公开(公告)号：WO1998029441A1

公开(公告)日：1998-07-09

申请号：PCT/US1997023892

申请日：1997-12-18

Applicant: MERCK & CO., INC. ,  UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER AT SAN ANTONIO ,  UNIVERSITY OF TORONTO ,  SULLIVAN, Kathleen ,  KOLAKOWSKI, Lee, F., Jr. ,  O'DOWD, Brian

Inventor： MERCK & CO., INC. ,  UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER AT SAN ANTONIO ,  UNIVERSITY OF TORONTO

IPC: C07K14/00

CPC classification number: C07K14/72 ,  G01N2333/72

Abstract: A new galanin receptor, GALR2, is described. Also provided are nucleic acids encoding same and various assays to identify ligands particular to said receptor. Ligands so identified are useful for the treatment of obesity, treatment of pain, and treatment of cognitive disorders.

Abstract translation: 描述了一种新的甘丙肽受体GALR2。 还提供了编码相同的核酸和用于鉴定所述受体特异性的配体的各种测定法。 如此鉴定的配体可用于治疗肥胖症，治疗疼痛和治疗认知障碍。

公开(公告)号：WO1998028000A1

公开(公告)日：1998-07-02

申请号：PCT/US1997023668

申请日：1997-12-18

Applicant: MERCK & CO., INC. ,  VOLKIN, David, B. ,  BURKE, Carl, J. ,  SHEU, Su-Pi

Inventor： MERCK & CO., INC.

IPC: A61K39/00

CPC classification number: A61K39/25 ,  A61K9/19 ,  A61K39/0015 ,  A61K39/12 ,  A61K39/13 ,  A61K39/165 ,  A61K39/20 ,  A61K47/26 ,  A61K47/42 ,  A61K2039/5254 ,  A61K2039/70 ,  C12N2710/16734 ,  C12N2760/18434 ,  C12N2760/18734 ,  C12N2770/36234 ,  Y02A50/466

Abstract: Vaccine stabilizers, vaccine formulations and lyophilized vaccines with enhanced thermostability are disclosed. The vaccine formulations comprise an increased amount of a 6-carbon polyhydric alcohol (such as sorbitol), an increased amount of a disaccharide (such as sucrose) and an amount of a physiologically active buffer to adjust the pH from about 6.0 to about 7.0.

Abstract translation: 公开了具有增强的热稳定性的疫苗稳定剂，疫苗制剂和冻干疫苗。 疫苗制剂包含增加量的6-碳多元醇（例如山梨醇），增加量的二糖（例如蔗糖）和用于将pH调节至约6.0至约7.0的生理活性缓冲液的量。

公开(公告)号：WO1998025623A1

公开(公告)日：1998-06-18

申请号：PCT/US1997022344

申请日：1997-12-05

Applicant: MERCK & CO., INC. ,  FUH, Vivian, L. ,  KAUFMAN, Keith, D. ,  WALDSTREICHER, Joanne

Inventor： MERCK & CO., INC.

IPC: A61K31/56

CPC classification number: A61K31/568 ,  A61K45/06

Abstract: The present invention provides for a method of inhibiting bone loss in a subject in need of such treatment comprising administration of a therapeutically effective amount of the 5 alpha -reductase type 2 inhibitor finasteride to the subject. The present invention further provides for a method for treating and preventing osteoporosis and osteopenia and other diseases where inhibiting bone loss may be beneficial, including: Paget's disease, malignant hypercalcemia, periodontal disease, joint loosening and metastatic bone disease, comprising administration of therapeutically effective amount of the 5 alpha -reductase type 2 inhibitor finasteride to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for inhibiting bone loss and treating or preventing osteoporosis and osteopenia.

Abstract translation: 本发明提供了一种在需要这种治疗的受试者中抑制骨丢失的方法，包括向受试者施用治疗有效量的5α-还原酶2型抑制剂非那雄胺。 本发明还提供了治疗和预防骨质疏松症和骨质减少症等抑制骨丢失可能有益的疾病的方法，包括：佩吉特氏病，恶性高钙血症，牙周病，关节松动和转移性骨病，包括给予治疗有效量 的5α-还原酶2型抑制剂非那雄胺。 此外，本发明提供了可用于本发明方法的组合物，以及用于抑制骨丢失和治疗或预防骨质疏松症和骨质减少症的药物的制备方法。

公开(公告)号：WO1998025463A1

公开(公告)日：1998-06-18

申请号：PCT/US1997022045

申请日：1997-12-05

Applicant: MERCK & CO., INC. ,  FUH, Vivian, L. ,  KAUFMAN, Keith, D. ,  WALDSTREICHER, Joanne

Inventor： MERCK & CO., INC.

