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Efficient synthetic routes of 2-amino-4-(omega-hydroxyalkylamino)pyrimidine derivatives were investigated in relation to the anti-influenza virus activity of these compounds. The derivatives in which cyclobutyl and cyclopentyl groups were introduced to the beta-position of the aminoalkyl group (especially the cyclobutyl group substituted by a phenylalkyl group at the 3'-position) resulted in improved antiviral potency: i.e. an average 50% effective concentration for inhibition of plaque formation (EC50, microM) of 0.1-0.01 microM for both types A and B influenza virus. The antiviral efficacies were in the order of amino group > hydroxyiminomethyl group > halogen substitution at the 5-position, and chlorine or methoxy group > hydrogen at the 6-position of the pyrimidine ring. The antiviral indices of these compounds were 2-6 with respect to the 50% inhibitory concentration for cell proliferation (IC50, microM) for growing cells, but > 500 to > 10(4) with respect to the IC50 for stationary cells, indicating that these compounds may be efficacious for the topical treatment of influenza virus infection.

Described is a new range finder using a self-mixing laser diode (SM-LD). The range finder has a high accuracy of +or-0.15% and a wide dynamic range of 0.2-1 m using only one sensor head. Compared to ultrasonic range finders, the light beam of this laser range finder can be focused and scanned. The feasibility study shows a possible application of the range finder to a visual sensor of a robot. The proposed range finder has been successfully applied as an infrared (IR) active type range finder of a single-lens reflex camera. >

The laser scanning system with three corner cubes to measure the position and heading of a vehicle is described. The high performance and short distance (50m class) equipment for a low speed vehicle was manufactured and evaluated. The system meets expected performance, or plus minus 2 cm position accuracy and plus minus 5 arc minutes heading accuracy.

A polarization-maintaining erbium-doped fiber amplifier (PM-EDFA) for optical sensing systems has been achieved with newly developed PANDA fiber based optical components. It employs 980 nm pumping for good noise performance. A noise figure of 4.1 dB and polarization crosstalk of less than -30 dB have been achieved with a gain of 22 dB.

The authors describe a compact range-finder that uses a frequency-modulated self-mixing laser diode which measures the averaged time interval of successive external-mode hops to give a short distance from the laser diode to a resting target with rough surface. With a triangular current modulation of an optimum amplitude, the measured dynamic range is from 0.2 m to 0.5 m; the standard deviation and the repeatability are less than +or-0.25 mm and +or-1.1 mm, respectively. With a decreased amplitude, i.e. half of the optimum, the dynamic range is widened to the range of 0.2 m to 1 m; the standard deviation and the repeatability are less than +or-1.6 mm and +or-2.8 mm, respectively. This type of range-finder is suitable for application as a visual sensor of an industrial robot. >

It is proposed to use an infrared semiconductor laser rangefinder to get a just-focusing signal, for the auto-focus (AF) system of a camera. Using both a measured distance to a moving object and its speed, the lens position of a single-lens reflex (SLR) camera is controlled. The range measurement error when installed in the AF system of an SLR camera is within 1% in a range of 0.3 m to 0.6 m. The error of 1% is below the normalized depth of field of 1.5-4.0% of the camera lens, which is consistent with the fact that some clear photographs are obtained from a moving object. >

It is proposed that a novel infrared range finder be used to get a just-focusing signal for an autofocus (AF) system employing both a measured distance to a moving object and its speed, and to control the lens position of video and single-lens reflex (SLR) cameras using the AF system. Some clear photographs of a moving object have been obtained by an SLR camera using the proposed AF system. >

X-Ray crystallographic analyses of fluorocyanides anti-1 and 2 revealed a novel intramolecular through-space interaction between F and CN in an acyclic system, which was applied to a stereoselective protonation of acyclic fluorocyanides 2 having flexible conformation.

