公开(公告)号：US06924388B2

公开(公告)日：2005-08-02

申请号：US10630872

申请日：2003-07-31

Applicant: Jean-Michel Bernardon

Inventor： Jean-Michel Bernardon

IPC: C07D295/08 ,  A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/195 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P27/00 ,  A61P27/02 ,  A61P29/00 ,  C07C43/253 ,  C07C47/575 ,  C07C57/42 ,  C07C59/48 ,  C07C59/56 ,  C07C59/60 ,  C07C59/64 ,  C07C59/72 ,  C07C59/90 ,  C07C69/618 ,  C07C235/16 ,  C07D211/34 ,  C07D295/10 ,  C07C69/76

CPC classification number: C07C59/72 ,  C07C59/64

Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds having the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): and Ar2, X1, R1, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in the specification.

Abstract translation: 具有结构式（I）的新型药物/化妆活性双环芳族化合物：其中Ar 1是具有结构式（a） - （c）中的一个的基团：和Ar < 2个，X 1，R 1，R 4，R 5，R 3， R 6，R 7，R 8，R 9，R 10和R 13， 11 如说明书中所定义。

公开(公告)号：US20040192771A1

公开(公告)日：2004-09-30

申请号：US10743951

申请日：2003-12-24

Inventor： Jean-Louis Henri Dasseux ,  Carmen Daniela Oniciu

IPC: A61K031/275 ,  A61K031/20

CPC classification number: C07D257/04 ,  A61K31/20 ,  A61K31/275 ,  C07C43/132 ,  C07C43/135 ,  C07C43/1782 ,  C07C43/295 ,  C07C59/305 ,  C07C59/60 ,  C07C59/64 ,  C07C59/66 ,  C07C59/68 ,  C07C69/708 ,  C07C69/712 ,  C07C261/04 ,  C07C309/10 ,  C07D233/74 ,  C07D233/84 ,  C07D261/08 ,  C07D261/12 ,  C07D305/12 ,  C07D307/12 ,  C07D307/33 ,  C07D307/42 ,  C07D309/06 ,  C07D309/30 ,  C07D309/38 ,  C07D309/40

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. 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：US06794328B2

公开(公告)日：2004-09-21

申请号：US10452729

申请日：2003-06-03

Applicant: Tohru Yokozawa ,  Takao Saito

Inventor： Tohru Yokozawa ,  Takao Saito

IPC: B01J3100

CPC classification number: B01J31/2457 ,  B01J31/2291 ,  B01J31/2295 ,  B01J2231/643 ,  B01J2231/645 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/824 ,  B01J2531/827 ,  B01J2531/847 ,  C07B2200/07 ,  C07C51/36 ,  C07D321/00 ,  C07F9/65527 ,  C07C59/64

Abstract: The present invention provides a novel phosphine compound, specifically to provide a novel phosphine compound useful as a ligand for the above catalysts, in particular, a novel catalyst having an excellent performance (chemical selectivity, enantio-selectivity, catalytic activity) as a catalyst for asymmetric synthetic reactions, particularly asymmetric hydrogenation. A diphosphine compound represented by the general formula (1): wherein R1 and R2 each independently represents a lower alkyl group, a cycloalkyl group, an unsubstituted or substituted phenyl group, or a five-membered heteroaromatic ring residue.

Abstract translation: 本发明提供了一种新的膦化合物，特别是提供一种可用作上述催化剂配体的新型膦化合物，特别是具有优异性能（化学选择性，对映选择性，催化活性）作为催化剂的新型催化剂 不对称合成反应，特别是不对称氢化。 由通式（1）表示的二膦化合物：其中R 1和R 2各自独立地表示低级烷基，环烷基，未取代或取代的苯基或五元杂芳环。

公开(公告)号：US20040101523A1

公开(公告)日：2004-05-27

申请号：US10689919

申请日：2003-10-20

Applicant: G.D. Searle & Co.