IPC: A01N43/42

CPC classification number: C07D401/06 ,  C07D221/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07J73/005

Abstract: The present invention provides for a method of inhibiting bone loss in a subject in need of such treatment comprising administration to the subject of a therapeutically effective amount of a compound of structural formula (I). The present invention further provides for a method for treating and preventing osteoporosis and osteopenia and other diseases where inhibiting bone loss may be beneficial, including: Paget's disease, malignant hypercalcemia, periodontal disease, joint loosening and metastatic bone disease, comprising administration of therapeutically effective amount of a compound of structural formula (I) to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for inhibiting bone loss and treating or preventing osteoporosis and osteopenia.

Abstract translation: 本发明提供一种抑制需要这种治疗的受试者的骨丢失的方法，其包括向受试者施用治疗有效量的结构式（I）的化合物。 本发明还提供了治疗和预防骨质疏松症和骨质减少症等抑制骨丢失可能有益的疾病的方法，包括：佩吉特氏病，恶性高钙血症，牙周病，关节松动和转移性骨病，包括给予治疗有效量 的结构式（I）的化合物。 此外，本发明提供了可用于本发明方法的组合物，以及用于抑制骨丢失和治疗或预防骨质疏松症和骨质减少症的药物的制备方法。

公开(公告)号：WO1998012178A1

公开(公告)日：1998-03-26

申请号：PCT/US1997016171

申请日：1997-09-12

Applicant: MERCK & CO., INC. ,  DORZIOTIS, Ilias, K. ,  HOUPIS, Ioannis, N. ,  LEE, Jaemoon ,  VOLANTE, Ralph, P.

Inventor： MERCK & CO., INC.

IPC: C07D213/30

CPC classification number: C07D213/16 ,  C07D213/30

Abstract: This invention is concerned with a novel process for the preparation of a compound of structural formula (I) wherein R and R independently are aryl, C2-15 alkenyl or C1-15 alkyl, either unsubstituted or substituted with one or three substituents, which can be the same or different, selected from the group consisting of Ra, wherein Ra belongs to a group consisting of C1-6 alkyl, aryl, halo, -N(R )2, -NO2, -CN, -OR , -C3-6 cycloalkoxy, -CO(R ), -COOR , SO2R and -SR ; wherein R is selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl and aryl, said alkyl, alkenyl or aryl optionally substituted with 1 to 3 groups of R , which is an important antiasthmatic agent.

Abstract translation: 本发明涉及制备结构式（I）的化合物的新方法，其中R 1和R 2独立地是芳基，C 2-15烯基或C 1-15烷基，未取代或被一个 或三个取代基，其可以相同或不同，选自Ra，其中Ra属于由C 1-6烷基，芳基，卤素，-N（R 3）2，-NO 2， -CN，-OR 3，-C 3-6环烷氧基，-CO（R 3），-COOR 3，SO 2 R 3和-SR 3; 其中R 3选自氢，C 1-6烷基，C 2-6烯基和芳基，所述烷基，链烯基或芳基任选被1-3个R a基团取代，R a是重要的抗哮喘 剂。

公开(公告)号：WO1998010653A1

公开(公告)日：1998-03-19

申请号：PCT/US1997016103

申请日：1997-09-10

Applicant: MERCK & CO., INC. ,  NARGUND, Ravi ,  PATCHETT, Arthur, A. ,  TATA, James

Inventor： MERCK & CO., INC.

IPC: A01N43/08

CPC classification number: A61K31/663 ,  C07D401/06 ,  C07D471/10

Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of general structural formula (I) wherein B is selected from (A) and (B) and R , R , R , R , R , R , R , R , R , D, E, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract translation: 本发明涉及通式（I）的某些哌啶，吡咯烷和六氢-1H-吖庚因，其中B选自（A）和（B）和R 1，R 1a，R 2a ，R 3a，R 3b，R 4，R 4a，R 4b，R 5，D，E，X，Y，n，x和y如本文所定义。 这些化合物促进人和动物中生长激素的释放。 该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，可以治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并治疗由生长激素的合成代谢作用改善的医疗状况。 还公开了含有这些化合物作为其活性成分的生长激素释放组合物。

公开(公告)号：WO1998009632A1

公开(公告)日：1998-03-12

申请号：PCT/US1997015504

申请日：1997-09-03

Applicant: MERCK & CO., INC. ,  CUKIERSKI, Mark, A. ,  SPENCE, Stanley, G. ,  WALDSTREICHER, Joanne

Inventor： MERCK & CO., INC.