A new platinum complex, nedaplatin, has been reported to be effective for both ovarian and cervical cancers. We designated a phase I dose-escalation study of a combination chemotherapy of nedaplatin and cisplatin to investigate the dose-limiting toxicity (DLT) and the maximum tolerated dose (MTD). Six patients, including two with advanced cervical cancer, three with ovarian clear cell adenocarcinoma and one with endometrial clear cell adenocarcinoma, were enrolled in this study. The doses of the two agents were escalated alternatively, i.e., a tandem method, from 40 to 80 mg/m2 by 20 mg/m2. Nedaplatin and cisplatin were administrated by intravenous drip infusion and repeated after an interval of at least 4 weeks, as a rule. The major toxicity observed was hematotoxicity. One of the 6 patients dropped out of this study because of severe hematotoxicity after 80 mg/m2 of nedaplatin and 60 mg/m2 of cisplatin were administered. With a dose of 80 mg/m2 nedaplatin and 80 mg/m2 cisplatin, severe neutropenia was found in all 6 patients, and thrombocytopenia and anemia were found in 1 patient, respectively. A slight hearing loss was detected by audiometry in 5 patients, but no one was inconvenienced in daily life. Mild nausea and vomiting were also observed in all 6 patients. In conclusion, the DLT of this combination therapy was hematotoxicity and the MTD was 80 mg/m2 for nedaplatin and 60 mg/m2 for cisplatin, respectively. Thus, 60 mg/m2 of nedaplatin and 60 mg/m2 of cisplatin may be recommended for combined administration.

Measured FM responses of a semiconductor laser optically coupled off-axis to a confocal Fabry-Perot cavity are discussed. It was found that this cavity acted as a frequency discriminator and as a phase comparator for slow and fast frequency fluctuations, respectively. The crossover between them was determined by a half linewidth of the cavity. On the basis of these investigations, two kinds of coherent semiconductor laser modules were constructed. External Fabry-Perot cavities were made by using an optical fiber and a hemispherical microlens. The linewidths of these lasers were less than 25 kHz. >

New optical fiber filters are fabricated using a Mach Zehnder interferometric structure in a twin core fiber. It is possible to change the filtering characteristics by bending the twin core fiber.

We evaluated the incidence of synchronous or metachronous multiple primary cancer, hereditary or familial cancer, and the familial aggregation of cancer in 142 patients who were treated for endometrial cancer at Tsukuba University Hospital in the period 1977 to 1995. Synchronous multiple primary cancers were identified in 6 of the 142 patients (4.2%). Eleven patients (7.7%) had a history of extraendometrial cancer. Patients with endometrial cancer had a significantly high incidence of a history of breast cancer. Endometrial cancer was diagnosed in two patients who were screened before menopause. Four patients with endometrial cancer (2.8%) subsequently developed extraendometrial forms of cancer. One patient (0.7%) was considered to have a hereditary form of cancer, and 5 patients (3.5%) had familial forms of cancer. A total of 86 cases of cancer were found among 53 kindred (37.3%). More detailed studies are needed to elucidate the aggregation of cancers in the families of patients with endometrial cancer in Japan. Patients with a history of breast cancer should be screened for the presence of endometrial cancer.

Ninety-five specimens from patients with endometrial carcinoma (82 of endometrial type, 6 of adenoacanthoma, 4 of adenosquamous carcinoma, 3 of atypical endometrial hyperplasia) and 13 with ovarian endometrioid carcinoma were stained immunohistochemically with a rabbit polyclonal antibody prepared against the placental form of the enzyme glutathione S-transferase pi (GST-pi). Histological studies showed that the degree of staining decreased as the tumor lost its differentiation in endometrial carcinoma, but the degree of staining was independent of the differentiation in the case of ovarian endometrioid carcinoma. A comparison between the grade of staining of GST-pi in 82 cases of the endometrial type of endometrial carcinoma and 13 cases of ovarian endometrioid carcinoma revealed a stronger stain for the endometrial carcinoma than for ovarian endometrioid carcinoma (p0.01, Mann-Whitney's U test). Therefore, the GST-pi value for endometrial carcinoma was different from that for endometrioid carcinoma. In general, as compared with ovarian endometrioid carcinoma, endometrial carcinoma is considered to be resistant to chemotherapeutic agents. In conclusion, these results suggest that there is an apparent correlation between the GST-pi value and chemoresistance of the tumor.

We have developed a prototype fiber optic sensor that detects thickness of clear-ice and density of anti/de-ice fluids on aircraft wing. It was confirmed that our proposed sensor satisfies user's basic requirements.