Inventor： David B. Reitz ,  John P. Koepke ,  Edward H. Blaine ,  Joseph R. Schuh ,  Robert E. Manning ,  Glenn J. Smits

IPC: A61K038/43 ,  C12N009/99

CPC classification number: C07D213/73 ,  C07C59/64 ,  C07C59/90 ,  C07C237/12 ,  C07C237/22 ,  C07D209/08 ,  C07D209/20 ,  C07D209/34 ,  C07D213/50 ,  C07D213/65 ,  C07D213/80 ,  C07D213/81 ,  C07D213/86 ,  C07D215/227 ,  C07D233/64 ,  C07D233/88 ,  C07D233/90 ,  C07D235/30 ,  C07D241/42 ,  C07D241/44 ,  C07D263/58 ,  C07D265/36 ,  C07D285/14 ,  C07D307/46 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/66

Abstract: Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-null-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-null-hydroxylase inhibitors, of which N-acetyl-null-glutamyl fusaric acid hydrazide (shown below) is preferred. 1

Abstract translation: 描述了肾选择性前药，其优先在肾中转化成能够抑制参与肾交感神经活性的儿茶酚胺型神经递质合成的化合物。 本文所述的前药衍生自能够抑制一种或多种参与儿茶酚胺合成的酶的抑制剂化合物，这些化合物可分类为酪氨酸羟化酶抑制剂，或作为多巴 - 脱羧酶抑制剂，或作为多巴胺-β-羟化酶抑制剂。 这些抑制剂化合物通过由主要位于肾中的酶选择性识别的可切割键与化学部分如谷氨酸衍生物连接。 释放的抑制剂化合物然后可用于肾脏中以抑制参与儿茶酚胺合成的一种或多种酶。 抑制肾脏儿茶酚胺合成可以抑制与钠滞留相关的疾病如高血压相关的增强的肾神经活动。 特别感兴趣的缀合物是多巴胺-β-羟化酶抑制剂的谷氨酰衍生物，其中N-乙酰基-γ-谷氨酰镰孢酸酰肼（如下所示）是优选的。

公开(公告)号：US06730798B2

公开(公告)日：2004-05-04

申请号：US10312987

申请日：2003-01-03

Applicant: Stefan Stutz ,  Peter Herold ,  Felix Spindler

Inventor： Stefan Stutz ,  Peter Herold ,  Felix Spindler

IPC: C07D30512

CPC classification number: C07D207/33 ,  C07C57/42 ,  C07C59/64 ,  C07C69/734 ,  C07C231/02 ,  C07C247/12 ,  C07D303/38 ,  C07D307/33 ,  C07C237/20

Abstract: Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).

Abstract translation: 式（II）化合物在5位上同时卤化并在内酯化下在4位羟基化，将卤代内酯转化为羟基内酯，然后将羟基转化为离去基团，离去基团被叠氮化物取代，内酰胺酰胺化 然后将叠氮化物转化成胺基，以获得式（I）化合物。

公开(公告)号：US20040019033A1

公开(公告)日：2004-01-29

申请号：US10432411

申请日：2003-05-21

Inventor： Tord Inghardt ,  Anders Johansson ,  Arne Svensson

IPC: A61K031/397 ,  A61K031/506 ,  A61K031/501 ,  A61K031/4545 ,  A61K031/497 ,  C07D43/02 ,  C07D41/02 ,  C07D211/68

CPC classification number: C07D401/12 ,  C07C45/004 ,  C07C45/29 ,  C07C45/516 ,  C07C45/673 ,  C07C45/71 ,  C07C47/575 ,  C07C59/56 ,  C07C59/64 ,  C07C69/732 ,  C07C69/734 ,  C07C69/738 ,  C07C205/59 ,  C07D205/04 ,  C07D207/16 ,  C07D403/12 ,  C07C49/84 ,  C07C47/565

Abstract: There is provided a compound of formula I 1 wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Abstract translation: 提供式I化合物，其中R a，R 1，R 2，Y和R 3具有本说明书中给出的含义及其药学上可接受的衍生物（包括前体药物），该化合物和衍生物 可用作胰蛋白酶样蛋白酶的竞争性抑制剂如凝血酶的前体药物，因此特别是用于治疗需要抑制凝血酶（例如血栓形成）或作为抗凝剂的病症。

公开(公告)号：US20030216592A1

公开(公告)日：2003-11-20

申请号：US10150106

申请日：2002-05-20

Applicant: AJINOMOTO CO., INC.

