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    COMPOUNDS AND COMPOSITIONS FOR TREATING HIV INFECTIONS
    43.
    发明申请
    COMPOUNDS AND COMPOSITIONS FOR TREATING HIV INFECTIONS 审中-公开
    用于治疗艾滋病毒感染的化合物和组合物

    公开(公告)号：WO1993012138A1

    公开(公告)日：1993-06-24

    申请号：PCT/US1992010506

    申请日：1992-12-10

    Applicant: SCHERING CORPORATION

    Inventor： SCHERING CORPORATION ,  RANE, Dinanath, F. ,  GIRIJAVALLABHAN, Viyyoor, M. ,  SAKSENA, Anil, K. ,  GANGULY, Ashit, K.

    IPC: C07K05/02

    CPC classification number: A61K38/04 ,  A61K31/195 ,  A61K31/22 ,  A61K31/335 ,  A61K31/38 ,  C07C59/76 ,  C07C69/60 ,  C07D303/48 ,  C07D331/02 ,  C07K5/06034 ,  C07K5/06086

    Abstract: The use of a compound respresented by formula (I) in the manufacture of a medicament for treating a mammal infected with human immunodeficiency virus, acquired immune deficiency syndrome caused by human immunodeficiency virus or acquired immunodeficiency syndrome-related complex caused by immunodeficiency virus, and stereochemical isomers and pharmaceutically acceptable salts thereof. In formula (I), W = (C1-C5) alkyl, NHR3 or OR1; B = two hydrogens, a double bond, >O, or >S; Q = R3 or AA; Z = NHR3, OR1 or AA; R1 = H, or (C1-C5) alkyl; R2 = H, CH3, -(CH2)sNHR3 or -(CH2)sAA; R3 = H or (C1-C5) alkyl or (C1-C6); alkanoyl n = 1 to 3; s = 0 to 3; q = 0 or 1; AA = a natural or unnatural-(L)- amino acid moiety; the asterisk (*) carbon atom indicate an asymmetric center; and the wavy line represents a single bond to place the (1) moiety in the cis- or trans-configuration relative to the (2) moiety except when B is two hydrogens; with the proviso that in formula (I) when B = >O, n = q = 1, W = NH2, R2 = R1 = R3 = H, Z = OH and the wavy line has the trans-configuration, then Q NOTEQUAL CO-CH(NH2)CH3.

    Abstract translation: 由式（I）表示的化合物在制备用于治疗感染人类免疫缺陷病毒的哺乳动物，由免疫缺陷病毒引起的人类免疫缺陷病毒或获得性免疫缺陷综合征相关复合物引起的获得性免疫缺陷综合征的药物的用途和立体化学 异构体及其药学上可接受的盐。 在式（I）中，W =（C1-C5）烷基，NHR3或OR1; B =两个氢，一个双键，> O或> S; Q = R3或AA; Z = NHR3，OR1或AA; R1 = H或（C1-C5）烷基; R2 = H，CH3， - （CH2）sNHR3或 - （CH2）sAA; R3 = H或（C1-C5）烷基或（C1-C6）; 烷酰基n = 1至3; s = 0〜3; q = 0或1; AA =天然或非天然 - （L） - 氨基酸部分; 星号（*）碳原子表示不对称中心; 并且波浪线表示相对于（2）部分将（1）部分置于顺式或反式构型的单键，除非B是两个氢; 条件是当B => O时，在式（I）中，n = q = 1，W = NH 2，R2 = R1 = R3 = H，Z = OH，波浪线具有反式构型，则Q NOTEQUAL CO -CH（NH 2）CH 3。

    TRIPEPTIDE DERIVATIVE ANTI-INFLAMMATORY AGENTS
    44.
    发明申请
    TRIPEPTIDE DERIVATIVE ANTI-INFLAMMATORY AGENTS 审中-公开
    TRIPEPTIDE衍生抗炎剂

    公开(公告)号：WO1993008211A1

    公开(公告)日：1993-04-29

    申请号：PCT/US1992008901

    申请日：1992-10-19

    Applicant: THE PROCTER & GAMBLE COMPANY

    Inventor： THE PROCTER & GAMBLE COMPANY ,  McIVER, John, McMillan

    IPC: C07K05/06

    CPC classification number: C07K5/06191 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06086