One hundred and six patients with endometrial cancer were treated at Tsukuba University Hospital between 1983 and 1992. Sixteen patients who underwent complete resection were at high risk for recurrence and were given adjuvant platinum-based, multiagent chemotherapy instead of adjuvant radiotherapy. Eligibility criteria included outer-third myometrial invasion (group 1; n = 5), pelvic lymph node metastasis (group 2; n = 3) or both myometrial invasion and lymph node metastasis (group 3; n = 8). Of these three groups at high risk for recurrence, each patient in groups 1 and 2 developed recurrence and died. In group 3 two patients developed recurrence and one patient has died. There was one treatment death due to neutropenic sepsis in group 3. The recurrence sites in all four patients were local and no distant recurrence was noted. In other words, of 15 patients (excluding one treatment death) at high risk for recurrence, three of 12 patients (25%) with deep myometrial invasion and three of 10 patients (30%) with positive pelvic lymph nodes developed recurrence and died. The other 12 patients (include one patient with recurrence; 100 months) have survived for a long interval (range, 45-131 months). The survival rates for stage I, II, III, and IV are 92.6, 89.5, 60.0%, respectively. Patients with stage I in this study had a better survival than those with stage I in the 1984 annual report of the Japan Society of Obstetrics and Gynecology (p0.05). The findings of this prospective clinical trial supported those of the randomized trial comparing adjuvant CAP with radiation therapy.

Specimens from 102 cases of ovarian cancer were stained immunohistochemically with a rabbit polyclonal antibody prepared against the placental form of the enzyme glutathione S-transferase (GST-pi). All 28 cases of mucinous adenocarcinoma, 19 of clear cell carcinoma and 4 of malignant transformed dermoid cysts were stained positively with the GST-pi antibody. These tumors are considered to be resistant to chemotherapeutic agents as compared with other epithelial tumors. With regard to the histological grade, the degree of staining was reduced according to the loss of differentiation. An investigation of the relationship between GST-pi stain and the prognosis of the 50 patients with stage 2,3 or 4, according to the Kaplan-Meier method, revealed that the prognosis improved as the staining decreased. In conclusion, results suggested that immunohistochemical staining of GST-pi is correlated with the chemoresistance of the tumor, and may predict the outcome in patients with ovarian cancer.

This paper describes an autonomous dump trucks system being developed to overcome worker shortage problems and to prevent accidents in heavy construction sites (i.e., darn constructions , road constructions, etc.). The major distinctive functions of this system arc: (1) the autonomous driving function: this system enables unmanned dump trucks to autonomously drive at 40 km/h as planned. The difference between the planned path and the trajectory is within ±90 cm; the vehicle command system can recognize obstacles and prevent their being crashed or destroyed by, utilizing a color image processor; (2) the advanced measurement function: the laser navigation system provides measurement function (i.e., the measurement errors regarding the position and the direction are within ±50 cm and ±1 degree, respectively). This system enables two operators to manage dump trucks without drivers. It is anticipated that this system could reduce approximate 30% of the workers required at heavy construction sites in the future.

To analyze the healing process after laser therapy for cervical lesions, the clinical, cytologic, histologic and colposcopic features in 109 cases were studied chronologically. The healing process of the cervical epithelium usually began from both the squamous and columnar epithelial borders, starting around the 10th day after laser therapy; the process covered the whole tissue defect with multilayered epithelium within seven weeks. Inflammatory changes also usually abated within that time. Cytomorphologically, laser therapy resulted in the occurrence of (mostly degenerated) "fiber-type" and orangeophilic cells in smears taken during the first two weeks after treatment. Tissue repair cells were seen in smears collected from the first posttherapy day through the fourth week after laser therapy. Using computer-assisted image cytometry, the reparative cells in samples taken shortly after treatment (roughly, the first to fifth days) exhibited more hyperchromatic (3-4N) nuclei than did those in later samples; however, the mean DNA content of the early reparative cells was generally concentrated around that of the 2N reference cells. These findings suggest that follow-up, including cytologic and colposcopic examination, for the early detection of residual or recurrent lesions should start in the eighth week and continue periodically for at least one year.

Recently, the semiautomated tetrazolium-based MTT colorimetric assay have been used to measure chemosensitivity. We also have been used this assay for 4 ovarian clear cell carcinoma cell lines to investigate the chemosensitivity of this tumor. In this study, several problems have been faced to be solved. In this paper, we pointed out these problems and indicated solutions.

