sub.4 using cultured human liver cells.

Abstract translation: 新型1α-羟基维生素D4和新型类似物，1,25二羟基维生素D4和1,24二羟基维生素D4，其可用于治疗钙代谢紊乱。 新型1α-羟基维生素D4的制备从麦角甾醇开始，其以六步转化为22,23-二氢麦角甾醇。 22,23-二氢麦角甾醇被照射以产生维生素D4，其使用产生新的中间体维生素D4甲苯磺酸盐，3,5环维生素D4和1α-羟基环维生素D4的环维生素程序将其四步转化为1α-羟基维生素D4 。 使用培养的人肝细胞，分离出1,25二羟基维生素D4和1,24二羟基维生素D4作为新型1α-羟基维生素D4代谢的生物学产物。

公开(公告)号：US5420343A

公开(公告)日：1995-05-30

申请号：US299173

申请日：1994-08-31

Applicant: Francis J. Koszyk ,  Richard M. Weier

Inventor： Francis J. Koszyk ,  Richard M. Weier

IPC: C07C17/12 ,  C07C17/16 ,  C07C22/04 ,  C07C25/02 ,  C07C33/26 ,  C07C35/21 ,  C07C45/44 ,  C07C45/67 ,  C07C47/228 ,  C07C49/657 ,  C07C59/72 ,  C07C69/757 ,  C07C255/33 ,  C07C309/73 ,  C07C323/52 ,  C07D307/20 ,  C07D493/04 ,  C07C59/40

CPC classification number: C07D493/04 ,  C07C17/12 ,  C07C17/16 ,  C07C22/04 ,  C07C25/02 ,  C07C255/33 ,  C07C309/73 ,  C07C323/52 ,  C07C33/26 ,  C07C35/21 ,  C07C45/44 ,  C07C45/676 ,  C07C47/228 ,  C07C49/657 ,  C07C59/72 ,  C07C69/757 ,  C07D307/20

Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: R.sup.1 and R.sup.2 are each alkyl;n is an integer of from 1 to 4;x is oxygen or --(CH.sub.2).sub.m --;m is an integer of from 1 to 3;y is oxygen or sulfur; andp is an integer of from 1 to 4.These compounds are inhibitors of COX-I and/or COX-II, and are useful for the treatment of inflammation-associated disorders.The present invention also provides pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for treating inflammation-associated disorders in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract translation: 本发明提供下式的化合物：其中：R 1和R 2各自为烷基; n为1〜4的整数， x是氧或 - （CH 2）m - ; m为1〜3的整数， y是氧或硫; 并且p是1至4的整数。这些化合物是COX-1和/或COX-II的抑制剂，并且可用于治疗炎症相关疾病。 本发明还提供药物组合物，其包含治疗有效量的式I化合物与药学上可接受的载体的组合，和用于治疗动物中炎症相关疾病的方法，包括给予治疗有效量的化合物 的I型动物。

公开(公告)号：US5101061A

公开(公告)日：1992-03-31

申请号：US520459

申请日：1990-05-08

Applicant: Bernd Wolf ,  Hans Theobald ,  Norbert Goetz

Inventor： Bernd Wolf ,  Hans Theobald ,  Norbert Goetz

IPC: C07C29/136 ,  C07C25/02 ,  C07C25/18 ,  C07C25/22 ,  C07C25/24 ,  C07C27/00 ,  C07C29/16 ,  C07C33/20 ,  C07C33/22 ,  C07C33/30 ,  C07C33/34 ,  C07C33/46 ,  C07C33/50 ,  C07C35/21 ,  C07C35/50 ,  C07C45/00 ,  C07C45/44 ,  C07C47/542 ,  C07C47/546 ,  C07C47/548 ,  C07C47/55 ,  C07C67/00 ,  C07C255/50

CPC classification number: C07C33/34 ,  C07C25/02 ,  C07C25/18 ,  C07C25/22 ,  C07C25/24 ,  C07C255/50 ,  C07C33/20 ,  C07C33/30 ,  C07C33/46 ,  C07C33/50 ,  C07C45/44 ,  C07C47/542 ,  C07C47/546 ,  C07C47/548 ,  C07C47/55 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/10 ,  C07C2101/14 ,  C07C2101/16 ,  C07C2101/18 ,  C07C2102/42

Abstract: Novel benzonitriles, benzaldehydes and benzyl alcohols of the formula I ##STR1## where R.sup.1 is methyl or ethyl, R.sup.2 is alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, bicycloalkenyl, or C.sub.1 -C.sub.5 -alkyl-substituted cycloalkyl, cycloalkenyl, bicycloalkyl or bicycloalkenyl, X is hydrogen, chlorine or fluorine and Z is --CN, CHO or ##STR2## where R.sup.3 is hydrogen, cyano, C.sub.2 -C.sub.4 -alkynyl, C.sub.2 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkyl, with the proviso that R.sup.2 is not --CH.sub.2 -CH.dbd.CH--B when B is hydrogen, alkyl or alkenyl and at the same time R.sup.1 is methyl and Z is ##STR3## and with the proviso that R.sup.2 is not methyl or ethyl when R.sup.1 is methyl and at the same time Z is ##STR4## and further more with the proviso that R.sup.2 is not methyl when R.sup.1 is methyl or ethyl and at the same time Z is --CN or --CHO.