    Abstract: The subject invention involves anti-inflammatory compounds having structure (1), wherein (a) n is an integer of from 0 to about 2; (b) -R is selected from straight or branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; and cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and the carbon atom to which -R is bonded is in either D or L configuration; (c) -R' is selected from branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 6 carbon atoms; cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and arylalkyl, the alleyl portion being saturated and having from 1 to about 3 carbon atoms; and the carbon atom to which -R' is bonded is in L configuration; (d) -R'' is -(CH2)m-A-NH2 or -(CH2)m-A-B-C(NH2)=NH, wherein m is an integer of from 1 to about 5; -A- is a covalent bond, or p-phenyl or p-cyclohexyl; and -B- is a covalent bond or -NH-; and the carbon atom to which -R'' is bonded is in L configuration; (e) -Y is hydrogen or trifluoromethyl; (f) -Z- is -O- or -NH-; (g) -V- is selected from -OC(O)-, -N(Q)C(O)-, -N(Q)C(S)-, -C(O)-, -SO2- and -P(O)(OH)-; when -V- is -OC(O)-, -Z- is -NH-; (h) -X is selected from the group consisting of cyclic alkyl, branched alkyl having at least two branches, and aryl, each having from 5 to about 20 carbon atoms; and (i) -Q is selected from the group consisting of hydrogen; and straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; or -Q and -X are covalently linked forming a cyclic moiety which includes the nitrogen to which -Q is bonded and from 5 to about 20 carbon atoms. The subject invention also involves pharmaceutical compositions comprising the above compounds, and methods for treating inflammation or pain using such compounds and compositions.

    Abstract translation: 本发明涉及具有结构（1）的抗炎化合物，其中（a）n为0至约2的整数; （b）-R选自具有1至约6个碳原子的具有1或2个双键的饱和或不饱和的直链或支链烷基; 具有3至约13个碳原子的具有1或2个双键的饱和或不饱和环状烷基; R结合的碳原子为D或L构型; （c）-R'选自具有3至约6个碳原子的具有1或2个双键的饱和或不饱和的支链烷基; 具有3至约13个碳原子的具有1或2个双键的饱和或不饱和环状烷基; 和芳基烷基，所述烷基部分是饱和的且具有1至约3个碳原子; 且R'键合的碳原子为L构型; （d）-R“是 - （CH 2）m -A-NH 2或 - （CH 2）m -A-B-C（NH 2）= NH，其中m是1至约5的整数; -A-是共价键，或对 - 苯基或对 - 环己基; 和-B-是共价键或-NH-; 并且与R“结合的碳原子为L构型; （e）-Y是氢或三氟甲基; （f）-Z-是-O-或-NH-; （O） - ， - N（Q）C（O） - ， - N（Q）C（S） - ， - （O） - ， - SO 2 - 呸）-; 当-V-为-OC（O） - 时，-Z-为-NH-; （h）-X选自具有至少两个分支的环烷基，支链烷基和具有5至约20个碳原子的芳基; 和（i）-Q选自氢; 和具有1至约6个碳原子的具有1或2个双键的饱和或不饱和的直链或支链烷基; 或-Q和-X共价连接形成环状部分，其包括与Q键合的氮和5至约20个碳原子。 本发明还涉及包含上述化合物的药物组合物，以及使用这些化合物和组合物治疗炎症或疼痛的方法。

    SYNTHETIC INHIBITORS OF MAMMALIAN COLLAGENASE
    45.
    发明申请
    SYNTHETIC INHIBITORS OF MAMMALIAN COLLAGENASE 审中-公开
    合成抑制剂MAMMALIAN COLLAGENASE

    公开(公告)号：WO1988006890A1

    公开(公告)日：1988-09-22

    申请号：PCT/US1988000879

    申请日：1988-03-17

    Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.

    Inventor： RESEARCH CORPORATION TECHNOLOGIES, INC. ,  GRAY, Robert, D. ,  SPATOLA, Arno, F. ,  MILLER, Robert, B.

    IPC: A61K37/02

    CPC classification number: C07K5/0812 ,  A61K38/00 ,  C07D209/20 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06156

    Abstract: The present invention relates to compounds of the formula R1SCH(R2)CH(R3)CO-AA1[AA2]m[AA3]n-X, wherein m is the integer 0 or 1; n is an integer from 0-2; AA1 is a hydrophobic amino acid; AA2 is an amino acid selected from the group consisting of alanine, glycine, leucine, isoleucine phenylalanine; AA3 is any amino acid; R1 is hydrogen, alkyl having from 1-10 carbon atoms, alkanoyl having from 2-10 carbon atoms, or aroyl having from 7-10 carbon atoms; R2 is hydrogen or alkyl having from 1-6 carbon atoms; R3 is hydrogen, alkyl having from 2-10 carbon atoms, cycloalkyl having from 3-6 carbon atoms, aryl or arylalkyl, wherein aryl moieties have from 6-10 carbon atoms; X is NH2, OH, OCH3 or OCH2CH3; and salts thereof.