Design and manufacturing of dispersion-shifted fibers with a Gaussian profile, which is compatible to the VAD process, are studied. From the viewpoint of stable cabling, the parametric analysis is made with emphasis on the bending loss. To make the bending sensitivity of the Gaussian core fibers comparable with the conventional 1.3- μm zero-dispersion fibers, an 0.8 percent or higher index difference is required. In the experiment, the achieved loss at the 1.55-μm dispersionless wavelength is 0.21 dB/km. The effects of a ring profile around the Gaussian core on the fiber transmission characteristics also are examined. While the cutoff wavelengths are greatly lengthened by the ring, the bending sensitivity is not so affected. It is found that the index difference of the main core still dominates the bending loss of the fiber.

Various types of 1.55-μm dispersion-shifted fiber have been presented. Among them, triangular core1 and similar fibers have the advantage in terms of optical loss. Recently, a triangular profile with a ring in the cladding was proposed to minimize the bending loss.2 Our paper now describes the effect of the ring on the transmission characteristics of triangular and Gaussian core fibers.3

In the present study, the physiologically based pharmacokinetic model, which succeeded previously in predicting the pharmacokinetics of beta-lactam antibiotics in rats [A. Tsuji, T. Yoshikawa, K. Nishide, H. Minami, M. Kimura, E. Nakashima, T. Terasaki, E. Miyamoto, C.H. Nightingale, and T. Yamana: Physiologically based pharmacokinetic model for beta-lactam antibiotics. I: tissue distribution and elimination in rats. J. Pharm. Sci. 72, 1239-1252 (1983)], was applied to cefazolin pharmacokinetics in rabbits and man. After iv bolus dosing in normal rabbits, the time courses of cefazolin concentration in plasma and various tissues (lung, heart, muscle, skin, bone, gut, liver, and kidney) were found to be very similar to those in rats. The values of physiological parameters (tissue plasma flows, tissue volumes, tissue/plasma albumin ratio) and biochemical parameters determined in this study (for nonlinear plasma protein binding, intrinsic renal clearance of active secretion and reabsorption) were incorporated into mass balance equations derived from the model. There was reasonable agreement between the model predictions and the observed data for cefazolin and inulin in rabbits. The model was also successful in the prediction of cefazolin disposition in rabbits with renal failure. Using available information reported for cefazolin in man, a preliminary extrapolation from the present model was attempted, and the overall predicted results after iv administration of 1 g cefazolin in man were compared with the serum and bone tissue data. The length of the effective antibacterial period for the drug is also discussed in terms of its predicted concentration unbound with proteins in various tissue interstitial fluids in man.

The mechanism of right-sided traumatic diaphragmatic hernia following blunt trauma was examined. In 13 cases of Traumatic diaphragmatic hernia admitted to the Department of Traumatology Osaka University Hospital, 3 cases were on the right. All cases were associated with severe injuries in the chest, abdomen and pelvis. Rib fractures, hemothorax, and liver injury were seen in the same site of the ruptured diaphragm. So it seemed that there were some differences in the force itself caused diaphragmatic rupture between right-sided and left. We reviewed 40 cases of right-sided traumatic diaphragmatic hernia reported in Japan. The following results were obtained. Main force which caused right-sided diaphragmatic rupture was the blunt impact to the right thoracic wall. In the right-sided diaphragmatic hernia, the most frequently herniated organ was the right lobe of the liver and there was high-frequency of G-I tract herniation in delayed types. Herniation of the abdominal organs seemed to be varied as the time passed.

Hypersonic projectiles whose speed was beyond the Chapman-Jouguet (C-J) detonation speed, were fired into stoichiometric hydrogen-oxygen premixed gases. The flowfield around the projectile was visualized using a gated CCD camera. A steady-state detonation wave was generated around the projectile. With respect to the flow Mach number behind the wave front, the whole detonation-wave was partitioned into four parts; (i) strong overdriven detonation wave, (ii) weak overdriven detonation wave, (iii) quasi C-J detonation wave, and (iv) C-J detonation wave. It has been found that a rarefaction wave generated at the projectile shoulder has a significant effect on the structure of the detonation wave.