公开(公告)号：US5075513A

公开(公告)日：1991-12-24

申请号：US397720

申请日：1989-08-23

Applicant: Paul H. Briner

Inventor： Paul H. Briner

IPC: A01N43/20 ,  C07C29/10 ,  C07C35/21 ,  C07C35/50 ,  C07C41/00 ,  C07C43/23 ,  C07C45/00 ,  C07C45/63 ,  C07C45/67 ,  C07C45/68 ,  C07C45/70 ,  C07C45/71 ,  C07C49/83 ,  C07C65/17 ,  C07C67/00 ,  C07C67/317 ,  C07C67/343 ,  C07C69/76 ,  C07C201/00 ,  C07C205/13 ,  C07C205/21 ,  C07C205/26 ,  C07C215/70 ,  C07C235/42 ,  C07C303/28 ,  C07C309/65 ,  C07C309/68 ,  C07C309/72 ,  C07C309/75 ,  C07C317/22 ,  C07C323/19 ,  C07D303/14

CPC classification number: C07D303/14 ,  A01N43/20 ,  C07C309/68 ,  C07C309/75 ,  C07C35/21 ,  C07C45/63 ,  C07C45/673 ,  C07C45/68 ,  C07C45/71

Abstract: The invention provides cyclopentane derivatives of the general formula ##STR1## in which n represents an integer from 0 to 5, each R represents a halogen atom, nitro, cyano, hydroxyl, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkythio, alkysulphinyl, alkylsulphonyl, carbamoyl, alkylamindo, cycloalkyl or phenyl group, R.sup.1 and R.sup.2 independently represent a hydrogen atom or an alkyl group, and R.sup.3 represents an optionally substituted alkyl or aryl group; and a process for their preparation. Compounds of formulae I, II and IV are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives. Also, certain compounds of formula IV are themselves fungicidally active.

公开(公告)号：US4943384A

公开(公告)日：1990-07-24

申请号：US2596

申请日：1986-11-21

Applicant: Wolfgang Sucrow ,  Herbert Wolter ,  Rudolf Eidenschink

Inventor： Wolfgang Sucrow ,  Herbert Wolter ,  Rudolf Eidenschink

IPC: G02F1/13 ,  C07C1/00 ,  C07C13/28 ,  C07C17/00 ,  C07C25/18 ,  C07C27/00 ,  C07C35/21 ,  C07C41/00 ,  C07C43/18 ,  C07C43/184 ,  C07C45/00 ,  C07C49/00 ,  C07C49/417 ,  C07C49/613 ,  C07C49/657 ,  C07C49/753 ,  C07C67/00 ,  C07C69/013 ,  C07C69/03 ,  C07C69/14 ,  C07C69/24 ,  C07C69/75 ,  C07C69/757 ,  C07C201/00 ,  C07C209/00 ,  C07C253/00 ,  C07C255/45 ,  C07C255/56 ,  C07D239/26 ,  C07D319/06 ,  C09K19/30 ,  C09K19/34 ,  C09K19/42 ,  C09K19/46

CPC classification number: C07D239/26 ,  C07C13/28 ,  C07C255/00 ,  C07C35/21 ,  C07C43/184 ,  C07C49/417 ,  C07C49/613 ,  C07C49/657 ,  C07C49/753 ,  C07C69/14 ,  C07C69/24 ,  C07C69/757 ,  C07D319/06 ,  C09K19/3001 ,  C09K19/3003 ,  C09K19/3068 ,  C09K19/3098 ,  C09K19/3402 ,  C09K19/3441 ,  C09K2019/3422

Abstract: Cyclohexane derivatives of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 IwhereinR.sup.1 and R.sup.2 are each H or an alkyl group which has 1-10 C atoms and in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or --CO-groups, and/or --CO--O-- groups and/or --CH.dbd.CH-- groups, or are F, Cl, Br, CN or R.sup.3 --A.sup.3 --Z.sup.2 --,A.sup.1 is --A--, A.sup.4 --Z.sup.o --A-- or --A--Z.sup.o --A.sup.4 --,A is a trans-1,4-cyclohexylene or 1,4-cyclohexenylene group which is unsubstituted or is monosubstituted or polysubstituted in the 2-, 3-, 5- and/or 6-position by F and/or Cl and/or Br and/or CN and/or an alkyl group or a fluorinated alkyl group each of which has 1-10 C atoms and in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or --CO-- groups and/or --CO--O-- groups, which trans-1,4-cyclohexylene or 1,4-cyclohexenylene group can optionally also be substituted in the 1-position and/or 4-position and one or two CH.sub.2 groups therein are replaced by --CO--, orR.sup.1 --A.sup.1 -- is a cyclohexyl group which is substituted in the 3-position by an alkyl group which has 1-10 C atoms and in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or --CO-- groups and/or --CO--O-- groups and/or --CH.dbd.CH-- groups, or is substituted in the 3-position by CN, in which cyclohexyl group one or two nonadjacent CH.sub.2 groups can also be replaced by --O-- or --CO--, A.sup.2, A.sup.3 and A.sup.4 are each 1,4-phenylene which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups and/or CN groups and in which one or two CH groups can also be replaced by N atoms and/or NO, or are 1,4-cyclohexylene wherein one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms, or are 1,3-dithiane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo(2,2,2)-octylene, decahydronaphthalene-2,6-diyl or 1,2,3,4-tetrahydronaphthalene-2,6-diyl groups or are --A--, Z.sup.o, Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, -- CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 CHCN--, --CHCNCH.sub.2 -- or a single bond, andR.sup.3 is H or an alkyl group which has 1-10 C atoms and in which one or two non-adjacent CH.sub.2 groups can also be replaced by 0 atoms and/or --CO-- groups and/or --CO--O-- groups and/or --CH.dbd.CH-- groups, or is F, Cl, Br or CN, are suitable for use as components of liquid-crystal phases.