    Abstract translation: 本发明涉及式R1SCH（R2）CH（R3）CO-AA1 [AA2] m [AA3] n-X的化合物，其中m为整数0或1; n是0-2的整数; AA1是疏水性氨基酸; AA2是选自丙氨酸，甘氨酸，亮氨酸，异亮氨酸苯丙氨酸的氨基酸; AA3是任何氨基酸; R1是氢，具有1-10个碳原子的烷基，具有2-10个碳原子的烷酰基，或具有7-10个碳原子的芳酰基; R2是氢或具有1-6个碳原子的烷基; R3是氢，具有2-10个碳原子的烷基，具有3-6个碳原子的环烷基，芳基或芳烷基，其中芳基部分具有6-10个碳原子; X是NH 2，OH，OCH 3或OCH 2 CH 3; 及其盐。

    IMMUNOREGULATORY PEPTIDES
    46.
    发明申请
    IMMUNOREGULATORY PEPTIDES 审中-公开
    免疫球蛋白

    公开(公告)号：WO1986004334A1

    公开(公告)日：1986-07-31

    申请号：PCT/EP1986000012

    申请日：1986-01-15

    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ...

    Inventor： MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER ... ,  HAHN, Gary, Scott

    IPC: C07K05/00

    CPC classification number: C07K16/065 ,  A61K38/00 ,  C07K5/06086 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/1016 ,  C07K14/575

    Abstract: Peptides and peptide derivatives, and method of using the same in mammalian immune systems to suppress autoimmune responses, organ transplantation rejection responses, or neoplastic cell growth. The peptides are characterized by the formula A-X-(B-Y)n-C wherein X and Y are residues of amino acids or amino acid derivatives with positively charged side chains, e.g., Lys, Orn, Arg, His, D-Lys, D-Orn, D-Arg, or D-His, or D-enantiomers of any of these residues, A and C are any substituents that preserve or augment the immunoregulatory activity of the peptides, B is a residue of an amino acid or amino acid derivative that preserves or augments the immunoregulatory activity of the peptide, and n is 0 or 1. The activity of the subject peptides includes suppression of the proliferation of T-lymphocytes in in vitro systems that are analogous to mammalian in vivo disease conditions, regulation of tumor cell proliferation in vitro and in vivo, and reduction of autoimmune disease-associated lesions in vivo. The peptides have potential human therapeutic benefits related to the treatment of autoimmune, organ or graft rejection, neoplastic and other diseases.

    Abstract translation: 肽和肽衍生物，以及在哺乳动物免疫系统中使用它们抑制自身免疫应答，器官移植排斥反应或肿瘤细胞生长的方法。 肽通过式AX-（BY）nC表征，其中X和Y是具有带正电荷侧链的氨基酸或氨基酸衍生物的残基，例如Lys，Orn，Arg，His，D-Lys，D-Orn， 任何这些残基的D-Arg或D-His或D-对映异构体，A和C是保留或增强肽的免疫调节活性的任何取代基，B是氨基酸或氨基酸衍生物的残基，其保留 或增加肽的免疫调节活性，n为0或1.本发明肽的活性包括在体外系统中抑制T淋巴细胞的增殖，其类似于哺乳动物体内疾病状况，调节肿瘤细胞增殖 体内和体内，以及体内自身免疫性疾病相关病变的减少。 这些肽具有与治疗自身免疫，器官或移植排斥，肿瘤和其他疾病相关的潜在的人类治疗益处。

    DIPEPTIDES AS INHIBITORS OF HUMAN IMMUNOPROTEASOMES
    50.
    发明申请
    DIPEPTIDES AS INHIBITORS OF HUMAN IMMUNOPROTEASOMES 审中-公开
    作为人类免疫球蛋白抑制剂的代表

    公开(公告)号：WO2015106200A3

    公开(公告)日：2015-09-11

    申请号：PCT/US2015011022

    申请日：2015-01-12

    Applicant: UNIV CORNELL

    Inventor： LIN GANG ,  NATHAN CARL ,  DING AIHAO ,  MA XIAOJING

    IPC: C07K5/06

    CPC classification number: C07K5/06104 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/06113 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0806 ,  C07K5/0821

    Abstract: The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R1-R10, X, Y, k, m, n, q, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

    Abstract translation: 本发明的化合物由以下具有式（I）的化合物表示，其中取代基R 1 -R 10，X，Y，k，m，n，q和s如本文所定义。 这些化合物用于治疗癌症，免疫障碍，自身免疫性疾病，神经变性疾病或炎症性疾病，或用于为移植的器官或组织提供免疫抑制。

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