IPC: A61K31/58

CPC classification number: A61K45/06 ,  A61K31/00 ,  A61K31/58

Abstract: The present invention provides for a method of treating preterm labor in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5 DOLLAR (a)-reductase type 1 to the subject. The present invention further provides for a method of preventing premature labor in a subject susceptible thereto comprising administration of a labor-preventive amount of an inhibitor of 5 alpha -reductase type 1 to the subject. Further, the present invention also relates to a method of reducing the risk of premature labor in a subject at risk therefor. The present invention also provides for a method for stopping labor preparatory (i.e., prior) to Cesarean delivery in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5 alpha -reductase type 1 to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating preterm labor and for stopping labor preparatory to Cesarean delivery.

Abstract translation: 本发明提供了在需要这种治疗的受试者中治疗早产的方法，包括向受试者施用治疗有效量的5型DOLLAR（a） - 1型还原酶的抑制剂。 本发明进一步提供一种防止易感的受试者中的过早劳动的方法，其包括向受试者施用预防劳动的量的5型α型还原酶抑制剂。 此外，本发明还涉及一种降低患有风险的受试者的过早劳动的风险的方法。 本发明还提供了一种用于在需要这种治疗的受试者中停止对剖腹产的准备（即先前）进行剖宫产的方法，其包括向受试者施用治疗有效量的5型α-还原酶抑制剂。 此外，本发明提供了可用于本发明方法的组合物，以及制备用于治疗早产和用于停止预备剖腹产的药物的方法。

公开(公告)号：WO1998006865A1

公开(公告)日：1998-02-19

申请号：PCT/US1997014136

申请日：1997-08-11

Applicant: MERCK & CO., INC. ,  CHARTRAIN, Michel ,  HEIMBUCH, Brian ,  JACKEY, Barbara, A. ,  TAYLOR, Colleen, S.

Inventor： MERCK & CO., INC.

IPC: C12P07/22

CPC classification number: C07C213/02 ,  C12P7/22

Abstract: A process is disclosed that bioconverts indene to (1S)-amino-(2R)-indanol substantially free of any of its stereoisomers, by the action of the enzyme monoxygenase and, optionally, epoxide hydrolase, followed by various chemical step(s), e.g., chiral specific crystallization, treatment with strong acid in the presence of acetonitrile.

Abstract translation: 公开了通过酶单加氧酶和任选的环氧化物水解酶的作用，接着进行各种化学步骤，将生物转化体茚（1S） - 氨基 - （2R） - 茚醇基本上不含任何其立体异构体， 例如手性特异结晶，在乙腈存在下用强酸处理。

公开(公告)号：WO1998001116A1

公开(公告)日：1998-01-15

申请号：PCT/US1997012426

申请日：1997-07-03

Applicant: MERCK & CO., INC. ,  MITCHEL, Yale, B. ,  MELINO, Michael, R.

Inventor： MERCK & CO., INC.

IPC: A61K09/20

CPC classification number: A61K31/366 ,  A61K31/351

Abstract: The instant invention provides methods and pharmaceutical compositions for treating combined hyperlipidemia and for lowering elevated levels of very low density lipoprotein cholesterol in mammals who have combined hyperlipidemia comprising the administration of a therapeutically effective amount of at least 160 mg per day of simvastatin or a pharmaceutically acceptable salt or ester thereof to a mammal in need of such treatment.

Abstract translation: 本发明提供了用于治疗联合高脂血症并降低具有组合高脂血症的哺乳动物中极低密度脂蛋白胆固醇水平升高的方法和药物组合物，其包括施用治疗有效量的至少160mg /天的辛伐他汀或药学上可接受的 盐或酯对于需要这种治疗的哺乳动物。

公开(公告)号：WO1998000401A1

公开(公告)日：1998-01-08

申请号：PCT/US1997011047

申请日：1997-06-25

Applicant: MERCK & CO., INC. ,  YOUNG, Steven, D. ,  HARTMAN, George, D. ,  LIBBY, Laura, A. ,  EGBERTSON, Melissa, S. ,  SLAUGHTER, Donald, E.

Inventor： MERCK & CO., INC.

IPC: C07D211/32

CPC classification number: C07D213/73 ,  C07D209/46 ,  C07D211/34 ,  C07D211/76 ,  C07D295/155 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04

Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, of X-W-Y-Z-A-B more particularly of formula (A).

Abstract translation: 具有例如更特别是式（A）的X-W-Y-Z-A-B结构的纤维蛋白原受体拮抗剂醇前药。