Inventor： Shigeru Kawahara ,  Kenichi Mori ,  Kazutaka Nagashima ,  Tadashi Takemoto

IPC: C07K005/04 ,  C07C39/46

CPC classification number: C07C51/367 ,  C07C45/41 ,  C07C47/277 ,  C07C303/30 ,  C07K5/06113 ,  C07C59/64 ,  C07C309/66

Abstract: The present invention relates to a 3-substituted-phenyl-3-merthylbutyric acid and 3-substituted-phenyl-3-merthylaldehyde derivatives, which are useful in the production of N-nullN-null3-(3-hydroxy-4-methoxyphenyl)-3-methylbutylnull-L-null-aspartylnull-L-phenylalanine 1-methyl ester, which is a sweetener with high sweetening potency.

Abstract translation: 本发明涉及3-取代的苯基-3-三甲基丁酸和3-取代的苯基-3-甲基乙醛衍生物，其可用于制备N- [N- [3-（3-羟基-4- 甲氧基苯基）-3-甲基丁基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲基酯，其是具有高甜味效力的甜味剂。

公开(公告)号：US20030207859A1

公开(公告)日：2003-11-06

申请号：US10339043

申请日：2003-01-09

Inventor： James M. Balkovec ,  Mark L. Greenlee ,  Steven H. Olson ,  Gregory P. Rouen

IPC: A61K031/498 ,  A61K031/407 ,  A61K031/4172 ,  A61K031/381 ,  A61K031/343 ,  C07D43/14 ,  C07D333/20

CPC classification number: C07D307/91 ,  C07C57/38 ,  C07C57/58 ,  C07C59/64 ,  C07C69/612 ,  C07C69/734 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/20 ,  C07D405/06 ,  C07D409/06

Abstract: This invention relates to novel substituted succinic acid metallo-null-lactamase inhibitors which are useful potentiators of null-lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I: 1 including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.

公开(公告)号：US06632963B1

公开(公告)日：2003-10-14

申请号：US09277953

申请日：1999-03-29

Applicant: Jean-Michel Bernardon

Inventor： Jean-Michel Bernardon

IPC: C07C6206

CPC classification number: C07C59/72 ,  C07C59/64

Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract translation: 新颖的药物/美容活性双环芳族化合物具有结构式（I）：其中Ar PDAT>是具有结构式（a） - （c）之一的基团， 具有下式（d） - （h）之一的基团：X是具有下式（i） - （I）中的一个的基团 ）：并且可用于治疗各种各样的疾病状态，无论是人类还是兽医，例如皮肤病学，风湿性，呼吸道，心血管和眼科疾病，以及用于治疗哺乳动物皮肤和毛发状况/病症。 / PTEXT>

公开(公告)号：US06608194B1

公开(公告)日：2003-08-19

申请号：US09853177

申请日：2001-05-10

Applicant: Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Ashok Channaveerappa Bajji ,  Shivaramayya Kalchar ,  Rao Bheema Paraselli ,  Ranga Madhavan Gurram

Inventor： Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Ashok Channaveerappa Bajji ,  Shivaramayya Kalchar ,  Rao Bheema Paraselli ,  Ranga Madhavan Gurram

IPC: C07D26538

CPC classification number: C07D413/06 ,  C07C59/64 ,  C07C69/734 ,  C07D265/28 ,  C07D265/38 ,  C07D279/22 ,  C07D279/26 ,  C07D417/06

Abstract: A compound of Formula (Ih) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.

Abstract translation: 式（Ih）的化合物该化合物尤其用于制备β芳基-α-氧取代的烷基羧酸。